Review of Rhubarbs: Chemistry and Pharmacology

Rhubarb is a perennial herb belonging to the genus Rheum L. (Polygonaceae). Rhei Radix et Rhizoma (rhubarb roots and rhizomes) is one of the most popular Chinese materia medica and has been widely used for strong laxative function. About 200 compounds with six different types of skeletons (anthraquinone, anthrone, stilbene, flavonoids, acylglucoside, and pyrone) have so far been isolated from eighteen species of the genus Rheum L. These constituents showed extensive pharmacological activities including cathartic, diuretic, anticancer, hepatoprotective, anti-inflammatory, and analgesic effects, as well as toxicological effects. Chemical fingerprint, LC-MS, and other analytical techniques have been used for the quality control of rhubarb. This comprehensive review summarizes the researches into the isolation, pharmacological activities, and phytochemical analysis reported since investigations began in the late 1940s. In addition, pharmacokinetic studies and clinical application of rhubarb are also discussed in present paper.     

Recent Advance in Chemical and Biological Studies on Cimicifugeae Pharmaceutical Resources

Cimicifugeae is one of the rich sources for various active components and the health promoting and therapeutic values of the components have been corroborated by long-term use in folk medicine and traditional Chinese medicine.Increasing interest in Cimicifugeae pharmaceutical resources has led to the further discoveries of triterpenoid saponins, phenolic compounds, chromones, and many other compounds in various species of Cimicifugeae, and to the investigations on their chemotaxonomy, molecular phylogeny, and bioactivities. Based on our pharmacophylogenetic studies, the progress in phytochemistry, chemotaxonomy, molecular biology, and phylogeny of Cimicifugeae had been summarized since 2007, especially Cimicifuga L. ex Wernisch. and Actaea L., and their relevance to therapeutic efficacy. An exhaustive literature survey is used to characterize the global scientific effort in the phytochemical and biological studies of Cimicifugeae. More triterpenoid saponins have been found in various species, among which the cimigenol type(type A) is predominant. The versatile bioactivities of saponins and extracts,as well as those of phenolics and other ingredients, were summarized and discussed. The morphology-based five-genus classification of Cimicifugeae is not supported by molecular phylogeny. Molecular phylogeny based on nuclear and chloroplast DNA sequences tends to merge Cimicifuga Wernisch., Souliea Franch., and Actaea L. into a single genus. It is indispensable to integrate the emerging technologies into Cimicifugeae research for both the sustainable utilization of Cimicifugeae pharmaceutical resources and finding novel compounds with potential clinical utility and less adverse effects. Systems biology and omics technologies would play an increasingly important role in booming pharmaceutical research involving bioactive compounds of Cimicifugeae.     

Phytochemicals and Their Biological Activities of Plants in Tagetes L.

Tagetes L.,the genus in the family Asteraceae,consists of about 30 species spread in South and Middle America as well as Mexico.More than one hundred secondary metabolites have been obtained in phytochemical investigation on the species,some of which have potent biological activities.The advances in phytochemical studies and biological activities of the plants in Tagetes L.from 1925 to 2011 are summarized in this paper.     

Pharmacophylogenetic Study on Plants of Genus Salvia L. from China

In China,many species of genus Salvia L.(Lamiaceae)are important medicinal plants with a long history.Due to their marked ethnopharmacological uses in folk medicine and a large number of active constituents with therapeutic potential found recently,they have become a rich source for new drug discovery,mechanism research,and biological experiment.All medicinal plants of Salvia L.could be divided into three groups(Groups 1,2,and 3).The plants in Group 1 were used as"Danshen"and are rich in diterpenoids and caffeic acid derivatives.Few introduced plants in Group 2 from America or Europe have been used to clear body-heat and toxins.Abietane diterpenes of medicinal species in Group 3(the species are from Subg.Allagospadonopsis Briq.,Sect.Plethiosphace,or Sect.Notiosphace)are absent,and the contents of caffeic acid derivatives are considerably lower than those in plants of Group 1.     

Network pharmacology in quality control of traditional Chinese medicines

Traditional Chinese medicine (TCM) has been widely used to treat and prevent diseases for thousands of years in China and is generally recognized for its unique holistic view and remarkable therapeutic effect on complex diseases. The worldwide interest to TCM has been increasing in recent years, especially since TCM has shown inspiring efficacy in the treatment of COVID-19. These attentions include both recognition of the important role of TCM and doubts about its efficacy and safety. At present, the internationalization and modernization of TCM are facing many challenges, such as unclear biological mechanism of herbs and formulae, and the difficulty of ensuring the quality and safety of TCM. Given the multi-component and multi-target characteristics of TCM, how to systematically describe the interaction between TCM and complex diseases, evaluate the efficacy and toxicity of TCM and carry out quality control has become the focus and difficulty of research. Network pharmacology, as a systematic and holistic medical research paradigm, can help to systematically reveal the biological basis of TCM, and has been widely used in the research of TCM bioactive ingredients, syndromes, formulae, and other topics. The concept of "network target" based on TCM research (Li et al., 2011) has been used to explore new methods and applications since its inception, leading to a new discipline of TCM network pharmacology (Li and Zhang, 2013). On the one hand, TCM network pharmacology research shows the tendency of combining computational, experimental and clinical approaches (Wang et al., 2021), and the research paradigm is improving continuously. On the other hand, the application of network pharmacology is expanding to a variety of aspects in TCM research. It has been applied in fields such as exploring the biological basic of disease and syndrome, uncovering the mechanism of TCM formulae, identifying toxic components and quality markers (Q-Marker) of traditional Chinese medicine and so on. The concept of Q-Marker which was proposed by Prof. Liu to standardize the quality research of TCM has established an effective research framework for the quality control of traditional Chinese medicine (Liu et al., 2017). Since it was proposed, Q-Marker has been utilized by researchers to analyze many TCM herbs and formulae, making an important contribution to the TCM quality control system. A previous research strategy of predicting and determining Q-Marker based on network pharmacology method (Wang et al, 2019) shows the potential of network pharmacology combined with Q-Marker in the application of quality control of TCM. The effectiveness and safety of TCM are taken into consideration when determining Q-Marker. There have been many successful application cases of network pharmacology in studying the effective ingredients and mechanism of TCM, and network pharmacology is also being used more and more frequently in the study of TCM toxicity. This issue will publish a research paper titled “Integrating systematic pharmacology-based strategy and experimental validation to explore mechanism of Tripterygium glycoside on cholangiocyte-related liver injury” on the use of network pharmacology to explore the toxic components of TCM and their underlying mechanisms. Tripterygium glycoside (TG) extracted from Tripterygium wilfordii have been used in clinical treatment of rheumatoid arthritis and other diseases, and there are several new indications under study. However, hepatotoxicity, the main adverse effect of TG in clinical practice, is an urgent problem to be solved. By combining network pharmacological analysis with in vivo and in vitro experimental verification, the authors discovered that triptolide, the primary toxic component of TG, could inhibit proliferation and promoted apoptosis of cholangiocytes by inhibiting the phosphorylation of ERK1/2 and AKT and activating Bax and cleaved-Caspase 3 signaling. This study is a typical example of using network pharmacology to predict the toxic components and mechanisms of TCM. At the same time, it also shows that network pharmacology can be combined with Q-Marker strategy to identify the toxicity Q-Marker of TCM, and aids in the quality control and standardization of traditional Chinese medicine. As a discipline that has been developed for a short period of time, there are still many challenges in the theory, methodology and application of network pharmacology. The quality control research of TCM using network pharmacology also needs more investigation and exploration. The publication of Network Pharmacology Evaluation Method Guidance in 2021 has positive implications for the standardization of network pharmacology research and promotes the healthy development of the discipline (Li, 2021). However, as the fields of network pharmacology research continues to expand, the guidance cannot cover all kinds of research and need to be updated and revised in time. With the combination with new technologies such as artificial intelligence high-throughput technologies, network pharmacology will undoubtedly develop at a high speed. We look forward to a wider application of network pharmacology in TCM research, which will provide new scientific evidence for deciphering the mysteries of TCM and thus promote the inheritance, innovation and development of TCM.     

Salvia miltiorrhiza: Traditional medicinal uses,chemistry, and pharmacology

Salvia miltiorrhiza Bunge(SM) is a very popular medicinal plant that has been extensively applied for many years to treat various diseases, especially coronary heart diseases and cerebrovascular diseases, either alone or in combination with other Chinese plant-based medicines. Although a large number of studies on SM have been performed, they are scattered across a variety of publications. The present review is an up-to-date summary of the published scientific information about the traditional uses, chemical constituents, pharmacological effects, side effects, and drug interactions with SM, in order to lay the foundation for further investigations and better utilization of SM. SM contains diverse chemical components including diterpenoid quinones, hydrophilic phenolic acids, and essential oils. Many pharmacological studies have been done on SM during the last 30 years, focusing on the cardiovascular and cerebrovascular effects, and the antioxidative, neuroprotective, antifibrotic, anti-inflammatory, and antineoplastic activities. The research results strongly support the notion that SM has beneficial therapeutic properties and has a potential of being an effective adaptogenic remedy.     

Words for Cover Figure

正Engelhardia plants were one of the main components for wild forestry resources in many Southeast Asia countries and have been used medicinally for hundreds of years.As national medicine and health tea,the region of using Engelhardia plants is not extensive,which cause not much attention.With various biological activities,genus Engelhardia might have considerable potential value for the development of new drugs.A total of over 100 compounds have been isolated from the genus Engelhardia,in     

Anticancer and multidrug-resistance reversing potential of traditional medicinal plants and their bioactive compounds in leukemia cell lines

Multidrug resistance remains a serious clinical problem in the successful therapy of malignant diseases. It occurs in cultured tumor cell lines, as well as in human cancers. Therefore, it is critical to develop novel anticancer drugs with multidrug-resistance modulating potential to increase the survival rate of leukemia patients. Plant-derived natural products have been used for the treatment of various diseases for thousands of years. This review summarizes the anticancer and multidrug-resistance reversing properties of the extracts and bioactive compounds from traditional medicinal plants in different leukemia cell lines. Further mechanistic studies will pave the road to establish the anticancer potential of plant-derived natural compounds.     

Natural alkaloids： basic aspects,biological roles,and future perspectives

Natural products have gained popularity worldwide for promoting healthcare, as well as disease prevention. Alka- loids are important chemical compounds that serve as a rich reservoir for drug discovery. Several alkaloids isolated from natural herbs exhibit antiproliferation, antibacterial, antiviral, insecticidal, and antimetastatic effects on various types of cancers both in vi- tro and in vivo. This paper focuses on the naturally-derived alkaloids such as berberine, matrine, piperine, fritillarine, and rhyn- chophylline, etc., and summarizes the action mechanisms of these compounds. Based on the information in the literature that is summarized in this paper, the use of alkaloids as drugs is very promising, but more research and clinical trials are necessary before final recommendations on specific alkaloids can be made. Following this, it is hoped that as a result of this review, there will be a greater awareness of the excellent promise that natural alkaloids show for use in the therapy of diseases.     

A Network Pharmacology Approach to Decipher the Mechanisms of Anti-depression of Xiaoyaosan Formula

Objective: Depression is one of the prevalent and prominent complex psychiatric diseases, and the number of depressed patients has been on the rise globally during the recent decades.Xiaoyaosan, as a famous Chinese herbal formula, has been widely used in depression patients for a long time.However, the therapeutic mechanisms remain uncertain because of the difficulty of depression pathophysiology and the lack of bioinformatic approach to understand the molecular connection.Materials and Methods: In this thesis, we applied a network pharmacology approach to explain the potential mechanisms between Xiaoyaosan and depression involved in oral bioavailability screening, drug-likeness assessment, caco-2 permeability, blood–brain barrier target recognition, and network analysis.Results: Sixty-six active compounds in Xiaoyaosan formula with favorable pharmacokinetic profiles are predicted as active compounds for antidepression treatment.Network analyses showed that these 66 compounds target 40 depression-associated proteins including especially HTR2A, NR3C1, monoamine oxidase inhibitor B, XDH, and CNR2.These proteins are mainly involved in the neuroactive ligand–receptor interaction, serotonergic synapse, cAMP signaling pathways, and calcium signaling pathways.Conclusion: The integrated network pharmacology method can provide a new approach for understanding the pathogenesis of depression and uncovering the molecular mechanisms of Xiaoyansan, which will also facilitate the application of traditional Chinese herbs in modern medicine.     

Chemical constituents of the aerial parts of six species of Bupleurum genus medicinally used in south-west region of China]

The chemical constituents of the aerial parts of six species of Bupleurum genus (B. kunmingense, B. polyclonum, B. wenchuanense, B. longicaule var. franchetii, B. rockii and B. chaishoui) medicinally used in south-west region of China have been investigated with the results of obtaining eight flavonoid compounds and six triterpenoid saponins. The aglycones of these eight flavonoid compounds are quercetin and isorhamnetin, which are different from the aglycones of the flavonoid compounds isolated from the aerial parts of B. chinense, the official species in Chinese Pharmacopoeia. In the latter case, the aglycone is kaempferol. This difference may be of chemotaxonomic value in Bupleurum genus.     

我国西南地区六种药用柴胡属植物地上部分的化学成分研究

对西南地区6种药用柴胡地上部分的化学成分进行了研究,得到8个黄酮和6个皂甙化合物。8个黄酮的甙元为槲皮素和异鼠李素,与北柴胡地上部分黄酮的甙元为山奈酚有所不同,可供柴胡属植物化学分类参考。     

Medicinal plants of the genus Macleaya (Macleaya cordata,Macleaya microcarpa): A review of their phytochemistry,pharmacology, and toxicology

In the genus Macleaya, Macleaya cordata and Macleaya microcarpa have been recognized as traditional herbs that are primarily distributed in China, North America, and Europe and have a long history of medicinal usage. These herbs have been long valued and studied for detumescence, detoxification, and insecticidal effect. This review aims to provide comprehensive information on botanical, phytochemical, pharmacological, and toxicological studies on plants in the genus Macleaya. Plants from the genus of Macleaya provide a source of bioactive compounds, primarily alkaloids, with remarkable diversity and complex architectures, thereby having attracted attention from researchers. To date, 291 constituents have been identified and/or isolated from this group. These purified compounds and/or crude extract possess antitumor, anti‐inflammatory, insecticidal, and antibacterial activities in addition to certain potential toxicities. Macleaya species hold potential for medicinal applications. However, despite the pharmacological studies on these plants, the mechanisms underlying the biological activities of active ingredients derived from Macleaya have not been thoroughly elucidated to date. Additionally, there is a need for research focusing on in vivo medical effects of Macleaya compounds and, eventually, for clinical trials.     

Studies on the medicinal species of Bupleurum in Shanxi, Gansu, Ningxia, Qinghai and Xingjiang

The medicinal species of Bupleurum in Shanxi, Gansu, Ningxia, Qinghai provinces and Xingjiang Autonornous Region have been investigated. It is shown that there are twenty one medicinal species in the genus, of which nine are main stream species.     

Pharmacological and chemical features of Nepeta L. genus: Its importance as a therapeutic agent

Medicinal plants have always had great value for the human population due to their valuable constituents and potential bioactivities. The objective of this review is to present an updated overview of an important medicinal plant genus Nepeta L., from the family Lamiaceae, revealing its traditional utilization, biological activity, phytoconstituents, and mechanisms of action. For this purpose, a literature survey was carried out by using SciFinder, ScienceDirect, Scopus, PubMed, and Web of Science followed by a revision of the bibliographies of the related articles. We have described and analyzed the role of plants in drug discovery and the importance of Nepeta species. Information on the utilization purposes of Nepeta species in folk medicine has been emphasized, and scientific studies on the biological effects and secondary metabolites are addressed. Nepeta species are characterized by terpenoid‐type compounds and phenolic constituents, which exert several activities such as an antimicrobial, repellent against major pathogen vector mosquitoes, insecticide, larvicide against Anopheles stephensi, cytotoxic anticarcinogen, antioxidant, anticonvulsant, analgesic, anti‐inflammatory agent, and antidepressant, revealing its importance in medicinal and agricultural fields. On the basis of numerous studies, the Nepeta genus demonstrates remarkable therapeutic effects against various diseases. However, clinical studies are warranted to confirm preclinical findings.     

重楼属植物化学成分及药理活性研究进展

重楼属Paris隶属于百合科(Liliaceae),全世界共有24个种,我国有19个种,分布于云南、贵州、四川等西南地区。其主要化学成分有甾体皂苷类、黄酮类、三萜类、脂肪酸类等,具有抗肿瘤、抗菌、止血、驱虫等药理作用。总结了重楼属植物系统分类、化学成分和药理作用的研究现状,以期为该属植物的进一步研究提供参考。     

Passiflora: a review update

This review describes the morphology, microscopy, traditional and folklore uses, phyto-constituents, pharmacological reports, clinical applications and toxicological reports of the prominent species of the genus Passiflora. Flavonoids, glycosides, alkaloids, phenolic compounds and volatile constituents have been reported as the major phyto-constituents of the Passiflora species. A few species of Passiflora have been used for curing various ailments, the most important being Passiflora incarnata Linneaus which possesses significant CNS depressant properties. The studies performed by the authors with the newly isolated benzoflavone (BZF) moiety from P. incarnata have been discussed. In the concluding part, various virgin areas of research on the species of this genus have been highlighted with a view to explore, isolate and identify the medicinally important phyto-constituents which could be utilized to alleviate various diseases affecting the mankind.     

Genus Ilex L.: Phytochemistry, Ethnopharmacology, and Pharmacology

The genus Ilex L. has been used as remedies in traditional Chinese medicine in Aquifoliaceae and beverages for thousands of years due to abundant pharmaceutical bioactivities. There are 600 species in genus Ilex L. containing various compounds such as terpenoids, saponins, glycosides, etc. Three species, I. cornuta, I. chinensis, and I. rotunda have been admitted in Chinese Pharmacopoeia 2015 to treat dyspepsia, stomatitis, and hyperactivity cough and protect the liver and kidney. Recent studies showed that several species have been daily drunk to promote human health and prevent cardiovascular diseases in the folk. Here we reviewed the genus Ilex L. in phytochemistry, ethnopharmacology, and pharmacology.     

Genus llex L.: Phytochemistry,Ethnopharmacology, and Pharmacology

The genus llex L. has been used as remedies in traditional Chinese medicine in Aquifoliaceae and beverages for thousands of years due to abundant pharmaceutical bioactivities. There are 600 species in genus llex L. containing various compounds such as terpenoids, saponins, glycosides, etc. Three species, I. cornuta, I. chinensis, and I. rotunda have been admitted in Chinese Pharmacopoeia 2015 to treat dyspepsia, stomatitis, and hyperactivity cough and protect the liver and kidney. Recent studies showed that several species have been daily drunk to promote human health and prevent cardiovascular diseases in the folk. Here we reviewed the genus llex L. in phytochemistry, ethnopharmacology, and pharmacology.