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Anti-HIV-1 integrase compound from Pometia pinnata leaves
Pharmaceutical Biology
Abstract
Context:
HIV-1 integrase (HIV-1 IN) is a key enzyme involved in the replication cycle of the retrovirus. Any new knowledge on inhibitors of this enzyme could provide essential clues for the development of anti-HIV drugs.
Objective:
To evaluate anti-HIV-1 IN activity of some Thai medicinal plant extracts, and the extract that possessed the strongest anti-HIV-1 IN activity was subjected to isolation of the active compounds.
Materials and methods:
Ethanol extracts of eight Thai medicinal plants were evaluated for their inhibitory effect against HIV-1 IN. An extract of Pometia pinnata J. R. Forst. & G. Forst (Sapindaceae) leaves that possessed the strongest anti-HIV-1 IN activity was fractionated to isolate the active compounds by anti-HIV-1 IN assay-guided isolation process.
Results and discussion:
The leaf extract from P. pinnata had the strongest anti-HIV-1 IN activity with an IC50 value of 8.8 µg/mL. An anti-HIV-1 IN assay-guided isolation of the active compounds from a leaf extract of P. pinnata resulted in the isolation of one active compound, identified as proanthocyanidin A2. Proanthocyanidin A2 showed satisfactory anti-HIV-1 IN activity with an IC50 value of 30.1 µM. Three flavonoids, epicatechin, kaempferol-3-O-rhamnoside, quercetin-3-O-rhamnoside; a glycolipid, 1-O-palmitoyl-3-O-[α-.-galactopyranosyl-(1 → 6)-β-.-galactopyranosyl]-sn-glycerol; a steroidal glycoside; stigmasterol-3-O-glucoside; and a pentacyclic triterpenoid saponin, 3-O-α-.-arabinofuranosyl-(1 → 3)-[α-.-rhamnopyranosyl-(1 → 2)]-α-.-arabinopyranosyl hederagenin were also isolated but were inactive at a concentration of 100 µM.
... The nuclear magnetic resonance (NMR) spectrum of compound 1 showed a triterpene saponin composed of an aglycone moiety and a sugar moiety. Comparison of the spectra of compound 1 with those of saponins reported in the literature [19] identified the saponin as 3-O-α-L-arabinofuranosyl(1→3)-α-L-rhamnopyranosyl(1→2)-α-L-arabinopyranoside of hederagenin ( Figure S2). ...
... Additionally, we identified relatively high levels of the natural compound and potent candidate anti-obesity agent HGS 1 in matoa peel but not in salak peel. HGS 1 has already been isolated from matoa leaves [19], which also contain another type of HGS, 3-O-[α-L-arabinofuranosyl(1→4)-α-Lrhamnopyranosyl(1→2)-α-L-arabinopyranosyl]hederagenin [23]. Matoa (P. ...
... The eluted fractions were collected and dried to yield compound 1 (14.2 mg; 0.4% yield). Compound 1 was identified by NMR spectroscopy and compared with data from the literature [19,23,38,39]. NMR spectra were recorded on an ECZ-600R (JEOL Ltd., Tokyo, Japan). ...
Fruit peels, pericarps, or rinds are rich in phenolic/polyphenolic compounds with antioxi-dant properties and potentially beneficial effects against obesity and obesity-related non-communicable diseases. This study investigated the anti-obesity effects of matoa (Pometia pinnata) and salak (Salacca zalacca) fruit peel. Neither matoa peel powder (MPP) nor salak peel powder (SPP) affected the body weight, visceral fat weight, or serum glucose or lipid levels of Sprague-Dawley rats when included as 1% (w/w) of a high-fat diet (HFD). However, MPP significantly decreased the hepatic lipid level. MPP at a dose of 3% (w/w) of the HFD decreased body weight, visceral fat, and serum triglyceride levels as well as the hepatic lipid content. The inhibitory effect of MPP on hepatic lipid accumulation was not enhanced when its concentration was increased from 1% to 3% of the HFD. The anti-obesity effect of matoa was partly explained by the inhibitory effect of the matoa peel extract on fatty acid-induced secretion of ApoB-48 protein, a marker of intestinal chylomicrons, in differentiated Caco-2 cell monolayers. We identified hederagenin saponins that are abundant in MPP as potential anti-obesity substances. These results will contribute towards the development of functional foods with anti-obesity effects using the matoa fruit peel.
... Pometia pinnata English: Fijian longan Sinhala: Bulumora / Gal mora Leaves and bark P. pinnata leaves and bark are traditionally used for the treatment of fever and fester. The leaf extract had a strong anti-HIV-1 protease activity, which is a key enzyme involved in the replication cycle of the retrovirus (Suedee et al., 2013). ...
... Anthocyanin is a glycoside, while anthocyanidin is an aglycone (sugar free constituent) (Pour et al., 2019). They are responsible for the colors, red, purple, and blue; they are in grains, cereals, fruits and vegetables (Pour et al., 2019;Suedee et al., 2013). Cell culture studies, in silico studies, animal models, and human clinical trials, show that both anthocyanidins and anthocyanins possess antiviral activities. ...
... Moreover, studies report that anthocyanins could inhibit Infuenza virus adsorption on the cell surface, interfere with virus internalization and completely inhibit the growth of Infuenza A virus (Pour et al., 2019). Apart from anthocyanin, proanthocyanidin found in Pometia pinnata also showed in vitro antihuman immunodeficiency virus activity with the probable antiviral mechanism inhibiting viral RNA synthesis (Suedee et al., 2013). ...
The search for novel and effective drugs is an important challenge, as a severe acute respiratory syndrome caused by a zoonotic coronavirus (SARS-CoV-2) is affecting the entire world population. As of 18th April 2021 there were over 140 million confirmed cases and more than 3
million deaths due to COVID-19. Natural herbal drugs are a rich resource for novel antiviral drug development. Many studies and traditional medical practices have shown their effectiveness against
various human pathogens like the influenza virus, hepatitis C virus, coronavirus and the human immunodeficiency virus. Although modern synthetic drugs based on Western medicine are used in developed countries, traditional plant-based drugs are an integral part of medical treatment, including Sri Lanka. In Sri Lanka, the administration of crude herbal drug formulations dates back more than 3000 years. Numerous studies have shown that natural herbal drugs possess a wide spectrum of biological and pharmacological properties, such as anti-inflammatory, anti-angiogenic and anti-neoplastic. Accordingly, these herbs have been used for centuries in Sri Lankan traditional
medicine to treat various disorders. Despite the potency, none of these herbal medicines has yet been approved as a therapeutic antiviral agent against SARS-CoV-2 due to a lack of data from clinical trials. This review summarizes the current knowledge and future perspectives of the antiviral effects of potent Sri Lankan herbal drugs as potential sources of effective anti-coronavirus therapies.
... Each extract was collected and then evaporated using a rotary vacuum evaporator at a temperature of 50-60°C and a speed of 35 rpm, and then, placed in a water bath until a thick ethanol extract was obtained. The thick extract was then weighed, and the rendement was calculated [12]. ...
... This might be because the compounds that had high activity as DPPH radical scavenger in the matoa stem bark extract mostly presented in the ethyl acetate fraction. This might be because the compounds had high activity as DPPH radical [12,23]. The ethanol extract of matoa leaves also contained steroid compounds, but the concentration might have been too small to detect in the tests performed in this study. ...
... In addition, the polyphenolic compound was known to have activity as a tyrosinase inhibitor, but this activity was strongly influenced by the structure of the polyphenolic compound [2]. Polyphenolic compounds in the matoa leaves, based on the previous research, were proanthocyanidin A2, epicatechin, kaempferol-3-Orhamnoside, and quercetin-3-O-rhamnoside [12], while the matoa stem bark contained leucoanthocyanidin and condensed tannins [10]. These compounds had a high DPPH scavenging activity, such as quercetin (IC 50 = 0.83 µg/mL) and kaempferol (IC 50 = 1.87 µg/mL) (Cho et al., 2003). ...
Objective: This study aims to investigate the potency of matoa as a tyrosinase inhibitor and antioxidant and also to identify the chemical compounds in the most active fraction and an ethanol extract from the leaves and stem bark of matoa.Methods: The extracts were tested for their tyrosinase inhibitory activity by evaluating the formation of L-dopachrome at 490 nm. Antioxidant activity was tested using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The most active extract from liquid-liquid partition analysis was fractionated, and then, the assays were performed.Results: The ethanol extract of leaves and stem bark of matoa showed weak anti-tyrosinase activity (percent inhibition was 24.54±0.22% and 21.93±0.57%, respectively, final concentration 200 μg/mL), but they showed strong DPPH radical scavenging activity (IC50 values were 6.11 μg/mL and 5.47 μg/mL, respectively). The ethyl acetate fraction was the most active fraction with an IC50 value of 5.38 μg/mL. Ethanol extract from the leaves and stem bark of matoa and the ethyl acetate fraction contains flavonoids, tannins, saponins, triterpenoids, and glycosides.Conclusion: Matoa does not have potency as a tyrosinase inhibitor, but it has good antioxidant activity, although still lower than that of quercetin.
... Alpinia zerumbet procyanidins * influenza A virus, inhibition of attachment, virucidal [173,174] Chamaecrista nictitans procyanidins HSV-1 and HSV-2, NA [175] Cinnamomum cassia dimers, oligomers HIV-1, interaction with envelope glycoproteins [176] Cinnamomum zeylanicum trimers, tetramers Pomelia pinnata dimers HIV-1, inhibition of integrase activity [184] Sambucus nigra dimers HIV-1, interaction with envelope glycoproteins [176] Theobroma cacao dimers HSV and HIV, NA [124] Vaccinium macrocarpon monomers, dimers, trimers, tetramers, procyanidins nairovirus, inhibition of attachment [185] influenza A and B virus, inhibition of attachment [186,187] and entry, virucidal HSV-1 and HSV-2, inhibition of entry [188] human norovirus surrogates: murine norovirus (MNV-1), feline calicivirus (FCV-F9), virucidal [189,190] reovirus, NA [191] rotavirus, inhibition of attachment, interaction with capsid proteins [192,193] Vaccinium myrtillus dimers, trimers SARS-CoV-2, inhibition of entry and replication [194] HA, NA [195] HCV, inhibition of replication [196] Vitis vinifera dimers, trimers, tetramers, procyanidins rotavirus, affecting virion integrity HIV-1, inhibition of entry by down-modulation of co-receptors [193] [197] ...
... With the aim to investigate the anti-integrase (IN) activity of some Thai medicinal plant extracts, they discovered that PAC-A 2 derived from a leaf extract of Pometia pinnata inhibited the HIV-1 enzyme with an IC 50 value of 30.1 µM. However, this result was obtained from an in vitro enzymatic assay, and no evidence of this PAC-A 2 activity in the context of HIV-1 infection was reported [184]. Moreover, Tietjen et al. [180] identified the ixoratannin A-2 as HIV-1 inhibitor with an EC 50 value of 35 µM. ...
A-type proanthocyanidins (PAC-As) are plant-derived natural polyphenols that occur as oligomers or polymers of flavan-3-ol monomers, such as (+)-catechin and (−)-epicatechin, connected through an unusual double A linkage. PAC-As are present in leaves, seeds, flowers, bark, and fruits of many plants, and are thought to exert protective natural roles against microbial pathogens, insects, and herbivores. Consequently, when tested in isolation, PAC-As have shown several biological effects, through antioxidant, antibacterial, immunomodulatory, and antiviral activities. PAC-As have been observed in fact to inhibit replication of many different human viruses, and both enveloped and non-enveloped DNA and RNA viruses proved sensible to their inhibitory effect. Mechanistic studies revealed that PAC-As cause reduction of infectivity of viral particles they come in contact with, as a result of their propensity to interact with virion surface capsid proteins or envelope glycoproteins essential for viral attachment and entry. As viral infections and new virus outbreaks are a major public health concern, development of effective Broad-Spectrum Antiviral Agents (BSAAs) that can be rapidly deployable even against future emerging viruses is an urgent priority. This review summarizes the antiviral activities and mechanism of action of PAC-As, and their potential to be deployed as BSAAs against present and future viral infections.
... and Thonn. (Phyllanthaceae) (EC 50 : 0.4 mM; S.I. 29.7 (Notka et al. 2003), as well as camelliatannin H from C. japonica L (IC 50 0.9 mM), and chebulagic acid (Ajala et al. 2014) are active (Park et al. 2002), as well as the condensed tannin proanthocyanidin A2 (Suedee et al. 2013;Shahat et al. 1998). ...
... HIV integrase inhibitors are phenolics such as apigenin 7-Ob-D-(4 00 -caffeoyl) glucuronide (Lee et al. 2003), kuwanon L (Esposito et al. 2015), orobol, lithospermic acid (Bailly and Cotelle 2005), catechin (Panthong et al. 2015), wedelolactone (IC 50 4 lM), 1,3,6-tri-O-galloyl-b-D-glucopyranose, 1,2,3,4,6penta-O-galloyl-b-D-glucopyranose (Ahn et al. 2002), chebulagic acid (Ajala et al. 2014) as proanthocyanidin A2 (Suedee et al. 2013). ...
Context
The emergence of zoonotic viruses in the last decades culminating with COVID-19 and challenges posed by the resistance of RNA viruses to antiviral drugs requires the development of new antiviral drugs.
Objective
This review identifies natural products isolated from Asian and Pacific medicinal plants with in vitro and in vivo antiviral activity towards RNA viruses and analyses their distribution, molecular weights, solubility and modes of action.
Materials and methods
All data in this review was compiled from Google Scholar, PubMed, Science Direct, Web of Science, ChemSpider, PubChem and library search from 1961 to 2022.
Results
Out of about 350 molecules identified, 43 phenolics, 31 alkaloids, and 28 terpenes were very strongly active against at least one type of RNA virus. These natural products are mainly planar and amphiphilic, with a molecular mass between 200 and 400 g/mol and target viral genome replication. Hydroxytyrosol, silvestrol, lycorine, tylophorine and 12-O-tetradecanoylphorbol 13-acetate with IC50 below 0.01 µg/mL and selectivity index (S.I.) above 100 have the potential to be used for the development of anti-RNA virus leads.
Discussion and conclusions
The medicinal plants of Asia and the Pacific are a rich source of natural products with the potential to be developed as lead for the treatment of RNA viral infections.
... yang merupakan tanaman dari famili Sapindaceae telah banyak digunakan sebagai obat tradisional oleh masyarakat etnis tertentu sebagai antibakteri terhadap bakteri S. aureus, antivirus terhadap HIV-1N, dan antioksidan. 4,5,6 Hasil penelitian menunjukkan daun matoa mengandung senyawa golongan flavonoid, tanin, polifenol, alkaloid dan terpenoid. 7 Senyawa organik yang terisolasi dari daun matoa adalah golongan flavon (auron). ...
... Bahan utama yang digunakan adalah daun matoa yang didapatkan dari Desa Sarimulyo, Banyuwangi, Jawa Timur metanol (Brataco, Indonesia), etanol 96% (Brataco, Indonesia), etil asetat (Brataco, Indonesia), DPPH (Sigma-Aldrich, USA), Vitamin C (Sigma-Aldrich, USA), dapar fosfat pH 6,9 NaOH (Merck KGaA, Jerman), enzim α-amilase (Sigma-Aldrich, USA), Na 2 HPO 4 (Merck KGaA, USA), NaH 2 PO 4 (Merck KGaA, USA), KNaC 4 H 4 O 6 .4H 2 O (Pudak, Indonesia), subsrat pati kentang (Merck KGaA, Jerman), Akarbosa (Sigma-Aldrich, USA), 3,5-dinitrosalisilat (Sigma-Aldrich, USA), akuabides steril (Ikapharmindo Putramas, Indonesia). ...
Matoa (Pometia pinnata J.R. Forst. & G. Forst.) Matoa (Pometia pinnata J.R. Forst. & G. Forst.) is one of the plants that is used as a traditional medicine for diabetes mellitus due to an imbalance between the amount of ROS and antioxidants in the body. Therefore, it was carried out in vitro to see the antioxidant and antidiabetic activity in matoa leaf extract. The extraction of matoa leaves was carried out using the ultrasonication method for 30 minutes with methanol, ethanol, and ethyl acetate as solvents. Antioxidant activity is release through DPPH free radical inhibition, through the antidiabetic potential released by inhibiting the work of the α-amylase enzyme. Phytochemical test results showed the presence of secondary metabolites in the form of flavonoids, polyphenols, tannins, alkaloids, and terpenoids. The results of the research on methanol, ethanol, and ethyl acetate extracts of matoa leaves showed high antioxidant activity with IC50 values of 6.416 ± 0.176 ppm, 8.622 ± 0.066 ppm, and 170.637 ± 4.441 ppm, respectively, but they were less potent than vitamin C as a comparison which is 1.646 ± 0.015 ppm. Inhibition of the α-amylase enzyme showed IC50 values of 91.037 ± 0.750 ppm, 105,166 ± 2,423 ppm, and 785,436 ± 11,740 ppm in each of the methanol, ethanol, and ethyl acetate extracts while the IC50 value of acarbose as a comparison was 23,479 ± 0.347 ppm. The statistical data analysis of Pearson correlation showed that it had a positive relationship between the antioxidant and antidiabetic activity of matoa leaf extract as seen from the R-value of 0.998. The higher antioxidant activity, so the higher potential for inhibition of α-amylase enzyme.
... Hypertension is a condition where the systolic pressure is equal to or higher than 140 mmHg, and the diastolic pressure or diastolic blood pressure is more than 90 mmHg (Kumar et al., 2014). (Suedee, Tewtrakul & Panichayupakaranant, 2013). These compounds are thought to be responsible for ACE inhibition in matoa leaves. ...
... The mechanisms that occur in ACE inhibitors can be used as a reference for the inhibitory mechanisms that occur in plant compounds. It is possible that the matoa leaves may be able to act as a hypertension drug (Suedee, Tewtrakul & Panichayupakaranant, 2013). ...
Introduction: The matoa plant (Pometia pinnata) leaves can be used to treat hypertension. Matoa leaves are thought to have antihypertensive activity because they contain flavonoids. These flavonoids can reduce blood pressure that is modulated by the renin-angiotensin-aldosterone system (RAAS). It is suspected that matoa leaves have antihypertensive activity as they contain quercetin which is a compound that is presumed to be an angiotensin-converting enzyme (ACE) inhibitor. Aims: This study aims to determine which extracts and fractions from matoa leaves are able to decrease angiotensin I levels. Methods: The extraction was done by maceration with 96% ethanol solvent and fractionated by a liquid method using an n-hexane fraction solvent, an ethyl acetate fraction, and a water fraction. In this study, 21 male Wistar rats were used as test animals and divided into seven groups: Group I was the normal control, group II was the negative control (CMC-Na 1%), group III was the positive control (Irbesartan), group IV was given matoa leaf extract with 60 mg/200g body weight ratio, Group V was given 2.34 mg/g fraction of n-hexane, Group VI was given ethyl acetate fraction 9.54 mg/200g ethyl acetate fraction, and Group VII was given water fraction 7.98 mg/200g water fraction. The data obtained was analysed using the Shapiro-Wilk test, the Levene test, and analysis of variance (ANOVA). Results: The results showed that the angiotensin I levels induced by angiotensin II were more significant (p < 0,05) than those in the normal and negative groups. The ethyl acetate fraction showed a 23.6% decrease in angiotensin I level, which was close to the 24.8% decrease in the positive group. The extract from the matoa leaves showed a 17.2% decrease in angiotensin I levels which were close to the 20% decrease in the positive group.
... Recently, the tyrosinase inhibitory activities from the ethanol extract of the bark and leaves were studied (Sauriasari et al., 2017). Furthermore, the ethanol extract of the leaves and proanthocyanidin A2 from P. pinnata leaves indicated strong anti-HIV activity (Suedee et al., 2013). Nevertheless, there are no reported flavonol glycosides isolated from P. pinnata leaves as α-glucosidase inhibition. ...
... for C 21 H 20 O 10 Na, 455.0954; error 2.2 ppm). Compared the spectral data of the isolated compound with literature, we confirmed this isolated compound 1 as kaempferol-3-O-rhamnoside (afzelin) (Suedee et al., 2013). ...
Pometia pinnata belonging to the Sapindaceae family has been traditionally used as the therapeutic agent for burns and wounds in Indonesia. Based on the result of the experiment conducted, the ethyl acetate fraction of P. pinnata leaves showed strong α-glucosidase inhibitory activity. After two flavonol rhamnoside compounds were isolated from ethyl acetate fraction of P. pinnata leaves methanol extract using chromatography method, their structures were identified as kaempferol-3-O-rhamnoside (1) and quercetin-3-O-rhamnoside (2). The ultra-performance liquid chromatography-electrospray ionization time-of-flight mass spectrometry (UPLC-ESI-TOFMS) chromatogram showed compounds 1 and 2 were the major compounds of the ethyl acetate fraction. In this study, the structure-activity relationship among the kaempferol, quercetin, and their derivatives bearing sugar moiety were also evaluated. Among tested eight compounds, kaempferol 7 (percent inhibition = 80.10% ± 0.8) and quercetin 8 (percent inhibition = 82.93% ± 0.4) had stronger α-glucosidase inhibitory activity than that of other derivatives. Among kaempferol derivatives bearing sugar moiety, compound 1 showed the strongest activity. Moreover, compound 2 showed strong α-glucosidase inhibitory activity among quercetin derivatives. Therefore, it can be confirmed that the hydroxyl group at C-3 position is very important for α-glucosidase inhibitory activity of flavonol compounds.
... Until now, there have been very few studies on the chemical composition and pharmacological activities of this plant, with one report on an antifungal activity of P. pinnata leaf extracts against Phytophthora infestans [3]. In addition, our previous study on the isolation of an active compound from a crude ethanol extract of P. pinnata leaves using an anti-HIV-1 integrase assay-guide isolation afforded a polyphenol, proanthocyanidin A2 (Figure 1), which exhibited a satisfactory anti-HIV-1 integrase activity with an IC 50 value of 30.1 µM [4]. Proanthocyanidin A2 has also been shown to possess several pharmacological activities such as immunomodulatory [5], antioxidant [5,6], antiviral [5,7], and anti-HIV [8,9]. ...
... Standard proanthocyanidin A2 was previously purified [4]. Acetonitrile (HPLC-grade) and analyticalgrade methanol were from Labscan Asia (Bangkok, Thailand). ...
A reverse-phase high-performance liquid chromatographic method was described for the determination of proanthocyanidin A2 in Pometia pinnata leaf extracts. The method utilized a Phenominex® Luna 5u Hilic column with a mixture of 2% acetic acid and acetonitrile (step gradient elution as follows: 0-4 min, 5:95; 5-9 min, 10:90; 10-14 min, 80:20 v/v) as the mobile phase at a flow rate of 1 mL/min, and UV detection at 280 nm. The parameters of linearity, precision, accuracy, specificity and sensitivity of the method were evaluated. The extraction methods for proanthocyanidin A2 were also examined. Proanthocyanidin A2 was eluted within 7 min with a satisfactory peak resolution. The recovery of the HPLC method was 96-98% with a good linearity (r2≥ 0.9999) for proanthocyanidin A2 in the concentration range of 7.7 - 250 µg/mL. A high degree of specificity as well as repeatability and reproducibility (RSD values less than 5%) were also achieved. The limits of detection and quantification were 1.25 and 2.50 µg/mL, respectively. This eatablished specific, precise, accurate, rapid and reproducible HPLC method was successfully used to quantify the active principle, proanthocyanidin A2 in P. pinnata leaf extracts. Proanthocyanidin A2 was found to be a major constituent in the crude methanol extract of P. pinnata leaves, at 33.8 ± 0.4 mg/g dried extract. Microwave-assisted extraction (MAE) was selected as the best extraction method for proanthocyanidin A2. The optimized MAE method increased the amount of proanthocyanidin A2 extracted from the dried leaf powder up to 36.6 %w/w.
... -α-L-arabinopyranosil hederagenin [11]. ...
Matoa (Pometia pinnata) is a plant used as a floral identity in Indonesia, especially in Papua. Local people use boiled water from matoa leaves, which is believed to treat hypertension. Matoa leaves are traditionally used as a therapeutic agent for burns and wounds in Indonesia. Phytochemical screening of matoa leaf extract contains secondary metabolite compounds, including flavonoids, steroids, tannins, and saponins. So far, many of these activities have been reported from the polyphenol group. This research aimed to identify the phytochemical composition of matoa leaves from Kudus in the ethanolic extract using LC-MS. The total phenolic content of ethanol extract using the Folin Ciocalteu method was 35.689 ± 0.726 mg GAE/g extract. The total flavonoid content of ethanol extract using the AlCl3 colorimetric method was 1.384 ± 0.012 mg QE/g extract. Twelve compounds could be identified in the ethanol extract of matoa leaves. The phenolic compounds were vanillin, p-hydroxybenzaldehyde, p-Coumaroyl glycolic acid, syringic acid, gallic acid, phenol, and vanillic acid. The flavonoid compounds were identified as epigallocatechin and apigenin -7-O-diglucuronide. The organic compound was identified as jasmonic acid. The aromatic compound was identified as benzene. Besides, tannin compounds were also identified. The major compounds in matoa leaves from Kudus, Central Java, are vanillin, phenol, and benzene.
... 3.48 Me-6 00 ) prove the occurrence of rhamnosyl unit in the compound. Moreover, (Heteronuclear Multiple Bond Correlation) HMBC correlation between the anomeric proton at 5.52 ppm with the anomeric carbon at 134.9 ppm validates that sugar moiety is attached to the C-3 hydroxyl group (Suedee et al. 2013). ...
... Senyawa quercetin-3-Orhamnoside dan kaemferol -3-O-rhamnoside diduga memiliki aktivitas untuk menghambat ACE pada daun matoa. Mekanisme yang terjadi pada penghambatan ACE dapat dijadikan acuan mekanisme dalam penghambatan yang terjadi pada senyawa tanaman, sehingga dapat diduga daun matoa memiliki aktivitas sebagai obat hipertensi [8]. ...
Daun matoa (Pometia pinnata) merupakan salah satu tanaman yang diduga memiliki aktivitas hipertensi karena mengandung kuersetin. Penelitian yang dilakukan oleh (Purwidyaningrum, 2017) ekstrak dan fraksi-fraksi daun matoa memiliki aktivitas sebagai antihipertensi dengan dosis efektif 150 mg/kg. Penelitian lain yang dilakukan oleh (Elisa, 2019) efek yang dapat menurunkan tekanan darah adalah ekstrak dosis 300 mg dan fraksi etil asetat 30 mg yang diinduksi angiotensin II mampu menurunkan tekanan darah sistolik dan diastolik. Tujuan penelitian ini yaitu untuk mengetahui pemberian ekstrak dan fraksi-fraksi daun matoa dalam penurunan kadar renin dan kadar angiotensin II. Serbuk daun matoa diekstraksi dengan metode maserasi menggunakan pelarut etanol 96% dan difraksinasi menggunakan pelarut n-heksana, etil asetat, air. Dalam penelitian ini menggunakan 21 ekor tikus putih jantan galur wistar dibagi dalam 7 kelompok, kelompok I (normal), kelompok II kontrol negatif (CMC 1%), kelompok III kontrol positif (Irbesartan), kelompok IV (ekstrak daun matoa 60 mg/200g), Kelompok V (fraksi n-heksana 2,34 mg/200g), kelompok VI (fraksi etil asetat 9,54 mg/200g), kelompok VII (fraksi air 7,98 mg/200g). Hasil penelitian menunjukkan ekstrak dan fraksi-fraksi daun matoa tidak berbeda signifikan terhadap kelompok positif dalam menurunkan tekanan darah, kadar renin dan angiotensin II dan berbeda signifikan terhadap kelompok normal dan negatif. Fraksi air (7,98 mg/200g) menunjukkan penurunan tekanan darah sistolik 9,0% dan diastolik 7,1%, Fraksi etil asetat menunjukkan penurunan kadar renin 23,6%. EDM menunjukkan penurunan kadar angiotensin II 17,2%. Kata kunci : Pometia pinnata; kadar renin; kadar angiotensin II; induksi angiotensin II
... Matoa (Pometia pinnata) is an endemic tree species that grows rapidly in tropical and subtropical regions, including Indonesia. The leaves contain phenolic compounds such as proanthocyanidin A2, epicatechin, kaemferol-3-O-rhamnose, and quercetin-3-O-rhamnose [14]. This plays an active role as a reducing agent because it has free electrons that can be donated. ...
This paper reports the synthesis and its application to the adsorption of methylene blue dye using graphene-oxide (GO) and reduced graphene-oxide (RGO). Among carbon-based nanomaterials, graphene and its derivatives have received remarkable attention due to their unique thermal, mechanical, and electronic properties and two-dimensional structure. The GO was synthesized by the modified Hummers method (chemical exfoliation) of graphite flake. This reaction produced graphite oxide (GrO) as an intermediate material. The synthesized materials, namely graphite, graphene oxide, and reduced graphene oxide, were characterized by XRD, FTIR, and Raman spectroscopy. These materials were tested to evaluate their adsorption capacity, concentration, contact time, and adsorbent weight on methylene blue, which was analyzed using a UV-vis spectrophotometer. The XRD pattern showed the formation of 2θ peaks at 24° to 26 o for graphite, graphene oxide, and reduced graphene oxide, respectively. Furthermore, characterization by FTIR showed the appearance of O-H groups with peaks of 3358 cm ⁻¹ and 3342 cm ⁻¹ for graphene and reduced graphene oxides. Raman characterization indicated that reduced graphene oxide has a wavelength at the D-band peak of about 1375 cm ⁻¹ and the G-band peak reaching 1597 cm ⁻¹ with an ID/IG intensity ratio of 0.8. The adsorption test of methylene blue showed that reduced graphene oxide had the best adsorption capacity with an adsorbent, concentration, optimum time, and highest adsorption capacity value of 25 mg, 30 ppm, 45 minutes, and 15.642 mg/g. The adsorption process followed the Langmuir isotherm rule, as evidenced by the R ² value of 0.9881.
... Potensi senyawa ini diperkuat dengan penelitian yang pernah dilakukan oleh Suedee et al pada tahun 2013 bahwa pada daun matoa terkandung senyawa Quercetin-3-Orhamnoside dan Kaemferol 3-O-rhamnoside yang efektif dalam menurunkan sirkulasi blood flow dengan mekanisme penurunan tekanan darah. Senyawa ini telah diuji klinis dan dosis yang signifikan dalam menurunkan tekanan darah adalah 150 mg-730 mg per hari dengan penggunaan selama 4 sampai 5 minggu secara oral (Suedee, Tewtrakul, and Panichayupakaranant 2013). ...
Hipertensi adalah naiknya tekanan darah sistolik dan diastolik lebih dari 140/90. Salah satu tanaman yang berpotensi sebagai antihipertensi adalah matoa yang mengandung senyawa Quercetin-3-O-rhamnoside dan Kaemferol 3-O-rhamnoside yang diyakini berpotensi sebagai antihipertensi. Pada penelitian ini, peneliti ingin mengetahui persentase penurunan blood flow pada tikus jantan yang diinduksi angiotensin II menggunakan ekstrak etanol daun matoa. Pengerjaan ini dimulai dengan membuat ekstrak etanol dari daun matoa dan membaginya dalam 3 variasi dosis, yaitu 75 mg/kgBB, 150 mg/kgBB, dan 300 mg/kgBB, kemudian diberikan perlakuan ke hewan uji yang telah diinduksi angiotensin II. Hasil penelitian menunjukkan bahwa variasi 3 dosis ekstrak etanol daun matoa dengan dosis 75 mg/kgBB, 150 mg/kgBB, dan 300 mg/kgBB, menunjukkan hasil berbeda. Ekstrak etanol daun matoa dengan dosis 75 mg/kgBB memiliki persentase penurunan 44.47%. Ekstrak etanol daun matoa dengan dosis 150 mg/kgBB memiliki persentase penurunan 53.36%. Ekstrak etanol daun matoa dengan dosis 300 mg/kgBB memiliki persentase penurunan 67.35%. Disimpulkan bahwa ekstrak terbaik yang berpotensi dalam menurunkan sirkulasi aliran darah atau blood flow adalah ekstrak etanol daun matoa dosis 300 mg/kgBB.
... ] were identified as 1-O-palmitoyl-3-O-[α-D-galactopyranosyl-(1→6)-β-D-galactopyranosyl]glycerol (3)[33], gingerglycolipid C (4)[34], gingerglycolipid B (5)[35], 3-O-octadeca-9Z,12Z,15Z-trienoylglyceryl-6′-O-(α-D-galactopyranosyl)-β-D-galactopyranoside (6) [35], 1-O-palmitoyl-2-O-linoleoyl-3-O-[α-D-galactopyranosyl-(1→6)-β-D-galactopyranosyl]glycerol (7) [36], 1-O-octadecanoyl-2-O-(9Z,12Z-octadecadienoyl)-3-O-[α-D-galactopyranosyl-(1′′→6′)-O-β-D-galactopyranosyl] glycerol (8) [37], 1-O-linoleoyl-2-O-oleoyl-3-O-[α-D-galactopyranosyl-(1→6)-β-D-galactopyranosyl]-glycerol (9) [38], 2,3-O-dioctadeca-9Z,12Z-dienoylglyceryl-6′-O-(α-D-galactopyranosyl)-β-D-galactopyranoside (10) [35], 2-O-octadeca-9Z,12Z-dienoyl-9Z,12Z,15Z-trienoylglyceryl-6′-O-(α-D-galactopyranosyl)-β-D-galactopyranoside (11) [39], 1-O-(9Z,12Z-octadecadienoly)-3-O-β-galactopyranosylglycerol (12) [40], 3-O-octadeca-9Z,12Z,15Z-trienoylglyceryl-O-β-D-galactopyranoside (13) [33], 1-O-oleoyl-2-O-myristoyl-glyceryl-O-β-D-galactopyranoside (14) [35], 1,2-O-diacyl-3-O-β-D-galactopyranosyl glycerols (15) [37], 2,3-O-dioctadeca-9Z,12Z-dienoylglyceryl-O-β-D-galactopyranoside (16) [35], 1-O-(9Z, 12Z-octadecadienoyl)-3-O-[β-D-galactopyranosyl-(1→6)-O-β-D-galactopyranosyl-(1→6)-O-β-D-galactopyranosyl] glycerol (17) [41], 1,2-O-(9Z,12Z-octadecadienoyl)-3-O-[α-D-galactopyranosyl-(1′′′′′→6′′′′)-O-β-D-galactopyranosyl-(1′′′′→6′′′)-O-β-D-galactopyranosyl]-glycerol (18)[31]. Their chemical structures were described inFigure 4. ...
Two new (1, 2 viz Rubracin D and E) and sixteen known Glyceroglycolipids (3–18) in the saprophytic fungus Tubeufia rubra (PF02-2) from decaying wood in freshwater habitat were isolated and identified. Their chemical structures were elucidated via means of the extensive spectroscopic analyses of NMR, HR-ESI-MS and UV spectra, as well as comparison with literature data. The new compounds were assayed for the reversal activity of multidrug resistance (MDR) on MCF-7/ADM, K562/ADM and A549/ADM cell lines, and both compounds 1 and 2 reversed MDR in the three resistant cancer cell lines with concentration dependence. In the assay on K562/ADM, both new compounds had been proved to have remarkable MDR reversal effects, which were higher than those of the positive control viz Verapamil (Vrp). Meanwhile, in the assay on A549/ADM, compound 1 displayed significant MDR reversal effects, which were also higher than those of Vrp at certain concentrations. Furthermore, the Western blot assay proved that both new compounds reversed the MDR in the resistant cancer cell line viz MCF-7/ADM by inhibiting the overexpression of P-glycoprotein. This is the first report that the Glyceroglycolipids isolated firstly from the fungal genus Tubeufia reversed MDR in resistant cancer cells.
... However, the monomeric epicatechin recorded relatively lower activity at 34.6 μg/ml. Proanthocyanidin A 2 isolated from leaves of Pometia pinnata has been reported to have satisfactory anti-HIV-1 integrase activity with 50% inhibitory concentration (IC 50 ) value of 30.1 µM (Suedee et al., 2013). The compound has also been reported to exert in vitro anti-HIV-1 activity through the reduction of viral RNA synthesis (Gallina et al., 2011). ...
Background
Aphloia theiformis is used in Makete district, Tanzania, and other areas by HIV and AIDS patients as a weight loss remedy and for treatment of tuberculosis. However, there is no literature information on its antimycobacterial activity.
Purpose
To evaluate antimycobacterial activity of A. theiformis root ethanolic extract and isolated compounds.
Methods
The broth microdilution method was used to test the crude root ethanolic extract for activity against different non-pathogenic mycobacteria. Bioautography was used to identify the active constituents. Isolation of the active compounds was carried out using bioassay-guided fractionation. Chemical structures of compounds were established by comparison of their spectra with literature spectral data. The isolated compounds and some fractions were screened for activity against M. tuberculosis (MTB) subtype H37Rv and clinical isolates of MTB including strains resistant to rifampicin.
Results
The 80% ethanolic extract of A. theiformis displayed activity against all non-pathogenic mycobacteria. The most active fraction was the ethyl acetate fraction from which two compounds were isolated; an epicatechin dimer; proanthocyanidin A2 (1) and tormentic acid (2) belonging to ursane pentacyclic triterpenoid. Compound (1) had MICs of 60.7 µM against Mycobacterium madagascariense and Mycobacterium indicus pranii and 255 µM against both standard MTB (H37Rv) and clinical isolate of rifampicin-resistant MTB.
Conclusion
This study provides evidence in support of the use of A. theiformis extracts by traditional health practitioners for the management of tuberculosis. We recommend more studies to further assess efficacy and safety of the plant constituents using different models.
... pinnata) is a fruit tree widely grown in Southeast Asia. Studies on P. pinnata showed that the plant has antibacterial effects, antioxidant benefits, and anti-HIV properties, [26] while its diuretic activity has also been determined on rats [27]. Although ferric oxide has been synthesized using aqueous leaf extract of P. pinnata [28]; however, to the authors' knowledge, there has been no report on the synthesis of CeO 2 using the aforementioned plant extract. ...
Cerium oxide nanoparticles (CeO2 NPs) were synthesized using aqueous leaf extract of Pometia pinnata acting as an oxidizing, capping, and stabilizing agent. The structural, morphological, and optical properties of the synthesized CeO2 NPs (S-CeO2) were characterized by X-ray diffraction (XRD), Fourier transform-infrared spectroscopy (FT-IR), field emission-scanning electron microscopy (FE-SEM), field emission-transmission electron microscopy (FE-TEM), selected area electron diffraction (SAED), X-ray photoelectron spectroscopy (XPS), UV–Visible diffuse reflectance spectroscopy (UV–Vis DRS), and photoluminescence (PL). XRD results confirmed the formation of a single and pure cubic phase of CeO2 NPs with crystallite sizes ranging 6–9 nm. The FT-IR analysis exhibit Ce–O stretching around 600–400 cm⁻¹. SEM and TEM images showed almost spherical shapes of synthesized CeO2 NPs with particle size 3–28 nm. FE-TEM and SAED displayed highly crystalline lattice fringes. The optical studies using UV–Vis DRS and PL showed lowered band gap energy of 2.66 eV and stimulated response, respectively. XPS studies further confirmed the formation of S-CeO2 and valence band-XPS revealed reduction of band gap energy. This study showed that the green synthesized CeO2 NPs using aqueous leaf extract of Pometia pinnata have acquired enhanced optical properties and could be extended for synthesis of other metal oxides.
... 14,24 This research is supported by Kuspradini research that there is an antioxidant and antibacterial activity in Matoa leaf extract, where Matoa Leaf extract has a strong enough ability to inhibit the growth of gram-negative and positive bacteria at a concentration of 100%. 14,25 Previous research conducted by Tiffanny stated that the content of basil extract with a concentration of 80% with 0 live colonies was effective in inhibiting the growth of Neisseria Gonorrhoeae 15 , and research conducted by Marera stated that mangosteen peel extract with concentrations of 80% effectively inhibited the growth of Neisseria gonorrhoeae with 0 live colonies. 16 However, in this study, Matoa leaf extract with practical live colony measurements at concentrations of 20% with 0 live colonies stated that Matoa leaf extract was more sensitive than basil leaf extract. ...
Background: Gonorrhea cases experiencing antibiotic resistance are increasing due to inadequate treatment or failure to contribute to an increase in antibiotic resistance cases; WHO suggests adding herbal therapy treatment methods is expected to minimize the occurrence of drug resistance as much as possible. Previous studies that have been carried out using other herbal plants have not shown any potential to inhibit the growth of Neisseria gonorrhoeae bacteria, seen from the amount of extract concentration and the dosage and content of the compounds in the contents monitoring the time.Objective: To analyze the difference in the effect of various concentrations of Matoa Leafs Extract (Pometia Pinnata) compared to 500mg Levofloxacin on the increase in the growth inhibition of Neisseria gonorrhoeae.Methods: This is true-experimental research with a post-test-only control group with a randomized design. The sample in this study was the microorganism Neisseria gonorrhoeae obtained through vaginal swabs in 2 females (FSW) positive for Gonorrhea by gram staining and microscopic examination and culture on Chocolate Agar Plant (CAP) media. The culture was then suspended in CAP media. Matoa Leaf extract concentration of 100%, 80%, 60%, 40%, 20%, positive control with Levofloxacin 500 mg and negative control with distilled water with four replications and monitoring in 24 hours, 48 hours, 72 hours, and 96 hours. Data analysis used Kruskal-Wallis, Mann-Whitney, and cohen's test. Result: Levofloxacin 500mg in inhibiting Neisseria Gonorrhoeae bacteria is very effective, and Matoa Leaf extracts 60% and 40% P=0,026 have a strong enough potential to inhibit the growth of Neisseria gonorrhoeae bacteria with the same potential strength. The cohen's test 1.4 effect the levofloxacin 500mg provides a significant influence inhibiting Neisseria Gonorrhoeae.Conclusion: Matoa Leaf extract 60%, and 40% have solid antibacterial potential, although not as strong as Levofloxacin 500mg.
... The disappearing peaks at the range of 500-600 nm is an indication of the reduction of some secondary metabolite. A previous study identified some secondary metabolites such as kaempferol-3-O-rhamnoside, glycolipid, epicatechin, quercetin-3-O-rhamnoside, steroid glycosides, and other saponin compounds as the components of PPE [23,24]; the reduction of Sn 2+ possibly involves the functional groups of those compounds. Taking quercetin as one of the bioreductors, the reduction mechanism is as presented in Figure 3. ...
The present study reported biofabrication of flower-like SnO2 nanoparticles using Pometia pinnata leaf extract. The study focused on the physicochemical characteristics of the prepared SnO2 nanoparticles and its activity as photocatalyst and antibacterial agent. The characterization was performed by XRD, SEM, TEM, UV-DRS and XPS analyses. Photocatalytic activity of the nanoparticles was examined on bromophenol blue photooxidation; meanwhile, the antibacterial activity was evaluated against Klebsiella pneumoniae, Escherichia coli Staphylococcus aureus and Streptococcus pyogenes. XRD and XPS analyses confirmed the single tetragonal SnO2 phase. The result from SEM analysis indicates the flower like morphology of SnO2 nanoparticles, and by TEM analysis, the nanoparticles were seen to be in uniform spherical shapes with a diameter ranging from 8 to 20 nm. SnO2 nanoparticles showed significant photocatalytic activity in photooxidation of bromophenol blue as the degradation efficiency reached 99.93%, and the photocatalyst exhibited the reusability as the degradation efficiency values were insignificantly changed until the fifth cycle. Antibacterial assay indicated that the synthesized SnO2 nanoparticles exhibit an inhibition of tested bacteria and showed a potential to be applied for further environmental and medical applications.
... It was reported that Pometia pinnata (P. pinnata) contains antibacterial capabilities, antioxidant benefits, and have anti-HIV properties [21]. This plant was used for the studies on the diuretic activity of rats and it was reported to be able to control the excretion of potassium and sodium levels in urine [22]. ...
Synthesized cerium oxide nanoparticles (S-CeO2 NPs) and 1%, 5% and 10% zirconium doped CeO2 (Zr-doped CeO2) NPs were fabricated using aqueous leaf extract of Pometia pinnata. The synthesized NPs were characterized using standard techniques which confirmed successful synthesis of NPs with particle size ranging from 12 to 23 nm and band gap energy of 2.54–2.66 eV. Photoantioxidant activities showed enhanced activities under visible light irradiation in comparison to the dark condition in the dose-dependent study. Biofilm inhibition studies showed ~ 73% biofilm inhibition of Staphylococcus aureus at 512 µg/mL for S-CeO2, whereas 10% Zr-doped CeO2 NPs showed biofilm inhibition of 52.7%. The bactericidal tests showed killing properties at 1024 µg/mL of S-CeO2 NPs and at 512 µg/mL of 1% Zr-doped CeO2. Reduced bactericidal activities were observed for 5% and 10% Zr-doped CeO2. These studies showed that the fabricated NPs have both good photoantioxidant and antibacterial properties.
... Similar trends were also reported on anti-HIV-1 IN inhibitory activities of A. galanga, Piper betel, Plumbago indica, R. nasutus, Z. cassumunar, [37] Caesalpinia sappan, [38 -39] Citrus hystrix, [25] and G. cowa, [40][41] and on anti-HIV-1 protease (PR) inhibitory activities of Caesalpinia sappan, S. tora, [38,42] and G. mangostana. [43] In addition, anti-HIV reverse transcriptase (RT) inhibitory activities of Punica granatum, Plumbago indica, Caesalpinia sappan, G. mangostana, R. nasutus, and Citrus hystrix have been indicated. ...
Viral protein R (Vpr) is an accessory protein in Human immunodeficiency virus‐1 (HIV‐1) and has been suggested as an attractive target for HIV disease treatment. Investigations of the ethanolic extracts of twelve Thai herbs revealed that the extracts of the Punica granatum fruits, the Centella asiatica aerials, the Citrus hystrix fruit peels, the Caesalpinia sappan heartwoods, the Piper betel leaves, the Alpinia galangal rhizomes, the Senna tora seeds, the Zingiber cassumunar rhizomes, the Rhinacanthus nasutus leaves, and the Plumbago indica roots exhibited the anti‐Vpr activity in Hela cells harboring the TREx plasmid encoding full‐length Vpr (TREx‐HeLa‐Vpr cells). Moreover, the investigation of the selected main constituents in Punica granatum , Centella asiatica , A. galangal , and Caesalpinia sappan indicated that punicalagin, asiaticoside, ellagic acid, madecassic acid, madecassoside, zingerone, brazilin, and asiatic acid possessed anti‐Vpr activities at the 10µM concentration. Among the tested extracts and compounds, the extracts from Centella asiatica and Citrus hystrix and the compounds, punicalagin and asiaticoside, showed the most potent anti‐Vpr activities without any cytotoxicity, respectively.
... Viral enzyme inhibition by polar extract: Ethanol extract of leaves inhibited Human immunodefciency virus type-1 integrase with an IC 50 value of 47.6 µg/mL (Suedee et al., 2013). ...
... The di-aromatic ring-fused 2, 8-dioxabicyclo[3.3.1]nonanes embodying a highly strained methylene-bridged polycyclic skeleton represent an interesting template in numerous pharmaceuticals, and their derivatives are known to exhibit useful biological and pharmacological properties such as inhibition versus antiviral [3], antiinflammatory [4], antitumor [5], antioxidant [6], anti-HIV-1 activities [7], and antimicrobial [8], etc. Well-known compounds bearing a methylene-bridged bicyclic moiety, e.g., biflavanoids, dracoflavan D and dracoflavan C are known to occur in medicinal plant sources ( Fig. 1) [9]. ...
An environmentally benign and straightforward synthetic approach for the assembly of a new class of diverse symmetrical substituted di-aromatic-fused 2,8-dioxa/dithiabicyclo[3,3,1]nonane derivatives containing methylene-bridged bicyclic framework via reusable cross-linked polystyrene-supported p-toluenesulfonic acid-catalyzed tandem reactions of substituted phenols/selected thiophenol with 1,1,3,3-tetramethoxypropane under neat conditions has been reported in which four new chemical bonds (two C–C/two C–O)-(two C–C/two C–S), two new six-membered cycles, and two new stereogenic tertiary carbon centers were constructed in a single operation. The synthetic utility of this method was also demonstrated. In addition, this present protocol could be successfully extended to the selected naphthols and dihydroxynaphthalenes as the enol partner of phenols with high efficiency. The developed transformation featured high efficiency, the use of commercially accessible feedstocks, excellent regioselectivity, simple operation, gram-scale synthesis, and good functional group compatibility. Furthermore, the solvent-free conditions, easily recoverable catalyst, and efficient recycling render the protocol green, economic and sustainable.
... Kadar fenolik ini merupakan kadar senyawa yang berperan sebagai antioksidan dalam ekstrak.6 Suedee et al. yang melakukan penelitian pada buah matoa menemukan senyawa fenolik seperti proantosianidin A2 yang dapat berperan sebagai anti HIV-1 integrase dan kaempferol-3-O-ramnosida dan kuersetin-3-O-ramnosida yang berfungsi sebagai antioksidan dan antibakteri.12 ...
ABSTRACT: Oxidative stress plays an important role in the pathogenesis of various diseases such as, diabetes, chronic obstructive pulmonary disease, chronic kidney disease, chronic cardiovascular disease, chronic neurodegenerative disease, and cancer. This oxidative stress occurs when there is an imbalance between free radicals and antioxidant. Therefore, in order to restore that balance a sufficient antioxidant is needed. This antioxidant can be obtained from phytochemical compounds in herbs such as matoa fruit (Pometia pinnata). This study aims to determine the phytochemical profile, antioxidant capacity, total phenolic content, total alkaloid content, and the toxicity of matoa fruit. Thus, several in vitro and bioassay tests were conducted, namely phytochemical test based on Harborne, antioxidant capacity based on DPPH method, total phenolic content, total alkaloid content, and toxicity test based on BSLT method.This study showed that the extract contains alkaloids, anthocyanin and betacyanin, cardioglycosides, flavonoids, glycosides, phenolics, quinones, saponins, terpenoids, tannin; antioxidant capacity test (IC50 = 4757.19 g/mL); total phenolic content (884.46 g/mL); total alkaloid content (2.59 g/mL); toxicity test (LC50 = 402.92 g/mL). From these results, it can be concluded that this matoa fruit extract is a weak antioxidant and toxic. This toxicity result indicates that this extract has an antimitotic potential while the phenolic and alkaloid content represent the level of compounds that act as antioxidants.
KEYWORDS: Pometia pinnata; phytochemical profile; antioxidant capacity; total phenolic and alkaloid content; toxicity test
... The α configuration of a glycosidic linkage was evidenced by a small coupling constant for the anomeric proton signal (J = 1.8 Hz) in the 1 H NMR spectrum and a large magnitude of the coupling constant between the anomeric proton and carbon signals, J = 172 Hz, determined from the residual signals in the HMBC spectrum. Hence, compound 8 was identified as kaempferol 3-Oα-rhamnopyranoside ( Figure 1) and the NMR spectra are in agreement with reported data [37,38]. ...
Three germacranolides, as well as five flavonoids, natural steroid and simple phenolic compounds, were isolated from the inflorescence of Stizolophus balsamita growing in Iran. The paper presents active compounds found for the first time in the inflorescence of this species. The flavonoids, simple phenolic compounds and natural steroids have been isolated for the first time in the genus Stizolophus. The MTT assay was employed to study in vitro cytotoxic effects of the taxifolin against human fibroblasts. We also evaluate the possible biological properties/cosmetic effects of Stizolophus balsamita extract and taxifolin on the human skin. Sixty healthy Caucasian adult females with no dermatological diseases were investigated. We evaluate the effects of S. balsamita extract and taxifolin on skin hydration and transepidermal water loss (TEWL). It was revealed that S. balsamita extract might decrease TEWL level and fixed the barrier function of the epidermis. The presence of bioactive phytochemical constituents in S. balsamita inflorescences makes them a valuable and safe source for creating new cosmetics and medicines.
... In this regard, Sanguisorba officinalis [11] and Pelargonium sidoides [12] extracts inhibited the entry of the virus into the cells. Pometia pinnata [13] and Mimusops elengi [14] leaf extracts can modulate the activity of HIV integrase and numerous vegetable extracts showed inhibitory potential on reverse transcriptase [15,16]. ...
... 3 Penelitian terbaru juga menunjukkan bahwa ektrak daun matoa berpotensi sebagai obat infeksi HIV. 4 Berdasarkan data diatas, peneliti tertarik untuk melakukan uji analgetik ekstrak kulit batang pohon matoa pada mencit. ...
Pain is an unpleasant sensation that derives from the complex neurochemical processes in the central and peripheral nervous systems. Side effects of drugs inter alia opioids and NSAIDs can cause serious disorders, therefore, it is necessary to find and develop other effective analgesic drugs with low toxicity. In Indonesia, matoa (Pometia pinnata) is known as a typical plant in Papua especially in West Papua. In some countries, parts of matoa plants are used as traditional medicine. This study aimed to determine the analgesic effect of matoa bark extract (Pometia pinnata) on mice Mus musculus. This was an experimental study. Nine male mice weighed 30 g were divided into 3 groups, each consisted of 3 mice. Group I, the negative control group, was given aquadest; group II, the positive control group, was given aspirin solution; and group III, the treated group, was given matoa bark extract. Analgesic effect was determined by counting the mice movements (licking their back legs or jumping) during 1 minute in a beaker with a temperature of 550C. The results showed that after 30 minutes the average number of movements of the treated group decreased from 22 times to 19.3 times, and continued to decrease until 1 movement after 120 minutes. Conclusion: Matoa bark extract showed analgesic effect on mice Mus musculus.Keywords: analgesic effect, matoa bark, miceAbstrak: Nyeri adalah sensasi yang tidak menyenangkan yang berasal dari proses neurokimia kompleks di sistem saraf pusat dan perifer. Opioid dan golongan AINS dapat menimbulkan efek samping yang cukup berat; oleh karena itu, diperlukan obat analgesik yang efektif dengan toksisitas rendah. Di Indonesia, matoa (Pometia pinnata) dikenal sebagai tanaman khas Papua terutama Papua Barat. Di beberapa negara, bagian-bagian dari tanaman matoa telah digunakan sebagai obat tradisional. Penelitian ini bertujuan untuk mengetahui efek analgesik ekstrak kulit batang pohon matoa (Pometia pinnata) pada mencit Mus musculus. Penelitian ini menggunakan metode eksperimental. Sembilan ekor mencit jantan dengan berat rata-rata 30 g dibagi atas 3 kelompok hewan uji yang masing-masing terdiri dari 3 ekor mencit. Kelompok I yaitu kelompok kontrol negatif diberikan akuades; kelompok II yaitu kelompok kontrol positif diberikan larutan aspirin; dan kelompok III yaitu kelompok perlakuan diberikan ekstrak kulit batang matoa. Efek analgesik berupa jumlah gerakan mencit selama 1 menit saat diletakan di dalam beker dengan suhu tetap 550C. Gerakan yang dihitung berupa gerakan menjilat kaki belakang atau meloncat. Hasil penelitian menunjukkan bahwa pada menit ke-30 terjadi penurunan rerata jumlah respon gerakan mencit dari 22 kali menjadi 19,3 kali yang terus berkurang hingga menit ke-120 dimana hanya terdapat 1 gerakan. Simpulan: Ekstrak kulit batang pohon matoa memiliki efek analgesik pada mencit Mus musculus.Kata kunci: efek analgesik, kulit batang matoa, mencit
... Matoa leaves (Pometia pinnata) contains antioxidant. Previous study by Suedee et al, 2013 succeed to isolate epicatechin, kaempferol-3-O-rhamnoside, quercetin-3-O-rhamnoside, glycolipid, 1-O-palmitoyl-3-O-[A-galactopyranosyl-(1→6)-β-galactopyranosyl]-sn-glycerol, steroid glycosides, stigmasterol-3-O-glucoside and triterpenoid saponin pentacyclic, 3-O-α-arabinofuranosyl-(1→3)-[α-rhamnopyranosyl-(1→2)]-α-arabinopyranosyl hederagenin from matoa leaves extract. A potential of hepatoprotective property underlying matoa leaves may be attributed to the antioxidative constituents (Akachi, et al., 2010). ...
The hepatoprotective effects of matoa leaves were evaluated by paracetamol-induced injury in rat’s hepatocytes. The ethanolic extract of matoa leaves (EEML) at doses of 200, 300, 500 mg/kg, po and silymarin at dose of 100 mg/kg, po were given for seven days. Silymarin was given as the reference drug. Hepatoprotective effect was studied by measuring the level of AST, ALT, ALP and total protein in serum. In vivo, oral treatment with EEML at dose of 500 mg/kg significantly reduced AST, ALT, ALP in serum whereas total protein was not significantly reduce in each groups. These results indicate that the hepatoprotective action of EEML is likely related to its potent antioxidative activity. Neutralizing reactive oxygen species enhancing the activity of original natural hepatic-antioxidant enzymes may be the main mechanisms of EEML against paracetamol-induced injury.
Keywords: Matoa Leaves (Pometia pinnata), Paracetamol, Silymarin, Hepatoprotection
... Ranting, daun Bahan obat tradisional Mahang Tirik *Bahan obat tradisional yang telah diketahui kandungan kimianya. Sumber: Al-Abd et al. (2015), Anoop dan Bindu (2015), Ee et al. (2011), Hassan et al. (2013), Ibrahim et al. (2014), Katrin et al. (2014), Kinghorn et al. (2011), Lai et al. (2009), Mah et al. (2011), Mailina et al. (2010, Muharn dan Elfita (2011), Mulyadi et al. (2014), Naemsuvan et al. (2015), Palanisamy et al. (2011, Pasaribu dan Setyawati (2011), Suedee et al. (2013), Zuhud et al. (2013. ...
p> Abstract
Central Kalimantan has diversity of peat swamp forests that contribute to germplasm repository, especially of medicinal plants. The objective of this study was determine the conservation status of medicinal plant, especially the structure, composition, and diversity. Data were obtained by Line Transect Plot Method, made 40 observation plots different of levels, each measuring 20 m × 20 m, 10 m × 10 m, 5 m × 5 m, and 1 m × 1 m with a total area of 2.104 ha. All plants were measured and identified from various diameter classes, which resides in the observation plots. Density level of the tree reached 93.140 stems/ha and basal area 10.606 m2/ha, pole level 622.50 stems/ha, basal area 17.1606 m²/ha, the sapling level 5,450 stems/ha, basal area 41.712 m2/ha, and seedling density 6,975 stems/ha. In all of the observation plots was found 56 medicinal plants species in 48 genera and 30 families. Based important value index (IVI), Diospyros borneensis Hiern and Combretocarpus rotundus Dans were the most dominating, and followed by seedlings level of Syzygium zeylanicum (L.) DC. Diversity index was in the range 1<H'≤3. There were six species of medicinal plants protected based PP No. 7/1999, three species in CITES, and 15 species in the IUCN.
Abstrak
Kalimantan Tengah memiliki keanekaragaman hutan rawa gambut yang berperan bagi gudang plasma nutfah, khususnya tumbuhan obat. Penelitian ini bertujuan untuk mengetahui status konservasi spesies tumbuhan obat, khususnya yang berhubungan dengan struktur, komposisi, dan keanekaragaman. Pengumpulan data menggunakan Metode Jalur Berpetak, dibuat 40 petak pengamatan pada berbagai tingkat pertumbuhan yang masing-masing berukuran 20 m × 20 m, 10 m × 10 m, 5 m × 5 m, dan 1 m × 1 m dengan luas total 2,104 ha. Semua tumbuhan berbagai kelas diameter yang berada di dalam petak pengamatan dicatat, diukur, dan diidentifikasi. Kondisi vegetasi tumbuhan obat dicirikan oleh tingkat kerapatan pohon dengan rata-rata 93,140 batang/ha dan luas bidang dasar 10,606 m2/ha, tiang 622,50 batang/ha, luas bidang dasar 17,1606 m2/ha, pancang 5.450 batang/ha, dan luas bidang dasar 41,712 m2/ha, serta semai tingkat kerapatan 6.975 batang/ha. Dalam seluruh petak pengamatan terdapat 56 spesies tumbuhan obat, termasuk dalam 48 marga dan 30 famili. Berdasarkan indeks nilai penting spesies, Diospyros borneensis Hiern dan Combretocarpus rotundus Dans merupakan spesies yang paling dominan, diikuti tingkat semai Syzygium zeylanicum (L.) DC. Nilai indeks keanekaragaman pada kisaran 1<H'≤3. Terdapat enam spesies tumbuhan obat yang dilindungi berdasarkan PP No. 7/1999, tiga spesies termasuk dalam CITES, dan 15 spesies termasuk dalam daftar IUCN.</p
... In this regard, Sanguisorba officinalis [11] and Pelargonium sidoides [12] extracts inhibited the entry of the virus into the cells. Pometia pinnata [13] and Mimusops elengi [14] leaf extracts can modulate the activity of HIV integrase and numerous vegetable extracts showed inhibitory potential on reverse transcriptase [15,16]. ...
New drugs would be beneficial to fight resistant HIV strains, in particular those capable of interfering with essential viral functions other than those targeted by highly active antiretroviral therapy drugs. Despite the central role played by Tat protein in HIV transcription, a search for vegetable extracts able to hamper this important viral function was never carried out. In this work, we evaluated the chemical composition and possible interference of essential oil from Thymus vulgaris, Cananga odorata, Cymbopogon citratus and Rosmarinus officinalis with the Tat/TAR-RNA interaction and with Tat-induced HIV-1 LTR transcription. GC/MS analysis demonstrated that biodiversity of herbal species translated into essential oils composed of different blends of terpenes. In all of them, 4-6 constituents represent from 81,63 to 95,19% of the total terpenes. Essential oils of Thymus vulgaris, Cymbopogon citratus and Rosmarinus officinalis were active in interfering with Tat functions, encouraging further studies to identify single terpenes responsible for the antiviral activity. In view of the quite different composition of these essential oils, we concluded that their interference on Tat function depends on specific terpene or a characteristic blend. This article is protected by copyright. All rights reserved.
... The previous study by Suedee et al. [9] succeed to isolate epicatechin, kaempferol-3-O-rhamnoside, quercetin-3-O-rhamnoside, glycolipid, 1-O-palmitoyl-3-O-[A-galactopyranosyl-(16)-β-galactopyranosyl]sn-glycerol, steroid glycosides, stigmasterol-3-O-glucoside and triterpenoid saponin pentacyclic, 3-O-α-arabinofuranosyl-(13)-[α-rhamnopyranosyl-(12)]-α-arabinopyranosyl hederagenin from matoa leaves extract that had activity as anti-HIV. ...
Objective: The purpose of this study was to determine diuretic activity of matoa leaves (Pometiapinnata) extracts and fraction and its influence on potassium and sodium levels.Methods: Matoa leaves were extracted by reflux method followed by evaporation using rotary evaporator. The subjects were male Wistar rats that were divided into 11 group furosemide (3.6 mg/kg bw), control group CMC 0.5%, matoa leaves extracts with doses of 50 mg/kg bw, 100 mg/kg bw, 150 mg/kg bw, matoa leaves aqueous fraction with dose of 10.94 mg/kg bw, 21.88 mg/kg bw, 32.82 mg/kg bw, matoa leaves ethyl acetate fraction with dose of 4.35 mg/kg bw, 8.71 mg/kg bw, 13.06 mg/kg bw. Rats were placed in metabolic cagesduring observation study. Urine volume was measured for 5 to 24 hours. Potassium and sodium levels in urine were determined by using Atomic Absorption Spectrophotometry.Results: The effective dose of matoa leaves extract and fractions for diuretic activity was matoaleaves ethyl acetate fraction 8.71 mg/kg bw which could increase the excretion of sodium and potassium in the urine of the male Wistar rats.Conclusion:Matoa leaves extract and fractions could increase the excretion of sodium and potassium in the urine of the male Wistar rats.
... It was demonstrated that they provide higher chemical diversity in comparison with the libraries of organic synthetic molecules [216]. Due to that, screening of plant extracts and other libraries of natural products is widely used for discovery of new anti-HIV agents [216][217][218][219][220][221][222][223][224][225][226][227][228][229][230][231][232][233] (http://www.ibscreen.com). We predicted the biological activities associated with the molecular mechanisms of anti-HIV action using computer program PASS (Prediction of Activity Spectra for Substances) [234] (http://www.way2drug.com/passonline) ...
Human immunodeficiency virus is responsible for acquired immunodeficiency syndrome (AIDS), an infectious disease that consists a serious concern worldwide for more than three decades. By the end of 2013 UNAIDS estimated that there were 35 million (range 33.2–37.2 million) adults and children living with HIV/AIDS worldwide. Despite the introduction of highly active antiretroviral therapy (HAART), the need for new anti-HIV agents is extremely high because the existing medicines do not provide the complete curation and exhibit serious side effects, and their application leads to the appearance of resistant strains. This chapter explores the medicinal chemistry efforts that gave rise to currently launched drugs as well as investigational anti-HIV agents. Currently used and studied molecular targets of antiretrovirals and the main classes of HIV-1 inhibitors are presented. Among the future prospects, we discuss the efforts directed to overcome the latent HIV infection, utilization of natural products as potential anti-HIV agents, recent trends on development of biologics as potential anti-HIV medicines, and application of computer-aided methods in the discovery of new anti-HIV drugs.
Hiperkolesterolemia dan hipertensi merupakan penyakit kardiovaskular yang berbahaya. Beberapa faktor resiko bersifat permanen seperti usia, jenis kelamin, genetik dan faktor lainnya dapat dimodifikasi seperti merokok, kurangnya aktivitas fisik, gizi buruk, tekanan darah tinggi, diabetes tipe II, dislipidemia dan obesitas. Aterosklerosis dan hipertensi berpotensi berkembang menjadi penyakit kardiovaskular yang berbahaya seperti infark miokard dan stroke. Bahan alam banyak digunakan sebagai alternatif pengobatan kardiovaskular seperti daun matoa, daun matoa banyak digunakan sebagai oabat diabetes melitus, diare dan disentri. Tujuan penelitian ini adalah untuk melihat efektivitas dan pengaruh lama pemberian ekstrak dan fraksi daun matoa Pometia pinnata J. R Forst & G. Forst terhadap penurunan kolesterolemia dan hipertensi pada hewan uji. Pada penelitian ini menggunakan hewan uji berupa tikus dan burung puyuh. Pengukuran tekanan darah menggunakan instrumen CODA®, dan pengukuran kadar kolesterol meggunakan fotometer klinik. Hasil dari penelitian ini menunjukkan bahwa pemberian ekstrak daun matoa dapat mempengaruhi kadar kolesterolemia dengan dosis yang efektif 300 mg/kgbb, dan fraksi daun matoa mempengaruhi tekanan darah dengan dosis efektif Kesimpulan dari penelitian ini menyatakan ekstrak dan fraksi daun matoa dapat menurunkan kadar kolesterol dalam darah dan tekanan darah pada hewan percobaan serta semakin tinggi dosis yang diberikan maka semakin tinggi juga penurunannya.
Nanoparticle investigation is an interesting field of science. The powerfully sized- cognate characteristics of nanoparticles provide numerous possibilities for unexpected innovations. The performance of nanoparticles endure tremendous opportunity for pioneering high-tech application programs, but also stances excessive concerns to the researchers. At present, engineered nanoparticles uphold the outstanding potential in diversified fields of society such as the field of medicine, science, and industry without revealing its toxic implications. However, the growing production and utilization of engineered nanoparticles also arouse concern about inattentive exposure and the feasibility of detrimental effects on human wellness and biological complex. Thus, it is the most pressing need for examining the toxicity along with the application of such advantageous nanomaterial. Nanoparticles are atomic or molecular clusters with the size varying between 1 to 100 nm. Toxicity mechanisms of metal and metal oxide nanoparticles can transpire by various approaches like non-homeostasis impacts, oxidative stress, genotoxicity, implications, etc. Components that influence the metal and metal oxide nanoparticles are size, dissolution, and ways of exposure.
This chapter will highlight an overview of metals and metal oxide nanoparticles and their toxic effects on living beings and biological systems.
Medicinal herbs are a rich source of therapeutic agents for the prevention and cure of diseases and ailments. They were used in folklore medicine in the treatment of toothache and strengthening of gums, anthelmintic, kidney diseases, analgesic, anti-inflammatory, hepatoprotective, antihyperglycaemic, antihyperglycaemic, and anticancer. There are many plants that have potential analgesic and anti-inflammatory activities and, many more plants are screened for the phyto-constituents having pain relief and anti- inflammatory properties to replace non-steroidal and opioid drugs, which have severe side effects. Different phyto-constituents like alkaloids, flavonoids, xanthone, coumarin, sterols, withaferin-A, andrographolide, etc., are proved effective as an analgesic and anti- inflammatory agents. Previous studies have contributed much to the understanding of the compound(s) responsible for the known anti-inflammatory and analgesic action. Drugs which are used presently for the management of pain and inflammatory conditions are either steroidal like corticosteroids or non-steroidal like aspirin. All of these drugs possess more or less side and toxic effects like renal failure, allergic reactions, hearing loss or they may increase the risk of hemorrhage by affecting platelet function. On the contrary, many medicines of plant origin had been used for ages without any adverse effects. It is therefore essential that efforts should be made to introduce new medicinal plants to develop more effective and cheaper drugs. Plants represent a large natural source of useful compounds that might serve as a source for the development of novel drugs. This chapter summarizes various medicinal plants and herbs with anti- inflammatory and analgesic properties that have been used by our ancestors to cure many of their ailments.
The kidney play essential biological roles necessary to maintain good health. The strategic physiological position of the kidney in metabolic processes expose it to the adverse effect of diseases emanating from other organs or systems. Abnormal metabolic processes as well as genetic defects can also induce injuries within the organ leading to kidney diseases that can progress to End Stage Renal Disease (ESRD). Prompt diagnoses and management are vital to reverse or slow the rate of progression and renal replacement therapy required for advanced stages to sustain life. This chapter is a review the biological roles of the kidneys in man, the diseases of the kidney, diagnostic parameters of kidney disease and nephroprotective mechanisms of phytochemicals in medicinal plants and natural drugs used by complementary and alternative medicine practitioners. Furthermore, factors militating against the application of herbal medicine in managing kidney diseases and some future perspectives are highlighted.
Camellia sinensis (tea) is an evergreen plant having bioactive compounds associated with various pharmacological effects, including anti-cancerous activity. These phytochemicals are variedly distributed in plant tissues. A detailed study to understand chemical composition within the economically underutilized tea tissues is required to generate value. Therefore, a comprehensive chemical profiling of underutilized C. sinensis parts [coarse leaves, flowers, fruits (immature); n = 9] was performed by NMR techniques. NMR (1D and 2D) spectroscopy ambiguously identified and quantified fifty-seven metabolites (Coarse leaves: 35, flowers; 42, immature fruits; 45). The statistical analysis showed apparent tissue-specific similarities (26 metabolites) and variations. Further, HPLC-DAD revealed absolute quantification of catechins, caffeine and theanine among the different parts of C. sinensis. Moreover, cytotoxicity studies of tea tissues against colorectal cancer cell lines showed anticancer potentials. This chemical information and anticancer activity of underutilized C. sinensis parts will help to develop value added nutraceutical and cosmeceutical products.
Traditional medicine utilizing different herbal formulations has been an age old tradition being practiced in Indian context. This very regime quintessentially caters to the concept of Ayurveda Yoga Unani Siddha and Homeopathy (AYUSH). Ailments pertaining to Ear, Nose and Throat (ENT) have been mitigated by modern medicinal practices. Given this fact, emergence of antimicrobial resistance owing to unprecedented use of antibiotics has crippled the scenario of modern medicine. Being as one of the emerging challenges, a need of Complementary and Alternative Medicine (CAM) has arisen in recent times. For this to accomplish, ethano-botanical studies based at phyto-chemical interventions are envisaged. These studies are to identify and validate potential bio-active compounds which can be utilized either singly or in a formulation as potential bio-therapeutic agents possessing promising pharmacological activity for circumventing ENT disorders. An emerging concept of re-purposing of drugs and respective molecular docking patterns is a focal theme of recent research investigations. This concept has led to emergence of Active Pharmaceutical Ingredients (API) aimed to ward off ENT ailments (bacterial and fungal) without posing an occurrence of adverse affects. The chapter would highlight significance of ethano-botanical studies with special reference of medicinal plants of Sub-himalayan region, screening of bio-active compounds in obliterating common ENT ailments, patho-physiology of associated pathogens, and concept of re-purposing of drugs thus proving an impetus towards green and herbal medicine.
Human immunodeficiency virus is recognized as a causative agent of the acquired immunodeficiency syndrome (AIDS) that comprises a serious concern globally for decades. Even after 40 years of the discovery of HIV, not many things have changed in the history of HIV/AIDS. Despite significant progress, mysteries related to HIV infection remain to be addressed. Highly active antiretroviral therapy (HAART), provides durable control of virus replication, however, it is not devoid of unwanted side effects, especially in persons undergoing long-term treatment. The current therapy finds its limitations in the emergence of multidrug resistance, the transmission of drug-resistant HIV strains, and life-long treatment. Further, AIDS patients suffer great socio-economic difficulties in obtaining treatment. Thus, there is an urgent need to develop novel anti-HIV agents. Plants/natural products continue to serve as a reservoir for the development of new drugs, including anti-HIV agents. This chapter deals with Plants/natural products that have shown anti-HIV activity.
Cerium oxide (CeO2) and 1%, 5% and 10% zirconium/tin-dual doped CeO2 nanoparticles (Zr/Sn-dual doped CeO2 NPs) were synthesized using an aqueous leaf extract of Pometia pinnata. By using UV-visible diffuse reflectance spectroscopy, the band gap energies of these materials were found to be in the range of ∼2.49 to 2.66 eV. The average crystallite sizes of the fluorite phase obtained from X-ray diffraction were between 7 and 16 nm. X-ray photoelectron spectroscopy (XPS) analysis further confirmed the synthesis of CeO2 and Sn-doped CeO2 NPs. Almost spherical shapes of the nanomaterials with an average particle size of 12-17 nm were determined using scanning electron microscopy and transmission electron microscopy studies. Photoantioxidant activities of the synthesized materials showed enhanced photoantioxidant response under visible light irradiation in comparison with those under dark conditions in both dose- and time-dependent manner. The CeO2 NPs exhibited a significant concentration-dependent antibiofilm activity against the Gram-positive bacteria Staphylococcus aureus (S. aureus) and Listeria monocytogenes (L. monocytogenes). Only the 10% Zr/Sn-dual doped-CeO2 NPs were found to inhibit S. aureus biofilm formation at higher concentrations. All Zr/Sn-dual doped CeO2 NPs exhibited a concentration-dependent biofilm inhibition of L. monocytogenes and also bactericidal activity towards S. aureus. These nanomaterials exhibited enhanced photoantioxidant activities and antibacterial properties, which make them suitable for various biological applications.
Matoa (Pometia pinnata JR Forst. & G Forst.) is one of Indonesia’s underutilized fruits, which can grow to giant trees up to 50 m (164 ft) and found naturally in the Asia-Pacific region, mainly in lowland tropical areas about 14°N to 20°S. Matoa fruit contains phytochemical compounds such as flavonoid, tannin, and saponin, secondary metabolite compounds derived from sugar metabolism. Sugar metabolism involved several genes that control the photosynthesis pathway. This research aimed to isolate and characterize the gene related to sugar metabolism depending on the assembled-transcriptome database genome against the UniProt database using the BLASTX program. Six gene sequences characterized 176,002 number of contigs that are nine contigs of Sucrose-phosphate synthase (SPS), four contigs of Sucrose-phosphate (SPP), 12 contigs of Sucrose synthase (SUS), 19 contigs of Alkaline/neutral invertase (INV), four contigs of Cytosolic invertase (CINV), 20 contigs of Beta-fructofuranosidase (CWINV). The research lays the foundation for a comprehensive study of biological mechanisms involved in sugar metabolism growth and the development life circle of matoa.
The single-step green synthesis has been successfully established to prepare a bi-phase structure of Zn/ZnO nanoparticles using laser ablation in a liquid medium. Nd: YAG laser with the wavelength of 1064 nm was employed to perform the laser ablation in pure water and Pometia pinnata (P. pinnata) leaf extract, with the leaf, were extracted in pure water and some concentration of ethanol. ZnO nanoparticles can be obtained via laser ablation in pure water, while the usage of P. pinnata leaf extract as the solution has caused the appearance of the bi-phase Zn/ZnO nanostructure. X-ray diffraction (XRD) pattern indicates the appearance of Zn peaks alongside with ZnO peaks with the inclusion of P. pinnata leaf extract. Transmission electron microscope (TEM) images show the change of shape from the rod-like shape into a spherical shape and smaller size spherical shape of Zn/ZnO nanoparticles in comparison with ZnO. Noticeable change of UV–visible spectrum emerges as the water was substituted by P. pinnata leaf extract. The zeta potential of Zn/ZnO prepared with P. pinnata extracted in water, with the value of − 18.9 V, reduces down to − 43.5 and − 41.1 for 20–40% of ethanol concentration, respectively. The as-prepared ZnO and Zn/ZnO colloidal samples were evaluated for their antibacterial activities against two strains Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). Zn/ZnO sample shows a more substantial antibacterial effect in comparison with pure ZnO, no bacteria alive after 12 and 24 h’ treatment for E. coli and S. aureus, respectively.
Nearly four decades have passed since the human immunodeficiency virus (HIV) was discovered as the causal agent of acquired immune deficiency syndrome (AIDS). Nevertheless, HIV continues to cause substantial morbidity and mortality, posing a formidable challenge to public health scenario all over the world. Globally, 36.9 million people were living with HIV at the end of 2017, with a burden of 1.8 million new cases added every year. In the meantime, the introduction of highly active antiretroviral therapy (HAART) could dramatically change the prognosis of HIV infection from high mortality to chronic illness. However, apart from the high cost and drug-induced toxicity, HAART in the long-term leads to the emergence of multidrug-resistant strains, which would surpass the rate of new drug development. Therefore, it is a challenge to discover safe and cost-effective drugs at the earliest, with the aim to hit specific targets in the HIV life cycle. Natural products, since time immemorial, serve as a prospective resource for the development of novel therapeutic agents. Many traditional medicinal plants exhibited anti-HIV activity, and a few of them were reportedly used for the management of HIV infections. Plants like Echinacea purpurea, Moringa oleifera, and Tripterygium wilfordii have undergone clinical trials for anti-HIV therapy. Quite a few phytochemicals like andrographolide, calanolide A, mangiferin, 3-O-(3′,3′-dimethylsuccinyl), betulinic acid (PA-457) are expected to play promising roles in future. Presently, we compiled recent findings on novel plant-derived products showing activity against HIV, along with putative mechanisms of action. Mainly, up-to-date information on target-based strategies to identify anti-HIV plant constituents will be presented in this chapter.
Pometia pinnata (Matoa) is widely known for its use in traditional medicines and as fruit sources in Indonesia. Stem bark and leaves of Matoa are the most used parts. Each part contains secondary metabolites, including flavonoids, tannins, triterpenoids, glycosides, and saponins. These compounds could act as reducing agents in the biosynthesis of silver nanoparticles. Our research attempts to compare the efficacy of aqueous extracts of Matoa leaf and stem bark in the biosynthesis of silver nanoparticles. We characterized products of silver nanoparticles using UV-Vis spectrophotometer, transmission electron microscope, and particle size analyzer to compare the biosynthesis between the two parts based on ratios of various concentrations of plant extract to silver nitrate (AgNO3). We found that the solution (extract and AgNO3) became darker as the concentration and reaction time increased. Increasing reaction time also caused an increase in absorption peak intensity due to the reduction process of silver ions. The use of leaf and stem bark for biosynthesis resulted in different shapes and sizes of silver nanoparticles; the use of leaves and stem bark resulted in sphere-shaped silver nanoparticles, whereas the use of aqueous leaf extracts triangle-shaped silver nanoparticles formed.
Traditionally, Pacific Islanders depended on crop production and fishing to sustain their daily diets and livelihoods. In recent years, Pacific consumers have become increasingly reliant on non-traditional and processed foods; which are often nutritionally poor, and high in fats, salts and sugars, which negatively impact Food and Nutrition Security (FNS). There is a rich biodiversity of terrestrial and marine organisms in the Pacific Island countries (PICs), many of which are yet to be fully studied and utilised for the bioactive compounds and health or nutritional value. Traditional local food crops and seafood that can contribute towards improving the health and nutrition situation and provide new income generation opportunities for local communities are underutilised. This report gives insights into the current status of knowledge on composition of key nutrients and bioactive compounds, known or associated with traditional crops and seafood consumed in seven Pacific Island countries, namely Fiji, Kiribati,Marshall Islands, Samoa, Solomon Islands, Tonga, and Vanuatu. Information was initially gathered through guided interviews with traditional knowledge experts. Based on their responses and a systematic literature review of 433 scientific articles, a total of 75 crops and marine resources were identified as commonly consumed and/or having health and nutrition benefits or foods which could be better used in the daily diets. Traditional leaders also gave reasons for declining consumption and limited utilisation of traditional foods. These included loss of traditional varieties, e.g. breadfruit and yam; loss of traditional knowledge on edible plants and seaweed from the wild, and lack of awareness on nutritional value and health benefits. For the fisheries and seafood sector there is scope for more sustainable management of resources, as stocks e.g. of sea cucumbers (bêche-de-mer) are dwindling due to overexploitation and climate change. Seaweeds are a relatively inexpensive source of protein, vitamins and minerals and contain bioactive compounds. However, more research is needed on the bioactive principles and associated health benefits of Pacific seaweed varieties and protocols should be developed for value added products for local consumption and for export markets. Some species e.g. sea cucumbers and shellfish could also be better targeted for development through aquaculture. Leguminous food crops and green leafy vegetables such as drumstick leaves, water spinach, and leaves of some root crops e.g. cassava and taro leaves, as well as fruits such as soursop and star fruit are nutritious and contain a number of bioactive compounds but remain underutilised and not part of a diversified diet of the Pacific Islanders. There is scope for further research on optimum production and postharvest handling systems to retain the health benefit (bioactive properties) and nutritional value and to enhance the agribusiness and market potential. Traditional knowledge of Pacific Islanders needs to be better harnessed and integrated with modern scientific knowledge to address the nutritional and health problems. The academic and research community need to provide the scientific evidence to validate the health and nutritional benefits and support Pacific communities in making more informed decisions. The consumption of local green leafy vegetables, fruits and leguminous crops as well as seaweeds and sea cucumbers need to be better promoted and their use encouraged. Affordability and consistent supply of these foods, which were identified as barriers to their uptake, could be improved. Overall, there is a need for greater collaborative research between governmental (Ministries of Agriculture, Ministries of Health), non-governmental and research and academic organisations, and local communities in Pacific Island countries to further develop crops and marine resources which are nutritious and also have bioactive compounds with health benefits e.g. anticancer, antidiabetic and cholesterol lowering.
Since the beginning of the epidemic, human immunodeficiency virus (HIV) has infected around 70 million people worldwide, most of whom reside is sub-Saharan Africa. There have been very promising developments in the treatment of HIV with anti-retroviral drug cocktails. However, drug resistance to anti-HIV drugs is emerging, and many people infected with HIV have adverse reactions or do not have ready access to currently available HIV chemotherapies. Thus, there is a need to discover new anti-HIV agents to supplement our current arsenal of anti-HIV drugs and to provide therapeutic options for populations with limited resources or access to currently efficacious chemotherapies. Plant-derived natural products continue to serve as a reservoir for the discovery of new medicines, including anti-HIV agents. This review presents a survey of plants that have shown anti-HIV activity, both in vitro and in vivo.
The purpose of this study was to determine diuretic activity of matoa (Pometia pinnata) extracts (leaves, peel, seeds) and its influence on potassium and sodium levels. Each crude drug was extracted by maceration method followed by evaporation using rotary evaporator. Male Wistar rats were divided into 11 groups i.e. furosemide (1.8 mg/ kg bw), control group CMC 0.5%, and matoa extracts (leaves, peel, seeds) each with doses of 50 mg/kg bw, 100 mg/kg bw, 150 mg/kg bw. Rats were placed in metabolic cages. Urine volume was measured for 4 hours. Potassium and sodium levels in urine were determined by using Atomic Absorption Spectrophotometry. The effective dose of ethanolic matoa leaves extract for diuretic activity was 100 mg/kg bw which could increase the excretion of sodium and potassium in the urine of the male Wistar rats. © 2016, International Journal of Pharmacognosy and Phytochemical Research. All rights reserved.
The dietary flavonoids, especially their glycosides, are the most vital phytochemicals in diets and are of great general interest due to their diverse bioactivity. The natural flavonoids almost all exist as their O-glycoside or C-glycoside forms in plants. In this review, we summarized the existing knowledge on the different biological benefits and pharmacokinetic behaviors between flavonoid aglycones and their glycosides. Due to various conclusions from different flavonoid types and health/disease conditions, it is very difficult to draw general or universally applicable comments regarding the impact of glycosylation on the biological benefits of flavonoids. It seems as though O-glycosylation generally reduces the bioactivity of these compounds - this has been observed for diverse properties including antioxidant activity, antidiabetes activity, antiinflammation activity, antibacterial, antifungal activity, antitumor activity, anticoagulant activity, antiplatelet activity, antidegranulating activity, antitrypanosomal activity, influenza virus neuraminidase inhibition, aldehyde oxidase inhibition, immunomodulatory and antitubercular activity. However, O-glycosylation can enhance certain types of biological benefits including anti-HIV activity, tyrosinase inhibition, antirotavirus activity, antistress activity, antiobesity activity, anticholinesterase potential, antiadipogenic activity, and antiallergic activity. However, there is a lack of data for most flavonoids, and their structures vary widely. There is also a profound lack of data on the impact of C-glycosylation on flavonoid biological benefits, although it has been demonstrated that in at least some cases C-glycosylation has positive effects on properties that may be useful in human healthcare such as antioxidant and antidiabetes activity. Furthermore, there is a lack of in vivo data that would make it possible to make broad generalizations concerning the influence of glycosylation on the benefits of flavonoids for human health. It is possible that the effects of glycosylation on flavonoid bioactivity in vitro may differ from that seen in vivo. With in vivo (oral) treatment, flavonoid glycosides showed similar or even higher antidiabetes, antiinflammatory, antidegranulating, antistress, and antiallergic activity than their flavonoid aglycones. Flavonoid glycosides keep higher plasma levels and have a longer mean residence time than those of aglycones. We should pay more attention to in vivo benefits of flavonoid glycosides, especially C-glycosides.
Seven compounds were isolated from the EtOH extraction of the twig of Carapa guianensis Aubl. (Meliaceae). On the basis of spectroscopic methods, their structures were elucidated as (-)-epicatechin-3-O-(3" , 5"-di-O-methyl) gallate (1), (-)-catechin (2), sciadopitysin (3), cleomiscosin B (4), photogedunin (5), chisocheton compound F (6) and odoratone (7), respectively. Among them compound 1 was a new flavane, compounds 2-7 were firstly obtained from this plant, and compound 5 was assigned the C-13-NMR data for the first time. Compound 7 exhibited strong antifeedant activity against Pieris brassicae, and compound 2 exhibited moderate activity, while the n-BuOH portion showed weak activity.
Antioxidant activity [1,1-diphenyl-2-picrylhydrazyl (DPPH) assay], antifungal activity against Gloeophyllum trabeum (brown-rot) and Pycnoporus sanguineus (white-rot), and total phenol content (Folin-Ciocalteu method) of 11 selected commercial Malaysian timbers were investigated. The extracts from Neem bark showed the highest yield, 25.59%. Kelat gelam bark showed the highest antioxidant activity, followed by Kelat jambu air bark. The extracts that showed the four highest antioxidant activities were all taken from bark samples. These extracts also showed high yields of methanol extracts and high total phenol content, suggesting that they have great potential as a source of antioxidant material. The highest total phenol content was found in Neem bark, while the lowest was in Ramin melawis bark. The methanol extracts from the heartwood of Neem showed the highest antifungal activity against G. trabeum. The methanol extracts from the sapwood and the heartwood of Neem, and the heartwood of Kulim showed the highest antifungal activity against P. sanguineus. The antifungal activities of these methanol extracts were higher than those of the positive control, glycyrrhizic acid dipotassium salt. Almost all wood species showed antifungal activity against either brown-or white-rot fungus. However, methanol extracts from the heartwood of Neem showed strong antifungal activity against brown and white-rot fungi, G. trabeum and P. sanguineus, suggesting that they have great potential as a source of fungistats.
The flavonoids kaempferol3OαLrhamnopyranoside, quercetin3OαLrhamnopyranoside together with luteolin, kaempferol and quercetin, were isolated from the methanolic extract of the leaves of Albizia chinensis collected from Egypt. Identification of the flavonoid constituents was carried by analysing their spectroscopic data and/or by comparing these data with those reported in the literature. The first three isolates were tested for their antimicrobial activity and the results revealed that the tested compounds exhibited moderate inhibiting activity against grampositive and gramnegative bacteria while no antifungal activity was observed.
Amygdalus lycioides var. horrida (Spach) Browicz (Rosaceae), also known as Prunus lycioides (Spach.) Schneid., is an endemic Iranian species of the genus Amygdalus. In Iranian traditional medicine, the aerial parts and roots of A. lycioides are used in the treatment of diabetes. Six flavonoids, i.e. quercetin 3-O-rhamnoside (1), luteolin 7-O-rhamnoside (2), isorhamnetin 3-O-rutinoside (3), kaempferol 3-O-rhamnoside (4), apigenin (5), and naringenin (6), have been isolated from the aerial parts of this plant. The structures of these compounds were elucidated by UV, MS, and NMR spectroscopic data analyses. While the antioxidant activity of these compounds was assessed by the 2,2-diphenyl-l- picryl-hydrazyl (DPPH) assay, the vasorelaxant effect was determined using the rat aortic vascular smooth muscle. Compounds 1-6 displayed significant antioxidant activity, with the RC50 values ranging from 0.0033 to 0.5186 mg/ml. Compound 2 showed a considerable vasorelaxant activity on rat aortic vascular smooth muscle in a dose-dependent manner. © TÜBİTAK.
Euphorbia heterophylla Linn (Euphorbiaceae) is a medicinal plant used by traditional herbal practitioners in Nigeria and some parts of West Africa for the treatment of constipation, bacterial and inflammatory disease conditions (arthritis and rheumatism). Powdered plant material was subjected to phytochemical screening using standard experimental procedures. The crude powdered sample of Euphorbia heterophylla leaves was extracted with n-hexane, chloroform, ethylacetate and methanol. The precipitates from the fractions were subjected to chromatographic and re-crystallization procedures. The structures of isolated compounds were characterized and elucidated with chemical and spectroscopic techniques such as IR, NMR and MS experiments. The in vitro biological activity of the isolated and characterized compounds were evaluated by superoxide scavenging assay using xanthine – xanthine oxidase system to generate superoxides. The result of the study showed that the crude plant material contained some secondary metabolites such as saponins, flavonoids and tannins. The phytochemical investigation led to the isolation of four known compounds stigmasterol, -stigmasterol glucoside, benzoic acid and 4 – hydroxyl benzoic acid. The four compounds exhibited good activity against the xanthine oxidase enzymes while the 4-hydroxybenzoic acid showed a marked activity. The isolation of the compounds from the leaves of E. heterophylla, which inhibited the xanthine oxidase enzyme, has justified the claims for which the plant is known and used.
Canine distemper virus (CDV) is a contagious and multisystemic viral disease that affects domestic and wild canines as well as other terrestrial and aquatic carnivores. The disease in dogs is often fatal and no specific antiviral therapy is currently available. In this study, we evaluated the in vitro antiviral activity against CDV of proanthocyanidin A2 (PA2), a phenolic dimer belonging to the class of condensed tannins present in plants. Our results showed that PA2 exerted in vitro antiviral activity against CDV with a higher selectivity index compared to ribavirin, included in our study for the previously tested anti-CDV activity. The time of addition assay led us to observe that PA2 was able to decrease the viral RNA synthesis and to reduce progeny virus liberation, at different times post infection suggesting multiple mechanisms of action including inhibition of viral replicative complex and modulation of the redox milieu. These data suggest that PA2, isolated from the bark of Aesculus hippocastanum, has potential usefulness as an anti-CDV compound inhibiting viral replication.
In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties, culminating with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in the overall process. In this review we have described the key synthetic issues and the structure-activity relationship of this family of integrase inhibitors. Crystallographic and docking studies that shed light on their mechanism of action are also examined.
Phytochemical investigation of the stem bark of Pometia pinnata resulted in the isolation of a new triterpenoidal saponin. The structure of the new compound, pometin (1), was established as 3-O-[beta-D-glucopyranosyl-(1 --> 2)-beta-D-glucopyranosyl-(1 --> 3)-beta-D-glucopyranosyl]-oleanolic acid based on 1D and 2D-NMR analysis including COSY, 2D J-resolved, HMQC, HMBC correlations and chemical transformations.
Proanthocyanidin, which consists of (+) catechin, (-) epicatechin and their gallates (15%), (-) epicatechin gallate-dimers, -trimers, and -tetramers (80%), and (-) epicatechin gallate-pentamers, -hexamers, and -heptamers (5%), was evaluated for its antiviral activity against feline calicivirus F9 strain (FCV/F9), which is thought to be a surrogate for noroviruses, and coxsackievirus A7 strain (Cox.A7), which was selected as a representative enteric virus. To achieve a viral inactivation rate of 99% or greater after contact for 10 sec., at least 1 mg/ml and 10 mg/ml of proanthocyanidin were required against FCV/F9 and Cox.A7, respectively. Although the antiviral mechanism of proanthocyanidin is not clear at present, proanthocyanidin may be an effective disinfectant against enteroviruses such as noroviruses.
MAP30 (Momordica anti-HIV protein of 30 kDa) and GAP31 (Gelonium anti-HIV protein of 31 kDa) are anti-HIV plant proteins that we have identified, purified, and cloned from the medicinal plants Momordica charantia and Gelonium multiflorum. These antiviral agents are capable of inhibiting infection of HIV type 1 (HIV-1) in T lymphocytes and monocytes as well as replication of the virus in already-infected cells. They are not toxic to normal uninfected cells because they are unable to enter healthy cells. MAP30 and GAP31 also possess an N-glycosidase activity on 28S ribosomal RNA and a topological activity on plasmid and viral DNAs including HIV-1 long terminal repeats (LTRs). LTRs are essential sites for integration of viral DNA into the host genome by viral integrase. We therefore investigated the effect of MAP30 and GAP31 on HIV-1 integrase. We report that both of these antiviral agents exhibit dose-dependent inhibition of HIV-1 integrase. Inhibition was observed in all of the three specific reactions catalyzed by the integrase, namely, 3' processing (specific cleavage of the dinucleotide GT from the viral substrate), strand transfer (integration), and "disintegration" (the reversal of strand transfer). Inhibition was studied by using oligonucleotide substrates with sequences corresponding to the U3 and U5 regions of HIV LTR. In the presence of 20 ng of viral substrate, 50 ng of target substrate, and 4 microM integrase, total inhibition was achieved at equimolar concentrations of the integrase and the antiviral proteins, with EC50 values of about 1 microM. Integration of viral DNA into the host chromosome is a vital step in the replicative cycle of retroviruses, including the AIDS virus. The inhibition of HIV-1 integrase by MAP30 and GAP31 suggests that impediment of viral DNA integration may play a key role in the anti-HIV activity of these plant proteins.
HIV integrase, the enzyme that inserts the viral DNA into the host chromosome, has no mammalian counterpart, making it an attractive target for antiviral drug design. As one of the three enzymes produced by HIV, it can be expected that inhibitors of this enzyme will complement the therapeutic use of HIV protease and reverse transcriptase inhibitors. We have determined the structure of a complex of the HIV-1 integrase core domain with a novel inhibitor, 5ClTEP, 1-(5-chloroindol-3-yl)-3-hydroxy-3-(2H-tetrazol-5-yl)-pro penone, to 2.1-A resolution. The inhibitor binds centrally in the active site of the integrase and makes a number of close contacts with the protein. Only minor changes in the protein accompany inhibitor binding. This inhibitor complex will provide a platform for structure-based design of an additional class of inhibitors for antiviral therapy.
Two new flavanone glucosides, (2R)- and (2S)-5-O-beta-D-glucopyranosyl-7,4'-dihydroxy-3',5'-dimethoxyflavanone[pervianoside I (3), peruvianoside II(4)] and a new flavonol glycoside, quercetin 3-O-[beta-D-glucopyranosyl-(1-->2)-[alpha-L-rhamnopyranosyl-(1-->6)]-beta-D-galactopyranoside] (peruvianoside III, 13) were isolated from the leaves of Thevetia peruviana Schum., together with nine known flavonol glycosides and two known iridoid glucosides. The structures of all compounds were determined on the basis of chemical and spectroscopic methods. Their inhibitory effects against HIV-1 reverse transcriptase and HIV-1 integrase were also investigated.
Three new eudesmane type sesquiterpenoid lindenanolides E (1), F (2) and G (3), and two new aporphine alkaloid lindechunines A (18) and B (20) were isolated from roots of Lindera chunii MERR., together with seven known sesquiterpenes including a new naturally-occurring lindenanolide H (4) and eight known aporphine alkaloids. The structures of these compounds were determined by spectroscopic means. Of the isolated compounds, hernandonine (14), laurolistine (16), 7-oxohernangerine (17) and lindechunine A (18) showed significant anti-human immunodeficiency virus type 1 (HIV-1) integrase activity with IC(50) values of 16.3, 7.7, 18.2 and 21.1 microM, respectively. The major alkaloids presented in the roots of L. chunii were quantitatively analyzed by an HPLC method.
An HTS campaign aimed at the identification of inhibitors of HIV integrase showed that the methanol extract from the buds of a Eucalyptus globoidea was active. Bioassay guided fractionation of this extract resulted in the purification and structural elucidation of the lignan, globoidnan A (1) as the only compound in the extract responsible for the inhibition of HIV integrase. The compound was found to inhibit the combined 3' processing and strand transfer activity of HIV integrase with an IC50=0.64 microM.
A monoacyldigalactosyl glycerol was isolated from the CH2Cl 2 soluble fraction of the MeOH extract from the green alga Enteromorpha prolifera. The structure was established as 1-O-palmitoyl-3-O- [α-D-galactopyranosyl(1→6)-β-D-galactopyranosyl]-sn-glycerol (1) by chemical and spectroscopic methods.
For the first time eleven compounds have been isolated from the ethyl acetate soluble fraction of whole plant of Grewia tenax namely, beta-sitosterol (1), beta-sitosteryl acetate (2), beta-amyrin (3), beta-amyrin acetate (4), 5 alpha,8 alpha-epidioxyergosta-6,22-diene-3 beta-ol (5), 5 alpha,8 alpha-epidioxyergosta-6,9(11),22-trien-3 beta-ol (6), alpha-taraxerol (7), betulin (8), stigmasterol (9), oleanolic acid (10) and stigmasterol 3-O-beta-D-glucoside (11) respectively. All the compounds were evaluated for their antimicrobial activity.
Drawing on the author’s extensive personal experience, Medicinal Plants of Asia and the Pacific provides comprehensive coverage of the medicinal plants of the region. Describing more than 300 compounds, the book discusses every important class of natural products while highlighting cutting-edge research and recent developments. With its broad scope and extensive compound listings, the presentation and approach of the book is completely original.
Substituted γ-chromones were found to weakly inhibit HIV-1 proteinase, an important enzyme in the replication and processing of the AIDS virus. Chromones bearing hydroxyl substituents and a phenolic group at the 2-position (flavones) were the most active compounds and structure-activity relationships for a limited series of flavone inhibitors are presented. Dixon plots are reported and a possible mechanism for flavone-induced inhibition is proposed. The results are also compared with those for some structurally related non-peptidic inhibitors of HIV-1 proteinase. Since some flavonoid compounds have already been shown to have antiviral activity against AIDS, the present observations of anti- HIV-1 proteinase activity may be particularly significant.
Three different solvent extracts (methanol, ethyl acetate, and n-hexane) of longan ( Dimocarpus longan Lour.) flowers were assayed with three different antioxidant capacity methods, namely, the DPPH free radical scavenging effect, the oxygen radical absorbance capacity (ORAC) assay, and the inhibition of Cu(2+)-induced oxidation of human low-density lipoprotein (LDL). It was revealed that the methanol extract has the best antioxidative activity, followed by ethyl acetate and n-hexane extracts. The methanol extract was separated by liquid-liquid partition into n-hexane, ethyl acetate, n-butanol, and water fractions. The ethyl acetate fraction was found to have the highest activity of delaying LDL oxidation. After silica gel column chromatography, the fraction having a superior activity was identified as containing two major compounds, (-)-epicatechin and proanthocyanidin A2.
Sexually transmitted diseases (STDs) and acquired immunodeficiency syndrome (AIDS) are gaining significant importance at present due to rapid spread of the diseases, high cost of treatment, and the increased risk of transmission of other STDs and AIDS. Current therapies available for symptomatic treatment of STDs and AIDS are quite expensive beyond the reach of common man and are associated with emergence of drug resistance. Many patients of STDs and AIDS are seeking help from alternative systems of medicines such as Unani, Chinese, Ayurvedic, naturopathy, and homeopathy. Since a long time, medicinal plants have been used for the treatment of many infectious diseases without any scientific evidence. At present there is more emphasis on determining the scientific evidence and rationalization of the use of these preparations. Research is in progress to identify plants and their active principles possessing activity against sexually transmitted pathogens including human immunodeficiency virus (HIV) with an objective of providing an effective approach for prevention of transmission and treatment of these diseases. In the present review, plants reported to possess activity or used in traditional systems of medicine for prevention and treatment of STDs including AIDS, herbal formulations for vaginal application, and topical microbicides from herbal origin, have been discussed.
The methanolic extracts of several natural medicines and medicinal foodstuffs were found to show an inhibitory effect on rat lens aldose reductase. In most cases, flavonoids were isolated as the active constituents by bioassay-guided separation, and among them, quercitrin (IC(50)=0.15 microM), guaijaverin (0.18 microM), and desmanthin-1 (0.082 microM) exhibited potent inhibitory activity. Desmanthin-1 showed the most potent activity, which was equivalent to that of a commercial synthetic aldose reductase inhibitor, epalrestat (0.072 microM). In order to clarify the structural requirements of flavonoids for aldose reductase inhibitory activity, various flavonoids and related compounds were examined. The results suggested the following structural requirements of flavonoid: 1) the flavones and flavonols having the 7-hydroxyl and/or catechol moiety at the B ring (the 3',4'-dihydroxyl moiety) exhibit the strong activity; 2) the 5-hydroxyl moiety does not affect the activity; 3) the 3-hydroxyl and 7-O-glucosyl moieties reduce the activity; 4) the 2-3 double bond enhances the activity; 5) the flavones and flavonols having the catechol moiety at the B ring exhibit stronger activity than those having the pyrogallol moiety (the 3',4',5'-trihydroxyl moiety).
For the purpose of discovering anti-HIV-1 agents from natural sources, water and EtOH extracts of 50 Thai plants were screened for their inhibitory activity against HIV-1 integrase (IN), an enzyme essential for viral replication. Of these plants, an EtOH extract of Coleus parvifolius Benth. (aerial parts) showed potent activity against HIV-1 IN with an IC50 value of 9.2 microg/mL. From this extract, 11 compounds were isolated and identified as luteolin 5-O-beta-d-glucopyranoside (1), luteolin (2), luteolin 7-methyl ether (3), luteolin 5-O-beta-d-glucuronide (4), 5-O-beta-d-glucopyranosyl-luteolin 7-methyl ether (5), rosmarinic acid (6), rosmarinic acid methyl ester (7), daucosterol (8), a mixture of alpha- and beta-amyrin (9, 10) and phytol (11). Of these compounds, rosmarinic acid methyl ester (7), rosmarinic acid (6), luteolin (2) and luteolin 7-methyl ether (3) exhibited inhibitory activities against HIV-1 IN with IC50 values of 3.1, 5.0, 11.0 and 11.0 microM, respectively. Among rosmarinic acid derivatives, the HIV-1 IN inhibitory activity increased in turn for a dimer (IC50 = 5.0 microM), a trimer (IC50 = 1.4 microM), and a tetramer (IC50 = 1.0 microM).
A novel flavonol glycoside, 7-O-methylmearnsitrin (7,4'-O-dimethylmyricetin 3-O-alpha-L-rhamnopyranoside), and myricetrin, kaempferol 3-O-alpha-L-rhamnopyranoside, europetin 3-O-alpha-L-rhamnoside, and 7-O-methyl quercetin 3-O-alpha-L-rhamnopyranoside were isolated from the leaves of Sageretia theezans, and their chemical structures were identified by spectroscopic analyses including two-dimensional NMR (HSQC, HMBC). Whereas myricetrin, europetin 3-O-alpha-L-rhamnoside, and 7-O-methylquercetin 3-O-alpha-L-rhamnopyranoside showed stronger activities than ascorbic acid and alpha-tocopherol, 7-O-methylmearnsitrin showed very weak antioxidant activities by ESR and LDL oxidation inhibition tests.
The urgent need for new anti-HIV/AIDS drugs is a global concern. In addition to obvious economical and commercial hurdles, HIV/AIDS patients are faced with multifarious difficulties associated with the currently approved anti-HIV drugs. Adverse effects, the emergence of drug resistance and the narrow spectrum of activity have limited the therapeutic usefulness of the various reverse transcriptase and protease inhibitors that are currently available on the market. This has driven many scientists to look for new anti-retrovirals with better efficacy, safety and affordability. As has always been the case in the search for cures, natural sources offer great promise. Several natural products, mostly of plant origin have been shown to possess promising activities that could assist in the prevention and/or amelioration of the disease. Many of these anti-HIV agents have other medicinal values as well, which afford them further prospective as novel leads for the development of new drugs that can deal with both the virus and the various disorders that characterize HIV/AIDS. The aim of this review is to report new discoveries and updates pertaining to anti-HIV natural products. In the review anti-HIV agents have been classified according to their chemical classes rather than their target in the HIV replicative cycle, which is the most frequently encountered approach. Perusal of the literature revealed that most of these promising naturally derived anti-HIV compounds are flavonoids, coumarins, terpenoids, alkaloids, polyphenols, polysaccharides or proteins. It is our strong conviction that the results and experiences with many of the anti-HIV natural products will inspire and motivate even more researchers to look for new leads from plants and other natural sources.
The bioassay-guided fractionation for anti-HIV-1 integrase activity led to the isolation of six compounds from the whole plant extract of Eclipta prostrata extract. They were identified as 5-hydroxymethyl-(2,2':5',2'')-terthienyl tiglate (1), 5-hydroxymethyl-(2,2':5',2'')-terthienyl agelate (2), 5-hydroxymethyl-(2,2':5',2'')-terthienyl acetate (3), ecliptal (4), orobol (5) and wedelolactone (6). Of these, compound 6 showed the highest activity against HIV-1 integrase (IN) with an IC50 value of 4.0+/-0.2 microm, followed by compound 5 (IC50=8.1+/-0.5 microm), whereas the four terthiophene compounds (1-4) were inactive (IC50>100 microm). Regarding HIV-1 protease (PR) inhibitory activity, compound 1 exhibited appreciable activity against HIV-1 PR with an IC50 of 58.3+/-0.8 microm, followed by compound 4 (IC50=83.3+/-1.6 microm) and compound 3 (IC50=93.7+/-0.8 microm), while compounds 2, 5 and 6 were inactive against HIV-1 PR (IC50>100 microm). This is the first report of anti-HIV-1 IN activities for wedelolactone (6), a coumarin derivative, and orobol (5), an isoflavone derivative. This study supports the use of E. prostrata in AIDS patients, which is in accord with its traditional use by Thai traditional doctors for curing blood related diseases.
13 C NMR, and EIMS and compared with data in the literature
- Adesegun
Identification of compounds 1–7 Compounds 1–7 were identified by 1 H NMR, 13 C NMR, and EIMS and compared with data in the literature (Adesegun et al., 2008; Chung et al., 2004; Falodun et al., 2008; Hsieh et al., 2008; Kim et al., 2004; Matsuda et al., 2002; Qi et al., 2003).
Pometia pinnata leaves extract to control late blight disease in potato
- D N Suprapta
- Igana Suwari
- N Arya
- K Ohsawa
Suprapta DN, Suwari IGANA, Arya N, Ohsawa K. (2002). Pometia
pinnata leaves extract to control late blight disease in potato. J Int Soc
Se Asian Agr Sci 8:31-6.
Medicinal plants of Asia and the Pacific Sesquiterpenes and alkaloids from Lindera chunii and their inhibitory activities against HIV-1 integrase
- C Wiart
- Francis Group Taylor
- Cf Zhang
- N Nakamura
- S Tewtrakul
Wiart C. (2006). Medicinal plants of Asia and the Pacific. New York: CRC Press, Taylor & Francis Group. Zhang CF, Nakamura N, Tewtrakul S, et al. (2002). Sesquiterpenes and alkaloids from Lindera chunii and their inhibitory activities against HIV-1 integrase. Chem Pharm Bull 50:1195–200.
85) nm; IR (KBr) max 3436, 1631, 1097 cm À1
Epicatechin (2): orange needles; UV (MeOH) l max (log ")
211 (4.43), 280 (3.54), 315 (2.85) nm; IR (KBr) max 3436,
1631, 1097 cm À1 ; 1 H NMR (CD 3 OD, 500 MHz) 2.73 (1H,
dd, J ¼ 2.8, 16.8 Hz, H-4b), 2.85 (1H, dd, J ¼ 4.6, 16.7 Hz,
H-4a), 4.17 (1H, m, H-3), 4.81 (1H, s, H-2), 5.90 (1H, d,
J ¼ 2.3 Hz, H-8), 5.93 (1H, d, J ¼ 2.5 Hz, H-6), 6.75 (1H, d,
J ¼ 8.2 Hz, H-5 0 ), 6.79 (1H, dd, J ¼ 2.1, 8.2 Hz, H-6 0 ), 6.96
(1H, d, J ¼ 2.1 Hz, H-2 0 ). 13 C NMR (CD 3 OD, 125 MHz)
Inhibition of viral RNA synthesis in canine distemper virus infection by proanthocyanidin A2
- L Gallina
- Fd Pozzoa
- V Galligionia
C-25), 17.8 (C-26), 18.0 (C-6 00 ), 18.8 (C-6)
- Hz
Hz, H-2 00 ), 3.98 (1H, br s, H-4 0 ), 4.05 (1H, br s, H-2 000 ),
4.50 (1H, d, J ¼ 6.4 Hz, H-1 0 ), 5.05 (1H, d, J ¼ 1.4 Hz, H-1 000 ),
5.10 (1H, br s, H-1 00 ), 5.23 (1H, t, J ¼ 3.7 Hz, H-12). 13 C NMR
(CD 3 OD, 125 MHz) 13.7 (C-24), 16.4 (C-25), 17.8 (C-26),
18.0 (C-6 00 ), 18.8 (C-6), 23.9 (C-30), 24.1 (C-16), 24.5 (C-11),
26.5 (C-2), 26.6 (C-27), 28.8 (C-15), 31.6 (C-20), 33.4 (C-7),
33.6 (C-29), 33.8 (C-22), 34.9 (C-21), 37.6 (C-10), 39.7 (C-1),
40.5 (C-8), 42.7 (C-18), 43.0 (C-14), 44.0 (C-4), 47.2 (C-19),
47.7 (C-17), 48.1 (C-9), 49.6 (C-5), 63.2 (C-5 000 ), 64.4 (C-23),
65.7 (C-5 0 ), 69.5 (C-4 0 ), 70.7 (C-5 00 ), 71.5 (C-2 00 ), 72.0 (C-3 00 ),
73.7 (C-4 00 ), 75.8 (C-2 0 ), 79.0 (C-3 000 ), 82.1 (C-3 0 ), 82.4
(C-2 000 ), 82.9 (C-3), 86.9 (C-4 000 ), 102.5 (C-1 00 ), 105.0 (C-1 0 ),
110.7 (C-1 000 ), 123.6 (C-12), 145.3 (C-13), 182.1 (C-28).