散沫花化学成分和生物活性研究进展

散沫花Lawsonia inermis,千屈菜科Lythtaceae散沫花属植物,其叶、花、果实、种子都可以作为传统中药使用.现代研究发现散沫花含有醌、苯丙素、黄酮、三萜、酚酸和脂肪酸等多种类型的化合物,并具有抗菌、抗肿瘤、抗氧化、抗寄生虫等广泛的药理活性,有很大的开发利用价值,因此受到各国学者的广泛关注.该文对散沫花的化学成分、生物活性及其应用的研究进展进行了综述,为其深入的开发研究提供参考.     

Helichrysum italicum: From traditional use to scientific data

Ethnopharmacological relevance

Helichrysum italicum (Roth) G. Don fil. (family Asteraceae) has been used for its medicinal properties for a long time and, even nowadays, continues to play an important role in the traditional medicine of Mediterranean countries. Based on this traditional knowledge, its different pharmacological activities have been the focus of active research. This review aims to provide an overview of the current state of knowledge of the pharmacological activities of Helichrysum italicum, as well as its traditional uses, toxicity, drug interactions and safety.

Materials and methods

The selection of relevant data was made through a search using the keywords “Helichrysum italicum” and “H. italicum” in “Directory of Open Access Journals”, “Google Scholar”, “ISI Web of Knowledge”, “PubMed”, “ScienceDirect” and “Wiley Online Library”. Information obtained in local and foreign books and other sources was also included.

Results

There are reports on the traditional use of Helichrysum italicum in European countries, particularly Italy, Spain, Portugal and Bosnia and Herzegovina. In these countries, its flowers and leaves are the most used parts in the treatment of health disorders such as allergies, colds, cough, skin, liver and gallbladder disorders, inflammation, infections and sleeplessness. In order to validate some of the traditional uses of Helichrysum italicum and highlight other potential applications for its extracts and isolated compounds, several scientific studies have been conducted in the last decades. In vitro studies characterized Helichrysum italicum as an antimicrobial and anti-inflammatory agent. Its flavonoids and terpenes were effective against bacteria (e.g. Staphylococcus aureus), its acetophenones, phloroglucinols and terpenoids displayed antifungal action against Candida albicans and its flavonoids and phloroglucinols inhibited HSV and HIV, respectively. Helichrysum italicum acetophenones, flavonoids and phloroglucinols demonstrated inhibitory action in different pathways of arachidonic acid metabolism and other pro-inflammatory mediators. Regarding Helichrysum italicum in vivo activity, the highlight goes to the anti-erythematous and photoprotective activities of its flavonoids, demonstrated both in animals and humans, and to the anti-inflammatory properties exhibited by its flavonoids, acetophenones and phloroglucinols, as seen in animal models. Concerning its safety and adverse effects, while Helichrysum italicum does not display significant levels of cytotoxicity or genotoxicity, it should be noticed that one of its flavonoids inhibited some CYP isoforms and a case has been reported of an allergic reaction to its extracts.

Conclusions

Helichrysum italicum is a medicinal plant with promising pharmacological activities. However, most of its traditionally claimed applications are not yet scientifically proven. Clinical trials are needed to further confirm these data and promote Helichrysum italicum as an important tool in the treatment of several diseases.     

Identification of Escherichia coli enterotoxin inhibitors from traditional medicinal herbs by in silico, in vitro, and in vivo analyses

Ethnopharmacological relevance

Glycyrrhiza uralensis has been used for the treatment of gastrointestinal disorders, such as diarrhea, in several ancient cultures. Glycyrrhizin is the principal component of liquorice and lots of pharmacological effects have been demonstrated.

Aim of the study

Heat-labile enterotoxin (LT), the virulence factor of enterotoxigenic Escherichia coli, induces diarrhea by initially binding to the G_M1 on the surfaces of intestinal epithelial cells and consequently leading to the massive loss of fluid and ions from cells. Therefore, we evaluated the inhibitory effects of traditional medicinal herbs (TMH) on the B subunit of LT (LTB) and G_M1 interaction.

Materials and methods

The inhibitory effects of TMH on LTB-G_M1 interaction were evaluated by G_M1-enzyme-linked immunosorbent assay (ELISA). The likely active phytochemicals of these TMH were then predicted by in silico model (docking) and analyzed by in vitro (G_M1-ELISA) and in vivo (patent mouse gut assay) models.

Results

We found that various TMH, which have been ethnomedically used for the treatment of diarrhea, inhibited the LTB-G_M1 interaction. Docking data showed that triterpenoids were the most active phytochemicals and the oleanane-type triterpenoids presented better LTB-binding abilities than other types of triterpenoids. Moreover, by in vitro and in vivo models, we demonstrated that glycyrrhizin was the most effective oleanane-type triterpenoid that significantly suppressed both the LTB-binding ability (IC₅₀ = 3.26 ± 0.17 mM) and the LT-induced fluid accumulation in mice.

Conclusions

We found an LT inhibitor, glycyrrhizin, from TMH by in silico, in vitro, and in vivo analyses.     

Rheum australe D. Don: a review of its botany, ethnobotany, phytochemistry and pharmacology

Ethnopharmacological relevance

Rheum australe D. Don (Polygonaceae) has been commonly used in traditional medicine for a wide range of ailments related to the circulatory, digestive, endocrine, respiratory and skeletal systems as well as to infectious diseases.

Aim of the review

To provide the up-to-date information that is available on the botany, traditional uses, phytochemistry, pharmacology and toxicology of Rheum australe. Additionally, to highlight the possible uses of this species to treat different diseases and to provide a basis for future research.

Materials and methods

The present review covers the literature available from 1980 to 2011. The information was collected from scientific journals, books, theses and reports via a library and electronic search (Google Scholar, Web of Science and ScienceDirect).

Results

Ethnomedical uses of Rheum australe have been recorded from China, India, Nepal and Pakistan for 57 different types of ailments. The phytochemical studies have shown the presence of many secondary metabolites belonging to anthraquinones, stilbenes, anthrones, oxantrone ethers and esters, chromones, flavonoids, carbohydrate, lignans, phenols and sterols. Crude extracts and isolated compounds from Rheum australe show a wide spectrum of pharmacological activities, such as antidiabetic, anti-inflammatory, antifungal, antimicrobial, antioxidant, anticancer, hepatoprotective and immune-enhancing activities, as well as a usefulness for improving renal function.

Conclusion

Rheum australe has been widely used source of medicine for years without any adverse effects. Many studies have provided evidence for various traditional uses. However, there is a need for additional studies of the isolated compounds to validate the traditional uses in human models. The present review on the botany, traditional uses, phytochemistry and toxicity has provided preliminary information for further studies and commercial exploitations of the plant.     

Senecio scandens Buch.-Ham.: A review on its ethnopharmacology,phytochemistry, pharmacology,and toxicity

Ethnopharmacological relevance

The aerial parts of Senecio scandens Buch.-Ham. (family Asteraceae) have a long history in traditional Chinese medicine as a treatment for various ailments, such as bacterial diarrhea, enteritis, conjunctivitis, and respiratory tract infections.

Materials and methods

A bibliographic investigation of Senecio scandens was accomplished by analyzing secondary sources, including the Chinese Medicinal plantal Classics, the Internet (Google Scholar and Baidu Scholar), and scientific databases accepted worldwide (Pubmed, Scopus, Web of Science, SciFinder, and CNKI). These sources were scrutinized for available information about the uses of Senecio scandens in traditional Chinese medicine, phytochemistry, pharmacology, and toxicology.

Results

Senecio scandens is a medicinal plant with a climbing woody stem. Phytochemical studies have shown the presence of numerous valuable compounds, such as flavonoids, alkaloids, phenolic acids, terpenes, volatile oils, carotenoids, and trace elements. Among them, PAs are the characteristic constituents, adonifoline is one of the index ingredients of Senecio scandens. Studies in modern pharmacology have demonstrated that extracts and compounds isolated from Senecio scandens show a wide spectrum of pharmacological activities, including anti-inflammatory, antimicrobial, anti-leptospirosis, hepatoprotective, anti-infusorial, antioxidant, antiviral, antitumoral, analgesic, mutagenic, and toxicological activities.

Conclusions

Phytochemical and pharmacological studies have demonstrated that the extracts of the plant possess various pharmacological activities that can be attributed to the presence of various flavonoids, phenolic acids, and alkaloids. Newer technologies for qualitative and quantitative methods of PAs need to be developed to obtain better accuracy and sensitivity. Due to the toxicity of PAs present in this medicinal plant, the regulations on PAs of Senecio scandens were varied among different countries and regions. In China, the PAs toxicity of Senecio scandens ranking criteria is not well defined in the Chinese Pharmacopoeia 2010, and there is no strict uniform requirement on the PAs in western countries. We propose that the use of Senecio scandens should be reevaluated based on a set of criteria, which includes risk–benefit analysis and severity of the toxic effects, clinical and preclinical data to ensure safe use while continuing to satisfy the need for access to the medicinal plant.     

Hypoxis (Hypoxidaceae) in African traditional medicine

Ethnopharmacological relevance

Hypoxis species (Hypoxidaceae) are popular medicinal plants used in the African traditional medicine to treat numerous ailments and are reported to have a wide spectrum of pharmacological properties. In this paper we reviewed and evaluated the traditional uses, pharmacological, phytochemistry and toxicity aspects of the genus Hypoxis. Potential medicinal prospects and possible knowledge gaps and pitfalls are discussed.

Materials and methods

A comprehensive and systematic review of literature on Hypoxis species was done using numerous resources such as books and scienti?c databases that include Pubmed, Scopus, Scirus, Google scholar, Web of Science and others. Information on the various pharmacological and chemical properties of Hypoxis extracts was critically analysed and discussed under the various topics.

Results

The literature indicated a broad range of uses, pharmacological and toxicological properties of different Hypoxis species extracts and their relevance to African healthcare systems. Several compounds, mostly glucosides, sterols and sterolins, have been isolated, identified and tested in various in vitro and in vivo models as well as in a couple of clinical trials with a lot of promising prospects reported in some studies.

Conclusion

A critical analysis of the available literature and studies identi?es positive potential for the future use of Hypoxis species in both traditional and modern medicine and concurrently so with possible pitfalls and research gaps in current knowledge. An integrated and holistic approach to addressing research issues, particularly toxicology aspects could be more effectively applied and incorporate conservation strategies for the species.     

Medicinal and therapeutic potential of Sea buckthorn (Hippophae rhamnoides L.)

Ethnopharmacological context

This review explores the medicinal and therapeutic applications of Sea buckthorn (Hippophae rhamnoides L.) in curtailing different types of acute as well as chronic maladies. The plant is being used in different parts of the world for its nutritional and medicinal properties.

Materials and methods

Sea buckthorn based preparations have been extensively exploited in folklore treatment of slow digestion, stomach malfunctioning, cardiovascular problems, liver injury, tendon and ligament injuries, skin diseases and ulcers. In the recent years, medicinal and pharmacological activities of Sea buckthorn have been well investigated using various in vitro and in vivo models as well as limited clinical trials.

Results

Sea buckthorn has been scientifically analyzed and many of its traditional uses have been established using several biochemical and pharmacological studies. Various pharmacological activities such as cytoprotective, anti-stress, immunomodulatory, hepatoprotective, radioprotective, anti-atherogenic, anti-tumor, anti-microbial and tissue regeneration have been reported.

Conclusion

It is clear that Sea buckthorn is an important plant because of its immense medicinal and therapeutic potential. However, several knowledge gaps identified in this paper would give impetus to new academic and R&;D activities especially for the development of Sea buckthorn based herbal medicine and nutraceuticals.     

Mycology,cultivation, traditional uses,phytochemistry and pharmacology of Wolfiporia cocos (Schwein.) Ryvarden et Gilb.: A review

Ethnopharmacological relevance

Wolfiporia cocos (Schwein.) Ryvarden et Gilb. has a long history as a Chinese traditional medicine with uses of inducing diuresis, excreting dampness, invigorating the spleen, and tranquilizing the mind. Recently, Wolfiporia cocos has received increasing interest, and phytochemical and pharmacological studies have validated the traditional uses of this species.

Aims of the review

To provide an up-to-date and comprehensive overview of the mycology, cultivation, traditional uses, chemical constituents and pharmacological activities aspects of Wolfiporia cocos in order to highlight its ethnopharmacological use and to explore its therapeutic potentials and to provide a basis for future research.

Materials and methods

The accessible literature, from 1980 to 2012, on Wolfiporia cocos written in English, Chinese, French, Korean, Spanish and Turkish were selected and analyzed.

Results

The phytochemical and modern pharmacological studies demonstrated that Wolfiporia cocos possess a wide spectrum of pharmacological activities, such as anti-tumor, anti-oxidant, anti-rejection, nematicidal, anti-hyperglycemic, antibacterial, anti-inflammatory and anti-hypertonic stress activities, which could be explained by the presence of various triterpenes and polysaccharides.

Conclusions

Modern phytochemical and pharmacological investigations showed that major active components separated from Wolfiporia cocos had anti-tumor, anti-oxidant, anti-rejection activities, and so on. Further investigations are needed to explore the relationship of the molecular mass, chain stiffness, and water solubility of polysaccharide from Wolfiporia cocos with the antitumor activities.     

列当属、肉苁蓉属和草苁蓉属植物传统药物学调查

通过野外资源调查、整理各大标本馆标本原始记录和查阅文献记载等方法,系统整理、总结、归纳了列当属、肉苁蓉属和草苁蓉属民族药用植物种类、功效及民间使用情况,结果表明列当属6种药用植物在4个少数民族间作为7种民族药应用,草苁蓉属2种药用植物在8个少数民族间作为10种民族药应用,肉苁蓉属2种药用植物在3个少数民族间作为3种民族药应用,且同种药用植物常作不同民族药;发现3属植物的传统疗效主要集中在补肾壮阳、止血和止痛3个方面,并且该传统疗效与现代药理研究结果基本吻合。因此深入研究植物种类丰富的列当属植物资源对缓解肉苁蓉植物资源匮乏局面和扩大药源具有积极意义。     

Antifungal activity and cytotoxicity of isolated compounds from leaves of Breonadia salicina

Ethnopharmacological relevance

Breonadia salicina is used traditionally to treat wounds, ulcers, fevers, headaches, and fungal infections. The aim of this study was to investigate the antifungal activity of the plant extract and compounds isolated there from.

Materials and Methods

Leaf extracts of Breonadia salicina were screened for antifungal activity against seven plant pathogens: Aspergillus niger, Aspergillus parasiticus, Colletotrichum gloeosporioides, Trichoderma harzianum, Penicillium expansum, Penicillium janthinellum and Fusarium oxysporum. Bioautography assay was used to determine the presence and number of antifungal compounds of the plant extracts. Bioassay-guided fractionation using column chromatography of the chloroform extract led to the isolation of four antifungal compounds. Nuclear Magnetic Resonance (NMR) spectroscopy, Mass Spectrometry (MS) and Electron Impact Mass Spectrometry (EIMS) were used for the identification of antifungal compounds. Cytotoxicity of the chloroform crude extract and isolated compounds was determined using the MTT (3-(4,5-dimethylthiazol)-2,5-diphenyl tetrazolium bromide) assay against Vero monkey kidney cells.

Results

Compound 1 was identified as ursolic acid, while compounds 2, 3 and 4 were not identified conclusively owing to the presence of mixtures of long chain fatty acids. Compounds 3 and 4 had good antifungal activity against Aspergillus parasiticus and Penicillium janthinellum with MIC values of 10 and 16 µg/ml respectively. Compound 2 and ursolic acid had some activity with MIC values ranging between 20 and 250 µg/ml. The crude extract was less toxic to the Vero cells (LC₅₀=82 µg/ml) than ursolic acid (LC₅₀=25 µg/ml). Compounds 2 and 3 were not toxic at the highest concentration tested (LC₅₀=200 µg/ml). Compound 4 was the most toxic to the cells with an LC₅₀ of 35 µg/ml.

Conclusions

The results support the traditional use of Breonadia salicina for antifungal applications, and demonstrate the potential value of developing antifungal compounds from plant natural products. Indications of toxicity should be evaluated at an early stage as the selectivity of the product in affecting fungi preferentially to plant or mammalian cells should be identified when assessing the potential usefulness of the product.     

百合科药用植物丫蕊花的研究进展

丫蕊花Ypsilandra thibetica是百合科丫蕊花属植物,以全草入药,具有清热解毒、散结等功效,主治瘰疬,小便不利等症,在民间应用较广泛。化学研究显示,甾体皂苷是丫蕊花的主要成分和有效成分。据作者统计,到目前为止从丫蕊花中共报道了51个甾体皂苷类化合物,包括螺甾烷和呋甾烷2种主要类型;药理实验及临床研究表明,丫蕊花具有抗肿瘤、缩宫止血及抗菌作用,尤其对多种妇科出血症的治疗有显著疗效。该文对国内外有关丫蕊花的植物学研究、品种鉴定、化学成分和药理活性等方面进展进行了详细的总结,并分析了丫蕊花作为中药重楼资源替代品的优势,同时探讨了今后研究的方向,以期为该药材的进一步研究提供有益参考,为今后的深入开发利用提供科学依据。     

Pharmacological effects and active phytoconstituents of Swietenia mahagoni: a review

The usage of Swietenia mahagoni, a popular medicinal plant in India and some African countries, dates back to ancient times for its curative properties in diseases like malaria, diabetes, and diarrhea. It is also used as an anti-pyretic, bitter tonic and astringent. Its pharmacological activities are being widely explored. Although many important groups of phytochemicals have been identified and isolated from various parts of the plant, most of these researches have been focused on seeds. Toxicological studies have established the safety of many of these plant extracts, and found insignificant side effects. Here we present a comprehensive review of all the pharmacological effects and constituent phytochemicals of the plant.     

Antiurolithic effect of Bergenia ligulata rhizome: An explanation of the underlying mechanisms

Ethnopharmacological relevance

Bergenia ligulata is widely used plant in South Asia, mainly India and Pakistan, as a traditional medicine for treatment of urolithiasis.

Aim of the study

To rationalize the Bergenia ligulata use in kidney stones and to explain the underlying mechanisms.

Materials and methods

The crude aqueous-methanolic extract of Bergenia ligulata rhizome (BLR) was studied using in vitro and in vivo methods.

Results

BLR inhibited calcium oxalate (CaC₂O₄) crystal aggregation as well as crystal formation in the metastable solutions and exhibited antioxidant effect against 1,1-diphenyl-2-picrylhydrazyl free radical and lipid peroxidation in the in vitro. BLR caused diuresis in rats accompanied by a saluretic effect. In an animal model of urolithiasis, developed in male Wistar rats by adding 0.75% ethylene glycol (EG) in drinking water, BLR (5–10 mg/kg) prevented CaC₂O₄ crystal deposition in the renal tubules. The lithogenic treatment caused polyuria, weight loss, impairment of renal function and oxidative stress, manifested as increased malondialdehyde and protein carbonyl contents, depleted reduced glutathione and decreased antioxidant enzyme activities of the kidneys, which were prevented by BLR. Unlike the untreated animals, EG intake did not cause excessive hyperoxaluria and hypocalciuria in BLR treated groups and there was a significant increase in the urinary Mg²⁺, instead of a slight decrease.

Conclusions

These data indicate the antiurolithic activity in Bergenia ligulata mediated possibly through CaC₂O₄ crystal inhibition, diuretic, hypermagneseuric and antioxidant effects and this study rationalizes its medicinal use in urolithiasis.     

紫堇属藏药的化学与药理学研究进展

我国有紫堇属植物约298种,其中特有10组219种,广泛用于藏医藏药。紫堇属藏药主要用于感冒发烧、肝炎、水肿、胃炎、胆囊炎、高血压等多种疾病。其化学成分主要为异喹啉生物碱。现代药理学研究表明紫堇属植物对心血管系统、中枢神经系统、抗菌、镇痛、抗炎、保肝、抗氧化等,皆有明显的作用。该文对我国紫堇属藏药的种属、分布、化学成分、药理活性等进行系统综述,并对其相关研究现状和前景进行了展望,以期为紫堇属藏药的深入研究和开发利用提供参考。     

樟科药用植物山鸡椒的化学成分和药理活性研究进展

山鸡椒是樟科木姜子属植物,其根、茎和果实均可入药,具有祛风散寒、理气止痛等功效,在民间应用广泛。该植物主要含有生物碱类,特别是阿朴啡生物碱,也含有少量的黄酮、木脂素及其他类成分。相关药理研究显示,山鸡椒在治疗心血管疾病、抗肿瘤、抗炎、提高免疫力、平喘抗过敏、抗氧化、抗菌、杀虫等多方面都有较好的效果。该文对山鸡椒的化学成分及药理活性进行了全面的归纳,以期对本种药用植物的综合研究和应用提供参考。     

Ethnobotany,phytochemistry and pharmacology of the genus Caragana used in traditional Chinese medicine

The genus Caragana is a member of the family Fabaceae, subfamily Faboideae and is native to arid and semi-arid areas of the temperate zones of Asia and Eastern Europe. Many species are cultured for dune-fixation, livestock forage and biological resources for fuel energy and fiber production. More than 10 species in this genus have a long history of use in traditional Chinese, Mongolian and Tibetan medicines and are believed to “nourish yin, invigorate the spleen, temper the blood and promote blood flow”. They have been used for the treatment of a wide range of ailments including fevers, inflammation, wounds and infections, dizziness, headache, hypertension, female disorders, arthritis and cancer. Over 100 phytochemicals have been identified with flavonoids and stilbenoids being the major constituents of this genus. Clinical studies have demonstrated the pharmacological activities of different Caraganum species, e.g. Caragana sinica for the treatment of hypertension, and in vivo and/or in vitro studies have provided some support for other traditional uses, e.g. anti-cancer, anti-inflammatory, phytoestrogenic, immunostimulant and immunosuppressant activities. However, further studies to identify the active components and further verify the pharmacological activities are warranted. This review presents a comprehensive analysis of the ethnobotany, phytochemistry and pharmacology of the genus Caragana.     

The genus Scutellaria an ethnopharmacological and phytochemical review

Scutellaria (HUANG QIN) (Lamiaceae), which includes about 350 species commonly known as skullcaps, is widespread in Europe, the United States and East Asia. Some species are taken to clear away the heat-evil and expel superficial evils in traditional Chinese medicine (TCM). The present paper reviews the ethnopharmacology, the biological activities and the correlated chemical compounds of Scutellaria species. More than 295 compounds have been isolated, among them flavonoids and diterpenes. Studies show that Scutellaria and its active principles possess wide pharmacological actions, such as antitumor, anti-angiogenesis, hepatoprotective, antioxidant, anticonvulsant, antibacterial and antiviral activities. Currently, effective monomeric compounds or active parts have been screened for pharmacological activity from Scutellaria in vivo and in vitro. Increasing data supports application and exploitation for new drug development.     

Hepatoprotective action of Orthosiphon diffusus (Benth.) methanol active fraction through antioxidant mechanisms: An in vivo and in vitro evaluation

Ethnopharmacological relevance

Preparations of Orthosiphon diffusus (Benth.) have been used by folk medicinal practitioners in the Western Ghats of India for treating inflammation, hepatitis and jaundice for many years and their effectiveness is widely acclaimed among the tribal communities.

Aim of the study

To evaluate the mechanisms behind the antioxidant and hepatoprotective potential of Orthosiphon diffusus methanol active fraction (MAF) using in vivo (rat) and in vitro (cell culture) models.

Materials and methods

Neutralization of CCl₄-induced hepatotoxicity by MAF was evaluated in rats. Towards this, serum levels of hepatic injury markers (lactate dehydrogenase and alkaline phosphatase), antioxidant enzymes in the liver homogenates, and histological examination were performed. In in vitro studies, mechanisms of neutralization of H₂O₂-induced toxicity by MAF using MTT, Comet assay and up-regulation of antioxidant enzymes at genetic level (RT-PCR) was performed in HepG2 cells.

Results

Rats pre-treated with Orthosiphon diffusus MAF demonstrated significantly reduced levels of serum LDH (1.3-fold, p<0.05) and ALP (1.6-fold, p<0.05). Similarly, multiple dose MAF administration demonstrated significantly enhanced levels (p<0.05) of antioxidant enzymes in the liver homogenates. Histological analysis revealed complete neutralization of CCl₄-induced liver injury by the extract. The in vitro studies demonstrated that, pre-treatment of MAF effectively prevented H₂O₂-induced oxidative stress, genotoxicity and significantly enhanced (~6-fold, p<0.01) expression of genes for antioxidant enzymes.

Conclusions

Orthosiphon diffusus MAF demonstrated significant hepatoprotection against CCl₄-induced hepatotoxicity by antioxidant mechanisms comparable to silymarin. H₂O₂-induced oxidative stress was completely neutralized by MAF through enhanced expression of genes for antioxidant enzymes. Therefore, this study validates the use of Orthosiphon diffusus by folk medicinal practitioners in India. Further, MAF of Orthosiphon diffusus can serve as a strong candidate for the development of herbal hepatoprotective agents.     

Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis

Aim of the study

Previously, we reported that the petroleum ether fraction, RC-1, and EtOAc fraction, RC-2, of the medicinal plant Rhus chinensis showed potent anti-HIV-1 activities. To address anti-HIV-1 constituents of RC-1 and RC-2, 17 compounds were isolated. Anti-HIV-1 activities and possible action mechanisms of these compounds were investigated.

Methods

The syncytial formation induced by HIV-1 was determined under the inverted microscope, cellular toxicity and protection assay were assessed by MTT method, reduction of p24 antigen expression level and RT activity were measured by ELISA, and inhibition of recombinant HIV-1 PR was monitored by the fluorescent signal.

Results

The compounds 1 and 13 inhibited HIV-1-induced syncytium formation potently with TI value of 42.31 and 19.07, respectively. Compounds 4, 5, 6, 9 and 10 were less potent with TI value of 8.94, 8.22, 4.14, 5.11 and 5.34, respectively. Compound 1, a benzofuranone-type compound, previously reported as a novel anti-HIV-1 agent, might target late-steps of HIV-1 life cycle. Compound 13 inhibited HIV-1 replication with EC₅₀ of 7.16 μg/ml and might target at/before integration step.

Conclusion

These compounds might contribute to anti-HIV-1 activities extracts of the medicinal plant Rhus chinensis.