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Antifungal activity in plants from Chinese traditional and folk medicine
Abstract
From over 100 Chinese clinical trial publications, we retrieved 22 commercial preparations and 17 clinical prescriptions used as Traditional Chinese Medicine (TCM) for treating mycotic vaginitis, typically caused by Candida albicans. The 8 most frequently used plants as well as another 7 TCM and 18 folk medicinal plants used in the South of China for antifungal therapy were investigated for in vitro antifungal activity.
For each plant we tested 4 extracts prepared with different solvents (water, ethanol, acetone, and n-hexane) for inhibition of Candida albicans and Saccharomyces cerevisiae growth in liquid culture.
Some plants have quite strong antifungal activity, such as Tujinpi (Pseudolarix kaempferi Gord.), of which each extract could significantly inhibit the growth of both tested fungi. In addition, the acetone extract of Kushen (Sophora flavescens Ait.), the ethanol, acetone, and hexane extracts of Guanghuoxiang (Pogostemon cablin (Blanco) Benth.) and Gaoliangjiang (Alpinia officinarum Hance), the hexane extract of Dingxiang (Eugenia caryophyllata Thunb.), and the ethanol and acetone extracts of Kulianpi (Melia toosendan Sieb. et Zucc.) and Laliao (Polygonum hydropiper L.), all inhibited Candida albicans growth by more than 50%. In some cases growth inhibition was even comparable to that by the clinically used antifungal miconazole, which we used as our positive control.
The majority of plants, whose clinical use for antifungal treatment is well supported within TCM or Chinese folk medicine, show in vitro antifungal activity against Candida albicans. Since Candida species represent the most common fungal pathogen of humans, these results provide more scientific evidence supporting the clinical application of these plants, and can serve as a starting point for new drug discovery from TCM and Chinese folk medicine.
... These oils are insoluble and include various groups, for example, terpenes, alcohols, and aldehydes 5,6 . Aromatic plants are widely used in medicine and food storage, and their essential oils have been shown to interfere with the growth and enzymatic reactions of microbes in vivo and in vitro 7,8 . In the Mediterranean region, fallen litter or living parts of aromatic plants release essential oils that remain in the soil for up to 1 year 6,9 . ...
... Polygonum hydropiper, a common aromatic plant in East Asia, is famous for its antimicrobial activity and is used as a pharmaceutical 11,12 . Previous studies have reported on its secondary compounds 8 , among which its essential oils (mainly terpenes) are reported to affect microbes 12 . The objective of this study was to investigate the overall effect of P. hydropiper on the decomposition of leaf litter of Miscanthus sacchariflorus and Carex brevicuspis, two dominant plants at Dongting Lake, the second largest freshwater lake in China. ...
... Another explanation may be the antifungal activity of essential oils, as indicated by the decreases in fungal biomass in both litters after P. hydropiper addition. The antifungal activity of P. hydropiper essential oils has been reported previously 8,11 . Given the fundamental role of fungi in litter consumption, this inhibition of fungal activity by P. hydropiper addition might lead to a decreased litter decomposition rate. ...
Aromatic plants show antimicrobial activity due to their essential oils, but their effect on litter decomposition is unclear. In this study, we evaluated the biomass loss and nutrient dynamics in leaf litters of two macrophytes (Miscanthus sacchariflorus and Carex brevicuspis) with and without addition of powdered material of the aromatic plant Polygonum hydropiper or the non-aromatic plant C. brevicuspis. The two powders had similar basic chemical qualities but P. hydropiperi had a higher essential oils concentration. Leaf litters of M. sacchariflorus and C. brevicuspis were incubated with powdered P. hydropiper or C. brevicuspis (500 g m−3, 250 g m−3, and no addition) for 120 days in a mesocosm experiment. Compared with the control (no addition), P. hydropiperi addition decelerated nutrient release and litter decomposition, while C. brevicuspis addition accelerated those processes. The nitrogen concentrations in both leaf litters and the phosphorus concentration in C. brevicuspis leaf litter were increased by addition of both plant powders. The fungal biomass in both leaf litters decreased after P. hydropiperi addition, due to the antifungal activity of its essential oils. These data indicate that the aromatic plant P. hydropiperi inhibits litter decomposition via its essential oils and that such inhibition is not species-specific.
... Additionally, the essential oil obtained from the B. scoparia shoots, with α-thujaplicin as the main compound (22.91%), did not inhibit the growth of A. niger, while it showed moderate activity towards C. albicans (MIC= 12.5 μg/mL) (cefroperazone was used as a positive control, MIC=5.0 μg/mL) (El-Shamy et al. 2012). In another study, Liu et al. (2012) screened the antifungal activity of different extracts of Kochiae fructus (0.2 g fruits/mL) towards Saccharomyces cerevisiae and C. albicans. The aqueous extract showed the best fungistatic activity and suppressed growth by 52% and 29%, respectively (control: miconazole (2 mg/ mL) inhibited growth by 89-90%). ...
... The aqueous extract showed the best fungistatic activity and suppressed growth by 52% and 29%, respectively (control: miconazole (2 mg/ mL) inhibited growth by 89-90%). In turn, the acetone extract exhibited a lower potential for both S. cerevisiae and C. albicans (24% and 15%), while the ethanol extract as well as the hexane extract showed a poor activity (5-10%) (Liu et al. 2012). On the other hand, ethanol extract of B. scoparia fruits (2 mg/mL) strongly inhibited the growth of the plant necrotrophic fungus-Valsa mali (by 96.16% after 96 h). ...
Bassia All. is a genus from the Amaranthaceae family, which was created by merging selected species belonging to the former Bassia and Kochia genera with those classified to Chenolea, Londesia, Kirilowia and Panderia. The reorganised Bassia genus currently comprises around 20 species, which are annual herbs or perennial subshrubs native to Eurasia and Africa. Bassia plants are well known for their therapeutic applications in folk medicine and traditional medical systems, and they are also used for nonmedical purposes. Some members of this genus, such as Bassia scoparia (syn. Kochia scoparia) is of great medical importance and economic value. The plant is cultivated in some regions of Asia as a crop to collect Kochiae fructus, which is used for both curative and food purposes. Phytochemical studies carried out on Bassia species indicate that these plants synthesize metabolites belonging to different groups of compounds (e.g., triterpene saponins, sterols, flavonoids, fatty acids, lignanamides, alkaloids, organic acids). Some of the structures are rarely found in the plant kingdom. Biological activity studies carried out on Bassia plants revealed various effects exerted by extracts and isolated compounds, including anti-inflammatory, cytotoxic, antioxidant, antimicrobial, hypoglycemic, anti-obesity, etc. Modern research explained some of the mechanisms of action. This review covers literature from 1935 to 2022, and assembles and discusses data on phytochemistry, biological activity, as well as medical and nonmedical use of the representatives of the genus Bassia. In this review we present the current state of knowledge about the plants of the genus.
... Many herbs, documented in ancient Chinese medical books and modern literature, have been used to treat fungal infections. The efficacy of some TCM preparations, prescriptions and folk medicine has been firmly established [4][5][6][7][8][9][10]. Many studies have also reported on TCM preparations and chemical constituents isolated from TCM herbs. ...
... The known antifungal herbs, Quercus infectoria Oliv., Coptis chinensis Franch., Sophora flavescens Ait., and Pseudolarix kaempferi Gord. [6,[26][27][28], were selected and extraction was performed with water, 75% ethanol and 99% ethanol. The extracts were then screened for their activities against C. albicans. ...
Introduction
Different extraction, screening and testing methods have made it difficult to compare the antifungal activities of traditional Chinese medicine (TCM) extracts. In this study, the antifungal activities of TCM herbs recorded in the Chinese Materia Medica were evaluated using consistent methods and standards.
Methods
A total of 163 TCM herbs were tested for antifungal activity against four strains of fungi using a broth microdilution assay and a hyphal growth inhibition assay was performed against Candida albicans. The antifungal activities of the most biologically active herbs were evaluated against six other fungal strains. They were also tested in combination with fluconazole against a fungicide-resistant Candida albicans strain. The main chemical constituents of Rosa chinensis were evaluated for their antifungal activity and mode of action.
Results
A total of 52 herb extracts exhibited inhibitory effects against Cryptococcus neoformans, 22 worked against Candida albicans and six acted against Aspergillus fumigatus. Syzygium aromaticum, Phellodendron chinense, Neopicrorhiza scrophulariiflora, Curcuma longa and Rosa chinensis exerted potent and broad-spectrum antifungal activities. The hyphal growth inhibition assay demonstrated that extracts of six herbs completely inhibited hyphal growth. The main antifungal constituents of Rosa chinensis were gallic acid and flavonoids. These compounds exhibited synergistic and additive antifungal effects.
Conclusion
Rosa chinensis, Neopicrorhiza scrophulariiflora, Phellodendron chinense and Syzygium aromaticum displayed the strongest antifungal effects. The antifungal effects of the main chemical constituents of Rosa chinensis provide a basis for further studies on their biological activities.
... A ação do produto restrita a apenas uma das cepas testadas pode ser resultado de resistência adquirida por parte das outras cepas, visto que, por serem de origem clínica, estas podem ter sido expostas a um tratamento antifúngico ineficaz que promoveu o desenvolvimento de resistência [17]. Liu et al. (2012) [18], ao estudar mais de 100 ensaios clínicos para tratar vaginite micótica causada por Candida sp., observou que os extratos etanólico, hexânico e acetônico de P. cablin apresentaram efeito antifúngico para as cepas testadas de C. albicans, comparando-se clinicamente ao antifúngico miconazol. Yi et al. (2013) [19], ao avaliar a atividade antifúngica da pogostona, um dos metabólitos segundários de P. cablin, e uma série de análogos deste metabólito, observou forte atividade antifúngica da pogostona e de um dos análogos sobre todas as cepas de C. albicans utilizadas no teste. ...
... A ação do produto restrita a apenas uma das cepas testadas pode ser resultado de resistência adquirida por parte das outras cepas, visto que, por serem de origem clínica, estas podem ter sido expostas a um tratamento antifúngico ineficaz que promoveu o desenvolvimento de resistência [17]. Liu et al. (2012) [18], ao estudar mais de 100 ensaios clínicos para tratar vaginite micótica causada por Candida sp., observou que os extratos etanólico, hexânico e acetônico de P. cablin apresentaram efeito antifúngico para as cepas testadas de C. albicans, comparando-se clinicamente ao antifúngico miconazol. Yi et al. (2013) [19], ao avaliar a atividade antifúngica da pogostona, um dos metabólitos segundários de P. cablin, e uma série de análogos deste metabólito, observou forte atividade antifúngica da pogostona e de um dos análogos sobre todas as cepas de C. albicans utilizadas no teste. ...
A candidíase invasiva é uma ameaça crescente entre pacientes imunocomprometidos, sendo uma causa significativa de morbidade e mortalidade. Epidemiologicamente, as espécies não-albicans estão adquirindo relevância por se tornarem os agentes causadores cada vez mais frequentes de candidíase. O uso indiscriminado de medicamentos para combater as diversas variedades de candidíase tem trazido um aumento expressivo no número de leveduras resistentes aos antifúngicos tradicionais. Desta forma, produtos de origem vegetal podem ser utilizados como alternativa para os antifúngicos sintéticos. Com base nestas informações, esta pesquisa objetivou avaliar a possível atividade antifúngica do óleo essencial de Pogostemon cablin (Blanco) Benth. (Lamiaceae) contra cepas de Candida glabrata através da técnica de microdiluição para a determinação da Concentração Inibitória Mínima (CIM) e Concentração Fungicida Mínima (CFM). Após o experimento, observou-se que o produto inibiu a cepa LM-302 de C. glabrata com uma CIM de 256 μg/mL. O mesmo valor foi obtido para a CFM contra esta mesma cepa. Portanto, pode-se concluir que o óleo essencial de P. cablin testado apresenta um efeito antifúngico contra as leveduras de C. glabrata.
... Bốn chủng vi khuẩn Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli và Enterococus feacalis được cung cấp bởi Bộ môn Công nghệ sinh học Phân tử và Môi trường, Trường Đại học Khoa học Tự nhiên. Chứng dương là ampicillin 0,1 mg/mL (tetracycline 0,3 mg/mL đối với P. aeruginosa) [14]. Đường kính vòng vô khuẩn được tính bằng hiệu số giữa đường kính vô khuẩn và đường kính lỗ thạch. ...
... Để đánh giá khả năng kháng khuẩn của cao chiết ethanol và các phân đoạn, phương pháp khuếch tán trên đĩa thạch được sử dụng với các nồng độ mẫu khác nhau. Kết quả đường kính vòng vô khuẩn được ghi nhận như Bảng 1. Đường kính vòng vô khuẩn của chứng dương nằm trong khoảng ức chế đối với vi khuẩn theo CLSI [14]. Kết quả cho thấy cao chiết ethanol có hoạt tính kháng các chủng S. aureus ở các nồng độ 100-400 mg/mL và P. aeruginosa, E. feacalis ở nồng độ 200-400 mg/mL nhưng không có tác dụng với E. coli. ...
Melicope pteleifolia (Champ. ex benth.) T.g. Hartley, a folk medicinal plant, is used by ethnic minorities in Bidoup–Nui Ba National Park, Lam Dong Province, Vietnam to treat effectively wound, inflammation and skin ulcer. To scientifically prove the claimed utilization and understand the mechanism of action of the plant, the in vitro and in vivo healing properties of the extract and fractions of the plant were investigated. The ethanol 70 % extract (50 – 400 mg/mL), aqueous (200 mg/mL), ethyl acetate (100 mg/mL) and petroleum ether (50 mg/mL) fractions were used to evaluate the antibacterial activities by using agar diffusion method. The healing properties were in vitro investigated through fibroblasts and keratinocytes proliferation and migration (7.8 g/mL to 250 g/mL in accordance with each extract and fraction). Besides, the macrophage-induced inhibition of the nitric oxide (NO) production was examined (15.6 – 62.5 g/mL). In addition, the excision wound model was used to test the wound healing activity on mice model. We found that the ethanol extract and the ethyl acetate fraction showed potent activity against Staphylococcus aureus, Enterococcus feacalis and Pseudomonas aeruginosa. The extract and fractions stimulated fibroblasts and keratinocytes proliferation in a concentration-dependent way. They also inhibited macrophage produce NO. In addition, mice treated by the extract formed scabs on wound excision of mice model faster than the control group. The wound healing efficiency seems to involve antibacterial, stimulating fibroblasts and keratinocytes proliferation, inhibition of macrophages produce NO.
... According to the World Health Organization, the statistics suggest that a substantial population in developed countries have resorted to the usage of traditional practices of health, particularly the use of the medicinal plants [5]. Among various remedial uses of plants, several species have antimicrobial, antifungal, antiparasitic, antihelminthic and antiviral properties [6][7][8]. ...
... Antibiotics are one of our most important armaments in fighting bacterial infections and have significantly benefited the healthrelated features of human life since their discovery [6][7][8][9][10]. However, for the last few years these antibiotics had become less effective against infections because of the toxicities they cause inside our bodies and (mainly) due to the emergence of resistance in the microbial pathogens towards these administered drugs [11]. ...
Cassia absus is used for medicinal purposes for a long time all over the world. In this study, the authors report the antimicrobial potential of C. absus extracts obtained with different solvents. The extract(s) obtained with ethyl acetate yielded the best antibacterial effects because of a rich supply of oxalates and alkaloids in it. The same extract was also exploited for reducing Ag⁺ ions (to metallic Ag⁰) for the synthesis of nanoparticles. Electron microscopy revealed that the silver nanoparticles were ∼18–25 nm in diameter. The Fourier-transform infrared evaluation pointed towards the fact that flavonoids present in the plant extract were acting as reductants while amino groups were the bound stabilisation agents to the synthesised nanoparticles limiting the diameter to a certain threshold and avoiding aggregation naturally. A comparative antibacterial assay of C. absus versus Ag nanoparticles showed that the nanoparticles as well as organic (ethyl acetate) extract of the plant checked the growth of selected (MDR) superbugs. However, the biosynthesised Ag nanoparticles returned better antibacterial efficacies than ethyl acetate extract.
... Co. Ltd. (Beijing, China, http://www.tongrentang.com/en/). The plant material was ground to a fine powder and small-scale extracts were prepared as described before [15]. One gram of plant powder was used in the small-scale extracts. ...
... The antiviral profile of the peaks from fraction 28 of Cimicifuga heracleifolia revealed that peak 15 (table 1). A proton NMR was performed to confirm F33P13 as cimicifugic acid A. Interestingly, the adjacent peak 14 (F33P14), which did not show activity against EV-A71, was identified on the basis of MS/MS and proton NMR as cimicifugic acid B. We were unable to identify F33P11. ...
Human enterovirus 71 (EV-A71) infections cause a wide array of diseases ranging from diarrhoea and rashes to hand-foot-and-mouth disease and, in rare cases, severe neurological disorders. No specific antiviral drug therapy is currently available. Extracts from seventy-five Chinese medicinal plants selected for antiviral activity based on the Chinese pharmacopeia and advice from traditional Chinese medicine clinicians were tested for activity against EV-A71. The aqueous extract of the rhizome of Cimicifuga heracleifolia (Sheng Ma) and Arnebia euchroma (Zi Cao) showed potent antiviral activity. The active fractions were isolated by bioassay-guided purification, and identified by a combination of high-resolution mass spectrometry and NMR. Fukinolic acid and cimicifugic acid A and J, were identified as active anti-EV-A71 compounds for Cimicifuga heracleifolia, whereas for Arnebia euchroma, two caffeic acid derivatives were tentatively deduced. Commercially available fukinolic acid analogues like L-chicoric acid and D-chicoric also showed in vitro micromolar activity against EV-A71 lab-strain and clinical isolates.
... Relatively, an alkaloid of bi-diarylheptanoids containing a pyridine ring (36) , a diarylheptanoid containing a monoterpene unit (37) , and a diarylheptanoid containing a flavonol unit (38) (Ling et al., 2010) were subsequently isolated from the rhizome along with other diarylheptanoids (39-46) Zhang et al., 2010aZhang et al., , 2010bLiu et al., 2014aLiu et al., , 2014b, and an unusual diarylheptanoid containing furan ring (47) . Furthermore, an alkaloid of diarylheptanoid containing pyridine ring named officinin B (48) (Zhao et al., 2012) and alpinin A (49) (Liu et al., 2012a(Liu et al., , 2012b were also isolated from the rhizome as dimeric diarylheptanoid. A phytochemical investigation on the rhizome A. officinarum further revealed the isolation of another three dimeric diarylheptanoids namely alpinin B (50), C (51), and D (52) (Fig. 4) (Liu et al., 2014a) along with compound 53-58 Itokawa et al., 1985;Liu et al., 2014a;Tang et al., 2015). ...
... Methanolic extract from the rhizome displayed antifungal activity on clotrimazole-resistant Candida albicans at a minimum inhibitory concentration (MIC) value of 2.5 mg/ml (Shahidi Bonjar, 2004a). Similarly, the hexane, ethanol, and acetone extracts obtained from the rhizome inhibited 50% growth of Candida albicans (Liu et al., 2012a(Liu et al., , 2012b. In contrast, ethanolic extract showed no antifungal activity on C. albicans at a concentration of up to 1 mg/ml, whereas, over 100% growth inhibition was observed against Staphylococcus aureus (Zhang et al., 2013c(Zhang et al., , 2013d. ...
Ethnopharmacological relevance
Alpinia officinarum Hance is a perennial plant that has been traditionally used for many decades to treat several ailments including inflammation, pain, stomach-ache, cold, amongst others. Pharmacological studies over the years have demonstrated remarkable bioactivities that could be further explored for development of new therapeutic agents against various ailments.
Aim of the study
The paper critically reviewed the ethno-medicinal uses, pharmacology, and phytochemistry of A. officinarum.
Methods
Keywords including A. officinarum and its synonyms were searched using electronic databases including ISI web of knowledge, Science direct, Scopus, PubMed, Google scholar and relevant database for Masters and Doctoral theses.
Results
A. officinarum is prepared in Asia, Turkey, Morocco and Iran as a decoction, infusion or juice as a single preparation or in combination with other herbs, food or drinks for the treatment of general health problems including cold, inflammation, digestive disorders, etc. Pharmacological studies revealed the potent in vitro and in vivo bioactivities of various parts of A. officinarum that include anti-inflammatory, cytotoxicity, homeostasis, lipid regulation, antioxidant, antiviral, antimicrobial, antiosteoporosis, etc. Over 90 phytochemical constituents have been identified and isolated from A. officinarum comprising vastly of phenolic compounds especially diarylheptanoids isolated from the rhizome and considered the most active bioactive components.
Conclusion
In vitro and in vivo studies have confirmed the potency of A. officinarum. However, further studies are required to establish the mechanisms mediating its bioactivities in relation to the medicinal uses as well as investigating any potential toxicity for future clinical studies.
... Many studies on the biological properties of Alpinia officinarum indicated its antioxidant [23,24], antiviral [25,26], antibacterial [27,28], antifungal [29,30], antimicrobial [31], analgesic and anti-inflammatory effects [32,33]. Aqueous extracts have also been studied in skin problems [34], showing antiphotoaging effects [35] and in studies on the pharmacological activity and therapeutic potential of galangin in age-related diseases [36]. ...
Alpinia officinarum is a representative of the Zingiberaceae family, which is known for its wide use in the food and pharmaceutical industries also due to its precious pharmacological potential. The major aim of the present study was to evaluate the influence of thermal treatment on the composition of the rhizome of Alpinia officinarum and its antioxidant activity. The fresh rhizome was subjected to various thermal treatment processes—boiling, frying and microwave heating during various time intervals—and their composition and antioxidant activity were determined using chromatographic (HPLC – High Performance Liquid Chromatography and HPLC-MS - High Performance Liquid Chromatography Mass Spectrometry) and spectrophotometric (DPPH and TPC – Total Phenolic Content) methods. Pinobanksin was the main compound found in the extract of the fresh rhizome (537.79 mg/kg), followed by galangin (197.7 mg/kg) and zingerone (185.5 mg/kg). The effect of thermal treatment on the rhizome composition was varied. In general, thermal processing significantly decreased the content of active compounds in the rhizome. However, there were some exceptions—boiling for 4 min significantly increased the content of pinobanksin (1162.4 mg/kg) and galangin (280.7 mg/kg), and microwave processing for 4 min increased the content of pinocembrin (213 mg/kg). It was found that boiling and microwave treatment significantly increased the antioxidant activity of the processed rhizomes.
... In recent years, traditional Chinese medicine (TCM) has been widely concerned in the treatment of dermatophytosis due to its outstanding advantages of broad-spectrum antifungal activity, low toxicity and low incidence of drug resistance [9][10][11]. Huangqin decoction (HQD), as a classical TCM formula, was first mentioned in the book Shang Han Lun compiled by Zhang Zhongjin in the Han dynasty, and it has been used to treat complex gastrointestinal disorders for nearly 1800 years [12,13]. ...
Introduction. Trichophyton rubrum is a major causative agent of superficial dermatomycoses such as onychomycosis and tinea pedis. Huangqin decoction (HQD), as a classical traditional Chinese medicine formula, was found to inhibit the growth of common clinical dermatophytes such as T. rubrum in our previous drug susceptibility experiments.
Hypothesis/Gap Statement. The antifungal activity and potential mechanism of HQD against T. rubrum have not yet been investigated.
Aim. The aim of this study was to investigate the antifungal activity and explore the potential mechanism of action of HQD against T. rubrum .
Methodology. The present study was performed to evaluate the antifungal activity of HQD against T. rubrum by determination of minimal inhibitory concentrations (MICs), minimal fungicidal concentrations (MFCs), mycelial growth, biomass, spore germination and structural damage, and explore its preliminary anti-dermatophyte mechanisms by sorbitol and ergosterol assay, HPLC-based ergosterol test, enzyme-linked immunosorbent assay and mitochondrial enzyme activity test.
Results. HQD was able to inhibit the growth of T. rubrum significantly, with an MIC of 3.125 mg ml ⁻¹ and an MFC of 12.5 mg ml ⁻¹ . It also significantly inhibited the hyphal growth, conidia germination and biomass growth of T. rubrum in a dose-dependent manner, and induced structural damage in different degrees for T. rubrum cells. HQD showed no effect on cell wall integrity, but was able to damage the cell membrane of T. rubrum by interfering with ergosterol biosynthesis, involving the reduction of squalene epoxidase (SE) and sterol 14α-demethylase P450 (CYP51) activities, and also affect the malate dehydrogenase (MDH), succinate dehydrogenase (SDH) and ATPase activities of mitochondria.
Conclusion. These results revealed that HQD had significant anti-dermatophyte activity, which was associated with destroying the cell membrane and affecting the enzyme activities of mitochondria.
... Overall, The current promising antifungal activity of n-hexane extract could be due to the presence of various important phytochemicals including terpenoids, phytosterols, flavonoids, and phenolic acids. [28][29][30] The activity observed in methanolic and chloroform extracts may also be attributed to the flavonoids and polyphenolic constituents. 31 Congruently, previous studies also reported that fungal pathogens cause infection in or around the human breast, [32][33][34] and nausea and vomiting. ...
Background
Erianthemum aethiopicum Wiens and Polhill (Loranthaceae) is a parasitic plant native to north eastern Africa and Ethiopia. In Ethiopia, it is traditionally used to treat breast swelling, mastitis, morning illnesses and vomiting.
Objective
This study aimed to screen the main phytochemical constituents; determine the total amounts of phenolics, flavonoids, and tannins; and evaluate the antimicrobial (against Escherichia coli, Staphylococcus sciuri, Candida glaebosa and Cryptococcus albidus) and antioxidant (against DPPH radical and ferric ion) activities of E. aethiopicum leaves extracts.
Methods
Powdered E. aethiopicum leaves were macerated using n-hexane, chloroform, ethyl acetate, ethanol, and methanol. All crude extracts were qualitatively screened for phytochemical identification. The total phenolic, flavonoid, and condensed tannin contents of the chloroform, ethanol, and methanol extracts were determined by UV-Vis spectrophotometry. The n-hexane, chloroform, and methanol extracts were evaluated for their antimicrobial activity against the aforementioned microbes using agar disc diffusion and broth micro-dilution techniques. Chloroform, ethanol, and methanol extracts were also evaluated for antioxidant activity by DPPH and ferric ion reduction antioxidant power (FRAP) assays.
Results
Methanol (17.56 ± 16%) and ethanol (16.45 ± 19%) showed better extraction efficiency. Flavonoids, polyphenols, tannins, terpenoids, saponins, and sterols were detected in all extracts. The highest total content of phenolics (22.63 ± 0.69 mgGAE/gDCE), flavonoids (5.38 ± 0.52 mgCE/gDCE) and tannins (39.18 ± 38 mg CE/g DCE), as milligram of gallic acid and catechin per gram of dried crude extract, were recorded in the methanolic extract. The methanolic extract also presented best anti -DPPH strength (IC50, 4.31 μg/mL) and ferric ion reduction power (absorbance of 0.71) though found weak compared to the ascorbic acid (IC50 of 0.49 μg/mL and absorbance of 0.93, respectively).
Conclusion
All evaluated extracts displayed antifungal activity against both Cryptococcus albidus and Candida glaebosa strains (minimum inhibitory concentration values of 12.5–25 mg/mL), whereas they were found to have negligible activity against all tested bacterial strains. This report provides preliminary information for further phytochemical investigation of Erianthemum aethiopicum to isolate potential antioxidant and antifungal compounds.
... Patchouli alcohol is a tertiary alcohol, a sesquiterpenoid and belong to a carbotricyclic compound (https://pubchem.ncbi.nlm.nih.gov/). Patchouli alcohol exhibited antifungal activity against a Aspergillus species, Candida albicans and also showed antioxidant activity[4,[30][31][32]. ...
... In addition, pogostone which is one of the secondary metabolites in patchouli, is very effective for treating Candida infections, especially for vulvovaginal candidiasis which has been proven by . Likewise, patchoulol is able to inhibit Candida albicans (Liu et al. 2012) effectively ...
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a new type of virus that attacks the respiratory system and has caused the global epidemic of coronavirus disease 2019 (COVID-19). Some persons who are infected with this virus develop symptoms ranging from a typical cold to fever to more severe illnesses, such as Severe Acute Respiratory Syndrome (SARS) and Middle East Respiratory Syndrome (MERS). The development of a SARS-CoV-2 vaccine is being actively researched but will likely take more than a year to become available to the general public. As a result, numerous researchers are actively extracting the components of active chemicals in herbal plants with antiviral potentials, such as patchouli (Pogostemon cablin Benth.). Patchouli essential oil, found in this Lamiaceae plant, has a wide range of effects, including antibacterial, antifungal, antioxidant, antimutagenic, anticancer, anti-inflammatory, and aromatherapy. More than 140 chemicals have been isolated and identified from the patchouli plant, including terpenoids, phytosterols, flavonoids, organic acids, lignins, alkaloids, glycosides, alcohols, and aldehydes. Patchouli essential oil is mainly composed of sesquiterpene molecules, most of which are patchouli alcohol. Essential oils derived from herbal plant extracts have also been shown to be potent antiviral agents against various viruses. The efficacy of patchouli essential oil, as well as its potential as an antiviral agent to treat SARSCoV-2, will be investigated in this review.
... Many bioactive compounds from medicinal plants have been discovered and purified to produce drugs, such as artemisinin from Artemisia annua for antimalarial activity, paclitaxel from Taxus brevifolia for antitumor activity, vinblastine from Catharanthus roseus for anticancer chemotherapy, and berberine from different plant genera for antimicrobial activity [46]. Due to safety and ecological friendliness, plant extracts and their bioactive metabolites are emerging as potential alternatives to synthetic fungicides for controlling fungal pathogens [21,26,27,47]. In the present study, we inspected twelve medicinal plants in Northern Vietnam for their antagonistic behavior toward four common pathogenic fungi causing diseases in humans and plants, including P. digitatum, A. flavus, A. fumigatus, and C. albicans. ...
Medicinal plants play important roles in traditional medicine, and numerous compounds among them have been recognized for their antimicrobial activity. However, little is known about the potential of Vietnamese medicinal plants for antifungal activity. In this study, we examined the antagonistic activity of twelve medicinal plant species collected in Northern Vietnam against Penicillium digitatum, Aspergillus flavus, Aspergillus fumigatus, and Candida albicans. The results showed that the antifungal activities of the crude extracts from Mahonia bealei, Ficus semicordata, and Gnetum montanum were clearly detected with the citrus postharvest pathogen P. digitatum. These extracts could fully inhibit the growth of P. digitatum on the agar medium, and on the infected citrus fruits at concentrations of 300–1000 µg/mL. Meanwhile, the other tested fungi were less sensitive to the antagonistic activity of the plant extracts. In particular, we found that the ethanolic extract of M. bealei displayed a broad-spectrum antifungal activity against all four pathogenic fungi. Analysis of this crude extract by enrichment coupled with high-performance liquid chromatography revealed that berberine and palmatine are major metabolites. Additional inspections indicated berberine as the key compound responsible for the antifungal activity of the M. bealei ethanolic extract. Our study provides a better understanding of the potential of Vietnamese medicinal plant resources for combating fungal pathogens. This work also highlights that the citrus pathogen P. digitatum can be employed as a model fungus for screening the antifungal activity of botanicals.
... Three important bioactive groups (flavonoids, glycosides and diarylheptanoids) were detected in Galanga extracts and are involved in antioxidant and pharmacological properties of its extracts [13]. Additionally, the isolated diarylheptanoid from Galanga extracts showed strong inhibitory and antibacterial effects [14] and the methanolic extracts of rhizomes displayed antifungal activities [15]. Furthermore, the presence of bioactive components inside polymers were exploited previously to extend the shelf life during storage of grass carp fillets [16], preservation of chicken breast [17] and sliced Omega-3 rich mortadella [18]. ...
The current study was performed to develop biodegradable films with matrix composed from gum Arabic (GA) and different concentrations from Alpinia officinarum phenolic extract (AOE). The color indices, physical properties, surface shape, crystallinity, mechanical properties and thermal stability of produced films were investigated. The incorporation of AOE extract (0.25 g/100 mL) inside GA films increased dark yellow color, reduced moisture, swelling, solubility and water vapor permeability (WVP) of films up to 10.29%, 21.05%, 14.15% and 4.20 × 10⁻¹⁰ g H2O/m s p.a., respectively. Furthermore, the scanning electron micrographs showed uniform structure with rough surface and turmoil spots in the structure by increasing AOE concentration inside films. The FT-IR analysis showed typically bands that proved physical interaction between AOE extract and GA polymer. The fabricated films showed satisfied thermal stability manners with declining trend by incorporation of AOE inside GA films. Furthermore, the developed films showed significant effects on reducing the changes of browning index from 17.20 to 24.54 and firmness from 33.98 to 22.65 N of Agaricus bisporus caps during storage days compared with commercial packaging materials.
... Sichuan pepper is one of the main spices used in Chinese food and has anti-inflammatory, antifungal, and analgesic activities [139]. GX-50, a natural ingredient extracted from Sichuan pepper, is a promising agent for AD therapy [140][141][142]. ...
Alzheimer’s disease (AD) is a progressive neurodegenerative disease that primarily manifests as memory deficits and cognitive impairment and has created health challenges for patients and society. In AD, amyloid β-protein (Aβ) induces Toll-like receptor 4 (TLR4) activation in microglia. Activation of TLR4 induces downstream signaling pathways and promotes the generation of proinflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β), which also trigger the activation of astrocytes and influence amyloid-dependent neuronal death. Therefore, TLR4 may be an important molecular target for treating AD by regulating neuroinflammation. Moreover, TLR4 regulates apoptosis, autophagy, and gut microbiota and is closely related to AD. This article reviews the role of TLR4 in the pathogenesis of AD and a range of potential therapies targeting TLR4 for AD. Elucidating the regulatory mechanism of TLR4 in AD may provide valuable clues for developing new therapeutic strategies for AD.
... Plant extract is a general term used for a product of natural origin whose chemical constituents have not been expounded. A variety of extracts have exhibited explicit antifungal activity including Curcuma zedoaria [32], Plectranthus barbatus, Hydrocotyle bonariensis, Lippia alba, Aristolochia cymbifera, Hydrocotyle bonariensis, Plectranthus amboinicus, Herreria salsaparilha [33,34], Mentha X piperita, Justicia pectoralis, Calamintha adscendens, Eleutherine bulbosa, Albizia inundata, Baccharis trimera, Plectranthus grandis, Cymbopogon citratus, Bauhinia forficate [35,36] and Euphorbia hirta L. [37]. ...
The current COVID-19 epidemic is a sobering reminder that human susceptibility to infectious diseases remains even in our modern civilization. After all, infectious diseases are still the major reason of death globally. Healthcare authorities have often underestimated and ignored the threat posed by “microbial dangers,” although they put millions of lives at risk every year. Overlooked developing diseases including fungal infections (FIs) contribute to roughly 1.7 million fatalities per year. As many as 150 million cases of severe and potentially life-threatening FIs are reported each year. In the last few years, the number of instances has steadily increased. Most of them are invasive fungal infections that require specialized treatment and hospital care. In recent years herbal antifungal compounds have been explored to acquire effective and safe therapy against fungal infections. However, potential therapeutic effects are hampered by the poor solubility, stability, and bioavailability of these important chemicals as well as the gastric degradation that occurs in the gastrointestinal tract. To get around this issue, researchers have turned to novel drug delivery systems such as nanoemulsions, ethosomes, metallic nanoparticles, liposomes, lipid nanoparticles, transferosomes, etc by improving their limits, nanocarriers can enhance the medicinal effects of herbal oils and extracts. The present review article focuses on the available antifungal agents and their characteristics, mechanism of antifungal drugs resistance, herbal oils and extract as antifungal agents, challenges in the delivery of herbal drugs, and application of nano-drug delivery systems for effective delivery of antifungal herbal compounds.
... The Minimum Inhibitory Concentration (MIC) value of CGA against Salmonella was determined according to the agar dilution method (Liu et al., 2012(Liu et al., , 2017Fu et al., 2016), with minor modifications as follows: (1) 100 µL of LB liquid culture medium was added into the 1st to 10th wells of a 96-well microplate, and then 100 µL CGA solution (0.1 g/L) extracted from the leaves of EU was added to the 1st well and mixed well; (2) 100 µL of the mixed solution from the 1st well was pipetted and added into the next well, and then a double dilution was performed in turn. After mixing in the 10th well, 100 µL of the mixed solution was discarded; (3) Bacterial suspension was collected (OD 600 = 0.5), and 100 µL was added into each well from the 1st to the 10th, and then mixed well. ...
Chlorogenic acid (CGA) is an antibacterial agent that can be isolated from Eucommia ulmoides Oliver, a Chinese medicinal and edible plant food. The inhibitory effect of CGA on bacterial growth and stiffness of the outer membrane (OM) had been reported, while more evidence were required to elucidate its impairment of cell wall. In this study, the morphological and physiochemical changes of Salmonella cells under CGA treatment were investigated. Firstly, the minimum inhibitory concentration (MIC) of CGA against Salmonella was assayed. Later, the permeability of OM and activity of the proteins released were measured and observed to reveal the alteration of OM characteristic and cellular morphology. Finally, reactive oxygen species and cell membrane fluidity were analyzed, respectively, to elucidate how CGA damaged cell surface. The results showed that MIC of CGA against Salmonella was 6.25 mg/L. Under sub-lethal doses of CGA, the OM permeability and the release of soluble proteins were enhanced evidently, and Salmonella cells showed more deformed and shrunken, confirming the impairment of cellular integrity under CGA. Finally, the possible cause of cell surface damage was investigated. the fluidity of the membrane was increased upon CGA treatment, which may the possible cause of OM by CGA.
... KBN is composed of Coptis chinensis Franch (Huanglian), Saururus chinensis (Lour.) Baill (Sanbaicao), Isatidis folium (Daqingye), Celosia cristata L. Their bioactive properties include anti-fungal (Liu et al., 2012;Yang et al., 2015;Niu et al., 2019) and anti-inflammatory (Lee et al., 2014;Yang et al., 2019;Ji et al., 2020;Pudziuvelyte et al., 2020). The previous research found that KBN significantly alleviated the vaginal inflammation in VVC model mice. ...
Vulvovaginal candidiasis (VVC) is an infectious disease caused by Candida species, which affects millions of women worldwide every year. The resistance to available antifungal drugs for clinical treatment is a growing problem. The treatment of refractory VVC caused by azole-resistant Candida is still facing challenges. However, research on new antifungal drugs is progressing slowly. Although a lot of reports on new antifungal drugs, only three new antifungal drugs (Isavuconazole, ibrexafungerp, and rezafungin) and two new formulations of posaconazole were marketed over the last decade. Chinese botanical medicine has advantages in the treatment of drug-resistant VVC, such as outstanding curative effects and low adverse reactions, which can improve patients’ comfort and adherence to therapy. Kangbainian lotion (KBN), a Chinese botanical formulation, has achieved very good clinical effects in the treatment of VVC. In this study, we investigated the antifungal and anti-inflammatory effects of KBN at different doses in fluconazole-resistant (FLC-resistant) VVC model mice. We further studied the antifungal mechanism of KBN against FLC-resistant Candida albicans (C. albicans) and the anti-inflammatory mechanism correlated with the Dectin-1 signaling pathway. In vivo and in vitro results showed that KBN had strong antifungal and anti-inflammatory effects in FLC-resistant VVC, such as inhibiting the growth of C. albicans and vaginal inflammation. Further studies showed that KBN inhibited the biofilm and hypha formation, reduced adhesion, inhibited ergosterol synthesis and the expression of ergosterol synthesis-related genes ERG11, and reduced the expression of drug-resistant efflux pump genes MDR1 and CDR2 of FLC-resistant C. albicans in vitro. In addition, in vivo results showed that KBN reduced the expression of inflammatory factor proteins TNF-α, IL-1β, and IL-6 in vaginal tissues, and inhibited the expression of proteins related to the Dectin-1 signaling pathway. In conclusion, our study revealed that KBN could ameliorate vaginal inflammation in VVC mice caused by FLC-resistance C. albicans. This effect may be related to inhibiting the growth of FLC-resistance C. albicans and Dectin-1 signaling pathway activation.
... Chinese herbal medicine is considered a natural reservoir of active compounds, and many researchers have investigated various phytochemicals, including proteins, amino acids, coumaric acid, aldopentose, calcium oxalate and polysaccharides. The composition of these bioactive molecules validates the synergistic effect against microbial pathogenicity [53,54]. ...
Recent advances in nanotechnology have opened up new avenues for the controlled synthesis of nanoparticles for biomedical and pharmaceutical applications. Chinese herbal medicine is a natural gift to humanity, and it has long been used as an antibacterial and anticancer agent. This study will highlight recent developments in the phytonanotechnological synthesis of Chinese herbal medicines to utilize their bioactive components in biomedical and therapeutic applications. Biologically synthesized silver nanoparticles (AgNPs) have emerged as a promising alternative to chemical and physical approaches for various biomedical applications. The comprehensive rationale of combinational or synergistic effects of Chinese herb-based AgNPs synthesis was investigated with superior physicochemical and biological properties, and their biomedical applications, including antimicrobial and anticancer activity and wound healing properties. AgNPs can damage the cell ultrastructure by triggering apoptosis, which includes the formation of reactive oxygen species (ROS), DNA disintegration, protein inactivation, and the regulation of various signaling pathways. However, the anticancer mechanism of Chinese herbal medicine-based AgNPs is more complicated due to the potential toxicity of AgNPs. Further in-depth studies are required to address Chinese herbs' various bioactive components and AgNPs as a synergistic approach to combat antimicrobial resistance, therapeutic efficiency of drug delivery, and control and prevention of newly emerged diseases.
... The antibacterial activity of H. syriacus extracts has been studied by Punasiya et al. [23] against B. cereus, S. aureus, and K. pneumonia; by Mak et al. [41] against S. typhimurium and S. aureus; and by Seyyednejad et al. [42] against B. anthracis, B. cereus, S. aureus, S. epidermidis, L. monocytogenes, S. pyogenes, E. coli, S. typhy, K. pneumonia, and P. aeruginosa, but no assays against E. amylovora and E. vitivora pathogens have been carried out. Regarding the antifungal activity, it has been assayed against C. albicans and S. cerevisiae by Liu et al. [43], and against T. mentagrophytes [8], but no data on Diplodia spp. (or other Botryosphaeriaceae) is available. ...
Phytochemicals are essential raw materials for the production of formulations that can be helpful in crop protection. In particular, Hibiscus spp., which are often used in traditional medicine, are rich in potential bioactive molecules. This study presents an analysis of the thermal, vibrational, and phytochemical characteristics of a light purple variety of Hibiscus syriacus, using thermal gravimetric and differential scanning calorimetry, Fourier-transform infrared spectroscopy, and gas chromatography-mass spectroscopy techniques. Further, with a view to its valorization, the antimicrobial activity of its extracts has been investigated in vitro against Erwinia amylovora (the phytopathogen responsible for fire blight in apples, pears, and some other members of the family Rosaceae), Erwinia vitivora (the causal agent of the “maladie d’Oléron” in grapevines), and Diplodia seriata (responsible for “Bot canker”). Higher heating values and thermal features showed similarities with kenaf biomass. The main compounds identified in the hydro-methanolic extracts were: in flowers, 1-heptacosanol, heptacosane, 1-tetracosanol, hexadecenoic acid, 9,12,15-octadecatrienoic acid, and 9,12-octadecadienoic acid; and in leaves, the coumarin derivative 4,4,6,8-tetramethyl-2-chromanone, vitamin E, phytol, and sitosterol. MIC values of 500 and 375 μg·mL−1 were obtained against E. amylovora for flower and leaf extracts, respectively, upon conjugation with chitosan oligomers (to improve solubility and bioavailability). In the case of E. vitivora, MIC values of 250 and 500 μg·mL−1, respectively, were registered. Regarding the antifungal activity, EC90 values of 975.8 and 603.5 μg·mL−1, respectively, were found. These findings suggest that H. syriacus (cv. ‘Mathilde’) may be a promising source of antimicrobials for agriculture.
... Coumarins, the main active components of Cnidii Rhizoma, experience a variety of biological activities, including anti-tumor (Shokoohinia et al., 2018), anti-inflammatory (Lee et al., 2014), antispasm (Sadraei et al., 2012), anti-virus (Tamura et al., 2010), and antifungal properties (Matsuda et al., 2002). In order to select effective traditional Chinese medicine preparations based on clinical trial information, Liu et al. (2012) used Chinese e-journal databases to search the relevant Chinese clinical study literature and concluded that C. monnieri (L.) should be preferably selected as one of the antifungal plant candidates since they were mostly consistently present in prescriptions or preparations used to treat mycotic vaginitis. ...
Trichoderma rubrum (T. rubrum) is one of the important pathogens because it is the cause of most dermatomycosis. The treatment of Trichophyton rubrum infection is time-consuming and very expensive; it is easy for the infections to reoccur, leading to therapeutic failures, persistence, and chronic infection. These issues have inspired researchers to study natural alternative therapies instead. Cnidium monnieri (L.), as a kind of traditional Chinese medicine, has a variety of pharmacological activities and a wide range of applications, so it has a high potential for researching and economic value. We detected the effect of aqueous extract of C. monnieri (L.) on the activity of T. rubrum by Cell Count Kit-8 assay (CCK-8), and we found that 128 and 256 μg/ml of aqueous extracts of C. monnieri (L.) co-cultured with T. rubrum for 24 h showed the inhibitory effect on T. rubrum. The results of scanning electron microscopy (SEM) and transmission electron microscopy (TEM) confirmed that aqueous extract of C. monnieri (L.) damaged the T. rubrum. At the same time, mass spectrometry screening with T. rubrum before and after the treatment of 256 μg/ml of aqueous extracts of C. monnieri (L.) showed that 966 differentially expressed proteins were detected, including 524 upregulated differentially expressed genes (DEGs) and 442 downregulated DEGs. The most significantly downregulated protein was chitin synthase (CHS); and the results of qRT-PCR and Western blotting demonstrated that the expression level of CHS was downregulated in the 256 μg/ml group compared with the control group. The study showed that the aqueous extract of C. monnieri (L.) could destroy the morphology of mycelia and the internal structure of T. rubrum, and it could inhibit the growth of T. rubrum. The antifungal effect of aqueous extract of C. monnieri (L.) may be related to the downregulation of the expression of CHS in T. rubrum, and CHS may be one of the potential targets of its antifungal mechanism. We concluded that aqueous extract from C. monnieri (L.) may be a potential candidate for antifungal agents.
... Similar results were obtained with C. baccifera in different geographical regions (Ning et al., 2010a(Ning et al., , 2010b(Ning et al., , 2010b. (Liu et al., 2012) were reported the leaf parts were used to treat gastroenteritis, Diabetes mellitus, catharsis from the Wuliang mountains of China. Further, CPT was first to isolate from the endophytic fungi of C. baccifera from Sathyamangalam Tiger Reserve Forest. ...
Endophytic wild fungal strain Phyllosticta elongata MH458897 isolated from medicinal plant Cipadessa baccifera from the Western Ghats region of Sathyamangalam Tiger Reserve Forest. This endophytic fungus has potential of effective anticancer drug Camptothecin (CPT). Endophytic fungi act as key symbionts in-between plants and ecosystem in the biosphere. This recently identified microbial population inside the plants produces many defence metabolites against plant pathogens. Among these defense metabolites, CPT gained much attention because of its effective anticancer activity. The maximum yield of CPT produced by optimizing the various factors like DEKM07 medium, pH 5.6, incubation time using Response Surface Methodology based on Central Composite Design. Extracted CPT is characterized using High Performance Liquid Chromatography and Electrospray ionization-Mass spectrometry. The highest yield of CPT was 0.747 mg/L was produced at optimized factors of dextrose - 50 g L-1, peptone - 5.708 g L-1, magnesium sulphate - 0.593 g L-1, and incubation time - 14 days. In-vitro MTT assay revealed the CPT derivatives were cytotoxic to A-549 cancer cell line (IC50 58.28 μg/ml) as nearly compared to the (IC50 51.08 μg/ml) standard CPT. CPT producing strain P. elongata from C. baccifera has the potential of CPT biosynthesis, and could be an effective anticancer bio metabolite. This compound has been described in the literature to be an effective anticancer metabolite. Our findings support the novel lifesaving anticancer drug from endophytic fungus in forest ecosystem concludes effective utilization of key symbionts will safeguard the humans and forest ecosystem.
... In this context, natural products arise as an important and promising source for the discovery of novel antifungal agents . Since these products have traditionally been used in controlling various diseases, as they are sources of multiple active compounds possessing therapeutic properties and are part of different synthesis of various natural products (Liu et al., 2012). Furthermore, the use of native plant species can be an economical alternative to the use of sustained region. ...
The aim of this study was evaluate the in vitro antifungal activity of crude extracts from Eugenia uniflora, Libidibia ferrea and Psidium guajava. The extracts were obtained by turbo-extraction using water (AQ) or acetone-water (AC-W) (7:3, v/v) as solvents and lyophilized to obtain the crude extracts (CE). The CE were characterized by UV-Vis, TLC and HPLC. The activity of CEs was investigated against clinical isolates of Candida spp. and the Minimum Inhibitory Concentration (MIC), MIC50 and MIC90 were determinated. The analysis by TLC showed that all CEs presented polyphenols (flavonoids and tannins). The CEs from E. uniflora showed higher amount of polyphenols (30.35 ± 2.15%, AC-W) and the HPLC analysis revealed the tannins in all extracts. The CEs of E. uniflora showed MIC range from 1.9 to 500.0 µg/mL, and lower values of MIC50 and MIC90 against non-albicans Candida isolates. Regarding L. ferrea and P. guajava, the results showing MIC from 3.9 to 1000.0 µg/mL (CE-AQ) against C. albicans. The results demonstrate antifungal performance from CE against various species of Candida spp., suggesting that the herbal species may be use as new potential antifungal agents. Additionally, the polyphenol content can play a pivotal role in the antifungal properties of CE.
... It is found on spoiled food, in soils, and is dispersed in hot dry weather; the spores are allergy by chronic cough, dyspnea, chest tightness, chronic phlegm, snuffle, and allergic rhinitis [14].The research aimed to used crude extracted of A. graveolens of roots for inhibition R.nigricans which were fungicides in phytopathogenic fungi in the orchids farms. Antifungal methods were used disc diffusion dilution and measurement by % transmitting at 625 nm by spectrometer and were IC 50 of the minimum fungicidal concentration (MFC) [15,16]. In vitro anti-fungal activities were developed against for plant pathogenic strained of R. nigricans by using the roots ...
... Other herbal medicines have a neuroprotective effect on dopaminergic neurons and improve motor symptoms by inhibiting oxidative stress and cell death [25] and by improving mitochondrial dysfunction [15]. Chunggantang is regarded as an efficient drug for improving the symptoms of PD. e modified form of Chunggantang (KD5040) is widely used in Traditional Oriental Medicine and has many effects, including anti-inflammatory and neuroprotective properties [26], improvement of motor function [27], decreasing the dose of levodopa, and relieving LID [28]. KD5040 also involved the neuronal survival in the brain by the expression of salusin-β and MrgprA1 [29]. ...
Parkinson’s disease is the second most common neurodegenerative disease. Patients with Parkinson’s disease can be treated with a combination of acupuncture and herbal medicine, but studies on the synergistic effects of the combined treatment have not yet been conducted. Thus, we subjected an MPTP-induced Parkinson’s disease mouse model to the combined treatment. We used acupoint GB34 for acupuncture and modified Chunggantang (KD5040) as the herbal medicine, as they have been reported to be effective in Parkinson’s disease. We investigated the suboptimal dose of KD5040 and then used this dose in the combined treatment. The results showed that the combined treatment had a synergistic effect on improvements in abnormal motor function and neurodegeneration compared with the use of acupuncture or herbal medicine alone. The combined treatment also had a neuroprotective effect via the PI3K/AKT and MAPK/ERK signaling pathways. These findings suggest that the combined treatment with acupuncture and KD5040 can help improve the symptoms of Parkinson’s disease.
... Galangin (Gal) is an active flavonoid extracted and isolated from the roots of Alpinia officinarum Hance, an annual plant, and has a long history of use as a medicine and edible herb in China to warm the stomach, prevent vomiting, and remove cold and pain. It is also listed in the Chinese Pharmacopoeia [1]. Many studies have reported that galangin possesses a broad range of pharmacological activity such as being anti-inflammatory, antibacterial, and antifungal and suppressing vitiligo, Alzheimer's disease, and cancer [2]. ...
Galangin has been reported to have many pharmacological effects including being anti-inflammatory, antibacterial, and antifungal and a suppressor of vitiligo, Alzheimer’s disease, and cancer. The purpose of this research was to characterize and determine the efficacy of the antitumor activity and pharmacokinetics of galangin-loaded PEGylated liposomes compared with free galangin. Galangin-loaded liposomes and galangin-loaded PEGylated liposomes were prepared using thin-film dispersion prior to ultrasonication. The mean particle size of the galangin-loaded PEGylated liposomes was approximately 120 nm, the polydispersity index was 0.212, the zeta potential was -2.24 mV, and the entrapment efficiency was 76.31%. The release of galangin from galangin-loaded PEG-modified liposomes was slowest as gauged by dynamic dialysis in vitro . In the apoptosis experiment, galangin-loaded PEG-modified liposomes demonstrated cytotoxicity to hepatoma cells by apoptosis that was greater than the two other forms of drug carrier. In vivo experiments demonstrated that the half-life of galangin in PEG-modified liposomes was 4 hours in the plasma of rats, significantly longer than that of free galangin. The experimental results suggest that the PEG modification of liposomes effectively increases the solubility of galangin and alters its pharmacokinetic parameters, such that it may be effective in the treatment of liver cancer.
... The minimum inhibitory concentration and minimal fungicidal concentration values were 1.2 and 2.0 mg/mL, respectively (Klahan et al., 2011). Antifungal activity against C. albicans was also observed in the ethanol, acetone, and hexane extracts of A. officinarum (Liu et al., 2012a). ...
... Using T. rubrum, we tested the antifungal activity of leaves from 15 Japanese folk herbs belonging to different plant families and extracted using five different solvents. The solvents were chosen based on previous studies that demonstrated antifungal properties in different herb extracts Dellavalle et al., 2011;Guedes et al., 2012;Guo et al., 1997;Liu et al., 2012;Wilson et al., 1997;Zhu et al., 2005 . Of the herbs surveyed, six were strongly antifungal in vitro, with activity comparable to that of amphotericin B implying one or more antifungal components active against T. rubrum. ...
Folk herbs are vital to the Japanese health care system, with some being used to treat fungal skin infections. We tested folk herbs used in traditional Japanese medicine for in vitro antifungal activity against Trichophyton rubrum, the most common pathogen in patients with superficial dermatitis. Acetone, ethanol, methanol, water, and acetic acid extracts from 15 species of Japanese folk herbs (Bi-wa, Aka-me-gashiwa, Ta-mushi-ba, Yomogi, Shi-so, Ku-ko, So-ba, Yama-momo, Kuro-mo-ji, Ichi-ji-ku, Kaki-no-ki, Kuwa-no-ki, Kusa-gi, Chimaki-zasa, and I-buki-jya-kou-sou) were evaluated for fungal growth inhibition, as measured by absorbance. Crude acetic acid extracts of Aka-me-gashiwa, Ta-mushi-ba, Yomogi, Ku-ko, Kaki-no-ki, and I buki-jya-kou-sou exhibited antifungal activity comparable to that of amphotericin B. Although the active compounds and underlying antifungal mechanisms are not known, the data contribute to the development of new and safe antifungal drugs, highlight new extraction methods for herbs, and support the traditional use of Japanese folk herbs against fungal infections.
Trichophyton mentagrophytes (T. mentagrophytes) is a prevalent pathogen that causes human and animal dermatophytosis. The clinical treatment of the infections is challenging due to the prolonged treatment duration, limited efficacy, antifungal resistance and side effects of existing drugs. Modern research has reported that the classic Traditional Chinese medicine (TCM) prescription Huangqin decoction (HQD) along with its principal ingredients could exhibit antifungal properties. Given the valued advantages of TCM such as broad-spectrum antifungal activity, low incidence of drug resistance and low toxicity, this study investigated the antifungal activity of HQD against T. mentagrophytes and explored the potential inhibitory mechanism, aimed to provide new clues for the treatment of dermatophytosis. By detecting minimal inhibitory concentration (MIC) using the broth microdilution method, the results showed that HQD could significantly inhibit the growth of T. mentagrophytes, with a minimal inhibitory concentration (MIC) of 3.13 mg/mL. The transcriptome sequencing and quantitative real-time PCR (qRT-PCR) technology were combined to shed light on the complicated adaptive responses of T. mentagrophytes upon HQD. The results demonstrated that at MIC, compared with the control group, a total of 730 differentially expressed genes (DEGs) were detected in T. mentagrophytes after HQD exposure (FDR adjusted p-value < 0.05), of which 547 were up-regulated and 183 were down-regulated. These DEGs were abundant in “single-organism metabolic process”, “catalytic activity” and “oxidoreductase activity”, and were significantly enriched in seven signaling pathways including glutathione metabolism, DNA replication, glyoxylate and dicarboxylate metabolism, taurine and hypotaurine metabolism, carotenoid biosynthesis, ubiquitin-mediated proteolysis, and cyanoamino acid metabolism. The results of transcriptome profiling were verified using qRT-PCR for a subset of 10 DEGs. The overall evidence indicated that HQD had a significant anti-dermatophyte activity and the adaptive responses of T. mentagrophytes upon HQD might be related to targeting glutathione S-transferase (GST) gene that could conjugate with toxic xenobiotics to defense oxidative stress, the inhibition of DNA replication pathway by downgrading the DNA replication licensing factors MCM3, MCM5 and ribonuclease H1 (RNaseH1) genes, and the repressed expression of phosphatidylserine decarboxylase (PSD) gene related to phospholipid synthesis which was indispensable for hyphal morphology, hyphal differentiation and cell wall integrity. Our study showed a new theoretical basis for the effective control of T. mentagrophytes infection and the effect of HQD on fungi, which are expected to offer aids for discovering new antifungal agents upon dermatophytosis.
Currently, natural bioactive ingredients and/or raw materials are of significant interest to scientists around the world. Flavonoids and other polyphenols are a major group of phytochemicals that have been researched and noted as bioactive molecules. They offer several pharmacological and medical benefits. This current review aims to (1) illustrate their benefits for human health, such as antioxidant, anti-aging, anti-cancer, anti-inflammatory, anti-microbial, cardioprotective, neuroprotective, and UV-protective effects, and also (2) to perform a quality evaluation of traditional medicines for future application. Consequently, keywords were searched on Scopus, Google Scholar, and PubMed so as to search for related publications. Then, those publications were carefully checked in order to find current and non-redundant studies that matched the objective of this review. According to this review, researchers worldwide are very interested in discovering the potential of flavonoids and other polyphenols, used in traditional medicines and taken from medicinal plants, in relation to medical and pharmaceutical applications. Many studies focus on the health benefits of flavonoids and other polyphenols have been tested using in silico, in vitro, and in vivo models. However, few studies have been carried out using clinical trials that have trustworthy subject sizes and are in accordance with clinical practice guidelines. Additionally, interesting research directions and perspectives for future studies are highlighted in this work.
Herbs rich in secondary metabolites may possess beneficial properties in livestock nutrition and health. 49 Polygonaceae species of European mountain regions were included in a qualitative systematic review based on the methodological framework of the PRISMA statement. 174 relevant publications were identified. They comprised 231 in vitro and 163 in vivo experiments with cattle, sheep, goats, poultry, pigs, and rodents. For 16 Polygonaceae species no reports were found. Fagopyrum esculentum and Fagopyrum tataricum showed potential as anti-inflammatory, antioxidative and metabolic modifying herbs and feeds improving intake and nitrogen conversion in broiler as well as milk quality and ruminal biotransformation in dairy cows. Polygonum aviculare was promising as an antimicrobial and anti-inflammatory drug or feed, improving performance and affecting ruminal biotransformation in sheep, and Polygonum bistorta as an anti-inflammatory drug or feed, improving performance in broiler and mitigating methane emissions in ruminants. Rumex obtusifolius showed potential as an antibacterial drug or feed improving ruminal biotransformation and preventing bloating in cows, while Rumex acetosa and Rumex acetosella had antimicrobial and anti-inflammatory properties. Furthermore, Polygonum minus, Polygonum persicaria, Rumex crispus and Rumex patientia possess interesting anti-inflammatory and antimicrobial activities. In conclusion, some Polygonaceae species show relevant properties that might be useful to prevent and treat livestock diseases, combined with nutritional benefits in performance, product quality, lowering ruminal methane and ammonia formation and transferring omega-3 fatty-acids from feed to tissue. The potential of such multifunctional plants for a holistic integration of veterinary, nutritional and ecological perspectives under a one-health approach of livestock management is discussed.
Antifungal agents play a crucial role in the treatment of fungal infections, which can range from minor skin conditions to life-threatening systemic diseases. These abstract reviews the pharmacological objectives, mechanisms of action, and clinical applications of antifungal agents. The primary objectives of antifungal therapy include achieving fungicidal or fungi static activity against fungal pathogens while minimizing toxicity to host cells. Despite the fact that Trichosporon spp. are probably the second or third most prevalent non-Candida yeast infection that causes invasive disease in hematological cancer patients. Central and vesical venous catheters, as well as devices related to peritoneal venous catheters, are the primary vectors of invasive Trichosporon spp. infection. Antifungal medications and host immune responses can be avoided by these organisms because they are adept at adhering to these devices and forming biofilms. Mechanisms of action vary widely among antifungal drugs, targeting fungal cell walls, membranes, nucleic acids, or metabolic pathways essential for fungal survival. Clinical efficacy is influenced by factors such as spectrum of activity, pharmacokinetic properties, and the emergence of resistance. Challenges in antifungal therapy include the rise of resistant fungal strains, limited treatment options, and the complexity of treating immune compromised patients. Future research directions include the development of novel antifungal agents, strategies to combat resistance, and improvements in diagnostic and therapeutic approaches. Overall, antifungal therapy continues to evolve, driven by ongoing research aimed at enhancing treatment outcomes and reducing the global burden of fungal infections.
Pogostemon cablin (Patchouli) is a significant herb of Lamiaceae family with broad range of therapeutic advantages and it is extensively used in cosmetics as well as pharmaceutical industries. P. cablin owing to its tremendous commercial, economic as well as potential medicinal properties, it has been grown in various parts of Southeast Asia and China for more than 1000 years. P. cablin is a native plant of Philippine and prefers tropical and sub-tropical countries for its optimum growth and production. Understanding biology as well as chemistry of any plant is very necessary for its relevant uses in any field. Therefore, this chapter in addition to biological and pharmacological applications, provides a brief description of chemical composition as well as nutritive status of P. cablin. There are approximately one 140 beneficial compounds discovered so far from P. cablin, some of the top-notch compound which are responsible for its medicinal values includes terpenoids, flavonoids, alcohol and several glycosides along with various phytochemical compounds. Moreover, in this chapter we will discuss major advantageous application of P. cablin in detail. P. cablin is used for the treatment of colds, fever, emetic problems, diarrhea, headache, abdominal pain as well as it is used to fight against various insect pests and snake bites. Furthermore, many other biological aspects regarding P. cablin involves defensive action against oxidative damages instigated by certain xenobiotics, exerts anti-analgesic actions, anti-platelet, aphrodisiac, anti-inflammatory, anti-thrombotic, anti-depressant, anti-emetic along with antimutagenic as well as cytotoxic and fibrinolytic capabilities. In aromatherapy, P. cablin is reported to relieve against depression and have potential role to control nerves, stress and appetite as well as significantly improve the libido of exposed individuals.
Context
Polygonum hydropiper L. (Polygonaceae) (PH) is a traditional Chinese traditional medicine with a pungent flavor and mild drug properties. PH is mainly distributed in the channel tropism in the stomach and large intestine. PH has multiple uses and can be used to treat a variety of diseases for a long time.
Objective
This review summarizes the phytochemical and pharmacological activities, and applications of PH from 1980 to 2022. We also provide suggestions for promoting further research and developing additional applications of PH.
Methods
The data and information on PH from 1980 to 2022 reviewed in this article were obtained from scientific databases, including Science Direct, PubMed, Science Citation Index, SciFinder Scholar (SciFinder), Springer, American Chemical Society (ACS) Publications, and China National Knowledge Infrastructure (CNKI), etc. Some information was obtained from classic literature on traditional Chinese medicines. The search terms were Polygonum hydropiper, phytochemistry compositions of Polygonum hydropiper, pharmacological activities of Polygonum hydropiper, and applications of Polygonum hydropiper.
Results
The comprehensive analysis of the literature resulted in 324 compounds being isolated, identified, and reported from PH. Regarding traditional uses, the majority of phytochemical and pharmacological studies have indicated the diverse bioactivities of PH extracts, flavonoids, and volatile oil elements, including antibacterial, antifungal, insecticidal, antioxidant, and anti-inflammatory.
Conclusions
PH has a long history of diversified medicinal uses, some of which have been verified in modern pharmacological studies. Further detailed studies are required to establish scientific and reasonable quality evaluation standards and action mechanisms of active constituents from PH.
Pogostemon cablin (Pogostemon patchouli or Patchouli) is known for its essential oil and is a popular medicinal herb in Indian Ayurveda and traditional Chinese medicine. This review covers patent articles on the P. cablin plant's therapeutic effects. The patent literature was collected using a thorough, comprehensive search on databases like Thomson Innovation, Espacenet, Patentscope, The Lens and Patent digital libraries of different Jurisdictions, including IPO, USPTO, CNIPA, inPASS, KIPO, JPO, etc. Despite the vast number of review articles on non-patent literature, none of the articles reviewed the patent literature. This current P. cablin literature analysis study will facilitate bridging the gap between further exploring the potential of this plant through novel investigations.
Ayurvedic Medicine, or Ayurveda, is a traditional Indian health care system. Research into the medicinal plants utilised in Ayurveda is becoming a global endeavour, and large pharmaceutical companies are investing in novel drug discovery from Ayurvedic sources as a number of clinical studies have demonstrated efficacy of natural products from Ayurvedic plant extracts against common ailments such as arthritis and diabetes.
Ayurvedic medicine and its components have been well described in the past, but this book represents a comprehensive source on the biochemistry and mechanisms of the pharmacological effects of natural products from Ayurvedic sources.
This book is a valuable resource for researchers in natural products and alternative sources of bioactive compounds in drug discovery, as well as pharmaceutical experts and those in industry.
The current study was performed to develop biodegradable films forming matrix composed from gum Arabic (GA) and different concentrations from Alpinia officinarum phenolic extract (AOE). The color indices, physical properties, surface shape, crystallinity, mechanical properties and thermal stability of produced films were investigated. The grafting of AOE extract inside GA films increased dark yellow color and reduced moisture, swelling, solubility and water vapor permeability (WVP) of films. Furthermore, the scanning electron micrographs showed uniform structure with rough surface and turmoil spots in the structure by increasing AOE concentration inside films. Additionally, physically interaction occurred between AOE extract and GA polymer was proven by using FT-IR analysis. The fabricated films showed satisfied thermal stability manners with declining trend by incorporation of AOE inside GA films. Furthermore, the developed films showed significant effects on reducing the changes of browning index and firmness of Agaricus bisporus caps during storage days compared with commercial packaging materials.
Background
Sophora flavescens Aiton (SF), also known as Kushen (Chinese:苦参), has been an important species in Chinese medicine since the Qin and Han dynasties. It is also recognized as a plant resource suitable for the globalization of Chinese medicine. Traditionally, it has been used in various ethnic medical systems in East Asia, especially in China, to kill insects and dispel dampness. Sophora flavescens is commonly used for clearing heat-clearing, killing worms, and diuretic. Nowdays, accumulating studies demonstrated its anticancer and cardioprotection.
Objective of the review
This paper aims to systematically review information on the genus, pharmacological and toxicological significance, chemical composition and biological activity of Sophora flavescens. To promoting its development and application. To summarize recent findings regarding to the metabolism, pharmacological/toxicological effects of Sophora flavescens.
Material and methods
Online academic databases (including PubMed, Google Scholar, Web of Science and CNKI) were searched using search terms of “Sophora flavescens Aiton”, “Ku shen”, “Pharmacology”, “Active ingredient”, “Toxicology” and combinations to include published studies of Sophora flavescens Aiton primarily from 1970–2021. Several critical previous studies beyond this period were also included and other related terms.
Conclusion
Sophora flavescens has a broad spectrum of biological activities associated with Sophora flavescens has been considered a valuable resource in both traditional and modern medicine. However, there is a lack of in-depth studies on the medicinal uses of Sophora flavescens. Moreover, further studies on single chemical components should be conducted based on the diversity of chemical structures, significant biological activities and clinical applications. The discovery of its bioactive molecules and multi-component interactions would be of great importance for the clinical application of Sophora flavescens spp. Detailed pharmacological and toxicological studies on the classic prescriptions of Sophora flavescens are also needed. It is more beneficial to the wide application of SF plant and facilitates the worldwide promotion of modern Chinese medicine. However, an increasing number of reports indicate that the administration of Sophora flavescens has serious adverse effects. Its main toxic effects are neurotoxicity and acute toxicity, which have caused widespread concern worldwide. In addition, the alkaloids of Sophora flavescens are distributed in the heart, liver, stomach and large intestine. They are excreted from the body through gluconeogenesis, which is the mode of action of certain therapeutic mechanisms of action such as anticancer. The detailed metabolic study of alkaloids and other components of Sophora flavescens in vivo needs to be further investigated. It is important to improve the pharmacological effects and reduce the toxicity of Sophora flavescens. For this purpose, structural modification of active components of Sophora flavescens or combination with other drugs is very essential.
Euphorbia L. is the largest genus in the plant family Euphorbiaceae with about 2000 species ranging from herbs to trees. Plants of this genus are used around the world to treat different kinds of ailments such as skin diseases, migraine, gonorrhoea and intestinal parasites. The present review aims to provide a comprehensive summary on the medicinal uses, pharmacology, cytotoxicity, and phytochemistry of the Euphorbia species in southern Africa. The literature search was performed through scientific databases such as Google Scholar, ScienceDirect, PubMed, JSTOR, and Scopus. Textbooks and dissertations were also consulted. A total of 35 Euphorbia species that are used in traditional medicine in southern Africa were identified. Although 35 species are used as traditional medicines, pharmacological, cytotoxicity and phytochemical studies have been carried out only on 16, 19 and 9 species, respectively. The investigated species have exhibited a wide spectrum of pharmacological activities, including antibacterial, antifungal, antiviral, antiplasmodial, antioxidant, anticancer, larvicidal and molluscicidal. They also exhibited cytotoxicity activities against various cell lines, including A549, CACO2, CS12, HELA, HrpG2 and MCF-7. Phytochemical studies have resulted in the isolation and identification of several compounds including 7-galloyl catechin, 3β-acetyloxy-olean-13, β-amyrin, caffeic acid, euphol, euphorbin, luteolin and quercetin. Although the medicinal uses of Euphorbia species in southern Africa have been well documented, the pharmacological and phytochemical studies are limited. Therefore, further studies to validate the use of Euphorbia species as traditional medicines and to isolate and identify active compounds are warranted.
The rhizome of Alpinia officinarum Hance, a popular spice used as a condiment in China and Europe, has various reported bioactivities, including anticancer, anti-inflammatory and antioxidant effects. However, its anti-angiogenic activity has not previously been reported. In this study, a diarylheptanoid was isolated from Alpinia officinarum and identified as 1-phenyl-7-(4-hydroxy-3-methoxyphenyl)-4E-en-3-heptanone (PHMH). We demonstrated that PHMH exerts anti-angiogenic activity both in vitro and in vivo. PHMH inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro, and also suppressed VEGF-induced sprout formation of rat aorta ex vivo. Furthermore, PHMH was found to block VEGF-induced vessel formation in mice and suppress angiogenesis in both zebrafish and chorioallantoic membrane models. Mechanistic studies indicated that PHMH inhibited VEGF-induced VEGF receptor-2 (VEGFR-2) auto-phosphorylation and resulted in the blockage of VEGFR-2-mediated signaling cascades in HUVECs, including the Akt/mTOR, ERK1/2, and FAK pathways. Our findings provide new insights into the potential application of PHMH as a therapeutic agent for anti-angiogenesis.
The anti-lung cancer activity of volatile oil from Alpinia officinarum (VOAO) and the underlying mechanism has not been studied. Herein, VOAO was extracted by steam distillation and its component was identified by the GC-MS analysis. Cells viability was measured by MTT assay and cell survival capacity was tested via colony formation assay. Apoptosis cells were detected using Annexin V-FITC/PI method. Hoechst 33342 cell unclear staining was employed to evaluate the nuclear morphology change. Mitochondrial membrane potential was detected by JC-1 staining assay. Bcl-2, Mcl-1 and cleaved caspase-3 proteins were quantified by immune blotting. Furthermore, VOAO anti-cancer activity was evaluated on A549 cell xenograft nude mice model. Our results have revealed that VOAO could inhibit cell viability of lung carcinoma cell and the colony formation capacity. VOAO downregulates Bcl-2 and Mcl-1 and triggers dysfunction of mitochondrial membrane potential. VOAO further activates caspase-3 cleavage and induces lung cancer cells apoptosis. In addition, VOAO administration significantly suppresses lung cancer growth in xenograft mice without obvious hepatotoxicity. We conclude VOAO could be an effective, low cytotoxicity natural component for treatment of lung carcinoma.
The formation of metal nanoparticles is one of the most vast and intensifying research areas in favor of prospective applications for the advancement of new technologies. It is a well-founded, significant feature of green chemistry that making marvelous interconnection between nano-biotechnology and microbial biotechnology. In the present research, the aqueous extract of medicinally important plant Coptis Chinensis (in Chinese called “gold thread”) was applied for the synthesis of gold nanoparticles (Au-NPs). The crystalline structure, size, shape and dispersion of Au-NPs were confirmed by using various characterization techniques i.e. X-ray Diffraction (XRD), High Resolution Transmission Electron Microscope (HRTEM) and Energy Dispersive X-ray (EDX). Well dispersed face centered cubic crystalline structures were obtained in the this contribution. The possible phyto-chemicals involved in the reduction and stabilization of Au-NPs were confirmed by Fourier Transform Infrared Spectroscopy (FT-IR). The prepared NPs were tested against highly drug resistance bacterium Escherichia coli both in light and dark. The results illustrated that the antibacterial efficiency of photo irradiated Au-NPs was several times higher than in dark Au-NPs. The zone of inhibition for irradiated Au-NPs was19 ± 0.5 mm, which was higher than in dark 14 ± 0.4 mm. This high antibacterial activity of photo irradiated Au-NPs are due to the production of reactive oxygen species which is responsible for the inhibition of bacteria.
Six unusual matrine-type alkaloid dimers, flavesines A-F (1-6), together with three proposed biosynthetic intermediates (7-9) were isolated from the roots of Sophora flavescens. Compounds 1-5 were the first natural matrine-type alkaloid dimers, and compound 6 represented an unprecedented dimerization pattern constructed by matrine and (-)-cytisine. Their structures were elucidated by means of NMR, MS, single crystal X-ray diffraction, and chemical method. The hypothetical biogenetic pathways of 1-6 were also proposed. Compounds 1-9 exhibited inhibitory activities against hepatitis B virus.
Patchouli therapeutic effects were closely correlated with the non-volatile constituents except for patchouli oils. Few studies have been reported on the contents of non-volatile constituents, and it still remained unknown in the case what were the water-soluble components. The water-soluble components from roots, stems, leaves of P. cablin were isolated and identified by GC-MS in this paper. The result showed, a total of 25, 31 and 34 compounds were identified, accounting for 81.652%, 58.322% and 77.817% of water extracts from roots, stems and leaves, respectively. Six compounds (n-Pentadecanoic acid, [1,2′-Binaphthalene]-5,5′,8,8′- tetrone,1′,4-dihydroxy- 2,3′-dimethyl-, 1-Hexacosene, 1,2-Benzenediol, Docosane and Tricosane) were included in the water-soluble components from roots, stems and leaves. There were some differences in the water-soluble components from roots, stems and leaves of P. cablin. This might have been due the possibility that the accumulation and storage of the water-soluble components was with relative independence.
An essential oil obtained by water distillation from Zanthoxylum bungeanum Maxim. fruits was analyzed by GC and GC/MS. Terpinen-4-ol (19.7%), 1,8-cineole (16.0%), p-cymene (7.9%), γ-terpinene (7.3%) and α-terpineol (7.2%) were the major compounds of the 35 identified components. The antifungal activity of the oil against 15 plant pathogenic fungi was assayed by the mycelial growth inhibition method and the values of median inhibition concentration (IC50) were below 1.0 mg/mL. The results showed that the oil had a broad spectrum of inhibitory activity against the tested fungi. The volatile components of the oil also obviously inhibited the mycelial growth of Rhizoctonia solani and Rhizoctonia cerealis. These results indicate that Z. bungeanum oil could be a source of antifungal ingredients for plant disease control especially applied in fruit and vegetable preservation.
The water extracts and extracted phenols from gametophytes and different parts of sporophytes of the two ferns, Adiantum capillus-veneris L. and Adiantum lunulatum Burm. f., used as folkloric medicines in India, China, Tibet, America, Philippines and Italy, were investigated for their antifungal activity against Aspergillus niger and Rhizopus stolonifer. Both crude extracts and extracted phenols of gametophytes and different parts of sporophytes of both fern species were found to be bioactive against the fungal strains. Antifungal activity was found to be higher in gametophytes than different parts of sporophytes. Among the different parts of sporophyte, immature pinnule possesses highest fungistatic property. Adiantum capillus-veneris was found a better antifungal agent than Adiantum lunulatum.
During screening of twenty six essential oils against Botrytis cinerea, the essential oils of the ten plants viz. Chenopodium ambrosioides, Eucalyptus citriodora, Eupatorium cannabinum, Lawsonia inermis, Ocimum canum, O. gratissimum, O. sanctum, Prunus persica, Zingiber cassumunar and Z. officinale were found to exhibit absolute fungitoxic activity (100% growth inhibition). The essential oils of O. sanctum, P. persica and Z. officinale were selected for further investigation because these oils showed lower Minimum Inhibitory Concentration (MIC) as compared
to the other fungitoxic oils. The selected oils were subsequently standardized through physico-chemical and fungitoxic properties.
The MIC values of O. sanctum, P. persica and Z. officinale were found to be 200, 100 and 100ppm (mg/l) respectively. The oils showed fungistatic nature at their respective MIC. The
oils were thermostable, and exhibited a wide range of fungitoxicity against 15 other post-harvest fungal pathogens. The oils
had the potency to withstand high inoculum density. The antifungal potency of oils was found to be greater in comparison to
some prevalent synthetic fungicides. Practical applicability of the essential oils was observed in control of grey mould of
grapes caused by B. cinerea during storage. The O. sanctum- and P. persica-oil-treated grapes showed enhancement of storage life up to 5 and 4days respectively. The storage life of Z. officinale-oil-treated grapes was found to be enhanced up to 6days. The oils did not exhibit any phytotoxic effect on the fruit peel.
Therefore, the oils could be recommended as a potential source of ecofriendly botanical fungicide, after long term and wide
ranging trials.
One hundred and thirty endophytic fungi isolated from 12 Chinese traditional medicinal plants collected at Yuanmou county
and Dawei Mountain, Yunnan province, southwest China, were tested for antitumour and antifungal activities by MTT assay on
human gastric tumour cell line BGC-823 and the growth inhibition test against 7 phytopathogenic fungi. The results showed
that fermentation broths from 9.2% of the isolates exhibited antitumour activity and 30% exhibited antifungal activity, moreover,
some of them exhibited broad-spectrum antifungal activity. The active isolates were identified to 32 taxa. The results indicate
that the endophytic fungi of Chinese traditional medicinal plants are promising sources of novel bioactive compounds.
Candida species are a major cause of catheter infections. Using a central venous catheter Candida albicans biofilm model, we demonstrated that chitosan, a polymer isolated from crustacean exoskeletons, inhibits candidal biofilm
formation in vivo. Furthermore, chitosan statistically significantly decreased both the metabolic activity of the biofilms
and the cell viability of C. albicans and Candida parapsilosis biofilms in vitro. In addition, confocal and scanning electron microscopic examination demonstrated that chitosan penetrates
candidal biofilms and damages fungal cells. Importantly, the concentrations of chitosan that were used to evaluate fungal
biofilm susceptibility were not toxic to human endothelial cells. Chitosan should be considered for the prevention or treatment
of fungal biofilms on central venous catheters and perhaps other medical devices.
The essential oils of the aerial parts of Ocimum basilicum Linn.var. pilosum (Willd.) Benth., an endemic medicinal plant growing in China, was obtained by hydrodistillation and analysed by GC-MS. Fifteen compounds, representing 74.19% of the total oil were identified. The main components were as follows: linalool (29.68%), (Z)-cinnamic acid methyl ester (21.49%), cyclohexene (4.41%), alpha- cadinol (3.99%), 2,4-diisopropenyl-1-methyl-1-vinylcyclohexane (2.27%), 3,5-pyridine-dicarboxylic acid, 2,6-dimethyl-diethyl ester (2.01%), beta-cubebene (1.97%), guaia-1(10),11-diene (1.58%), cadinene (1.41%) (E)-cinnamic acid methyl ester (1.36%) and beta-guaiene (1.30%). The essential oils showed significant antifungal activity against some plant pathogenic fungi.
A new diarylheptanoid, along with five known diarylheptanoids, was isolated from the rhizomes of Alpinia officinarum (Zingiberaceae). The structure of the new compound was determined to be trans,trans-1(3'-methoxy-4'-hydroxyphenyl)-7-phenyl-5-ol-4,6-dien-3-heptanone on the basis of spectral and chemical evidence.
The phenolic substances isolated from Sophora flavescens and identified include norkurarinone, kurarinone, kurarinol, methylkushenol C, l-maackiain and trifolirhizin. These compounds were tested for their antifungal activities on Basidiomycetes (Rhizoctonia, Marasumius, and Lepista) and Phycomycetes (Pythium), which are pathogens to turfgrasses. Of these phenolic substances, kurarinone was the most active and inhibited the growth of Pythium vanterpooli and P. graminicola at a concentration of 12.5 μg/ml.
The antifungal and antibacterial activities of the patchouly [Pogostemon cablin (Blanco) Benth] oils from three geographical regions (China, India and Indonesia) are studied against seventeen pathogenic fungus strains and sixteen commensal bacteria strains of diverse organs (skin, mucous membrane, nail, foot and armpit). In vitro, they have a manifeste antifungal and antibacterial properties and present a certain phytotherapeutic interest. That of China is more active with MIC inferior to 400 μl/l. In these volatile oils, the twenty major components are analysed by means of GC-MS. The good performance of the Chinese oil could be linked to a high percentage of patchouli alcohol in vitro.
Genetic manipulation of Candida albicans is constrained by its diploid genome and asexual life cycle. Recessive mutations are not expressed when heterozygous and undesired mutations introduced in the course of random mutagenesis cannot be removed by genetic back-crossing. To circumvent these problems, we developed a genotypic screen that permitted identification of a heterozygous recessive mutation at the URA3 locus. The mutation was introduced by targeted mutagenesis, homologous integration of transforming DNA, to avoid introduction of extraneous mutations. The ura3 mutation was rendered homozygous by a second round of transformation resulting in a Ura- strain otherwise isogenic with the parental clinical isolate. Subsequent mutation of the Ura- strain was achieved by targeted mutagenesis using the URA3 gene as a selectable marker. URA3 selection was used repeatedly for the sequential introduction of mutations by flanking the URA3 gene with direct repeats of the Salmonella typhimurium hisG gene. Spontaneous intrachromosomal recombination between the flanking repeats excised the URA3 gene restoring a Ura- phenotype. These Ura- segregants were selected on 5-fluoroorotic acid-containing medium and used in the next round of mutagenesis. To permit the physical mapping of disrupted genes, the 18-bp recognition sequence of the endonuclease I-SceI was incorporated into the hisG repeats. Site-specific cleavage of the chromosome with I-SceI revealed the position of the integrated sequences.
The purpose of this work was to screen the endophytic fungi having antitumor or antifungal activity, which were isolated from the inner barks of three kinds of pharmaceutical plants, Taxus mairei, Cephalataxus fortunei and Torreya grandis, collected from Fujian province, China. Antitumor activity was studied by the MTT assay and antifungal activity was determined by observing fungal growth inhibition. 13.4% of endophytic fungi fermentation broths displayed cytotoxic activity on HL-60 cells at and below a dilution of 1:50, and 6.4% on KB cells. 52.3% of endophytic fungi fermentation broths displayed growth inhibition on at least one pathogenic fungi, such as Neurospora sp., Trichoderma sp. and Fusarium sp. Among all endophytic fungi isolated, the genus Paecilomyces sp. has the highest positive rate of antitumor and antifungal activity. These results indicate that endophytic fungi could be a promising source for antitumor and antifungal bioactive agents.
Three novel diterpenoids, pseudolaric acids A, B and C, were isolated from the root bark of Pseudolarix kaempferi Gorden used as an antifungal agent in folk medicine in China. The structures of pseudolaric acids B and C were assigned as 1 and 6 by spectral and chemical evidence. Pseudolaric acids A, B and C possess antifungal activity and pseudolaric acid B possesses an antifertility effect.
Candida albicans remains the most frequent cause of fungal infections in an expanding population of compromised patients and candidiasis is now the third most common infection in US hospitals. Different manifestations of candidiasis are associated with biofilm formation, both on host tissues and/or medical devices (i.e. catheters). Biofilm formation carries negative clinical implications, as cells within the biofilms are protected from host immune responses and from the action of antifungals. We have developed a simple, fast and robust in vitro model for the formation of C. albicans biofilms using 96 well microtiter-plates, which can also be used for biofilm antifungal susceptibility testing. The readout of this assay is colorimetric, based on the reduction of XTT (a tetrazolium salt) by metabolically active fungal biofilm cells. A typical experiment takes approximately 24 h for biofilm formation, with an additional 24 h for antifungal susceptibility testing. Because of its simplicity and the use of commonly available laboratory materials and equipment, this technique democratizes biofilm research and represents an important step towards the standardization of antifungal susceptibility testing of fungal biofilms.
Endophytic fungi in medicinal plants produce a variety of bioactivity compounds. In this study, an endophytic fungus zjqy610 with antifungal activity was isolated from Polygonatum cyrtonema in Zhejiang Qingyuan Baishanzu Mountain nature reserve.
Strain zjqy610 was identified as Penicillium canescens based on the morphology and its rDNA sequence analysis. Three antifungal compounds were isolated from the fermentation broth of zjqy610 through normal-phase silica gel column chromatography and gel (Sephadex LH-20) column chromatography, traced by ultraviolet light or iodine vapor with bioassay-guided fractionation.
These three compounds were elucidated as o-acetylbenzeneamidinocarboxylic acid (zjqy610B-g-3), griseofulvin (zjqy610D-4) and naphtho [1,2-b] furan-3-carboxylic acid, 4-hydroxy-5-methoxy-2-methyl-(zjqy610F-2) based on mass spectrometry and nuclear magnetic resonance spectroscopy. The antifungal activity assays showed that the three compounds had inhibitory to variety of plant pathogenic fungi. Compound zjqy610D-4 had strong antifungal activity against Botrytis cinerea, Colletotrichum orbiculare, Didymella bryoniae and Sclerotinia sclerotiorum. EC50 was 0.68, 0.38, 0.91 and 0.61 mg/L, respectively.
Zjqy610D-4 is deserved to develop an agricultural antibiotics.
Combination therapy can be used for the treatment of fungal infections, especially for those caused by antifungal-resistant fungi. In the present study, in vitro interactions and mechanisms between fluconazole and minocycline against Candida albicans were evaluated. The nature of the interactions determined by spectrophotometric method in a checkerboard assay was interpreted using nonparametric models of fractional inhibitory concentration index (FICI) and percentages of growth difference (ΔE). In the mechanism study, we evaluated the potential activity of minocycline on fluconazole penetrating the C. albicans biofilm. Furthermore, the effect of fluconazole and minocycline alone and in combination on the cellular calcium balance, as well as on the uptake and efflux of fluconazole were evaluated. It was found that fluconazole can work synergistically with minocycline against fluconazole-resistant C. albicans; the minimum inhibitory concentration of fluconazole decreased from 512 to 2 microgmL(-1) when fluconazole and minocycline were given in combination, with an FICI of 0.035 and 0.064 and high-percentage synergistic interactions of 1250% and 988% for the two resistant strains. The mechanism of action was suggested to be the enhancement of minocycline on fluconazole penetrating biofilm, and inducing the intracellular calcium release, instead of impacting on the uptake and efflux of fluconazole. Our results suggest that the combination of fluconazole and minocycline can reduce the fluconazole resistance of C. albicans in vitro.
The plants of the Asteraceae family have been used for medicinal purposes,in traditional Colombian medicine.
To evaluate the antifungal activity and the cytotoxic effects of 15 essential oils from plants of the Asteraceae family.
Antifungal activity was evaluated against Candida parapsilosis ATCC 22019, Candida krusei ATCC 6258, Aspergillus flavus ATCC 204304 and Aspergillus fumigatus ATCC 204305 following EUCAST and CLSI M38-A standard methods, for yeast and filamentous fungi, respectively. Cytotoxic effect was evaluated on Vero cell line by MTT assay.
The oils from the plants Achyrocline alata and Baccharislatifolia were the only ones active against A. fumigatus (GM-MIC=78.7 and 157.4 microg/ml, respectively). In contrast, there was no evidence of oils active against Candida species. In addition, these oils were not cytotoxic on Vero cells. The oils of A. alata and Baccharis latifolia could be candidates for disinfecting hospital environments and for inhibiting biofilm formation by A. fumigatus
The oils of A. alata and B. latifolia could be candidates for disinfecting hospital environments and for inhibiting biofilm formation by A. fumigatus.
Infections by opportunistic pathogenic fungi, especially Candida species, Cryptococcus neoformans, and Aspergillus fumigatus, are a serious medical problem in immunocompromised patients. Different classes of antimycotic drugs are available to treat fungal infections, but the pathogens can develop resistance to all these agents. A major mechanism of antifungal drug resistance is the overexpression of efflux pumps of the ABC transporter and major facilitator superfamilies, which confer resistance to many structurally and functionally unrelated toxic compounds. For some pathogenic fungi, like Candida albicans and Candida glabrata, the most important drug transporters, transcription factors controlling their expression, and mutations that cause the constitutive upregulation of the efflux pumps in drug-resistant clinical isolates have been identified. For other important pathogens comparatively little is known about the role of transporters in antimycotic resistance. This review summarizes our current knowledge about efflux pump-mediated drug resistance and its regulation in human-pathogenic fungi.
The potential of antifungal agents used as antimicrobial lock therapy (ALT) for the conservative management of catheter-related candidemia has not been fully defined. We sought to determine the antifungal effect of high-dose doxycycline (DOX), alone or in combination with standard concentrations of amphotericin B (AMB), caspofungin (CAS) or fluconazole (FLC), against biofilms formed by Candida albicans in vitro. DOX alone (at 2048 microg/mL and 1024 microg/mL) demonstrated up to an 85% reduction of the metabolic activity of the C. albicans biofilm. Regardless of the concentration tested, FLC alone showed minimal activity (mean 22.9% reduction) against the C. albicans biofilm. When DOX 2048 microg/mL was used in combination with FLC, antifungal activity also increased up to 85%, suggesting an additive effect. DOX 128 microg/mL in combination with FLC demonstrated synergy (mean 58.3% reduction). The combination of DOX 2048 microg/mL or 512 microg/mL and AMB was superior to AMB alone at low concentrations (0.25-0.03125 microg/mL). However, DOX 128 microg/mL was antagonistic in combination with low concentrations of AMB. Maximal efficacy against the biofilm was observed with CAS at 8-0.25 microg/mL compared with FLC and AMB alone. A paradoxical effect (PE) occurred with CAS at 16 microg/mL, which showed a marked reduction in antifungal activity compared with lower concentrations of CAS. CAS at 16 microg/mL in combination with either DOX 2048 microg/mL or 512 microg/mL resulted in attenuation of the PE. These findings suggest that a high-dose DOX-based ALT strategy in combination with traditional antifungal agents may be useful for the treatment of C. albicans biofilms.
The rattan stem of Fibraurea recisa Pierre. is known as an ethno-remedy commonly used for the treatment of various skin diseases by the minority Yao, Zhuang and Miao in Yunnan Province of China. The present study was designated to evaluate its antifungal activity, and to root out the antifungal substances from this ethical herb.
The in vitro antifungal assay was performed by agar diffusion test for extracts and fractions. Then, the active fractions were submitted to column chromatography on silica gel and LH-20 to isolate their compounds. And the antifungal activity of pure compounds has been examined by checkerboard microdilution test. Nine Candida strains and one Cryptococcus strain were used for the bioassay.
The MeOH extract exhibited significant antifungal activity, and the alkaloidal fractions were deduced as main active component. Subsequent studies led to the identification of a new alkaloid fibrecisine (1) and 21 known alkaloids including berberines, tetrahydroberberines and aporphine derivatives. The bioassay result indicated that the berberines showed more potent activity than aporphine derivatives against the test Candida strains, while tetrahydroberberines showed very weak activity against Cryptococcus neoformans.
The new alkaloid fibrecisine (1) was identified as 1,2-methylenedioxy-8-hydroxy-6a(R)-aporphine by detailed spectral analysis. The rattan stem of Fibraurea recisa Pierre. is an effective antifungal herb, and its major active component is alkaloidal compounds. Bioassay tests revealed that the water-soluble berberines are the most important antifungal substances. The study provides preliminary scientific validation for the traditional medicinal use of this ethno-remedy.
We report a full account of our work toward the total synthesis of pseudolaric acid B (1a), a diterpene acid isolated from the bark of Pseudolarix kaempferi Gordon (pinaceae). Compound 1a is an antifungal and antifertility agent. Furthermore, its capacity for inhibiting tubulin polymerization makes it a potential lead for cancer therapy. Herein, we describe the use of a Ru- or Rh-catalyzed [5 + 2] intramolecular cycloaddition reaction of an alkyne and a vinylcyclopropane for the construction of the polyhydroazulene core of the molecule. Our first unsuccessful strategy for the introduction of the quaternary center based on an epoxide opening with cyanide led to the discovery of a new TBAF-mediated isomerization of a 1,4-diene to a 1,3-diene and a vinylogous eliminative opening of an epoxide to form a dienol. Our second strategy, based on the cyclization of an alkoxycarbonyl radical upon a diene system, succeeded in forming the quaternary center. Detailed studies showed the dependence of this underutilized approach for the synthesis of lactones on substrate structure and reaction conditions. In the late stage of the synthesis, the unique capacity of cerium organometallic reagents to add to a sensitive, sterically hindered ketone was demonstrated. The easy formation of an oxo-bridged derivative was the major hurdle to the completion of the synthesis and showcased the intriguing reactivity of the complex core of the pseudolaric acids.
The rhizomes of Zingiber officinale (ginger) and Alpinia officinarum contain potent inhibitors against prostaglandin biosynthesizing enzyme (PG synthetase). Gingerols and diarylhepatanoids were identified as active compounds. Their possible mechanism of action which was deduced from the structures of active compounds indicated that the inhibitors would also be active against arachidonate 5-lipoxygenase, an enzyme of leukotriene (LT) biosynthesis. This was verified by testing their inhibitory effects on 5-lipoxygenase prepared from RBL-1 cells. A diarylheptanoid with catechol group was the most active compound against 5-lipoxygenase, while yakuchinone A was the most active against PG synthetase.
Pseudolaric acid B [1] was isolated and identified as the main antifungal constituent of Pseudolarix kaempferi using bioassay-directed fractionation. Pseudolaric acid B was active against Trichophyton mentagrophytes, Torulopsis petrophilum, Microsporum gypseum, and Candida spp., while its methylated or hydrolyzed derivatives were not active against these same organisms. The minimum inhibitory concentrations and minimum fungicidal concentrations of pseudolaric acid B [1] against Candida and Torulopsis species were comparable with those of amphotericin B. The in vivo activity of pseudolaric acid B was evaluated in a murine model of disseminated candidiasis. Pseudolaric acid B [1] reduced the number of recovered colony-forming units significantly at different dosages. Infected mice treated intravenously with pseudolaric acid B [1] also had a longer survival time than those treated with vehicle alone.
Genetic manipulation of Candida albicans is constrained by its diploid genome and asexual life cycle. Recessive mutations are not expressed when heterozygous and undesired mutations introduced in the course of random mutagenesis cannot be removed by genetic back-crossing. To circumvent these problems, we developed a genotypic screen that permitted identification of a heterozygous recessive mutation at the URA3 locus. The mutation was introduced by targeted mutagenesis, homologous integration of transforming DNA, to avoid introduction of extraneous mutations. The ura3 mutation was rendered homozygous by a second round of transformation resulting in a Ura- strain otherwise isogenic with the parental clinical isolate. Subsequent mutation of the Ura- strain was achieved by targeted mutagenesis using the URA3 gene as a selectable marker. URA3 selection was used repeatedly for the sequential introduction of mutations by flanking the URA3 gene with direct repeats of the Salmonella typhimurium hisG gene. Spontaneous intrachromosomal recombination between the flanking repeats excised the URA3 gene restoring a Ura- phenotype. These Ura- segregants were selected on 5-fluoroorotic acid-containing medium and used in the next round of mutagenesis. To permit the physical mapping of disrupted genes, the 18-bp recognition sequence of the endonuclease I-SceI was incorporated into the hisG repeats. Site-specific cleavage of the chromosome with I-SceI revealed the position of the integrated sequences.
A new prenylated flavonol, sophoflavescenol (1), together with five known flavonoids, kurarinol, kushenol K, kushenol H, trifolirhizin, and kuraidin, were isolated from the roots of Sophora flavescens. The structure of 1 was determined by spectroscopic analysis. Among the five known flavonoids, kurarinol, kushenol K, and kushenol H showed weak antiviral activity against Herpes simplex virus types I and II.
A new prenylated flavanone was isolated from the roots of Sophora flavescens. The structure of the new compound was elucidated as (2S)-7,4'-dihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone (1) on the basis of chemical and spectral evidence.
Antimicrobial activity of the 18 prenylated flavonoids, which were purified from five different medicinal plants, was evaluated by determination of MIC using the broth microdilution methods against four bacterial and two fungal microorganisms (Candida albicans, Saccaromyces cerevisiae, Escherichia coli, Salmonella typhimurium, Staphylococcus epidermis and S. aureus). Papyriflavonol A, kuraridin, sophoraflavanone D and sophoraisoflavanone A exhibited a good antifungal activity with strong antibacterial activity. Kuwanon C, mulberrofuran G, albanol B, kenusanone A and sophoraflavanone G showed strong antibacterial activity with 5-30 microg/ml of MICs. Morusin, sanggenon B and D, kazinol B, kurarinone, kenusanone C and isosophoranone were effective to only gram positive bacteria, and broussochalcone A was effective to C. albicans. IC50 values of papyriflavonol A, kuraridin, sophoraflavanone D, sophoraisoflavanone A and broussochalcone A in HepG2 cells were 20.9, 37.8, 39.1, 22.1, and 22.0 microg/ml, respectively. These results support the use of prenylated flavonoids in Asian traditional medicine to treat microbial infection and indicate a high potential for prenylated flavonoids as antimicrobial agents as well as anti-inflammatory agents.
Two benzoic acid allopyranosides, pseudolaroside A and pseudolaroside B, along with seven known compounds were isolated from the bark of Pseudolarix kaempferi. Their structures were determined by analysis of HR-ESI-MS, 1D and 2D NMR spectroscopic data, chemical analysis and comparison to the literature data.
We report the enantioselective synthesis of pseudolaric acid B (1a), a diterpene acid isolated from the bark of Pseudolarix kaempferi Gordon, which displays interesting antifungal, antifertility, and cytotoxic activity against multidrug resistant cell lines. Our synthesis utilizes a highly efficient metal-catalyzed [5 + 2] vinylcyclopropane-alkyne intramolecular cycloaddition to construct the polyhydroazulene core of the natural product. Elaboration to the tricyclic scaffold of the pseudolaric acids was completed with an intramolecular alkoxycarbonyl radical cyclization to form the quaternary center and a highly diastereoselective cerium acetylide addition to a methyl ketone for introduction of the acid side chain.
The in vitro antifungal activities of 19 structurally diversified analogues of pseudolaric acids tested against the major pathogenic fungus Candida albicans has led to the establishment of a very clear structure-activity relationship of pseudolaric acids derivatives. Pseudolaric acid A was first found to be a potent antifungal component comparable with pseudolaric acid B. Among the tested 19 diterpenoids, pseudolaric acids A2 (1), B2 (3), B3 (4) and methyl pseudolarate A2 (2) are new isolates of the root bark of Pseudolarix kaempferi, and their structures were elucidated mainly by 2D-NMR techniques and chemical methods. Compounds 12-19 were first semi-synthesized by efficient routines from pseudolaric acid B.
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- Yang
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Isolation and identification of an antifungal component pogostone from Traditional Chinese Medicinal plant Pogostemon cablin (Blanco) Benth
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