Review of Garcinia mangostana and its Xanthones in Metabolic Syndrome and Related Complications

Metabolic syndrome is coexistence of abdominal obesity, hyperglycemia, hyperlipidemia and hypertension that causes cardiovascular diseases, diabetes and their complications, low quality and short lifespan. Garcinia mangostana and its xanthones such as α‐mangostin have been shown desirable effects such as anti‐obesity, anti‐hyperglycemic, anti‐dyslipidemia, anti‐diabetic and antiinflammatory effects in experimental studies. Various databases such as PubMed, Scopus and Web of Science with keywords of ‘Garcinia mangostana’, ‘mangosteen’, ‘α‐mangostin’, ‘metabolic syndrome’, ‘hypoglycemic’, ‘antihyperglicemic’, ‘antidiabetic’, ‘hypotensive’, ‘antihypertensive’, ‘atherosclerosis’, ‘arteriosclerosis’ and ‘hyperlipidemia’ have been investigated in this search without publication time limitation. This study reviewed all pharmacological effects and molecular pathways of G. mangostana and its xanthones in the management of metabolic syndrome and its complications in in‐vitro and in‐vivo studies. Based on these studies, mangosteen and its xanthones have good potential to design human studies for controlling and modification of metabolic syndrome and its related disorders such as obesity, disrupted lipid profile, diabetes and its complications. Copyright © 2017 John Wiley & Sons, Ltd.     

In vivo Antimalarial Activity of α‐Mangostin and the New Xanthone δ‐Mangostin

Based on the previously reported in vitro antiplasmodial activity of several xanthones from Garcinia mangostana, two xanthones, α‐mangostin and a new compound, δ‐mangostin, were isolated from mangosteen husk, and the in vitro antiplasmodial and cytotoxic effects were determined. α‐Mangostin was more active against the resistant Plasmodium falciparum chloroquine‐resistant (FCR3) strain (IC₅₀ = 0.2 ± 0.01 μM) than δ‐mangostin (IC₅₀ = 121.2 ± 1.0 μM). Furthermore, the therapeutic response according to the administration route was evaluated in a Plasmodium berghei malarial murine model. The greatest therapeutic response was obtained with intraperitoneal administration; these xanthones reduced parasitemia by approximately 80% with a daily dose of 100 mg/kg administered twice a day for 7 days of treatment. Neither compound was effective by oral administration. Noticeable toxicological effects were not observed. In addition to the antimalarial effect of these xanthones isolated from G. mangostana husk, the availability of larger amounts of husk raw material to purify the bioactive xanthones is advantageous, permitting additional preclinical assays or chemical transformations to enhance the biological activity of these substances. Copyright © 2015 John Wiley & Sons, Ltd.     

Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity

Twelve xanthone constituents of the botanical dietary supplement mangosteen (the pericarp of Garcinia mangostana) were screened using a noncellular, enzyme-based microsomal aromatase inhibition assay. Of these compounds, garcinone D (3), garcinone E (5), alpha-mangostin (8), and gamma-mangostin (9) exhibited dose-dependent inhibitory activity. In a follow-up cell-based assay using SK-BR-3 breast cancer cells that express high levels of aromatase, the most potent of these four xanthones was gamma-mangostin (9). Because xanthones may be consumed in substantial amounts from commercially available mangosteen products, the consequences of frequent intake of mangosteen botanical dietary supplements require further investigation to determine their possible role in breast cancer chemoprevention.     

Genome-wide biological response fingerprinting (BioReF) of the Chinese botanical formulation ISF-1 enables the selection of multiple marker genes as a potential metric for quality control

Quality control plays a critical role in the process of translating the traditional/alternative medicines into modern evidence-based therapies. High performance liquid chromatography (HPLC) is widely applied to assess the chemical composition of botanical drug products. The chromatographic fingerprints or chemical profiles are currently used as the de facto quality control metric. As a complement to chemical profiles, a biological quality control assessment offers distinct advantages. This study describes a genome-wide biological response fingerprinting (BioReF) approach to define a set of marker genes that define a signature pattern for a specific botanical formulation. These marker genes are chosen on the basis of the levels of the regulated expression and the involvement in the cellular signaling pathways. Subsequently, qRT-PCR technique is used to simultaneously monitor the gene expression of multiple marker genes in an efficient and quantitative manner. This set of marker genes represents the biological responses of human cells to the chemical composition of the botanical drug that could serve as potential quality control of botanical drugs in terms of the consistency of biological activities. We demonstrate the BioReF approach with a well-documented Chinese Medicine formula, designated as ISF-1, traditionally used for the management of post-stroke disorders. A set of nine marker genes were selected to assess the batch-to-batch consistency of the biological effects of ISF-1. This approach provides a potential comprehensive and cost-effective quality control metric of the biological activities of botanical drugs.     

龙胆化学成分、生物活性及临床应用研究进展

龙胆Gentianae Radix et Rhizoma具有清热燥湿、泻肝胆火的功效。龙胆主要含有环烯醚萜类、三萜类、（口山）酮类及黄酮类等化学成分，具有抗炎镇痛、保肝、抗肿瘤、调节胃肠功能、调节神经系统等作用，临床上广泛应用于带状疱疹、高血压、突发性耳聋及各类炎症性疾病。通过对龙胆的化学成分、生物活性和临床应用进行综述，为其进一步开发和应用提供理论参考和科学依据。     

The development of USP botanical dietary supplement monographs, 1995-2005

The development of USP botanical dietary supplement monographs by the Subcommittee on Natural Products (1995-2000) and the Dietary Supplements-Botanicals Committee of Experts (2000-2005) of the USP is described in this review. Featured details include the USP as an organization, focusing upon its history, mission, and publication of the United States Pharmacopeia-National Formulary (USP-NF); the formulation and composition of botanical dietary supplement monographs and related general chapters, as well as appropriate admission criteria; and a summary of the accomplishments of the Committees (1995-2005).     

潺槁树的研究进展

潺槁树Litsea glutinosa系樟科(Lauraceae)木姜子属Litsea Lam.植物,主要分布于热带和亚热带地区。潺槁树在我国为民间常用药物,具有治疗糖尿病、抗炎、抗菌等多种药理活性。目前从潺槁树中分离得到黄酮类、生物碱、木脂素类等50余种成分,其中生物碱类成分为其特征性成分。首次综述潺槁树的化学成分及其药理活性的研究进展,潺槁树药理活性显著,但鲜见对其作用机制的研究。随着现代分离分析技术及分子生物学技术的飞速发展,潺槁树药理活性及其作用机制研究将是今后研究的主要方向。     

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??Botanical Drug Development Guidance for Industry, replaced the Guidance for Industry on Botanical Drug Products issued in June 2004, was issued at December 2016. With the understanding and experience acquired in the reviews of NDAs and INDs for botanical drugs, specific recommendations have been modified and new sections have been added in this new edition. Compared new version with the old, ??loose requirement?? policy in early IND on consideration of prior human experience of botanical products was unchanged, but the requirements of quality and the rapeutic consistency on botanical raw material, drug substance and finished product in late-phase development and NDA submission for botanical drugs was very strict, especially, requirement to ensure that different marketing batches, with their variations, have the therapeutic effect consistent with those of the batches used in the phase 3 clinical studies. The new analytical methods, such as??totality of the evidence?? approach, biological assays, mass balance of all ingredients, multiple batch analyses and dose-response effect, were introduced to ensure the quality and therapeutic consistency. The manufacturing of botanical drug substance should be in compliance with both GACP and CGMPs may be warranted to cover the way in which the botanical raw material is grown, collected, processed and stored.     

藤黄化学生物学研究进展

该综述通过对藤黄抗肿瘤药用历史的回顾、研究现状的总结,以及笔者课题组近年来的若干发现,探讨了藤黄化学生物学研究中3个关键科学问题,包括藤黄中有哪些化学成分,藤黄中的化学成分通过什么方式作用于肿瘤细胞,生物机体通过什么途径处置藤黄中的化学成分.此外,笔者还将在该综述中对以藤黄中主要化学成分为先导化合物的抗肿瘤新药开发前景提出一些思考和建议.     

Biological Properties and Therapeutic Applications of Propolis

Propolis is a resinous material collected by bees from bud and exudates of the plants, mixed with bee enzymes, pollen and wax. In this review, the biological properties of propolis and some therapeutic applications are discussed. The same biological activities have been investigated until today, using samples from different geographic regions. Thus, the study of the biological properties of a given sample should always be associated with its chemical composition and botanical source, representing a particular sample of a given geographic area, exploring its biological potential and the role of its constituents. Efforts have been carried out to explain propolis' mechanisms of action in vivo and in vitro, but the majority of propolis' targets and actions are still unclear. The number of formulations containing propolis and patents have increased, although propolis extracts have been used deliberately with different recommendations, not always mentioning the chemical composition, vegetal source and the methods of extraction. Clinical studies will help to obtain criterious recommendations in view of the expected outcomes. Further investigation should explore the effects of common compounds found in the samples from all over the world in an attempt to standardize the research on propolis and to obtain new drugs. Copyright © 2016 John Wiley & Sons, Ltd.     

美国《植物药指南》和植物药发展简介

药物的定义在中美之间有很大差别。众多中药产品用来治病救人在中国早已习以为常,但美国则把中药当食品或膳食补充剂来监管,且在销售时不能标明有任何药用作用。美国食品药品监督管理局FDA的《植物药指南》为中药和其他草药未经纯化就能进入临床试验成为处方新药铺平了道路。《植物药指南》中允许推迟减免一些毒理实验以及让相对安全的中药直接进入二期临床试验。通过原药材种植采收及加工工艺来保证药品批次间的一致性也是《指南》的基本精神之一。2016年,修改版的《指南》还增加了用生物活性检测及多批次多剂量的临床试验来验证或保证质量控制的合理性等内容。借用中药的使用经验来研究中药或其有效组分之间的协同或加作用,有望成为中药以植物处方药走向世界的突破口。同时,数百获批进行临床试验的植物药品种只有Veregen和Fylyzaq（Mytesi）两个植物药上市,也说明把中药开发成为与新分子实体（NewMoleculeEntity）和新化学实体（NewChemicalEntity）一样在多国上市的植物新药面临挑战。可以说,中药产品成为植物新药会是持久战,不宜急功近利。青蒿片剂能否经得起进一步的临床验证而与复方蒿甲醚"(Coartem)媲美,还需拭目以待。     

Review of the Botanical Characteristics,Phytochemistry, and Pharmacology of Astragalus membranaceus (Huangqi)

Astragalus membranaceus is one of the most widely used traditional Chinese herbal medicines. It is used as immune stimulant, tonic, antioxidant, hepatoprotectant, diuretic, antidiabetic, anticancer, and expectorant. The current paper reviews the botanical characteristics, phytochemistry, and pharmacology of Astragali Radix. Information on Astragali Radix was gathered via the Internet (using Google Scholar, Baidu Scholar, Elsevier, ACS, Medline Plus, CNKI, and Web of Science) as well as from libraries and local books. More than 100 compounds, including flavonoids, saponins, polysaccharides, and amino acids, have so far been identified, and the various biological activities of the compounds have been reported. As an important traditional Chinese medicine, further studies on Astragali Radix can lead to the development of new drugs and therapies for various diseases. The improvement of its utilization should be studied further. Copyright © 2014 John Wiley & Sons, Ltd.     

Nardostachys chinensis Batalin: A review of traditional uses,phytochemistry, and pharmacology

Nardostachys chinensis Batalin (Valerianaceae) has been widely used in different traditional systems of medicine, including Islamic, Ayurvedic, Chinese, and Korean folk medicine. It has been used in traditional medicine as a tranquilizer, hepatotonic, cardiotonic, diuretic, and analgesic. Preliminary in vitro and in vivo studies have provided valuable scientific evidence for its traditional uses. This review aims to summarize reported traditional uses, phytochemistry, and pharmacological potential of N. chinensis while identifying potential areas of further research of plant. The review comprises literature pertaining to the pharmacological potential and phytochemistry of N. chinensis using worldwide accepted scientific databases via electronic search (Elsevier, Google Scholar, Pub Med, Scopus, Springer, Wiley online library). Moreover, data from ethno botanical text books available in library and electronic search were also included. The Plant List and Kew Herbarium Catalogue databases were used to authenticate the scientific name. Different pharmacological experiments in many in vitro and in vivo models have proved the potential of N. chinensis, namely, anti‐inflammatory, anticonvulsant, antibacterial, antihypertensive, antifungal, neuroprotective, cardioprotective, aldose reductase inhibition, and antioxidant activities. The plant contains sesquiterpenenes of various varieties including aristolane, guaiane, and nardosinane types. Moreover, it also contains coumarins, phenols, lignans, neolignans, and glycosides. Reported activities suggested that there may be pharmacological potential for developing N. chinensis as a drug for infections, hypertension, cardiac diseases, Alzheimer's disease, insomnia, epilepsy, cancer, gastric, and liver diseases. More toxicological studies should be performed that will aid the progress to clinical trial studies of N. chinensis.     

Antidiabetic Effects of Simple Phenolic Acids: A Comprehensive Review

Diabetes mellitus (DM) has become a major public health threat across the globe. Current antidiabetic therapies are based on synthetic drugs that very often have side effects. It has been widely acknowledged that diet plays an important role in the management of diabetes. Phenolic acids are widely found in daily foods such as fruits, vegetables, cereals, legumes, and wine and they provide biological, medicinal, and health properties. Simple phenolic acids have been shown to increase glucose uptake and glycogen synthesis, improve glucose and lipid profiles of certain diseases (obesity, cardiovascular diseases, DM, and its complication). The current review is an attempt to list out the antidiabetic effects of simple phenolic acids from medicinal plants and botanical foods. Copyright © 2015 John Wiley & Sons, Ltd.     

A review of Neuropharmacology Effects of Nigella sativa and Its Main Component,Thymoquinone

Neuropharmacology is the scientific study of drug effect on nervous system. In the last few years, different natural plants and their active constituents have been used in neurological therapy. The availability, lower price, and less toxic effects of herbal medicines compared with synthetic agents make them as simple and excellent choice in the treatment of nervous diseases. Nigella sativa, which belongs to the botanical family of Ranunculaceae, is a widely used medicinal plant all over the world. In traditional and modern medicines several beneficial properties have been attributed to N. sativa and its main component, thymoquinone (TQ). In this review, various studies in scientific databases regarding the neuropharmacological aspects of N. sativa and TQ have been introduced. Results of these studies showed that N. sativa and TQ have several properties including anticonvulsant, antidepressant, anxiolytic, anti‐ischemic, analgesic, antipsychotic, and memory enhancer. Furthermore, its protective effects against neurodegenerative diseases such as Alzheimer, Parkinson and multiple sclerosis have been discussed. Although there are many studies indicating the beneficial actions of this plant in nervous system, the number of research projects relating to the human reports is rare. Copyright © 2016 John Wiley & Sons, Ltd.     

Advances in Isolation and Synthesis of Xanthone Derivatives

Xanthone and its derivatives occupy a large part of the family of natural polyphenolic compounds with various biological and pharmacological activities.In recent years(from 2006 to 2011),it was reported that 127 xanthones were discovered from plants and fungi using various modern separation methods including silica gel/polyamide column chromatography,HPLC,high-speed counter-current chromatography,high-performance centrifugal partition chromatography,etc.Since total synthesis and structure modification for xanthone and its derivatives have been given attention worldwide,we introduced the synthetic methods of xanthone skeletons as well.Unfortunately,to date,there are still weaknesses in current methods of separation and synthesis,which need to be improved.This review,to a certain extent,provides necessary foundation for the further research and development of medicines containing xanthone and its derivatives.     

Pharmacognosy,Phytochemistry and Pharmacological Properties of Achillea millefolium L.: A Review

Achillea millefoilum L. (Yarrow) is an important species of Asteraceae family with common utilization in traditional medicine of several cultures from Europe to Asia for the treatment of spasmodic gastrointestinal disorders, hepatobiliary, gynecological disorders, against inflammation and for wound healing. An extensive review of literature was made on A. millefoilum L. using ethno botanical text books, published articles in peer‐reviewed journals, unpublished materials and scientific databases. The Plant List, International Plant Name Index and Kew Botanical Garden databases were used to authenticate the scientific names. Monoterpenes are the most representative metabolites constituting 90% of the essential oils in relation to the sesquiterpenes, and a wide range of chemical compounds have also been reported. Different pharmacological experiments in many in‐vitro and in‐vivo models have proved the potential of A. millefoilum with antiinflammatory, antiulcer, anticancer activities etc. lending support to the rationale behind numerous of its traditional uses. Due to the noteworthy pharmacological activities, A. millefoilum will be a better option for new drug discovery. The present review will comprehensively summarize the pharmacognosy, phytochemistry and ethnopharmacology of A. millefoilum reported to date, with emphasis on more in vitro, clinical and pathological studies needed to investigate the unexploited potential of this plant. Copyright © 2017 John Wiley & Sons, Ltd.     

药用植物功能基因的研究思路与展望——以甘草为例

近些年来有关功能基因的研究已成为药用植物研究领域的热点,研究内容涉及基因克隆、功能鉴定、多态性分析、表达模式分析以及功能基因与代谢途径的相关性分析等诸多方面。甘草是我国最常用的大宗药材之一,其主要活性成分为甘草酸,具有多种药理功能,在国内外市场上应用广泛。本文以甘草为例,对甘草酸代谢途径中已报道的功能基因进行调查研究,在基因克隆、基因功能、基因多态性等方面进行分析,以期为揭示甘草酸合成代谢的分子机制奠定基础,并为其他药用植物功能基因的研究提供思路。     

知母宁在神经退行性疾病中作用机制的研究进展

知母宁是一种具有C-糖苷和氧杂蒽酮成分的天然化合物,具有抗氧化、抗炎性损伤、提高线粒体生物能量和改善认知缺陷等多种生物活性,可以通过血脑屏障在中枢神经系统中发挥神经保护作用。对知母宁在神经退行性疾病中的作用及机制研究进展进行综述,以此探究其发挥神经保护作用的潜在分子机制,为其进一步的研究和应用提供参考。     

中药品质生物评价的历史与发展

生物评价(biological assay)是药品质量控制的重要方法,由于中药成分的复杂性、功效的多样性特点,依靠化学成分理化分析的方法对中药进行品质评价还存在很大的局限性。近年来中药品质的生物评价日益得到广泛关注与应用。从中药历史发展的角度来看,中药品质生物评价的理念和方法自古有之,尤其是近年来我国CFDA及美国FDA强调了生物评价在中药或植物药新药注册与评审中的重要作用及意义,这标志着生物评价已成为国内外中药和植物药质量评控发展的共识性方向,当前正进入中药品质的生物评价时代。从回顾历史与展望发展的视角,对中药品质的生物评价进行了系统地梳理与总结,提出了以生物评价为核心的"中药整合质量观"。