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Antioxidant and antiproliferative capacities of phenolics purified from Phyllanthus emblica L. fruit
Abstract
Phyllanthus emblica is a widely distributed tropical medicinal plant with good therapeutic properties. Gallic acid, ellagic acid, mucic acid 1,4-lactone 3-O-gallate, isocorilagin, chebulanin, chebulagic acid and mallotusinin were isolated and purified from this plant. The antioxidant activities of these compounds were evaluated by in vitro models of scavenging superoxide anion radicals, DPPH radicals and ABTS radicals, chelating ability of ferrous ion and inhibition capability of Fe (II)-induced lipid peroxidation, respectively. The results revealed that all the tested phenolics showed strong radical scavenging activity, good potency to chelate Fe2+ and good inhibition ability of lipid peroxidation. Amongst mallotusinin and mucic acid 1,4-lactone 3-O-gallate were reported for the first time to have antioxidant activity. In addition, the in vitro antiproliferative activities of those phenolics against MCF-7 breast cancer cell lines were assessed. Although the growth inhibition values induced by different phenolics on MCF-7 cell line yielded different effects, all the tested phenolics had apparent capacities of inhibiting the survival of MCF-7 human cancer cell line.
... The medicinal values of fruits of P. emblica may be due to its phenolic compounds such as gallic acid, catechin, chlorogenic acid, caffeic acid, kaempferol, phyllanemblin, p-coumaric acid, quercetin, and geraniin. The methanolic crude extracts from P. acidus leaves and P. niruri had in-vitro porcine pancreatic lipase (PPL) inhibitory activity as 33.90% and 76.70%, respectively, when using p-nitrophenyl butyrate (pNPB) as a substrate [4]. Similarly, the chromatographic fractionation of the methanol extract of Eucalyptus globulus leaves yielded 2, 2,8-trimethyl-6-formyl-chrom-3-ene 7-O-β-D-glucopyranoside, quercetin 3-Oα-L-4C1 arabinopyranoside-2" gallate, cornusiin B, ellagitannins, galloyl esters, flavonoids, chromones, terpenoids, and eucalbanin B-like phenolic compounds, which have good antioxidant potential [5]. ...
... The ethanolic extracts of P. emblica demonstrated higher activity for scavenging DPPH radicals, reducing power, and inhibiting lipid peroxidation than the commercial and hot water extracts. This result agrees with Liu et al. (2008) and Luo et al. (2011), who reported that a phenolics compound isolated from P. emblica exhibited strong radical scavenging activity, good potency to chelate Fe 2+ , and good inhibition of lipid peroxidation [3,4]. These phenolics compounds included gallic acid, ellagic acid, mucic acid 1,4-lactone 3-O-gallate, isocorilagin, chebulanin, chebulagic acid, and mallotusinin, which could be the sources of antioxidant properties of ethanolic extracts. ...
... The ethanolic extracts of P. emblica demonstrated higher activity for scavenging DPPH radicals, reducing power, and inhibiting lipid peroxidation than the commercial and hot water extracts. This result agrees with Liu et al. (2008) and Luo et al. (2011), who reported that a phenolics compound isolated from P. emblica exhibited strong radical scavenging activity, good potency to chelate Fe 2+ , and good inhibition of lipid peroxidation [3,4]. These phenolics compounds included gallic acid, ellagic acid, mucic acid 1,4-lactone 3-O-gallate, isocorilagin, chebulanin, chebulagic acid, and mallotusinin, which could be the sources of antioxidant properties of ethanolic extracts. ...
Phyllanthus emblica L. is traditionally used as both medicine and food in Taiwan. In this study, we evaluated the antioxidant, anti-inflammatory, and neuroprotection bioactivities of P. emblica fruit. P. emblica fruit extracts had a high content of total phenol and flavonoids, and chlorogenic acids. For antioxidant capacity, 95% ethanol-extracted P. emblica had the best DPPH radical scavenging activity, ferrous ion chelating ability, and reducing power as compared with hot water, 50% ethanol, and commercial extracts, and showed the highest reducing power and lipid peroxidation inhibition. The present results have demonstrated that the P. emblica extracts can protect the oxidative degradation of lipids by inhibiting FeCl3-ascorbate-mediated lipid peroxidation. For anti-inflammatory activity, P. emblica fruit extracts showed dose-dependent inhibition of nitric oxide in lipopolysaccharide-stimulated RAW264.7 cells and significantly high COX-2 inhibition. For neuroprotection bioactivity, P. emblica extracts had higher percentages of pheochromocytoma cell protection than commercial extracts. Hot water and ethanol extracts showed higher percentages of PC12 cell protection than commercial extracts. P. emblica hydroalcoholic extracts had a neuroprotective effect against oxidative damage, which could be due to their antioxidant and anti-inflammatory activity. P. emblica extracts could be used in daily health beverages, foods, and cosmetic products.
... The antibacterial activity of FPE and its major phytocompounds, viz., gallic acid (Luo et al., 2011;Zhang et al., 2017), ellagic acid (Luo et al., 2011;Zhang et al., 2017), rutin (Che et al., 2022), and quercetin (Zhang et al., 2003;Liu et al., 2008), was evaluated by determining the minimum inhibitory concentration (MIC) using the broth dilution method, following the guidelines provided by the Clinical and Laboratory Standards Institute (CLSI, 2016). The FPE extract was dissolved in DMSO at a concentration of 1 mg/mL (w/v) and added to the first well of a 96-well microtiter plate. ...
... The antibacterial activity of FPE and its major phytocompounds, viz., gallic acid (Luo et al., 2011;Zhang et al., 2017), ellagic acid (Luo et al., 2011;Zhang et al., 2017), rutin (Che et al., 2022), and quercetin (Zhang et al., 2003;Liu et al., 2008), was evaluated by determining the minimum inhibitory concentration (MIC) using the broth dilution method, following the guidelines provided by the Clinical and Laboratory Standards Institute (CLSI, 2016). The FPE extract was dissolved in DMSO at a concentration of 1 mg/mL (w/v) and added to the first well of a 96-well microtiter plate. ...
Phyllanthus emblica L. (syn. Emblica officinalis), popularly known as amla, Indian gooseberry, or the King of Rasyana, is a member of Phyllanthaceae family and is traditionally used in Ayurveda as an immunity booster. The present study aimed to investigate the synergistic interaction of Phyllanthus emblica (FPE) fruits and its selected phytocompounds with ampicillin against selected bacteria. Further, an in silico technique was used to find if major phytocompounds of FPE could bind to proteins responsible for antibiotic resistance in bacterial pathogens and enhance the bioactivity of ampicillin. FPE and all the selected phytocompounds were found to have synergistic antibacterial activity with ampicillin against tested bacteria in different combinations. However, ellagic acid and quercetin interactions with ampicillin resulted in maximum bioactivity enhancement of 32–128 folds and 16–277 folds, respectively. In silico analysis revealed strong ellagic acid, quercetin, and rutin binding with penicillin-binding protein (PBP-) 3, further supported by MD simulations. Ellagic acid and quercetin also fulfill Lipinski’s rule, showing similar toxicity characteristics to ampicillin. FPE showed synergistic interaction with ampicillin, possibly due to the presence of phytocompounds such as gallic acid, ellagic acid, quercetin, and rutin. Molecular docking and MD simulations showed the strong interaction of ellagic acid and quercetin with PBP-3 protein. Therefore, these compounds can be explored as potential non-toxic drug candidates to combat bacterial antimicrobial resistance.
... Extracts prepared from plants rich in hydrolysable tannins (HTs) produced antiproliferative effects in various cancer cell lines [68,69]. For instance, pomegranate fruit husk water [70] and S. cumini pulp 75% aqueous acidified ethanol [71] extracts contained punicalagin and ellagic acid that contributed to their cytotoxic activities in cancer cells. ...
... Pellati et al. [72] determined chemoprotective activities of HTs isolated from T. chebula fruits decoction where punicalagin > chebulinic acid > chebulagic acid > 3,4,6-tri-O-galloyl-β-D-glucose > corilagin produced more than 80% cancer cell death. The ellagitannins (ETs) isolated from P. emblica, including ellagic acid, corilagin, chebulagic acid, and elaeocarpusin, also exhibited an anti-proliferative effect [68,69]. The findings from the present study also suggest that the observed impact on Hep G2 cell viability could be due to high EA or HT contents in the NT fruits. ...
Growing location is known to affect the metabolite content and functionality of wild harvested fruits. Terminalia ferdinandiana, commonly known as Kakadu plum (KP), is among the most commercially important native Australian bush foods. Therefore, we evaluated the composition and in vitro bioactivity of aqueous acidified ethanol (AAE) and water extracts prepared from KP fruit wild harvested in the Northern Territory (NT) and Western Australia (WA). Compositional analysis included vitamin C, total ellagic acid (TEA), and total phenolic content (TPC), while in vitro bioactivity was assessed through anti-inflammatory (RAW 264.7 macrophages) activity and cell viability (Hep G2) assay. The IC50 of the extracts ranged from 33.3 to 166.3 µg/mL for NO inhibition and CC50 from 1676 to 7337 µg/mL for Hep G2 cell viability inhibition. The AAE KP fruit extracts from the NT exhibited potent anti-inflammatory activity and impacted Hep G2 cell viability more than other extracts, most likely due to TEA (3189 mg/100 g dry weight (DW)), vitamin C (180.5 mg/g DW) and TPC (196 mg GAE/g DW) being higher than in any other extract. Overall, the findings of the present study are promising for using KP fruit and derived products in functional foods, nutraceuticals, or dietary supplements.
... such as mucic acid-1,4-lactone-3-O-gallate, ellagic acid, and isocorilagin in methanolic extracts from Amla could chelate ferrous ion [73]. Since Ag NPs have a negative zeta potential value in their pure form [67], a possible mechanism of silver particle capping should involve for the main part the interactions between hydrogen atom of the -OH groups and silver metal [75], as schematized in Fig. 6c. ...
Despite the growing need for effective and environmentally friendly antimicrobial agents, the synthesis methods for such materials often involve toxic chemicals and complex procedures. There is a pressing need for a sustainable approach to synthesize nanoparticles with potent antibacterial properties. This study aims to address this gap by developing a green synthesis method for silver nanoparticles (Ag NPs) using Amla extract. Powder X-ray diffraction (XRD), UV–Vis absorption spectroscopy, and Transmission Electron Microscopy (TEM) demonstrated that face-centered cubic Ag NPs with sizes in the range of 15–30 nm can be synthesized through an environmentally friendly process. Further, the formation mechanism of Ag NPs has been discussed in detail with the help of schematic diagrams. The Amla-derived Ag NPs have been further tested for their antibacterial activity against two different antibacterial strains: Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) using the plate count method. The NPs showed excellent biocompatibility where approximately 90% of growth reduction have been found for both strains at 100 μg/mL of Ag NPs and growth time of 30 min. These outcomes exhibited that Ag NPs, as a kind of antibacterial material, had an incredible guarantee for application in a wide scope of biomedical applications.
... Many pharmacological investigations have found that the therapeutic properties of P. emblica plants concentrate in the fruit, which is an excellent source of chemical metabolites, including saponins, flavonoids, tannins, steroids, and glycosides (Poltanov et al. 2009;Luo et al. 2011). Several flavonoid compounds found in P. emblica fruit are kaempferol-3-O-α-L-(6″-ethyl) rhamnopyranoside, kaempferol-3-O α-L-(6″methyl)-rhamnopyranoside, βamyrin, β-amyrin-3-palmitate, betulinic acid, daucosterol, oleanolic acid, triacontanoic acid, triacontanol, ketone, lupeol acetate, gallic acid, ursolic acid, quercetin, and bisabolane (Habib-ur-Rehman et al. 2007;Pientaweeratch et al. 2016). ...
Nazaruddin, Rosmaidar, Siregar TN, Wahyuni S, Sutriana A. 2024. Phytocomponents analysis and antioxidant activity of Malacca fruit extract (Phyllanthus emblica) using three different solvents. Biodiversitas 25: 1911-1919. Malacca plant (Phyllanthus emblica L.) grows widely in Aceh Province, Indonesia representing a wide group of phytochemical components of medicinal usage. This study aims to assess the antioxidant activity and bioactive compounds in P. emblica fruit extract, which was extracted by subsequent extraction using n-hexane, ethyl acetate, and ethanol. The extracts were then subjected to phytochemical and GC-MS to identify and quantify the bioactive compounds and measure the radical scavenging using DPPH assay to estimate the antioxidant activity. The results showed that P. emblica fruit extracted with ethanol and ethyl acetate contained flavonoids, phenolics, terpenoids, and saponin compounds, while n-hexane extract only contained steroids. The antioxidant activity of ethanol, ethyl acetate, and n-hexane extracts was very strong, with IC50 values of 18.81, 20.75, and 31.01 ppm, respectively. The highest antioxidant activity was found in the ethanol extract of P. emblica fruit. The GC-MS analysis revealed that the most abundant chemical component in ethanol and ethyl acetate extract was 1, 2, 3 benzenetriol, while in n-hexane extract was eugenol. Based on bioactive components and antioxidant activity, ethanol is suggested as the optimal solvent to gain a high content of polyphenols and flavonoids as well as high antioxidants from P. emblica fruit for utilization in pharmacognosy.
... Traditional medicine practices have often informed the identification of biologically active natural products, such as in the cases of artemisinin and reserpine, which had originally been isolated from traditional Chinese medicine (TCM) preparations and subsequently developed into medicines [5]. Phyllanthus emblica L., mainly distributed in subtropical and tropical parts of southeast Asia, has been used for thousands of years in traditional Chinese and Indian medicine for treating diseases such as hemorrhage, diarrhea, jaundice, and dyspepsia etc. [6][7][8][9]. Modern research has shown that the emblica fruit is a rich source of phenolics, which display a wide range of activities including anti-oxidant [10], anti-viral [11], anti-microbial [12], anti-tumor [13] and anti-bacterial effects [14]. In addition to its medicinal applications, the emblica fruit is also highly nutritious, containing high levels of vitamin C, amino acids, and various minerals [15][16][17]. ...
An undescribed pyrrole acid, 1-(4′-methoxy-4′-oxobutyl)-1 H -pyrrole-2,5-dicarboxylic acid ( 1 ) and one known pyrrole acid ( 2 ) were isolated from the fruits of Phyllanthus emblica. The structures of these compounds were elucidated via the comprehensive analyses of IR, HRESIMS, 1D and 2D spectroscopic data. A series of biological assays revealed that compounds 1 and 2 could inhibit LPS-induced over-production of nitric oxide (NO), interleukin-6 (IL-6), monocyte chemotactic protein 1 (MCP-1) and tumor necrosis factor-α (TNF- α ) by reducing the phosphorylation of extracellular regulated protein kinases (ERK) and c-Jun N-terminal kinases (JNK) in RAW 264.7 cells. Additionally, compounds 1 and 2 were found to reduce lipid deposition and increase the mRNA expression of ATP-binding cassette transporter A1 in oxidized low-density lipoprotein-treated RAW264.7 macrophages.
Graphical abstract
... Phyllanthus emblica (P emblica) L., family Euphorbiaceae, is widely distributed in the subtropical and tropical areas of Southeast Asia. 1 Its fruit, commonly known as Amla and Indian gooseberry, is well accepted by consumers for its sweet and slightly astringent taste 2 and various medicinal benefits, including antioxidant, [3][4][5] antimicrobial, 6 antidiabetic, 7 cardioprotective, 8 anticancer, 9,10 and anti-inflammatory 11 activities. Previous phytochemical studies of P emblica fruit have revealed the presence of ellagitannins, gallotannins, anthocyanins, vitamin C, mucic acids, and phenolic acids. ...
Objective: The present study aimed to investigate the potential bioactive compounds from Phyllanthus emblica L. fruit. Methods: Acetone extracts (60%) of P emblica fruit were dissolved in water and fractionated sequentially with light petroleum and ethyl acetate (EtOAc). The water fraction was separated using Sephadex LH-20 and the isolated compounds were purified by preparative high-performance liquid chromatography. The structures of the isolated compounds were determined through HR-ESI-MS and spectroscopic methods, including 1D- and 2D-NMR, and the antioxidant abilities of the isolates were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays. Results: Three new phenolic compounds, mucic acid 1-ethyl ester 3- O-gallate (1), mucic acid 6-methyl ester 3- O-gallate (2), and mucic acid 6-ethyl ester 2- O-gallate (3), together with 4 known compounds (4-7), were isolated from P emblica fruit. All phenolics exhibited potent antioxidant abilities (DPPH: IC 50 7.5-13.2 µM; ABTS: 1.12-2.84 µM Trolox/µM; FRAP: 1.11-2.26 µM Fe ²⁺ /µM). Conclusions: Our research contributes to the growing body of evidence demonstrating the benefits of P emblica for health and supports the functional food and nutraceutical applications of the fruit.
... In the presence of other chelating agents or antioxidants, the complex formation is disrupted, as determined by a reduction in the purple colour of the complexes. As the extract concentration is increased, the amount of iron (II) chelated is also increased (Luo et al., 2011). ...
Abstract
Berries are highly valued crops due to their unique flavour, texture, colour and phytochemicals. They are rich in phenolic compounds which have been recognized as having beneficial health effects in humans. Phenolic compounds are present in the free, soluble ester and insoluble-bound forms; these were extracted using four different solvents {methanol–acetone–water (7:7:6, v/v/v), acetone-water (80: 20, v/v), methanol-water (70: 30, v/v), and water}. The insoluble-bound phenolics were procured after alkaline hydrolysis and subsequent extraction into diethyl ether-ethyl acetate. Phenolic extracts of each fraction were separately assayed for their antioxidant activity using several methods, namely oxygen radical absorbance capacity (ORAC), the reducing power capacity, as well as iron (II) chelation capacity, among others. There were significant differences in the total content of phenolics, flavonoids, and anthocyanins between blackberry, black raspberry, and blueberry seed meals. The bound phenolics contributed the highest proportion to the total contents of different classes of phenolics. Furthermore, blackberry seed meals had higher total antioxidant activity compared with black raspberry and blueberry seed meals in all assays employed. High-performance liquid chromatography−diode array detection−electrospray ionization multistage mass spectrometry (HPLC-DAD-ESI-MSn) was used to identify and quantify the phenolic compounds. Hydroxybenzoic and hydroxycinnamic acids, anthocyanins, flavonols, flavan-3-ols, and proanthocyanidins were identified and quantified in the aforementioned fractions. Extracts were found to contain various levels of phenolic compounds that were specific to each berry seed meal type.
... Moreover, Phyllanthus Emblica fruit is one of the essential and broadly used herbs in traditional medicinal system such as Ayurvedic medicine, Chinese herbal medicine and Tibetan medicine Gaire et al. [8]. Previously, most of the studies exhibited that Phyllanthus emblica had good health effects as antioxidant, anti-diabetic, anti-microbial, anti-inflammatory and hepatoprotective agent (Yang et al. [9]; Yadav et al., [10]. The major phytochemical constituents present in Phyllanthus Emblica fruits, and their pharmacological activity is summarized in Table 4. ...
... ROS has been reported to be associated with diseases such as diabetes, Alzheimer's disease, coronary heart disease, nephritis, cancer, arteriosclerosis, and diseases related to ageing (Chen and Kan, 2018). Related scholars evaluated the free radical scavenging ability by in vitro anti-oxidant tests, which showed that PF extracts have strong metal chelating, reducibility, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) scavenging and DPPH scavenging ability (Wei et al., 2011;. PF also has a scavenging effect on hydroxyl radicals and superoxide radical O 2 via Fenton Reaction . ...
Phyllanthi Fructus (PF), the edible fruits of Phyllanthus emblica L., serves as an important resource for some health products, foods and drugs due to its high safety and sufficient nutritional value. In recent years, in vivo and in vitro experiments have been conducted to reveal the active components of PF. More than 180 compounds have been isolated and identified from the PF so far, primarily including tannins, phenolic acids, flavonoids, terpenoids, polysaccharides, fatty acids and amino acids. In traditional Chinese medicine (TCM), PF is used to cure several diseases such as bronchitis, asthma, diabetes, peptic ulcer, hepatopathy, leprosy, and jaundice. Consistent with ethnopharmacology, numerous modern studies have demonstrated that the extracts or monomeric compounds derived from PF exhibit various pharmacological effects including anti-oxidation, anti-bacteria, anti-inflammation, anti-tumour, anti-virus, immunity improvement, hypoglycemic and hypolipidemic effects, and multiple organ protective protection. Toxicological studies on PF indicated the absence of any adverse effects even at a high dose after oral administration. Due to strict quality control, these pharmacological activities and the safety of PF greatly improve the development and utilization of products. Our comprehensive review aims to summarize the phytochemistry, pharmacological effects, toxicology, and product development of PF to provide theoretical guidance and new insights for further research on PF in the future.
... Waktu perendaman semakin lama semakin melunakkan dinding sel bahan sehingga komponen bioaktif yang dapat dilepaskan semakin banyak. (Ghosal et al., 1996;Hasan et al., 2016;Usharani et al., 2013;Yang dan Liu, 2014) Emblicanin B C34H20O22 Antioksidan, kardioprotektif, antiinflamasi (Ghosal et al., 1996;Hasan et al., 2016;Usharani et al., 2013) (Luo et al., 2011;Variya et al., 2016) Kuersitin C15H10O7 Kemoprotektif, antidiabetes, hepatoprotektif (Luo et al., 2009;Srinivasan et al., 2017;Variya et al., 2016) Puniglukonin C34H26O23 Antioksidan, antiinflamasi (Hasan et al., 2016;Variya et al., 2016) Pedunkulagin C34H24O22 Antioksidan, gonadotropik, antiinflamasi (Hasan et al., 2016;Khaled et al., 2019;Variya et al., 2016) Antioksidan, antiinflamasi immunomodulator (Bhagat, 2016;Mathai et al., 2015;Scartezzini et al., 2006) Pelarut yang telah digunakan untuk ekstraksi buah malaka antara lain aseton (Zhang et al., 2001), air (Majeed et al., 2009), etanol (Luo et al., 2009Okonogi et al., 2010;Zhang et al., 2014), metanol (Liu et al., 2008), dan etil asetat (Kumari dan Khatkar, 2016). Pelarut yang paling efektif untuk mengekstrak komponen bioaktif buah malaka adalah metanol dibanding pelarut lainnya (etanol dan etil asetat, dan air). ...
The bioactive components of malacca (Emblica officinalis), which consist of phenolic, alkaloids, phytosterols, organic acids, and vitamins, are valuable for human health. T he yield and quality of the bioactive components in the extract highly depend on the extraction technique, so it is essential to know the development of research on extraction techniques of the bioactive components of malacca fruit. In addition, the bioactive components in the extract have limitations in their application due to their stability, solubility, absorption, and bioavailability properties. Currently, nanoencapsulation technology has been applied to extracts of bioactive components to improve their properties. This review aims to provide comprehensive information about extraction techniques to obtain bioactive components of malacca fruit and presents the technique and purpose of the nanoencapsulation of malacca fruit extract. In addition to conventional techniques, several modern extraction techniques such as microwave-assisted extraction (MAE), ultrasound (UAE), pulsed electric field (PEF), and supercritical fluid (SFE) have been used to extract bioactive components of malacca fruit. Modern extraction techniques can produce extracts of bioactive components with higher yields than conventional techniques. The application of nanoencapsulation technology to malacca fruit extract consists of nanoliposomes and nanoparticles can increase permeability, antioxidant activity, antidiabetic and anti-inflammatory properties of malacca fruit extract.
... Furthermore, Amla extracts have also been observed to alter the levels of lipid peroxidation and anti-oxidant enzymes [13] . The phenolic fraction of the fruit has been documented to achieve anti-oxidant dependent would healing activity both in vitro and in vivo [14,15,16] . Moreover, butanolic fraction of Amla has been shown to reduce Malondialdehyde (MDA), a product of lipid peroxidation and superoxide radical [15] . ...
The Indian Gooseberry is one of the commonly used plants in the Indian system of medicine. Amla is a wonder superfood, belonging to the genus Phyllanthus L. which is mainly distributed in tropical areas. It represents a phytochemical reservoir of biologically important molecules. The plant contains tannins, alkaloids, amino acids, carbohydrates, vitamins and organic acids. Various parts of the plant have been used to treat a wide array of diseases. The present article highlights the importance of Phyllanthus emblica in the prevention and treatment of ulcer. Gastrointestinal ulcer results due to an increase in the offensive factors as compared to defensive ulcer protective elements. The fruit extracts possesses potent anti-oxidant potential which is the key to its therapeutic effect. Additionally it is also capable of inducing neo-angiogenesis thereby helping in repair of gastric lesions. The anti-inflammatory potential of the above further accelerates ulcer healing. Owing to its anti-secretory and cyto-protective capacities, Phyllanthus emblica either alone or in combination represents a valuable natural strategy to treat several chronic diseases especially ulcer.
... Gallic acid present in small quantities in EOE also has similar effects. 42 The various compounds constituting EOE have excellent ROS inhibiting activity, thus, resulting in the reduction of oxidative stress, and consequently attenuate diabetic complications. ...
The efficacy of Emblica officinalis extract (EOE) containing 10% β-glucogallin was compared against metformin in newly diagnosed subjects with diabetic dyslipidemia which is a significant factor in cardiovascular disease. Daily administration with EOE-1 g, EOE-2 g, or metformin 500 mg for 90 days significantly decreased fasting blood sugar and postprandial blood sugar (FBS and PPBS), hemoglobin A1c (HbA1c) and lipid levels in all three treatment groups. The FBS, PPBS and HbA1c were significantly lower in the EOE-2 g group compared with metformin and EOE-1 g groups. The reductions in LDL and TC in the EOE-2 g group were also significantly higher than in the EOE-1 g group and were comparable to the metformin group. No serious adverse effects were observed in any study participants. EOE-1 g and 2 g day-1 are safe and potent antidiabetic agents, with comparable efficacy to the pharmaceutical drug, metformin. Supplementation with EOE-2 g day-1 showed greater efficacy than metformin in reducing circulating glucose levels.
... In general, phenolic compounds play a role in the protection of an organism against the actions of reactive oxygen species [54]. Polyphenols are compounds with antioxidant, anticancer, antiviral, antibacterial, and antimicrobial activities [55]. Recently, de Olivera et al. [56] found that p-coumaric acid, p-coumaric acid 4-O-hexoside, apigenin 7-glucoside, and quercetin-Opentosyl-hexoside are the main phenolics in PL. ...
Parsley leaves (PL) are a rich source of many bioactive compounds and show many health-promoting properties. The aim of this study is to analyze the effect of the addition of PL to wheat flour on the physical, antioxidant, and sensory properties of wheat bread. Wheat flour was partially substituted with 0, 1, 2, 3, 4, and 5% PL. Bread dough was prepared using the direct method. Bread loaves were cooled, and then their volume, texture, color, total phenolic content, and antioxidant activity were evaluated. In addition, a sensory evaluation of bread was performed. Incorporation of PL into wheat decreased the bread volume and increased the crumb moisture but had little influence on the crumb texture. The crumb of the enriched bread was darker and greener compared with the control sample. PL addition increased the redness of the crumb as well. The total color difference for the enriched bread ranged from 9.3 to 21.4. According to the sensory evaluation, the amount of wheat flour added to PL should not exceed 3%. Such a kind of bread showed about a twofold higher level of phenolic compounds and enhanced antioxidant activity compared with the control bread. This study showed that powdered PL can be a valuable nutritional supplement to wheat bread. Future research should focus on the possibilities of fortifying various types of food with this additive.
... So, the antigenotoxic potential of the leaves extract may be due to the presence of these phenolic and flavonoid compounds. A review of the literature revealed that many medicinal plants with high phenolic content have been linked to chemopreventive and anticancer activity [68][69][70][71][72] . ...
Roylea cinerea (D.Don) Baillon an indigenous medicinal plant of Lamiaceae family used for the treatment of several diseases. In the present study, its aqueous (leaves) extract was tested for genoprotective action against atrazine-induced chromosomal aberrations in the root tip cells of Allium cepa. Atrazine is a herbicide of triazine class commonly used to inhibit the growth of broad leaf and grassy weeds. In order to find the concentration of atrazine that exhibits maximum toxicity, its different concentrations (1, 5 and 10 µg/mL) were tested. It was observed that 10 µg/mL concentration was more toxic as it reduced the mitotic index and also increased the chromosomal aberrations. Among all the tested concentrations of aqueous (leaves) extracts (0.25. 0.5, 1.0, 1.5 and 3.0 µg/mL), the3.0 µg/mL concentration in both modes of experiments i.e. pre and post showed a significant reduction in chromosomal aberrations induced by atrazine. To understand the mechanism of protection by plant extract on atrazine-induced chromosomal abnormalities the RT-qPCR studies were conducted to observe the expression of marker genes Cyclin-dependent kinases (CDKs) (CDKA:1, CDKB2:1 and CDKD1:1. For this, the RNA was extracted from root tips treated with extract along with atrazine by TRIzol®. It was observed that aqueous extract of Roylea cinerea (D.Don) Baillon leaves upregulated the CDKs gene expression in both the modes i.e. pre and post treatments. A critical analysis of results indicated that aqueous extract ameliorated the chromosomal aberrations caused by atrazine which may be be due to the increased expression level of CDKs genes.
... Meanwhile, L. hatsudake extracts activate p38 and may also promote the apoptosis of cancer cell HCT116 ( Figure 6). Aside from altering apoptosis gene expression, DNA damage is also an important factor in HCT116-cell apoptosis, which is an important molecular target in the killing of tumor cells [34,35]. Importantly, the decreased phosphorylated proteins of ERK1/2 and JNK, were found to be downstream target kinases of DNA damage-induced apoptosis [36]. ...
Cancer is still the leading cause of death across the world, and there is a lack of efficient therapies. Lactarius hatsudake is a mushroom with a food and medicine homology that contains numerous biologically active substances. This study aimed to investigate the composition of extracts from Lactarius hatsudake (L. hatsudake) and their anti-cancer function and molecular mechanisms. Our results showed that the total phenolic content of L. hatsudake extracts was 139.46 ± 5.42 mg/g. The following six phenolic compounds were identified from L. hatsudake extracts by HPLC and UPLC-QTOF/MS: gallic acid, pyrogallol, chlorogenic acid, ferulic acid, myricetin, and cinnamic acid. Colorectal cancer cell HCT116 and hepatic cancer cell HepG2 were used to evaluate the anti-cancer function of the L. hatsudake extracts. Compared with HepG2 cells, the L. hatsudake extracts showed stronger anti-cancer activity against HCT116 cells and these were used to study molecular mechanisms. The results indicated that the L. hatsudake extracts could arrest the cancer cell cycle and inhibit cancer cell proliferation, which may be mediated by the MAPK/NFκB/AP-1 signalling pathway; the L. hatsudake extracts also promoted cancer cell apoptosis through a mitochondrial-dependent pathway. Taken together, these findings demonstrate that L. hatsudake ethanol extracts contain six main phenolics and illustrate the remarkable potentiality of L. hatsudake as a source of natural phenolics for cancer prevention and as an adjuvant in the treatment of functional foods.
... Bioactive compounds such as carotenoids, phenolic compounds and flavonoids have been widely studied for their health benefits [2]. The flavonoids including flavan-3-ols have been reported to have chelating, and radical scavenging properties, in addition to acting as enzymes mediator/inhibition, and having anti-viral activities [3]. ...
Baobab fruit (Adansonia digitata L) is rich in micronutrients and bioactive compounds, which are vital for healthy living. Boabab juice are produced locally and stored under different storage conditions in Malawi. However, storage of baobab juice under certain conditions can lead to degradation of its bioactive compounds. This study therefore investigated the bioactive compounds in Commercial baobab juice (CBJ) in Malawi, and determined the stability of the compounds under different storage conditions. The organic acids, flavan-3-ol aglycones, total phenolic contents and antioxidant activities of the CBJ were determined using standard methods. The stability of the bioactive compounds in CBJ were determined in the samples stored at 6, 15 and 30 ⁰C for 49 days. The ferric reducing antioxidant power of CBJ was 71.27±.04 TEAC/100 g FW, and the ABTS (2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid) was 112.62± 0.45 mg TEAC/100 g FW. The 2,2-diphenyl-1-picrylhydrazyl was 80.94 ± 0.72 %. CBJ bioactive compounds are stable at 15 ⁰C, and contains high concentrations of total phenolic compounds, antioxidant activities and procyanidin B2 . In conclusion, commercially sold baobab juice in Malawi is rich in bioactive compounds and have high antioxidant properties, thus, regular consumption of the juice can improve the health and wellbeing of Malawians. Information provided in this study will provide consumers with nutritional profile of CBJ and help juice processors establish adequate storage conditions for the juice.
... Also, PE fruit is rich in vitamin C, luteolin, and corilagin. [11][12][13][14] This study aim to determine the antioxidant activity, total phenol, and total flavonoid of Phyllanthus emblica ethanol extract. ...
... Their structure contains a number of hydroxyl groups that can provide hydrogen ions and then form strong coordination oxygen ion complexes with metal ion. Consequently, these polyphenols can directly trap free radicals and/or act through metal chelation, leading to the termination of free radical chain reactions [2,23]. In this study, flavanols and phenolic acids were identified as the most abundant phenolic compounds in PE fruits. ...
Phyllanthus emblica L. (PE) is commonly known as a medicine and food homologous plant, which is abundant in natural products polyphenols. In the present study, polyphenols were extracted from PE fruit by response surface method, and the anti-aging ability was determined. PE fruit polyphenols exhibited strong antioxidant capacities in scavenging free radicals, and anti-cholinesterase ability by inhibition of AChE (IC50 0.2186 ± 0.0416 mg/mL) and BuChE (IC50 0.0542 ± 0.0054 mg/mL) in vitro. Moreover, PE fruit polyphenols showed strong protective effect against the aging process in Caenorhabditis elegans model, including increased thermal resistance, extended lifespan by 18.53% (p < 0.05), reduced activity of AChE by 34.71% and BuChE by 45.38% (p < 0.01). This was accompanied by the enhancement in antioxidant enzymes activity of SOD by 30.74% (p < 0.05) and CAT by 8.42% (p > 0.05), while decrease in MDA level by 36.25% (p < 0.05). These properties might be interrelated with the presence of abundant flavonols and phenolic acids identified by UPLC-ESI-QTOF-MS, such as quercetin, myricetin, ellagic, gallic, and chlorogenic acids, together with their glycosides. The remarkable antioxidant and anti-aging potential of PE fruit polyphenols could be implemented in the food and pharmaceutical industry.
... The fruit of P. emblica contains many polyphenols, with a content as high as 14% of the dry fruit weight (Guo et al., 2013). Polyphenols are the main active substances with physiological functions (Luo et al., 2011;Majeed et al., 2009;Zhang et al., 2017). ...
Phyllanthus emblica L. pomace is a waste residue obtained following juicing that contains many polyphenols. In this study, NKA‐II resin was selected as the optimal macroporous resin for separation and employed to separate the crude polyphenol extract of P. emblica pomace. The separation conditions were optimized, and the polyphenol content, polyphenol components, antioxidant activity, and potential anti‐Alzheimer's effects of the extract were measured before and after purification. Results showed that the polyphenol content of the purified extract was 656.85 mg/g, which was 2.1 times higher than that of the nonpurified form. Further, the polyphenol components of the pomace, which was like that of the fruit, did not vary after purification. The antioxidant activity of the purified extract was also significantly improved. Moreover, purified extract significantly reduced the paralysis rate of the transgenic Caenorhabditis elegans model of Alzheimer's disease, and the mechanism was related to maintenance of redox homeostasis.
Practical Application
The polyphenol content and antioxidant activity of purified polyphenol from Phyllanthus emblica L. pomace extracts were significantly improved using optimal separation methods with NKA‐II macroporous resin and 70% aqueous ethanol as the eluent in this study. Moreover, purified polyphenols showed potential effects in alleviating Alzheimer's disease. These results suggest that polyphenols separated from P. emblica pomace are valuable for further research and development, and the utilization rate of P. emblica fruit is improved due to the further development of P. emblica pomace.
... A strong correlation between antioxidant activities and TPCs was also observed [9,10]. High antioxidant activity in P. emblica fruit resulted from the biological functions of its phenolics [11]. Phenolics in P. emblica fruit from China were geraniin, quercetin 3-β-D-glucopyranoside, isocorilagin, and kaempferol [7], while another group reported cinnamic acid, quercetin, 5-hydroxymethylfurfural, gallic acid, β-daucosterol, and ellagic acid [12]. ...
Thailand has vast areas of tropical forests with many indigenous plants, but limited information is available on their phytochemical profile and in vitro inhibitions of enzymatic and nonenzymatic reactions. This study investigated phenolic profiles using liquid chromatography–electrospray ionization tandem mass spectrometry (LC–ESI-MS/MS), antioxidant activities, and in vitro inhibitory activities of 10 indigenous plants on key enzymes related to obesity (lipase), diabetes (α-amylase and α-glucosidase), and Alzheimer’s disease (cholinesterases and β-secretase). The nonenzymatic anti-glycation reaction was also investigated. The 10 indigenous plants were Albizia lebbeck (L.) Benth, Alpinia malaccensis (Burm.) Roscoe, Careya arborea Roxb., Diplazium esculentum (Retz.) Swartz, Kaempferia roscoeana Wall., Millettia brandisiana Kurz., Momordica charantia, Phyllanthus emblica L., Zingiber cassumunar Roxb, and Zingiber citriodorum J. Mood & T. Theleide. Preparations were made by either freeze-drying or oven-drying processes. Results suggested that the drying processes had a minor impact on in vitro inhibitions of enzymatic and nonenzymatic reactions (<4-fold difference). P. emblica was the most potent antioxidant provider with high anti-glycation activity (>80% inhibition using the extract concentration of ≤6 mg/mL), while D. esculentum effectively inhibited β-secretase activity (>80% inhibition using the extract concentration of 10 mg/mL). C. arborea exhibited the highest inhibitory activities against lipase (47–51% inhibition using the extract concentration of 1 mg/mL) and cholinesterases (>60% inhibition using the extract concentration of 2 mg/mL), while Mi. brandisiana dominantly provided α-amylase and α-glucosidase inhibitors (>80% inhibition using the extract concentration of ≤2 mg/mL). Information obtained from this research may support usage of the oven-drying method due to its lower cost and easier preparation step for these studied plant species and plant parts. Furthermore, the information on in vitro inhibitions of enzymatic and nonenzymatic reactions could be used as fundamental knowledge for further investigations into other biological activities such as cell culture or in vivo experiments of these health-beneficial plants.
... µg/ml (Fig. 3). In the literature review on antioxidant activity of mucic acid derivatives, it was found that the fruit of Phyllanthus emblica L. yielded mucic acid derivatives with good antioxidant activity and the extracts from this fruit produced many phytochemical compounds having IC 50 values: gallic acid 18.71 ± 0.77, ellagic acid 13.81 ± 0.59, mucic acid 1,4-lactone 3-O-gallate 23.72 ± 1.05, isocorilagin 8.12 ± 0.59, chebulanin 11.27 ± 0.67, chebulagic acid 4.14 ± 0.19, and Mallotusinin 3.99 ± 0.11 µM, respectively (Luo et al., 2011). Another work also reported that mucic acid gallates isolated from P. emblica showed strong antioxidant activity with IC 50 values of 12.84 µM, by using DPPH method (Olennikov et al., 2015). ...
The main objective of the present study is to isolate and characterise the novel bioactive molecule, 2-methoxy mucic acid (4) from Rhizophora apiculate Blume under the Rhizophoraceae family. In this study, the 2-methoxy mucic acid (4) was isolated for the first time from the methanolic extract of the leaves of R. apiculata. Anticancer activity of 2-methoxy mucic acid (4) was evaluated against HeLa and MDA-MB-231 cancer cell lines and they displayed promising activity with IC50 values of 22.88283 ± 0.72 µg/ml in HeLa and 2.91925 ± 0.52 µg/ml in the case of MDA-MB-231, respectively. Furthermore, the antioxidant property of 2-methoxy mucic acid (4) was found to be (IC50) 21.361 ± 0.41 µg/ml. Apart from in vitro studies, we also performed extensive in silico studies (molecular docking and molecular dynamics simulation) on four critical antiapoptotic Bcl-2 family members (Bcl-2, Bcl-w, Bcl-xL and Bcl-B) towards 2-methoxy mucic acid (4). The results revealed that this molecule showed higher binding affinity towards Bcl-B protein (ΔG = -5.8 kcal/mol) and the structural stability of this protein was significantly improved upon binding of this molecule. The present study affords vital insights into the importance of 2-methoxy mucic acid (4) from R. apiculata. Furthermore, it opens the therapeutic route for the discovery of anticancer drugs. Research HighlightsThis is a first report on a bioactive compound identified and characterised; a novel 2-methoxy mucic acid derived from methanolic crude extract from the leaves of R. apiculata from ANI.Estimated binding free energy of 2-methoxy mucic acid is found to be -5.8 kcal/mol to the anti-apoptotic Bcl-B protein.2-methoxy mucic acid showed both significant anti-cancer and anti-oxidant activity.
... µg/ml (Fig. 3). In the literature review on antioxidant activity of mucic acid derivatives, it was found that the fruit of Phyllanthus emblica L. yielded mucic acid derivatives with good antioxidant activity and the extracts from this fruit produced many phytochemical compounds having IC 50 values: gallic acid 18.71 ± 0.77, ellagic acid 13.81 ± 0.59, mucic acid 1,4-lactone 3-O-gallate 23.72 ± 1.05, isocorilagin 8.12 ± 0.59, chebulanin 11.27 ± 0.67, chebulagic acid 4.14 ± 0.19, and Mallotusinin 3.99 ± 0.11 µM, respectively (Luo et al., 2011). Another work also reported that mucic acid gallates isolated from P. emblica showed strong antioxidant activity with IC 50 values of 12.84 µM, by using DPPH method (Olennikov et al., 2015). ...
The main objective of the present study is to isolate and characterise the novel bioactive molecule, 2-
methoxy mucic acid (4) from Rhizophora apiculate Blume under the Rhizophoraceae family. In this
study, the 2-methoxy mucic acid (4) was isolated for the first time from the methanolic extract of the
leaves of R. apiculata. Anticancer activity of 2-methoxy mucic acid (4) was evaluated against HeLa and
MDA-MB-231 cancer cell lines and they displayed promising activity with IC50 values of
22.88283 ± 0.72 mg/ml in HeLa and 2.91925 ± 0.52 mg/ml in the case of MDA-MB-231, respectively.
Furthermore, the antioxidant property of 2-methoxy mucic acid (4) was found to be (IC50)
21.361 ± 0.41 mg/ml. Apart from in vitro studies, we also performed extensive in silico studies (molecular
docking and molecular dynamics simulation) on four critical antiapoptotic Bcl-2 family members (Bcl-2,
Bcl-w, Bcl-xL and Bcl-B) towards 2-methoxy mucic acid (4). The results revealed that this molecule
showed higher binding affinity towards Bcl-B protein (DG ¼ �5.8 kcal/mol) and the structural stability
of this protein was significantly improved upon binding of this molecule. The present study affords
vital insights into the importance of 2-methoxy mucic acid (4) from R. apiculata. Furthermore, it opens
the therapeutic route for the discovery of anticancer drugs.
... Phosphatides, essential oils, phosphatides, essential oils, tannins (Luo et al. 2011) Phyllanthus niruri L Antimicrobial, anticancer, antinflammatory, antiplasmodial, antiviral, diuretic and hepatoprotective (Kaur et al. 2017) Rutin, Quercetin, Quercitrin, astragalin (Kaur et al. 2017) ...
The ethnopharmacological investigation was done to study the traditional usage of indigenous medicinal plants of Palampur, Himachal Pradesh. Therefore, an extensive ethnopharmacological survey was conducted to document the traditional knowledge of ethnomedicinal plants. Direct interviews of 77 informants were conducted with the help of a questionnaire. Three quantitative factors (use value, factor informant consensus and fidelity level) were used for the analysis of generated data. A total of 102 species, belonging to 90 genera and 30 families were identified and collected with the help of traditional healers and local informants from different locations of the study area. Total 19 medicinal plants species were reported for new or less known ethnomedicinal uses. Also, 3 threatened wild plants species were collected from the study area. The maximum number of species belongs to the family Lamiaceae (7), Fabaceae (7), Asteraceae (6), Moraceae (4 species), Apocyanaceae (4 species) and Euphorbiaceae (3 species). Different plant parts were used by local informants such as leaves, galls, fruits, seeds, latex, stem, root, flowers, bark, and rhizomes. It was also observed that maximum numbers of plant species were used to cure gastro-intestinal disorders (48 species), skin disorders (34 species) and respiratory disorders (25 species). Ethnopharmacological data depict that medicinal plants were extensively used by local people to cure gastrointestinal, dermatological disorders and skeletomuscular disorders. Traditionally used medicinal plants have enormous potential to provide the raw material for the discovery of new bioactive compounds and drugs.
... Phyllanthus L. is considered to be the largest genera of the family Phyllanthaceae having 900 species [8,9], distributed both tropically and subtropically [10]. Phyllanthus emblica L. is commonly used as medicine in Asia [11] for its antioxidant, anti-cancer, anti-inflammatory, anti-pyretic, diuretic, laxative, stomachic, cardioprotective, and hepatoprotective properties [9,10,[12][13][14][15]. The other genus, Leptopus Decne., is made up of nine species consisting of herbs and shrubs, which are distributed in Asia, America, and Europe and grow in open fields and in forests [16]. ...
Family Phyllanthaceae belongs to the eudicot order Malpighiales, and its species are herbs, shrubs, and trees that are mostly distributed in tropical regions. Here, we elucidate the molecular evolution of the chloroplast genome in Phyllanthaceae and identify the polymorphic loci for phylogenetic inference. We de novo assembled the chloroplast genomes of three Phyllanthaceae species, i.e., Phyllanthus emblica, Flueggea virosa, and Leptopus cordifolius, and compared them with six other previously reported genomes. All species comprised two inverted repeat regions (size range 23,921–27,128 bp) that separated large single-copy (83,627–89,932 bp) and small single-copy (17,424–19,441 bp) regions. Chloroplast genomes contained 111–112 unique genes, including 77–78 protein-coding, 30 tRNAs, and 4 rRNAs. The deletion/pseudogenization of rps16 genes was found in only two species. High variability was seen in the number of oligonucleotide repeats, while guanine-cytosine contents, codon usage, amino acid frequency, simple sequence repeats, synonymous and non-synonymous substitutions, and transition and transversion substitutions were similar. The transition substitutions were higher in coding sequences than in non-coding sequences. Phylogenetic analysis revealed the polyphyletic nature of the genus Phyllanthus. The polymorphic protein-coding genes, including rpl22, ycf1, matK, ndhF, and rps15, were also determined, which may be helpful for reconstructing the high-resolution phylogenetic tree of the family Phyllanthaceae. Overall, the study provides insight into the chloroplast genome evolution in Phyllanthaceae.
... µg/ml (Fig. 3). In the literature review on antioxidant activity of mucic acid derivatives, it was found that the fruit of Phyllanthus emblica L. yielded mucic acid derivatives with good antioxidant activity and the extracts from this fruit produced many phytochemical compounds having IC 50 values: gallic acid 18.71 ± 0.77, ellagic acid 13.81 ± 0.59, mucic acid 1,4-lactone 3-O-gallate 23.72 ± 1.05, isocorilagin 8.12 ± 0.59, chebulanin 11.27 ± 0.67, chebulagic acid 4.14 ± 0.19, and Mallotusinin 3.99 ± 0.11 µM, respectively (Luo et al., 2011). Another work also reported that mucic acid gallates isolated from P. emblica showed strong antioxidant activity with IC 50 values of 12.84 µM, by using DPPH method (Olennikov et al., 2015). ...
In this present study, the sugar based bioactive molecule, 2-methoxy mucic acid ( 4) was isolated for the first time from the methanolic extract from the leaves of Rhizophora apiculata . The structure of compound was well characterized by different spectroscopic analysis, including FT-IR, 1 H, 13 C NMR spectroscopy and HRMS. Anticancer activity of 2-methoxy mucic acid ( 4 ) was evaluated against HeLa and MDA-MB231 cancer cell lines and they displayed promising activity with the IC 50 values of 22.88283±0.72 µg/ml in HeLa and 2.91925±0.52 µg/ml in case of MDA-MB231, respectively. The antioxidant property of 2-methoxy mucic acid ( 4 ) was found to be (IC 50 ) 21.361±0.41 µg/ml. Apart from in vitro studies, we also performed extensive in silico studies (molecular docking and molecular dynamics simulation) on four key anti-apoptotic Bcl-2 family members (Bcl-2, Bcl-w, Bcl-xL and Bcl-B) towards 2-methoxy mucic acid ( 4) and the results revealed that this molecule showed higher binding affinity towards Bcl-B protein ( ΔG = -5.8 kcal/mol) and the structural stability of Bcl-B protein was significantly improved upon binding of this molecule. The present study affords key insights about the importance of 2-methoxy mucic acid ( 4 ), and thus leads to open the therapeutic route for anticancer drug discovery process.
... Many species of the genus have medicinal uses in Southeast Asian countries, including China, India, and Brazil [6]. Phyllanthus emblica L. is cultivated for fruit [9] and has many medicinal properties, including antioxidant, anti-cancer, anti-inflammatory, anti-pyretic diuretic, laxative, stomachic, cardioprotective, and hepatoprotective [6,8,[10][11][12][13]. ...
Family Phyllanthaceae is one of the largest segregates of the eudicot order Malpighiales and its species are herb, shrub, and tree, which are mostly distributed in tropical regions. Certain taxonomic discrepancies exist at genus and family level. Here, we report chloroplast genomes of three Phyllanthaceae species-Phyllanthus emblica, Flueggea virosa, and Leptopus cordifolius-and compare them with six others previously reported Phyllanthaceae chloroplast genomes. The species of Phyllanthaceae displayed quadripartite structure, comprising inverted repeat regions (IRa and IRb) that separate large single copy (LSC) and small single copy (SSC) regions. The length of complete chloroplast genome ranged from 154,707 bp to 161,093 bp; LSC from 83,627 bp to 89,932 bp; IRs from 23,921 bp to 27,128 bp; and SSC from 17,424 bp to 19,441 bp. Chloroplast genomes contained 111 to 112 unique genes, including 77 to 78 protein-coding, 30 transfer RNA (tRNA), and 4 ribosomal RNA (rRNA) that showed similarities in arrangement. The number of protein-coding genes varied due to deletion/pseudogenization of rps16 genes in Baccaurea ramiflora and Leptopus cordifolius. High variability was seen in number of oligonucleotide repeats while analysis of guanine-cytosine (GC) content, codon usage, amino acid frequency, simple sequence repeats analysis, synonymous and non-synonymous substitutions, and transition and transversion substitutions showed similarities in all Phyllanthaceae species. We detected a higher number of transition substitutions in the coding sequences than non-coding sequences. Moreover, the high number of transition substitutions was determined among the distantly related species in comparison to closely related species. Phylogenetic analysis shows the polyphyletic nature of the genus Phyllanthus which requires further verification. We also determined suitable polymorphic coding genes, including rpl22, ycf1, matK, ndhF, and rps15 which may be helpful for the reconstruction of the high-resolution phylogenetic tree of the family Phyllanthaceae using a large number of species in the future. Overall, the current study provides insight into chloroplast genome evolution in Phyllanthaceae.
... Researchers have also demonstrated excellent antiproliferative properties of different polyphenol compounds against various cell lines. Some of these compounds have been identified in kānuka extract such as catechin, 33 ferulic and gallic acid, 34,35 quercetin and derivatives, [36][37][38] and chlorogenic acid. 39 Notably, due to the excellent solvation properties of SWE, simultaneous extraction of different classes of phytochemicals with different polarities occurs as well as the formation of new bioactive compounds. ...
BACKGROUND
Subcritical water kānuka leaf extracts contain high levels of polyphenols. However, whether these extracts can serve as natural antimicrobial and chemopreventive agents is still a question. This study aimed to evaluate the antibacterial and antiproliferative efficacy of SWE kanuka leaf extracts. Subcritical water extraction (SWE) was used to obtain natural extracts from kānuka leaves potentially rich in biologically active compounds. The antibacterial and antiproliferative capacities were assessed by broth microdilution assay and MTT‐assay, respectively. The assessed properties were compared to extraction from ethanol extraction (EE).
Results
The screening results for antibacterial properties demonstrated that subcritical water kānuka leaf extracts were active against Escherichia coli (minimum conc. 0.8 mg/mL) and Staphylococcus aureus (minimum conc. 3.8 mg/mL). These extracts also exerted dose‐dependent antiproliferative effects on the viability of cancerous human cervical cell lines (Hep‐2 and RD cells) and mouse cell lines (L cells). The extraction temperature had significantly affected the extract's activities by enhancing neoformed compounds with beneficial effects.
CONCLUSIONS
Subcritical water extracts of kānuka demonstrated a better efficacy against bacterial growth and malignant cells viability in comparison to extracts obtained using conventional ethanol extraction. This SWE kānuka leaf product could be used in a range of applications where antimicrobial and antiproliferative properties are required. Further studies are needed to examine the mechanism and markers of these properties. © 2020 Society of Chemical Industry
The Coronavirus disease-2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). It has engulfed the whole world, and it looks difficult to end this worldwide health crisis without actual medication. Natural products have been utilized since ancient times and have been beneficial over time. The outcome of various research work revealed that pure compounds isolated from medicinal plants, such as Tinospora cordifolia, Withania somnifera, Ocimum sanctum, Glycyrrhiza glabra, Piper longum, Curcuma longa, Allium sativum, Zingiber officinalis, Coriandrum sativum, Azadirachta indica, Emblica officinalis, etc. have excellent Coronavirus (CoV) inhibitory effect. Several molecules, including glabridin, liquiritin, flavonoids, triterpene, glycyrrhizin, aliphatic compounds, sesquiterpenoids, β-sesquiphellandrene, zingerone, β-phellandrene, citral, zingiberene, bisabolene, shogaols, cineol, farnesene, gingerols, withasomniferols A-C, withanone, withasomniferin-A, withasomidienone, withanolides A, linalool, flavonoids, camphor, eugenol, estragole, methyl chavicol, tannins, glycyrrhizic acid, alkaloids, saponins, fatty acids, glycosides, and essential oils, etc. isolated from plants might serve as potential candidates in the treatment of COVID-19.
Alzheimer's disease (AD), also called senile dementia, is the most common neurological disorder. Around 50 million people, mostly of advanced age, are suffering from dementia worldwide and this is expected to reach 100-130 million between 2040 and 2050. AD is characterized by impaired glutamatergic and cholinergic neurotransmission, which is associated with clinical and pathological symptoms. AD is characterized clinically by loss of cognition and memory impairment and pathologically by senile plaques formed by Amyloid β deposits or neurofibrillary tangles (NFT) consisting of aggregated tau proteins. Amyloid β deposits are responsible for glutamatergic dysfunction that develops NMDA dependent Ca2+ influx into postsynaptic neurons generating slow excitotoxicity process leading to oxidative stress and finally impaired cognition and neuronal loss. Amyloid decreases acetylcholine release, synthesis and neuronal transport. The decreased levels of neurotransmitter acetylcholine, neuronal loss, tau aggregation, amyloid β plaques, increased oxidative stress, neuroinflammation, bio-metal dyshomeostasis, autophagy, cell cycle dysregulation, mitochondrial dysfunction, and endoplasmic reticulum dysfunction are the factors responsible for the pathogenesis of AD. Acetylcholinesterase, NMDA, Glutamate, BACE1, 5HT6, and RAGE (Receptors for Advanced Glycation End products) are receptors targeted in treatment of AD. The FDA approved acetylcholinesterase inhibitors Donepezil, Galantamine and Rivastigmine and N-methyl-D-aspartate antagonist Memantine provide symptomatic relief. Different therapies such as amyloid β therapies, tau-based therapies, neurotransmitter-based therapies, autophagy-based therapies, multi-target therapeutic strategies, and gene therapy modify the natural course of the disease. Herbal and food intake is also important as preventive strategy and recently focus has also been placed on herbal drugs for treatment. This review focuses on the molecular aspects, pathogenesis and recent studies that signifies the potential of medicinal plants and their extracts or chemical constituents for the treatment of degenerative symptoms related to AD.
Phyllanthus emblica L. (family Phyllanthaceae) is commonly known as Indian gooseberry, which yields edible fruit. Indian gooseberry is eaten raw and used for culinary purposes. The fruit are rich in nutrients, vitamins, amino acids and minerals. Fresh or dried fruit, seeds, leaves, roots and bark are used in the preparation of herbal medicines in the Ayurveda, Siddha, Unani, Tibetan and Chinese systems of medicine. It is used as the primary ingredient in the preparation of Ayurvedic polyherbal formulations such as chyawanprash and triphala. It is also used in shampoos and hair oils. The fruit and other parts of the plant are rich in flavonoids, tannins, phenolic acids, sterols and terpenoids. The fruit, seeds, leaves, roots and bark of the plant are used against varied ailments like diabetes, hypertension, inflammation, cancer, respiratory, neurological and other infectious disorders. This review summarizes the traditional uses, nutritional components, phytochemicals and biological activities of Indian gooseberry. Bioaccessibility and bioavailability of bioactive compounds, novel products or formulations of Indian gooseberry are also discussed.
Screening and identification of active components from traditional Chinese medicines is rather challenging due to the diversity and complexity of chemical components. Herein, a comprehensive strategy based on a spectrum‐effect relationship model and LC‒MS analysis was developed to screen active components from Terminalia chebula fruits. The water extract of T. chebula fruits was subjected to macroporous resin column and then eluted successively with water and 30%, 50%, 70%, and 95% ethanol. The 30% ethanol eluate fractions of eighteen batches from T. chebula fruits were used for the spectrum‐effect relationship study. The IC50 values for acetylcholinesterase inhibitory and 2,2‐diphenyl‐1‐picrylhydrazyl scavenging activities were measured, LC fingerprints were established, and 15 common peaks were specified. The spectrum‐effect relationship between common peaks and IC50 values was investigated by principal component analysis, gray relational analysis, partial least square and multiple linear regression. The 30% ethanol eluate fraction was further characterized by LC‒MS analysis. The chromatographic peaks (Peaks 1, 2, 3, 5, 12, 14, 15) making great contributions to the efficacy were screened through a spectrum‐effect relationship model, and sixteen components were further identified. The results suggested that the proposed strategy is simple and effective for acquiring active components from a complex matrix.
An attempt is made to write a review concerning the anticancer effect of hydrolysable tannin chebulagic acid obtained from Terminalia chebula Retz. Chebulagic acid has multitude of applications in medicine ranging from antidiabetic effect to antitumor effect. In this review, article we have analyzed the molecular mechanism behind the anticancer property of the compound. It has been observed from previous studies that regulation of apoptosis is one of the key factors in terminating cancer and chebulagic acid modulates apoptosis by altering the mitochondrial membrane potential which leads to a sequel of events. The dominant effect is the inhibition of expression of antiapoptotic factors and stimulation of expression of proapoptotic factors which paves the path for cell suicide. This in turn is due to the increase in life span of the factor IκBα which is a stumbling block for the translocation of nuclear factor NFκB to the nucleus of cells. Therapeutic efficacy of chebulagic acid, the potent tannin natural compound to combat cancer with updated review of literature and their mechanisms of action are discussed in detail. Further, more research needs to be done towards the utility of this compound for clinical utility.
An attempt is made to write a review concerning the anticancer effect of hydrolysable tannin chebulagic acid obtained from Terminalia chebula Retz. Chebulagic acid has multitude of applications in medicine ranging from antidiabetic effect to antitumor effect. In this review, article we have analyzed the molecular mechanism behind the anticancer property of the compound. It has been observed from previous studies that regulation of apoptosis is one of the key factors in terminating cancer and chebulagic acid modulates apoptosis by altering the mitochondrial membrane potential which leads to a sequel of events. The dominant effect is the inhibition of expression of antiapoptotic factors and stimulation of expression of proapoptotic factors which paves the path for cell suicide. This in turn is due to the increase in life span of the factor IκBα which is a stumbling block for the translocation of nuclear factor NFκB to the nucleus of cells. Therapeutic efficacy of chebulagic acid, the potent tannin natural compound to combat cancer with updated review of literature and their mechanisms of action are discussed in detail. Further, more research needs to be done towards the utility of this compound for clinical utility.
Ethnopharmacological relevance
The fruits of Phyllanthus emblica Linn or Emblica officinalis Gaertn (Phyllanthaceae), (FPE) commonly known as Indian gooseberry or Amla, gained immense importance in indigenous traditional medicinal systems, including Ayurveda, for its medicinal and nutritional benefits. It is used to cure several diseases such as common cold, fever, cough, asthma, bronchitis, diabetes, cephalalgia, ophthalmopathy, dyspepsia, colic, flatulence, hyperacidity, peptic ulcer, erysipelas, skin diseases, leprosy, hematogenesis, inflammation, anemia, emaciation, hepatopathy, jaundice, diarrhea, dysentery, hemorrhages, leucorrhea, menorrhagia, cardiac disorders, and premature greying of hair.
Aim of the study
In the present review, we presented a comprehensive analysis of the ethnopharmacology, bioactive composition, and toxicity of P. emblica to identify the gap between research and the current applications and to help explore the trends and perspectives for future studies.
Materials and methods
We collected the literature published before April 2021 on the phytochemistry, pharmacology, and toxicity of FPE. Literature in English from scientific databases such as PubMed, ScienceDirect, Wiley, Springer, and Google Scholar, books. These reports were analyzed and summarized to prepare this review. The plant taxonomy was verified by “The Plant List” database (http://www.theplantlist.org).
Results and conclusion
s: FPE have been used as a rich source of vitamin C, minerals, and amino acids. Several bioactive molecules were isolated and identified from FPE such as tannins, flavonoids, saponins, terpenoids, alkaloids, ascorbic acid etc. The in vitro and in vivo pharmacological studies on FPE revealed its antimicrobial, antioxidant, anti-inflammatory, anti-diabetic, anticancer, radioprotective, hepatoprotective, immunomodulatory, hypolipidemic, anti-venom, wound healing, HIV-reverse transcriptase effect. Toxicological studies on fruits indicated the absence of any adverse effect even at a high dose after oral administration.
Conclusions
Although FPE showed remarkable therapeutic activities against several diseases such as diabetes, cancer, inflammation, hepatitis B virus, and malaria, there were several drawbacks in some previous reports including the lack of information on the drug dose, standards, controls, and mechanism of action of the extract. Further in-depth studies are required to explain the mechanism of action of the extracts to reveal the role of the bioactive compounds in the reported activities.
Nowadays, the food industry is focused on improving the shelf life of products by controlling lipid oxidation using natural antioxidants. The study of natural antioxidants is a field that attracts great interest because of their greater safety compared to synthetic ones. Plant-derived antioxidants being eco-friendly and effective are increasingly playing an important role in food preservation. When incorporated into active packaging, plant-derived antioxidants have no direct contact with foods, and will not change the colour or taste of the foods. They will, however, inhibit the development of rancidity, retard formation of toxic oxidation products, maintain nutritional quality, and prolong the shelf life of products. This review summarises research on the development of plant-derived antioxidants in food packaging. Antioxidants are found in plants such as green tea, olive leaves, ginkgo leaves, rosemary, Indian gooseberry, cinnamon, savoury, bay leaves, mango leaves, sage and clove etc. Antioxidants can scavenge free radicals and inhibit the activity of polyphenol oxidase. Therefore, they can inhibit lipid oxidation and browning of fruit and vegetables. These active substances can be obtained through extracting the plants using solvents with different polarities. The oxidation resistance of active substances can be determined by DPPH radical scavenging capacity, oxygen radical absorbance capacity, PPO enzyme inhibition capacity and other methods. In recent years, research on the preparation of food packaging with plant-derived antioxidants has also made significant progress. One development is to encapsulate plant-derived antioxidants such as tea polyphenols with capsules containing inorganic components. Thus, they can be blended with polyethylene granules and processed into active packaging film by industrial production methods such as melting, extrusion and blowing film. This research promotes the commercial application of active packaging incorporated with plant-derived antioxidants.
Citation: Sinha, R.; Jindal, R.; Faggio, C. Protective Effect of Emblica officinalis in Cyprinus carpio against Hepatotoxicity Induced by Malachite Green: Ultrastructural and Molecular Analysis. Appl. Sci. 2021, 11, 3507.
Malachite green (MG) dye, besides coloring is used as an effective aquaculture therapeutic. The present study assesses the mitigating ability of Emblica officinalis (EO) fruit extract against the dye induced chronic (60 days) cyto-toxicity in Cyprinus carpio. For this, four experimental groups were maintained: group I—control, group II—MG, group III—EO (positive control), group IV—MG + EO. The study was made at three tiers: detailing structural anomalies using a light microscope and transmission electron microscope (TEM), biochemical estimation of antioxidant enzymes, and lipid peroxidation and molecular analysis of expression patterns of HSP70, and CYP1A genes. MG intoxication resulted in necrosis, cytoplasmic vacuolation, glycogen depletion, abundant macrophages, loss of cell integrity and prominent nuclear alterations. Significant (p < 0.05) inhibition in the activities of catalase (CAT), superoxide dismutase (SOD), glutathione-S-transferase (GST) and reduced glutathione (GSH), along with an elevation in malondialdehyde (MDA) levels, occurred after 60 days of MG exposure. CYP1A and HSP70 genes presented a significant change in their expression in MG treated fish. Whereas oral supplementation with EO significantly restored the histo-architecture, normalized the altered enzymatic activity, reduced the oxidative stress level and regulated the expression of HSP70 and CYP1A genes. Thus, it can be concluded that EO acted as an effective ameliorant against malachite green induced cyto-toxicity in Cyprinus carpio
In the present work, we focused on extracting, separating, formulating, and, finally, characterizing quercetin. Chitosan/GMO nanoparticles were investigated to controlled release for targeting colonic region. Quercetin is an active biomolecule isolated from peels of pomegranate fruit, separated by different chromatographic techniques, and formulated into nanoformulation to bring it to increase its aqueous solubility. Nanoparticles were prepared by using chitosan, glyceryl monooleate (GMO), and poloxamer 407 using probe sonicator and high-pressure homogenization method. Characterization of nanoparticles was carried out by particle size, zeta potential, differential scanning colorimetry (DSC), X-ray diffraction (XRD), scanning electron microscope (SEM), entrapment efficiency, loading content, in vitro release, and stability study. They showed approximately 78.82% encapsulation with an average size of 145.5 ± 0.66 nm and zeta potential + 14.7 mV. The cumulative in vitro drug release up to 24 h at 77.16% was achieved suggesting towards efficacy of green synthesized chitosan nanoparticles for colonic delivery applications. From all our findings, it can be concluded that work will facilitate the extraction, design, and fabrication of nanoparticles for the protection and sustained release of quercetin biomolecule, particularly to the colonic region. The release performance of chitosan/GMO nanoparticles loaded with quercetin at different pH conditions was greatly affected by the materials used in the preparation, which allows maximum release at colonic pH. Hence, it is a unique approach for colonic delivery of drugs having appropriate site specificity and feasibility and controlled release of biomolecule quercetin. Biomolecule quercetin isolated from peels of pomegranate fruit, then separated and characterized by Column, Flash, GC, IR, NMR, LC-MS, HPLC and HPTLC techniques. Formulation and characterization of Qu-loaded Chi nanoparticles by FTIR, XRD, DSC, SEM, Encapsulation effiency and Loading content results influencing on critical quality attributes analysed by central composite design. Optimized Qu-loaded Chi nanoparticles had a significant sustained in-vitrorelease at colonic region.
Medicinal plants are precious gifts of nature, which may serve as a source of food and medicine to humans. Phyllanthus emblica L has held a unique position in the Indian (Ayurvedic), Turkish, Unani, and Tibetan medicinal systems for centuries. Its nutritional, therapeutic and healing potentials have made it a valid research option for the development of novel drug formulations with few side effects. The presence of vitamin C, alkaloids, ellagitannins, gallic acid, emblicanin A and emblicanin B, flavonoids (especially rutin and quercetin), and a variety of biological molecules, makes P. emblica, a valued medicinal plant. This review article summarizes the recent literature relevant to the nutritional, health, and therapeutic benefits of P. emblica, such as potential chemo-preventive, anti-diabetic, anti-microbial, anti-inflammatory, analgesic, anti-mutagenic, antioxidant, diuretic, aphrodisiac, UV protectant, and anti-aging activities. Its applications in memory enhancing, respiratory, skin and ophthalmic disorders, and detoxification including that of snake venom, are also highlighted. It additionally reviews retrospective studies on P. emblica at the molecular level, for disease management and control. P. emblica is an important medicinal plant with many benefits. It has been used for centuries and generations as a source of food because of its unique restorative and rejuvenating potential. Thus, in light of the sum of these investigations, new studies could be designed to explore valuable bioactive compounds present throughout in nature in the form of plants.
Purpose
Rambutan ( Nephelium lappaceum ), a ubiquitous fruit in Southeastern Asia, was rich in vitamins and phytochemicals, which were beneficial for improving of skin conditions. The fermentation process increased phytochemicals and antioxidant capacity. Thus, the purpose of this paper is to examine whether phytochemicals can be increased through the fermentation process of rambutan extracts to improve skin aging.
Design/methodology/approach
In this study, the authors used the three stages of fermentation with Saccharomyces cerevisiae , Lactobacillus plantarum TCI028 and Acetobacter aceti under red light to develop a fermented rambutan extract.
Findings
The level of polyphenols of red-light-based fermented rambutan extract (RLFRE) were significantly increased 108.9% ( p < 0.01) and 97% ( p < 0.01) compared with fermented rambutan extract (FRE) and pure rambutan extract (RE), respectively. The human skin fibroblasts treated with 0.03 or 0.06% of RLFRE can significantly decrease reactive oxygen species (ROS) levels by 0.74- ( p < 0.001) and 0.84-fold ( p < 0.001) compared with H 2 O 2 group, respectively. And 0.03% of RLFRE can significantly increase in elastin content by 1.13-fold ( p < 0.05). Also, ten compounds were identified including one new phenolic compound and nine known compounds from RLFRE. Moreover, red light could enhance the levels of compounds 4, 9 and 3 by 5, 2.5 and 2.5-fold, respectively, relative to the results of FRE. The last, RLFRE isolated compounds significantly facilitated the elastin content on fibroblast (compound 1, 7, 9, 10 compared with control: p < 0.001, compound 2 compared with control: p < 0.001).
Originality/value
In short, this was the first study to unveil that the red-light-based fermentation can enrich the antioxidant content in a rambutan extract and its product had the potential to be developed a functional product for health-promoting effects such as skin aging.
There is more and more interest in caper (Capparis spinosa) in recent years as it has different areas to be applied especially within the food and cosmetic world. This study evaluated the in vitro antioxidant activity of water and ethanol extracts of capsules of caper (Capparis spinosa). The antioxidant properties of the caper were evaluated in vitro by antioxidant assays such as 2-azino-fcw(3-ethylbenzthiazoline-6- sulfonic acid) (ABTS) radical scavenging, l,l-diphenyl-2-picryI-hydrazyl free radical (DPPH*) scavenging, total antioxidant activity by ferric thio- cyanate method, total reductive capability using the potassium ferri- cyanide reduction method, superoxide anion radical scavenging and metal chelating activities. aα-Tocopherol, butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT) were used as the reference antioxidant compounds. The concentration of 10,30 and SO uμg/mL of water and ethanol extracts of caper showed 95.9, 96.4, 97.0, 97.04, 97.4, 94.8 % inhibition on peroxidation of linoleic acid emulsion, respectively. On the other hand, 30 uμg/mL of standard antioxidant such as aα-tocopherol indicated an inhibition of 88.1 % on peroxidation of linoleic acid emulsion. In addition capper is an effective ABTS + scavenging, DPPH' scavenging, superoxide anion radical scavenging, total reducing power and metal chelating on ferrous ions activities.
Epidemiological evidence suggests that consumption of vegetables can prevent degenerative diseases caused by oxidative stress. Considering scanty data available on antioxidant activity (AOA) of roots, tubers and vegetables commonly consumed in India, the objective of the present study was to assess their AOA and relate it to their total phenolic content. AOA was assessed in vegetables (n=19) and roots/tubers (n=10) by DPPH (2,2′-diphenyl-1-picryl hydrazyl) scavenging activity and FRAP (ferric reducing antioxidant power) methods and the total phenolic content (TPC) using Folin–Ciocalteu reagent. Although AOA as well as TPC showed wide variation among roots, tubers and vegetables studied. AOA (both DPPH and FRAP) was significantly correlated with TPC among all the foods studied, with the correlation coefficient (r) values being 0.76 and 0.85 (p
One of the focuses in current cancer chemoprevention studies is the search for nontoxic chemopreventive agents that inhibit the initiation of malignant transformation. Cancer biomarkers are quantifiable molecules involved in the physiologic or pathologic events occurring between exposure to carcinogens and the development, progression of cancer. Biomarkers may be the consequence of a continuous process, such as increased cell mass, or a discrete event, such as genetic mutation. Analysis of tumor markers can be used as an indicator of tumor response to therapy. Gallic acid is a naturally available polyphenol, possess strong antioxidant activity with a capacity to inhibit the formation of tumors in several cancer models. In the present study, we investigated the antiproliferative effect of gallic acid during diethylnitrosamine (DEN)-induced hepatocellular carcinoma (HCC) in male wistar albino rats. DEN treatment resulted in increased levels of aspartate transaminase, alanine transaminase, alkaline phosphatase, acid phosphatase, lactate dehydrogenase, gamma-glutamyltransferase, 5'-nucleotidase, bilirubin, alpha-fetoprotein, carcinoembryonic antigen, argyophillic nucleolar organizing regions, and proliferating cell nuclear antigen. Gallic acid treatment significantly attenuated these alterations and decreased the levels of AgNORs and PCNA. These finding suggests that gallic acid is a potent antiproliferative agent against DEN-induced HCC.
Ethanolic extracts of 30 Thai medicinal plants, traditionally used as alternative treatments in diabetes, were evaluated for antioxidative activity by the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) method. They were evaluated in vitro for oxidative stress by thiobarbituric acid-reactive substance (TBARS) assay in pooled plasma of diabetic patients compared to without treatment of the extracts (control). The extracts were also assayed for protein glycation. The results showed that five plants had strong antioxidant activity: Phyllanthus emblica Linn. (PE), Terminalia chebula Retz. (TC), Morinda citrifolia Linn. (MC), Kaempferia parviflora Wall. (KP) and Houttuynia cordata Thunb.(HC), respectively. Thirty plant extracts were good correlation between total antioxidant activity and antiradical activity by TBARS as well as by glycation (r = 0.856, p<0.01 and r = 0.810, p<0.01). PE had stronger antioxidative activity as well as inhibition of TBARS and glycation than the other plants. The investigation showed that total polyphenol and tannin content of PE and the flavonoid content of HC were the highest. The results imply that these plants are potential sources of natural antioxidants which have free radical scavenging activity and might be used for reducing oxidative stress in diabetes.
Hydrolysable tannins (HTs), secondary metabolites widely distributed in the plant kingdom, are generally multiple esters of gallic acid with glucose. HTs have been shown to be effective antagonists against viruses, bacteria and eukaryotic microorganisms. The present review examines the antimicrobial and antiviral activity of HTs, the mechanism(s) of action, and some structure-activity relationships.
Tannic acid (TA), a plant polyphenol, has been described as having antimutagenic, anticarcinogenic and antioxidant activities. Since it is a potent chelator of iron ions, we decided to examine if the antioxidant activity of TA is related to its ability to chelate iron ions. The degradation of 2-deoxyribose induced by 6 microM Fe(II) plus 100 microM H2O2 was inhibited by TA, with an I50 value of 13 microM. Tannic acid was over three orders of magnitude more efficient in protecting against 2-deoxyribose degradation than classical *OH scavengers. The antioxidant potency of TA was inversely proportional to Fe(II) concentration, demonstrating a competition between H2O2 and AT for reaction with Fe(II). On the other hand, the efficiency of TA was nearly unchanged with increasing concentrations of the *OH detector molecule, 2-deoxyribose. These results indicate that the antioxidant activity of TA is mainly due to iron chelation rather than *OH scavenging. TA also inhibited 2-deoxyribose degradation mediated by Fe(III)-EDTA (iron = 50 microM) plus ascorbate. The protective action of TA was significantly higher with 50 microM EDTA than with 500 microM EDTA, suggesting that TA removes Fe(III) from EDTA and forms a complex with iron that cannot induce *OH formation. We also provided evidence that TA forms a stable complex with Fe(II), since excess ferrozine (14 mM) recovered 95-96% of the Fe(II) from 10 microM TA even after a 30-min exposure to 100-500 microM H2O2. Addition of Fe(III) to samples containing TA caused the formation of Fe(II)n-TA, complexes, as determined by ferrozine assays, indicating that TA is also capable of reducing Fe(III) ions. We propose that when Fe(II) is complexed to TA, it is unable to participate in Fenton reactions and mediate *OH formation. The antimutagenic and anticarcinogenic activity of TA, described elsewhere, may be explained (at least in part) by its capacity to prevent Fenton reactions.
The antimutagenic properties of South African herbal teas were investigated using the Salmonella typhimurium mutagenicity assay. Aqueous extracts of fermented and unfermented rooibos tea (Aspalathus linearis) and honeybush tea (Cyclopia intermedia) both possess antimutagenic activity against 2-acetylaminofluorene (2-AAF) and aflatoxin B(1) (AFB(1))-induced mutagenesis using tester strains TA98 and TA100 in the presence of metabolic activation. A far less inhibitory effect was noticed against the direct acting mutagens, methyl methanesulfonate (MMS), cumolhydroperoxide (CHP), and hydrogen peroxide (H(2)O(2)) using TA102, a strain designed to detect oxidative mutagens and carcinogens. Depending on the mutagen used, the unfermented tea exhibited the highest protective effect. A similar response regarding the protection against mutagenesis was obtained when utilising different variations of the double layer Salmonella assay. The double layer technique proved to be more effective to detect the protective effect of the different tea preparations against the direct acting mutagens. With respect to indirect mutagens, the highest protection was noticed when the carcinogen was metabolically activated in the presence of the tea extract as compared with when the tea extract was incubated in a separate layer with the bacteria. The current data suggest that two mechanisms seem to be involved in the antimutagenicity of the tea extracts towards carcinogens that require metabolic activation: (i) the tea components may interfere with cytochrome P450-mediated metabolism of these mutagens and (ii) the direct interaction between the tea constituents, presumably the polyphenolic compounds, with the promutagens and/or the active mutagenic metabolites. However, the mild and/or lack of protection and in some cases even enhancement of mutagenesis induced by direct acting or oxidative mutagens, provide new perspectives regarding the role of the polyphenolic compounds known to exhibit antioxidant properties, in the protection against mutagenesis in the Salmonella assay. The present study provides the first evidence on the antimutagenic activity of honeybush tea and further evidence on the antimutagenicity of rooibos tea.
Eighteen main compounds, including four norsesquiterpenoids (1-4) and 14 phenolic compounds (5-18) isolated previously from Phyllanthus emblica, together with a main constituent, proanthocyanidin polymers (19) identified at this time from the roots, were estimated for their antiproliferative activities against MK-1 (human gastric adenocarcinoma), HeLa (human uterine carcinoma), and B16F10 (murine melanoma) cells using an MTT method. All of the phenolic compounds including the major components 5-8 from the fruit juice, 8, 9, and 12 from the branches and leaves, and 19 from the roots showed stronger inhibition against B16F10 cell growth than against HeLa and MK-1 cell growth. Norsesquiterpenoid glycosides 3 and 4 from the roots exhibited significant antiproliferative activities, although their aglycon 1 and monoglucoside 2 showed no inhibitory activity against these tumor cells.
Elevated expression of matrix metalloproteinases (MMPs), especially that of MMP-2 and MMP-9, is associated with increased metastatic potential in many tumor cells. Recently, green tea polyphenol epigallocatechin-3-O-gallate (EGCG) has been shown to inhibit the MMP-2/-9 activity as well as the invasiveness of tumor cells. In this study, we have examined the inhibitory effect of hydrolyzable tannins (plant polyphenols) on the tumor cell invasion. Our results demonstrate that beta-d-glucose whose hydroxy groups are substituted entirely with galloyl group and further some of them are cross-linked to form hexahydroxydiphenoyl group, for example, suppresses the invasiveness of tumor cells much more potently than EGCG via direct inhibition of the MMP-2/-9 activity. Among those examined, 1,2,4-tri-O-galloyl-3,6-hexahydroxydiphenoyl-beta-d-glucose (punicafolin) inhibits the invasion of HT1080 fibrosarcoma cells most potently. These hydrolyzable tannins would provide new leads for the development of potent inhibitors against tumor metastasis.
The cytotoxic effects of Triphala (TPL), an Indian Ayurvedic formulation with known anti-cancer properties, has been investigated on two human breast cancer cell lines differing in their p53 status. In vitro studies showed that MCF 7 with wild type p53 was more sensitive to TPL than T 47 D, which is p53 negative. TPL induced loss of cell viability was determined by MTT assay. After 72h incubation, the IC 50 values for MCF 7 was found to be approximately 8microg/ml and that for T 47 D was approximately 26microg/ml. Moreover, TPL inhibited the clonogenic growth of MCF 7 cells, which was significantly recovered by pifithrin-alpha, the p53 inhibitor. However, pifithrin-alpha, did not modify TPL induced cytotoxicity in T 47 D cells. Exogenous addition of antioxidants, glutathione (GSH) and N-Acetyl-Cysteine (NAC) inhibited the anti-proliferative ability of TPL in both MCF 7 and T47 D. Annexin-V and propidium iodide double staining of cells treated with TPL for 2h revealed that TPL induced significant apoptosis in both the cell lines in a dose dependant manner but magnitude of apoptosis was significantly higher in MCF 7 than in T 47-D cells. TPL was also found to induce dose and time dependent increase in intracellular reactive oxygen species in both the cell lines. Present results have demonstrated that MCF 7 and T 47 D cells exhibited differential sensitivity to TPL, which seems to be dependant on their p53 status. Inhibition of anti-proliferative ability of TPL by antioxidants suggests a role for TPL induced ROS in the induction of apoptosis. It is concluded that p53 status of cancer cells formed an important factor in predicting the response of cancer cells to prooxidant drugs.
The antioxidant activity and free radical scavenging activity of methanol extract of Hyoscyamus squarrosus leave was investigated employing various in vitro assay systems. IC50 for DPPH radical-scavenging activity was 215± 5.6 μg ml-1. The extracts showed weak nitric oxide-scavenging activity (IC50 was 0.75 ± 0.02 mg ml-1) and Fe2+ chelating ability (IC50 was 0.86 ± 0.02 mg ml-1). The extract had show good reducing power that was comparable with Vitamin C (p> 0.05). It exhibited no antioxidant activity in FTC method. It showed good H2O2 scavenging activity. Total phenol compounds, as determined by the Folin Ciocalteu method, were 98.95 ± 3.16 mg gallic acid equivalent/g of extract powder and the total flavonoid content, by AlCl3 method, was 44.94 ± 2.02 mg quercetin equivalent/g of extract powder. The results improved that the leaves extract can serve as an electron donor for terminating the radical chain reaction.
The present study estimated in vitro antioxidant activities of 68 common Chinese herbals both for medical and food uses, using Folin–Ciocalteu, ferric-reducing/antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assays. The results showed different extraction had various antioxidant properties. Six plant materials including Chinese White Olive, Clove, Pricklyash Peel, Villous Amomum Fruit, Chinese Star Anise and Pagodatree Flower appeared highest total phenolics (>45mg gallic acid equivalents (GAE)/g) and flavonoids content (>45mg rutin equivalents (RE)/g), which also showed highest antioxidant activity (FRAP value>2.5mmol/g, DPPH radical-scavenging capacity>85%), indicating they have potentials for use as natural sources of antioxidant foods. The total phenolics content of these 68 plant extracts was significantly positively correlated (r2=0.9467) with their antioxidant capacity. Therefore, the content of phenolic compounds could be used as an important indicator of its antioxidant capacity.
Emblica has been used as an important traditional herbal medicine in southeast Asia since ancient times. In this study, the air-dried hulls of emblica fruit were extracted with 95% ethanol, and then the extract was partitioned by diethyl ether and ethyl acetate (EA). The EA fraction was purified by silica gel column and thin layer chromatography (TLC) to obtain six compounds. They were identified as cinnamic acid (C1), quercetin (C2), 5-hydroxymethylfurfural (C3), gallic acid (C4), β-daucosterol (C5) and ellagic acid (C6) using mass spectrometry and nuclear magnetic resonance (NMR) spectroscopy. Cinnamic acid and 5-hydroxymethylfurfural were identified as components of emblica fruit for the first time. The DPPH and ABTS+ radical scavenging activities of components were evaluated. All the compounds showed significant DPPH and ABTS+ radical scavenging activity except for cinnamic acid. Gallic acid showed the highest DPPH radical scavenging activity while ellagic acid showed the highest ABTS+ scavenging activity amongst all the compounds tested.
The emblic is native to tropical southeastern Asia where the fruit is esteemed both fresh and preserved. It is valued as an
antiscorbutic and for treating digestive and other disorders. Since the emblic has a highly stable ascorbic acid content,
it is considered effective even when dried, powdered, or prepared in the form of candies or tablets. Scientific and industrial
institutions in India are developing new products and improved methods of processing this fruit; while Indian horticulturists
are active in the propagation of superior varieties. Long neglected in the western hemisphere, the emblic merits further investigation.
The antiradical activities of various antioxidants were determined using the free radical, 2,2-Diphenyl-1-picrylhydrazyl (DPPH*). In its radical form. DPPH* has an absorption band at 515 nm which dissappears upon reduction by an antiradical compound. Twenty compounds were reacted with the DPPH* and shown to follow one of three possible reaction kinetic types. Ascorbic acid, isoascorbic acid and isoeugenol reacted quickly with the DPPH* reaching a steady state immediately. Rosmarinic acid and δ-tocopherol reacted a little slower and reached a steady state within 30 min. The remaining compounds reacted more progressively with the DPPH* reaching a steady state from 1 to 6 h. Caffeic acid, gentisic acid and gallic acid showed the highest antiradical activities with a stoichiometry of 4 to 6 reduced DPPH* molecules per molecule of antioxidant. Vanillin, phenol, γ-resorcylic acid and vanillic acid were found to be poor antiradical compounds. The stoichiometry for the other 13 phenolic compounds varied from one to three reduced DPPH* molecules per molecule of antioxidant. Possible mechanisms are proposed to explain the experimental results.
Ultrasonic technique was employed to extract polysaccharides from longan fruit pericarp (PLFP). The optimal conditions for ultrasonic extraction of PLFP were determined by response surface methodology. Box–Behnken design was applied to evaluate the effects of three independent variables (ultrasonic power, time and temperature) on the recovery and 1,1′-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity of PLFP. The correlation analysis of two mathematical-regression models indicated that quadratic polynomial model could be employed to optimize the ultrasonic extraction of PLFP. From response surface plots, ultrasonic power, time and temperature exhibited independent and interactive effects on the extraction of PLFP. The DPPH radical scavenging activity of PLFP could be improved by application of various ultrasonic power, time and temperature, which was possible due to the degradation of polysaccharides to different extent. The optimal conditions to obtain the highest recovery and the strongest DPPH radical scavenging activity of PLFP were 120 W, 22 min and 60 °C, as well as 241 W, 18 min and 51 °C, respectively. Under these optimal conditions, the experimental values agreed with the predicted ones by analysis of variance. It indicated high fitness of two models used and the success of response surface methodology for optimizing PLFP extraction.
An activity-directed fractionation and purification process was used to identify the antioxidative components of emblica fruit. Dried fruit of emblica was extracted with methanol and then partitioned by ethyl ether, ethyl acetate, butanol and water. The ethyl acetate fraction showed the strongest 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity among four fractions. The ethyl acetate fraction was then subjected to separation and purification using Sephadex LH-20 chromatography and reverse-phase high-performance liquid chromatography (HPLC). Six compounds were identified to be geraniin (1), quercetin 3-β-d-glucopyranoside (2), kaempferol 3-β-d-glucopyranoside (3), isocorilagin (4), quercetin (5), and kaempferol (6), respectively, by spectral methods, (1)H and (13)C nuclear magnetic resonance (NMR) spectroscopy, ultraviolet-visible (UV-Vis) spectrophotometry and mass spectroscopy (MS), and comparison with literatures. Compounds 2-4 and 6 were identified from emblica fruit for the first time. Furthermore, the antioxidant activities of purified compounds were screened for their antioxidative potential using lipid peroxidation and DPPH systems. All the purified compounds showed strong antioxidant and radical scavenging activities. Amongst, geraniin showed the highest antioxidant activity (4.7 and 65.7μM of IC50 values for DPPH and lipid peroxidation assay, respectively) than other purified compounds.
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Eleven fruit and vegetable byproducts and two minor crops were screened for industrial polyphenol exploitation potential by determination of their extraction yield, total phenolic content (TPC, Folin–Ciocalteu), and antioxidant activity (NTZ/hypoxanthine superoxide assay, ferric thiocyanate method). Extracts with the highest activity, economic justification and phenolic content were obtained from apple (TPC maximum 48.6 ± 0.9 mg Gallic acid equivalents g−1 dry extract), pear (60.7 ± 0.9 mg GAE g−1), tomato (61.0 ± 3.0 mg GAE g−1), golden rod (251.4 ± 7.0 mg GAE g−1) and artichoke (514.2 ± 14.9 mg GAE g−1). Apple, golden rod and artichoke byproducts were extracted at pilot plant scale and their antioxidant activity was confirmed by determination of their free radical scavenging activity (DPPH) and the inhibition of stimulated linoleic acid peroxidation (TBA and Rancimat® methods). The preservative effect of the three extracts (determination of the peroxide value in test crème formulations with 0.1–1.0% extract concentrations) was similar to the established antioxidants Oxynex® 0.1%, Controx® KS 0.15%, and butylated hydroxytoluene (BHT) 0.01%. This study demonstrates the possibility of recovering high amounts of phenolics with antioxidant properties from fruit and vegetable residuals not only for food but also cosmetic applications.
The effects of natural and synthetic antioxidants on the oxidative stability of borage and evening primrose triacylglycerols (TAG), under Schaal oven conditions at 60 °C were evaluated. Conjugated dienes (CD) and 2-thiobrabituric acid-reactive substances were used as indicators for evaluation of primary and secondary lipid oxidation products, respectively. Results suggest that tocopherols are more effective antioxidants at 500 ppm than at 200 ppm. The most effective natural antioxidant was Tenox GT-2 (the formulation in oil was composed of 7.88 ppm of α-, 39.7 ppm of γ- and 21.8 ppm of δ-tocopherol) followed by δ- and α-tocopherols, while, among synthetic antioxidants, tert-butylhyroquinone (TBHQ) was more effective than butylated hydroxytoluene (BHA) and butylated hydroxyanisole (BHT) and served as the strongest antioxidant in borage and evening primrose oil TAG.
Polysaccharides of longan fruit pericarp (PLFP) were purified by gel filtration chromatography and methylated by methyl iodide. The structure of methylated PLFP was identified by gas chromatography/mass spectrometry. The results indicated that the percentages of methylated Ara, Glc and Gal increased gradually to a maximal value with increasing volume of methyl iodide. Methylation resulted in a decrease in the DPPH radical scavenging activity of PLFP, while the superoxide anion radical scavenging activity of PLFP decreased with increasing the degree of methylation. When the degree of methylation reached up to 47.4% or a higher value, a promoted effect on the generation of superoxide anion was observed. Furthermore, a high correlation coefficient between degree of methylation and superoxide anion radical scavenging activity of PLFP was determined, which indicated the important role of hydroxyl groups of monosaccharide units in the radical scavenging activity of PLFP.
We isolated 18 polyphenols with neuraminidase inhibitory activity from methanol extracts of the roots of Glycyrrhiza uralensis. These polyphenols consisted of four chalcones (1-4), nine flavonoids (5-13), four coumarins (14-17), and one phenylbenzofuran (18). When we tested the effects of these individual compounds and analogs thereof on neuraminidase activation, we found that isoliquiritigenin (1, IC(50)=9.0 microM) and glycyrol (14, IC(50)=3.1 microM) had strong inhibitory activity. Structure-activity analysis showed that the furan rings of the polyphenols were essential for neuraminidase inhibitory activity, and that this activity was enhanced by the apioside group on the chalcone and flavanone backbone. In addition, the presence of a five-membered ring between C-4 and C-2' in coumestan was critical for neuraminidase inhibition. All neuraminidase inhibitors screened were found to be reversible noncompetitive inhibitors.
Indian gooseberry (Emblica officinalis Gaertn.) (Euphorbiaceae) has a distinguished history in Ayurveda medicine and is ascribed a number of medicinal properties and as a dietary supplement, its use is increasing in Western countries. It is thought that its beneficial properties are a function of its antioxidant potency. The study investigated the chemistry and antioxidant properties of four commercial E. officinalis fruit extracts in order to determine if there are any qualitative-quantitative differences. All extracts produced positive responses in the total phenol, total flavonoid and total tannin assays. The presence of predominantly (poly)phenolic analytes, e.g. ellagic and gallic acids and corilagin, was confirmed by RP-HPLC coupled with photodiode array detection. Despite ascorbic acid being a major constituent of E. officinalis fruits, the furanolactone could not be identified in one of the samples. The extracts demonstrated varying degrees of antioxidative efficacy. The extract designated IG-3 was consistently amongst the most effective extracts in the iron(III) reduction and 1,1-diphenyl-2-picrylhydrazyl and superoxide anion radical scavenging assays while the extract designated IG-1 demonstrated the best hydroxyl radical scavenging activity. All extracts appeared to be incapable of chelating iron(II) at realistic concentrations.
Forty-five ellagitannins and related compounds were intraperitoneally injected into mice once, 4 d before intraperitoneal inoculation of S-180 cells, and their antitumor activities were evaluated. When an antitumor-active tannin was defined as one producing a 70% increase or more in the mean life span of mice or one regressor out of six mice, twenty-one ellagitannins were active. Among monomeric ellagitannins, tellimagrandin II was most active. Most of the oligomeric ellagitannins, consisting of tellimagrandins I and II as the monomer unit, had a significant antitumor activity. Macrocyclic ellagitannins were all active. Oenothein B, among them, had the most potent antitumor activity. In contrast, ellagitannins containing a casuarictin or potentillin moiety in their molecules, except for extensively oligomerized ones, showed very low or negligible activity. These results suggest that tannins need the ellagitannin monomer units, having galloyl groups at the O-2 and O-3 positions on the glucose core(s), such as tellimagrandins, in order to exhibit a strong antitumor activity.
A method for the screening of antioxidant activity is reported as a decolorization assay applicable to both lipophilic and hydrophilic antioxidants, including flavonoids, hydroxycinnamates, carotenoids, and plasma antioxidants. The pre-formed radical monocation of 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS*+) is generated by oxidation of ABTS with potassium persulfate and is reduced in the presence of such hydrogen-donating antioxidants. The influences of both the concentration of antioxidant and duration of reaction on the inhibition of the radical cation absorption are taken into account when determining the antioxidant activity. This assay clearly improves the original TEAC assay (the ferryl myoglobin/ABTS assay) for the determination of antioxidant activity in a number of ways. First, the chemistry involves the direct generation of the ABTS radical monocation with no involvement of an intermediary radical. Second, it is a decolorization assay; thus the radical cation is pre-formed prior to addition of antioxidant test systems, rather than the generation of the radical taking place continually in the presence of the antioxidant. Hence the results obtained with the improved system may not always be directly comparable with those obtained using the original TEAC assay. Third, it is applicable to both aqueous and lipophilic systems.
Aqueous extract of Emblica officinalis (E.O) was found to be cytotoxic to L 929 cells in culture in a dose dependent manner. Concentration needed for 50% inhibition was found to be 16.5 microg/ml. E.O and chyavanaprash (a non-toxic herbal preparation containing 50% E.O) extracts were found to reduce ascites and solid tumours in mice induced by DLA cells. Animals treated with 1.25 g/kg b.wt. of E.O extract increased life span of tumour bearing animals (20%) while animals treated with 2.5 g/kg b.wt. of chyavanaprash produced 60.9% increased in the life span. Both E.O and chyavanaprash significantly reduced the solid tumours. Tumour volume of control animals on 30th day was 4.6 ml where as animals treated with 1.25 g/Kg b.wt. of E.O extract and 2.5 g/kg b.wt. of chyavanaprash showed a tumour volume of 1.75 and 0.75 ml, respectively. E.O extract was found to inhibit cell cycle regulating enzymes cdc 25 phosphatase in a dose dependent manner. Concentration needed for 50% inhibition of cdc 25 phosphatase was found to be 5 microg/ml and that needed for inhibition of cdc2 kinase was found to be >100 microg/ml. The results suggest that antitumour activity of E.O extract may partially be due to its interaction with cell cycle regulation.
Methanolic extract (75%) of Terminalia chebula, Terminalia belerica, Emblica officinalis and their combination named 'Triphala' (equal proportion of above three plant extracts) are being used extensively in Indian system of medicine. They were found to inhibit lipid peroxide formation and to scavenge hydroxyl and superoxide radicals in vitro. The concentration of plant extracts that inhibited 50% of lipid peroxidation induced with Fe(2+)/ascorbate were food to be 85.5, 27, 74 and 69 micro g/ml, respectively. The concentration needed for the inhibition of hydoxyl radical scavenging were 165, 71, 155.5 and 151 micro g/ml, and that for superoxide scavenging activity were found to be 20.5, 40.5, 6.5 and 12.5 micro g/ml, respectively. Oral administration of the extracts (100 mg/kg body weight) reduced the blood sugar level in normal and in alloxan (120 mg/kg) diabetic rats significantly within 4 h. Continued, daily administration of the drug produced a sustained effect.
Flavonoids are well known as effective free radical scavengers exhibiting therefore an antioxidant behaviour. Another antioxidant mechanism however may result from the ability they have to chelate metal ions, rendering them inactive to participate in free radical generating reactions. Electrospray mass spectrometry has been used to study metal ion interactions with a set of flavonoids from different classes. Complexes with a range of stoichiometries, of metal: flavonoid, 1:1, 1:2, 2:2, 2:3 have been observed. The stoichiometry 1:2 is in general the preferred one. It is established for flavones and for the flavanone naringenin that the binding metal sites are preferentially at the 5-hydroxyl and 4-oxo groups. Redox reactions are also observed through the change of the oxidation state of the metal, jointly with the oxidation of the flavonoid by loss of hydrogen. Structures of the oxidized species of some flavonoids are proposed.
Grapes and wine contain high concentrations of polyphenolic compounds. Although their cancer protective effect has been well documented, their activity as anticarcinogens should be cautiously considered since the molecular bases of action and their applicability to human cancer prevention are still unclear.
We studied the antioxidant/antiradical activity and the antiproliferative effect in vitro of different polyphenolic mixtures, extracted from grapes and fractionated through RP-HPLC.
The polyphenolic fractions were chemically characterized and their antioxidant/antiradical activity was determined by the DPPH assay. Mouse hepatoma Hepa-1c1c7 cells were used to study the cell growth inhibition capacity of these fractions by MTT assay. Their capacity of altering cell cycle and possible induction of apoptosis was examined using FACS analysis.
The original polyphenolic fraction OW, which contained gallic acid (GA), (+)-catechin (Cat), (-)-epicatechin (Ec), glycosylated flavonols (F) and procyanidin oligomers was fractionated into fraction I, composed of monomers and small oligomers, and fraction II that included flavonols and procyanidin oligomers of higher molecular weight. The three polyphenolic fractions tested showed quite similar antiradical activity, although fraction I was the most potent antiradical agent (lowest ED(50) value: 9 microg). Fraction II was the least potent cell growth inhibitor (highest IC(50) value: 100 microg/ml) but showed the strongest effect on the cell cycle of Hepa-1c1c7, inducing apoptosis in those cells. The original fraction OW was demonstrated to have the most potent cell growth inhibition effect (lowest IC(50) value: 43 microg/ml). However, it only appeared to alter cell cycle of Hepa-1c1c7 at concentrations higher than its IC(50) and did not induce apoptosis in those cells. A similar effect on cell cycle and apoptosis was encountered for fraction I.
The polyphenolic fractions tested in this study were potent antiradical agents and exerted an antiproliferative effect in mouse hepatoma Hepa-1c1c7 cells; the fraction with the highest degree of polimerization and galloylation (fraction II) had the most influence on the cell cycle and induction of apoptosis on Hepa-1c1c7.
The photo-Fenton reaction, the reaction of photoproduced Fe(II) with H2O2 to form the highly reactive hydroxyl radical (OH*), could be an important source of OH* in sunlit natural waters. To determine if the photo-Fenton reaction is significant in mildly acidic surface waters, we conducted experiments simulating conditions representative of natural freshwaters using solutions of standard fulvic acid and amorphous iron oxide at pH 6.0. A probe method measuring 14CO2 produced by the reaction of 14C-labeled formate with OH* was used to detect small OH* production rates without otherwise influencing the chemical reactions occurring in the experiments. Net H2O2 accumulation was simultaneously measured using an acridinium ester chemiluminescence method. Measured losses of H2O2 by reaction with Fe(II) in dark experiments produced approximately the expected quantities of OH*. The difference between H2O2 accumulation in the presence and absence of Fe(III) in fulvic acid solutions exposed to light was interpreted as the loss of H2O2 by reaction with photoproduced Fe(II), consistent with measured OH* production rates. The Fe ligand desferrioxamine mesylate eliminated both OH* production and H2O2 photoloss induced by Fe. Our results imply that when Fe is a major sink of H2O2, the photo-Fenton reaction is likely to be the most important source of OH*, leading to a significant sink of organic compounds in a wide variety of sunlit freshwaters.
Screening was done of some plants of importance in the Ayurvedic system of traditional medicine used in India to treat enteric diseases. Fifty four plant extracts (methanol and aqueous) were assayed for their activity against multi-drug resistant Salmonella typhi. Strong antibacterial activity was shown by the methanol extracts of Aegle marmelos, Salmalia malabarica, Punica granatum, Myristica fragrans, Holarrhena antidysenterica, Terminalia arjuna and Triphal (mixture of Emblica of fi cinalis, Terminalia chebula and Terminalia belerica). Moderate antimicrobial activity was shown by Picorhiza kurroa, Acacia catechu, Acacia nilotica, Cichorium intybus, Embelia ribes, Solanum nigrum, Carum copticum, Apium graveolens, Ocimum sanctum, Peucedanum graveolens and Butea monosperma.
Emblica officinalis is widely used in Indian medicine for the treatment of various diseases. In the present study, it was found that fruits of E. officinalis inhibit thioacetamide-induced oxidative stress and hyper-proliferation in rat liver. The administration of a single necrotic dose of thioacetamide(6.6 mM kg(-1)) resulted in a significant (P < 0.001) increase in serum glutamic oxaloacetic transaminase(SGOT), serum glutamic pyruvic transaminase (SGPT) and gamma-glutamyl transpeptidase (GGT) levels compared with saline-treated control values. Thioacetamide caused hepatic glutathione (GSH) depletion and a concomitant increase in malanodialdehyde (MDA) content. It also resulted in an increase(P < 0.001) in the activity of glutathione-S-transferase (GST), glutathione reductase (GR), glucose 6-phosphate dehydrogenase (G6PD) and a decrease in glutathione peroxidase (GPx) activity (P < 0.001). Hepatic ornithine decarboxylase activity and thymidine incorporation in DNA were increased bythioacetamide administration. Prophylactic treatment with E. officinalis for 7 consecutive days before thioacetamide administration inhibited SGOT, SGPT and GGT release in serum compared with treated control values. It also modulated the hepatic GSH content and MDA formation. The plant extract caused a marked reduction in levels of GSH content and simultaneous inhibition of MDA formation. E. officinalis also caused a reduction in the activity of GST, GR and G6PD. GPx activity was increased after treatment with the plant extract at doses of 100 mg kg(-1) and 200 mg kg(-1). Prophylactic treatment with the plant caused a significant down-regulation of ornithine decarboxylase activity (P < 0.001) and profound inhibition in the rate of DNA synthesis (P < 0.001). In conclusion, the acute effects of thioacetamide in rat liver can be prevented by pre-treatment with E. officinalis extract.
A study on cytotoxic effect of acetone extract of "Triphala" whose antimutagenicity has already been tested. The in vitro antimutagenic activity of Triphala--an Indian herbal drug. Food Chemistry and Toxicology 40, 47-54) was extended to test its cytotoxic effects on cancer cell-lines using Shionogi 115 (S115) and MCF-7 breast cancer cells and PC-3 and DU-145 prostate cancer cells as models. The results revealed that acetone extract of "Triphala" showed a significant cytotoxic effect on these cancer cell-lines and the effect was similar on all cancer cell lines used in this study. The major phenolic compounds in the most potent acetone extracts were isolated and purified. Structural analysis was conducted using spectroscopic techniques including mass spectroscopy, nuclear magnetic resonance (NMR) and infrared (IR) which showed gallic acid as the major component. The suppression of the growth of cancer cells in cytotoxic assays may be due to the gallic acid-a major polyphenol observed in "Triphala".
Traditional Chinese medicinal plants associated with anticancer contain a wide variety of natural phenolic compounds with various structural features and possessing widely differing antioxidant activity. The structure-radical scavenging activity relationships of a large number of representative phenolic compounds (e.g., flavanols, flavonols, chalcones, flavones, flavanones, isoflavones, tannins, stilbenes, curcuminoids, phenolic acids, coumarins, lignans, and quinones) identified in the traditional Chinese medicinal plants were evaluated using the improved ABTS*+ and DPPH methods. Different categories of tested phenolics showed significant mean differences in radical scavenging activity. Tannins demonstrated the strongest activity, while most quinones, isoflavones, and lignans tested showed the weakest activity. This study confirmed that the number and position of hydroxyl groups and the related glycosylation and other substitutions largely determined radical scavenging activity of the tested phenolic compounds. The differences in radical scavenging activity were attributed to structural differences in hydroxylation, glycosylation and methoxylation. The ortho-dihydroxy groups were the most important structural feature of high activity for all tested phenolic compounds. Other structural features played a modified role in enhancing or reducing the activity. Within each class of phenolic compounds, the structure-activity relationship was elucidated and discussed. This study reveals the structure-activity relationships of a large series of representative natural phenolic compounds more systematically and fully than previous work. Structure-radical scavenging activity relationships of some natural phenolics identified in the medicinal plants were evaluated for the first time.
Phytochemicals from fruits such as the pomegranate (Punica granatum L) may inhibit cancer cell proliferation and apoptosis through the modulation of cellular transcription factors and signaling proteins. In previous studies, pomegranate juice (PJ) and its ellagitannins inhibited proliferation and induced apoptosis in HT-29 colon cancer cells. The present study examined the effects of PJ on inflammatory cell signaling proteins in the HT-29 human colon cancer cell line. At a concentration of 50 mg/L PJ significantly suppressed TNFalpha-induced COX-2 protein expression by 79% (SE = 0.042), total pomegranate tannin extract (TPT) 55% (SE = 0.049), and punicalagin 48% (SE = 0.022). Additionally, PJ reduced phosphorylation of the p65 subunit and binding to the NFkappaB response element 6.4-fold. TPT suppressed NFkappaB binding 10-fold, punicalagin 3.6-fold, whereas ellagic acid (EA) (another pomegranate polyphenol) was ineffective. PJ also abolished TNFalpha-induced AKT activation, needed for NFkappaB activity. Therefore, the polyphenolic phytochemicals in the pomegranate can play an important role in the modulation of inflammatory cell signaling in colon cancer cells.
In vitro antioxidant activity and quantitative estimation of phenolic content of antidiabetic plants
- U A Deokate
- S S Khadabadi
Deokate, U. A., & Khadabadi, S. S. (2009). In vitro antioxidant activity and quantitative estimation of phenolic content of antidiabetic plants. Pharmacologyonline, 3, 647–651.