ABSTRACT
The purpose of this study is to provide a summary of the various pyrazole moieties' pharmacological actions. Pyrazole is a well-known and essential nitrogen-containing 5-membered heterocyclic compound, and different techniques for synthesis have been developed. Pyrazole, also known chemically as 1, 2-diazole, has become a prominent subject due to its numerous applications. Numerous pyrazole derivatives have been discovered to have a wide range of biological functions, which has fueled study in this area. Pyrazoles and their variants are among the most powerful groups of chemicals, with anti-bacterial, anti-convulsant, analgesic, anti-microbial, anti-inflammatory, anti-diabetic, sedative, anti- rheumatic, anticancer, and anti-tubercular properties. The goal of this study was to compile literary work on pyrazole for its different pharmacological activities, as well as to report on new efforts made on this moiety.
ABSTRACT
As a rare Chinese medicinal material， Paridis Rhizoma is mainly distributed in Yunnan， Guangxi， and Guizhou in southwestern China， with the effect of clearing heat and detoxifying， alleviating edema and relieving pain， cooling liver and tranquilizing mind. It is particularly effective for injuries from falls， fractures， contusions and strains， snake bites， cold wind-induced convulsion， and other diseases， which has been used for more than 2 000 years. According to modern research， polyphyllin Ⅱ， one of the main active components of Paridis Rhizoma， belongs to diosgenin in structure. It has the anti-tumor， anti-inflammatory， antiviral， antibacterial， immune-regulating， antioxidant， and multidrug resistance-reversing activities， showing good application prospect. Especially， the anti-tumor effect of polyphyllin Ⅱ has attracted wide attention， and the mechanism is inhibiting proliferation， migration， and invasion of tumor cells， inducing cell cycle arrest， apoptosis， and autophagy， suppressing angiogenesis， and modulating tumor microenvironment. However， the pharmacokinetic results show that polyphyllin Ⅱ has low bioavailability in vivo due to the low solubility， poor absorption， unsatisfactory distribution， and slow metabolism， which limit the clinical application. In recent years， there has been an explosion of research on the adverse reactions of polyphyllin Ⅱ， such as the strong hemolytic activity and obvious cytotoxicity to liver， kidney， myocardium and cardiovascular cells. Thus， papers were retrieved from "CNKI"， "VIP"， "Wanfang Data"， "PubMed"， "Web of Science"， and "Elsevier SD" with "Paris saponin Ⅱ"， "Polyphyllin Ⅱ" as the main keywords， and the pharmacological activities and mechanisms， pharmacokinetics， and adverse reactions were summarized. The findings are expected to serve as a reference for the in-depth research， development， and utilization of polyphyllin Ⅱ.
ABSTRACT
Perilla frutescens, an annual herb of the Labiatae family, has been cultivated in China for more than 2000 years. P. frutescens is the one of the first medicinal and edible plant published by the Ministry of Health. Its leaves, stems and seeds can be used as medicine and edible food. Because of the abundant nutrients and bioactive components in this plant, P. frutescens has been studied extensively in medicine, food, health care and chemical fields with great prospects for development. This paper reviews the cultivation history, chemical compositions and pharmacological activities of P. frutescens, which provides a reference for the development and utilization of P. frutescens resources.
ABSTRACT
Ganoderma lucidum is a valuable medical macrofungus with a myriad of diverse secondary metabolites, in which triterpenoids are the major constituents. This paper introduced the germplasm resources of genus Ganoderma from textual research, its distribution and identification at the molecular level. Also we overviewed G. lucidum in the components, the biological activities and biosynthetic pathways of ganoderic acid, aiming to provide scientific evidence for the development and utilization of G. lucidum germplasm resources and the biosynthesis of ganoderic acid.
ABSTRACT
Halogenated sesquiterpenes are important derivatives of sesquiterpenes, referring to chemical components of sesquiterpenes that contain halogens such as chlorine, bromine, and iodine. Halogenated sesquiterpenes have attracted attention from researchers in China and abroad because of their diverse structures, unique halogen elements, and extensive pharmacological activities. Studies have shown that halogenated sesquiterpenes exhibit significant antimicrobial, anti-inflammatory, anticancer, insecticidal, hypoglycemic, and enzyme inhibitory activities. In order to better explore the potential pharmaceutical value of halogenated sesquiterpenes, this paper reviewed the structural characteristics and pharmacological activities of halogenated sesquiterpenes in the past two decades, aiming to provide references for further research and development of this class of compounds.
Subject(s)
Sesquiterpenes/chemistry , Anti-Inflammatory Agents/pharmacology , ChinaABSTRACT
Background: Tridax procumbens Linn. is a spreading herb found throughout India. Tridax procumbens is known for several potential therapeutic effects like antiviral, antioxidant, anti-infective, wound healing, insecticidal and anti- inflammatory, hepatoprotective, and antidiabetic. Novel therapies for inflammation are essential to overcome the adverse effects of existing anti-inflammatory drugs. Thus, this study was designed to evaluate anti-inflammatory activity in the experimental animal. Objective: To evaluate anti-inflammatory efficacy in experimental animal Materials and Methods: Tridax procumbens plant leaves were taken for the study. The Plant extraction was prepared by using the Soxhlet apparatus. The ethanolic extract was used as a test drug. Indomethacin and Dexamethasone were used as control drugs. Wistar rats weighing 150g to -200g were used in the study. Results: At dosages of 200 and 400 mg kg-1 , the ethanolic leaf extracts of Tridax Procumbens demonstrated substantial anti-inflammatory activity against Irish Moss-triggered inflammation. After 3 hours, 400 mgkg-1 showed a significant reduction in inflammation (48 percent), with the impact increasing after 3 hours (52 percent). The anti-inflammatory efficacy of Tridax Procumbens ethanol (EtOH) extracts was substantial and comparable to that of indomethacin (10 mg/kg). Tridax procumbens ‘s Ethanol (EtOH) leaf extract at a dose of 200 and 400 mgkg-1 , demonstrated considerable anti-inflammatory action. The average weight of granulomatous surrounding tissue in the threading was considerably smaller in the Tridax procumbens extraction group after 7 days than in the comparison group. The 400 mg kg-1 dose was shown to be the most effective of the two. the greatest reduction in the production of granuloma tissue. Tridax procumbens at doses of 200 mg/kg and 400 mg/kg resulted in substantial reductions in granuloma weights of 38.16 ± 0.04 (7.4 percent inhibition) and 34.58 ± 0.04 (16.1 percent inhibition), respectively. The lower dose of 400 mg/kg resulted in a little lesser reduction in granumola weight than the conventional medication dexamethasone (28.92 ± 0.04). (29.8 percent inhibition). Conclusion: The present study concludes that Tridax Procumbens possess anti-inflammatory effects in animal models.
ABSTRACT
Traditional Chinese medicines (TCMs) have continued to be a treasure trove. The study of chemodiversity and versatility of bioactivities has always been an important content of pharmacophylogeny. There is amazing progress in the discovery and research of natural components with novel structures and significant bioactivities in 2020. In this paper we review 271 valuable natural products, including terpenoids, steroids, flavonoids, phenylpropanoids, phenolics, nitrogen containing compounds and essential oil, etc., isolated and identified from TCMs published in journals of Chinese Traditional and Herbal Drugs (Zhong Cao Yao) and Chinese Herbal Medicines (CHMs), and focus on their structures, source organisms, and relevant bioactivities, paying special attention to structural characteristics of novel compounds and newly revealed pharmacological properties of known compounds. It is worth noting that natural products with antitumor activity still constitute the primary object of research. Among the reported compounds, two new triterpenoids, i.e., ursolic acid 3-O-β-cis-caffeate and mollugoside E, display remarkable cytotoxicity against PC-9 and HL-60 cell lines, respectively. Three known phenolic compounds, i.e., pyoluteorin, 4-hydroxy-3-methoxy cinnamaldehyde and 3,7-dimethoxy-5-hydroxy-1,4-phenanthrenequinone, exhibit significant cytotoxicity against multiple cell lines. Numerous studies on the free radical scavenging activity of reported compounds are currently underway. In vitro, three known phenolic compounds, i.e., 3,4-O-dicaffeoylquinic acid methyl ester, 3,4,5-O-tricaffeoylquinic acid methyl ester and arbutin, had more considerable antioxidant activities than vitamin C. The anti-inflammatory, anti-diabetic, hypolipidemic, neuroprotective and antimicrobial activities of isolated compounds are also encouraging. The structural characteristics and bioactivities of TCM compounds highlighted here reflect the enormous progress of CHM research in 2020 and will play a positive role in the future drug discovery and development. According to pharmacophylogeny, the phylogenetic distribution of compounds with different natures and flavors can be explored, with view to better mining TCM resources.
ABSTRACT
Evodiamine(EVO)is an indoloquinazoline alkaloid isolated from the fruits of Euodia rutaecarpa,which has long been used in traditional Chinese medicine to treat various diseases.Modern medical research shows that evodiamine has various pharmacological activities and extremely high medicinal value such as anti-inflammation,anti-tumor,losing weight,treating Alzheimer's,and antibacterium.Evodiamine can interact with a variety of proteins.For example,the interaction between evodiamine and TRPV1 induces its activation to exert anti-inflammatory and losing weight; the interaction with DNA topoisomerase I inhibits its function and thus inhibit bacterial proliferation; the interaction with tubulin promotes NLRP3 inflammasome activation,and exerts anti-tumor and anti-inflammatory functions.In recent years,with the in-depth study of evodiamine,pharmacological research and mechanism of evodiamine has significant improvement.Recent progress of pharmacological effect of evodiamine is highlighted in this review.
ABSTRACT
Smallanthus sonchifolius， a plant resource with both medicinal and edible values， has been taken as fruit for a long history. Studies have proved that phenolic acids， flavonoids， sesquiterpene lactones， and fructooligosaccharides are the major compounds in S. sonchifolius. The extract of S. sonchifolius demonstrates noticeable antioxidant， anti-inflammatory， antimicrobial， and anti-cancer effects， as well as the activities of lowering blood glucose level， regulating intestinal function and so on. The rhizomes and leaves of S. sonchifolius contain abundant phenolic acids， mainly caffeic acid and its derivatives， which endow S. sonchifolius with remarkable antioxidant effect. Moreover， these substances can reduce blood glucose by improving insulin sensitivity. Fructooligosaccharides are abundant in the tuber of this plant， which can improve intestinal function by regulating intestinal flora. The sesquiterpene lactones in glandular trichomes on the leaf surface can inhibit the proliferation of cancer cells， among which uvedafolin and enhydrofolin have particularly strong activities. Furthermore， the sesquiterpene lactones have obvious inhibitory effect on Gram-positive bacteria. In terms of structure， the number of epoxy groups is linked to the strength of anticancer and antimicrobial effects. In addition， S. sonchifolius contains other compounds such as volatile oils， fatty acids， sterols， diterpenes， p-hydroxyacetophenone derivatives， and octulosonic acid derivatives， thereby exhibiting the pharmacological effects of treating Alzheimer's disease， protecting kidney， and lowering blood lipids. However， the isolation and identification of the main compounds in S. sonchifolius need further exploration， and the mechanism of action remains to be studied. Here we summarized the principal chemical components and pharmacological activities of S. sonchifolius， aiming to give a clue for the comprehensive development and utilization of this plant.
ABSTRACT
Morus alba, a traditional economic crop, is also a significant medicinal plant. The branches(Mori Ramulus), leaves(Mori Folium), roots and barks(Mori Cortex), and fruits(Mori Fructus) of M. alba are rich in chemical components, such as alkaloids, flavonoids, flavanols, anthocyanins, benzofurans, phenolic acids, and polysaccharides, and possess hypoglycemic, hypolipidemic, anti-inflammatory, anti-tumor, anti-microbial, liver protective, immunoregulatory, and other pharmacological activities. This study analyzed the sources, classification, and functions of the main chemical components in M. alba and systematically summarized the latest research results of essential active components in M. alba and their pharmacological effects to provide references for in-depth research and further development as well as utilization of active components in M. alba.
Subject(s)
Anthocyanins , Flavonoids/pharmacology , Morus , Plant Extracts/pharmacology , Plant LeavesABSTRACT
Perilla frutescens is a traditional medicinal and edible plant widely distributed in China and enjoys an extensive usage. P. frutescens contains multiple essential oils， which are composed of monoterpenes， sesquiterpenes， and their oxygen-containing derivatives. Compared with other parts of P. frutescens， Perillae Folium produce more oils， with volatile oils as the main constituents. There are many active substances in the volatile oils from Perillae Folium， mainly including perillaldehyde， perillaketone， perillaalcohol， D-limonene， β-caryophylene， etc. Such factors as germplasm， growth environment， extraction method， cultivation time， and harvest period all can trigger changes in volatile oil constituents and content from Perillae Folium. The volatile oils from Perillae Folium have diverse pharmacological effects like anti-oxidation， anti-bacteria， anti-inflammation， vasodilation， anti-tumor， and anti-depression， implying its high clinical application value. However， the chemical constituents in volatile oils from Perillae Folium are complex and unstable and their pharmacological activities are affected by many factors， so the safety and effectiveness of clinical medication fail to be guaranteed， which may has impeded the rational and effective use of these volatile oils. Many scholars in China and abroad have conducted a lot of research on the volatile oils from Perillae Folium， but there is currently no systematic and comprehensive research report on the chemical constituents of volatile oils from Perillae Folium and their pharmacological effects. This paper reviewed the relevant domestic and foreign literature， analyzed the development status of volatile oils from Perillae Folium， and summarized their extraction process， chemical constituents， and pharmacological actions， aiming to provide a reference for their further development， clinical application， and risk assessment.
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Cadinanes are a class of bicyclic sesquiterpenes with complex stereochemistry and broad pharmacological activities, such as antibacterial, anti-inflammatory, and hypoglycemic activities. To date, structurally diverse and bioactive cadinane sesquiterpenes have been isolated and identified from a variety of plants and microorganisms. Moreover, deeper understandings on cadinane sesquiterpene synthases have been made. This article categorized the 124 new cadinanes which were published in the literatures in the past four years (2017-2020) into five structural types, and presented their pharmacological activities. We also illustrated the elucidation of the biosynthetic pathways for typical cadinanes, summarized the research progress on cadinane sesquiterpene synthases. Finally, current challenges and future prospects were proposed and discussed.
Subject(s)
Anti-Inflammatory Agents , Polycyclic Sesquiterpenes , SesquiterpenesABSTRACT
The tubers and roots of Aconitum (Ranunculaceae) are widely used as heart medicine or analgesic agents for the treatment of coronary heart disease, chronic heart failure, rheumatoid arthritis and neuropathic pain since ancient times. As a type of natural products mainly extracted from Aconitum plants, Aconitum alkaloids have complex chemical structures and exert remarkable biological activity, which are mainly responsible for significant effects of Aconitum plants. The present review is to summarize the progress of the pharmacological, toxicological, and pharmacokinetic studies of Aconitum alkaloids, so as to provide evidence for better clinical application. Research data concerning pharmacological, toxicological and pharmacokinetic studies of Aconitum alkaloids were collected from different scientific databases (PubMed, CNKI, Google Scholar, Baidu Scholar, and Web of Science) using the phrase Aconitum alkaloids, as well as generic synonyms. Aconitum alkaloids are both bioactive compounds and toxic ingredients in Aconitum plants. They produce a wide range of pharmacological activities, including protecting the cardiovascular system, nervous system, and immune system and anti-cancer effects. Notably, Aconitum alkaloids also exert strong cardiac toxicity, neurotoxicity and liver toxicity, which are supported by clinical studies. Finally, pharmacokinetic studies indicated that cytochrome P450 proteins (CYPs) and efflux transporters (ETs) are closely related to the low bioavailability of Aconitum alkaloids and play an important role in their metabolism and detoxification in vivo.
Subject(s)
Aconitum/chemistry , Alkaloids/toxicity , Biological Availability , Phytochemicals/toxicity , Plant Roots/chemistryABSTRACT
The medicinal part of Aucklandia lappa (Asteraceae) is its dried root, which is one of the commonly used Chinese medicinal materials. Here we reviewed sesquiterpene lactones isolated from A. lappa over the past ten years in the following aspects of pharmacological activities, pharmacokinetics, toxicology, structure–activity relationship. Pharmacological activities consist of anti-cancer, anti-inflammatory activity, anti-immunity activity, anti-oxidant activity, antimicrobial activity, spasmolytic activity and so on. The extractive, showing similar pharmacokinetics parameters, may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacromolecules through Michael-addition. However, the poor aqueous solubility, non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class. In order to evaluate the potential effect of the extractive applied in clinical trial, the present review outlines information on pharmacological activities, pharmacokinetics, toxicology, and structure–activity relationship, as well as the future research directions of the extractive for further development and utilization of A. lappa.
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At present, 141 compounds have been isolated from Picrorhiza scrophulariiflora and P. kurroa of the Scrophulariaceae plants, including 46 iridoid glycosides, 29 tetracyclic triterpenoids, 25 phenylpropanoids, and 11 phenylethanoid glycosides. Pharmacological studies have demonstrated that they have liver-, heart-, brain-, kidney-, and nerve cells-protecting effects as well as anti-tumor, anti-inflammatory, anti-bacterial, anti-asthma, anti-diabetic, immunomodulatory, and blood lipid-lowering activities. This article reviews the chemical components and pharmacological activities of P. scrophulariiflora and P. kurroa, aiming to provide a basis for the in-depth research, development, and utilization of the two plants.
Subject(s)
Iridoid Glycosides , Picrorhiza , Triterpenes/pharmacologyABSTRACT
Phenylpropanoids are one of the major chemical constituents in Zanthoxylum species. They include simple phenylpropanoids, coumarins, and lignans and possess anti-tumor, anti-inflammatory, anti-platelet aggregation, anti-bacterial, anti-viral, insecticidal, and antifeedant activities. This review summarizes the chemical constituents and pharmacological activities from the Zanthoxylum plants in hopes of providing reference for the research and application of phenylpropanoids from this genus.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Coumarins/pharmacology , Lignans , Plant Extracts , ZanthoxylumABSTRACT
The review outlines the current understandings of saponins and sapogenins in agave species with special focus on pharmacological role of hecogenin in numerous preclinical studies. A systematic literature survey was done on the pharmacological activities of hecogenin during the past 40 y with electronic databases like PubMed, Science Direct, Wiley, SciFinder, Google Scholar, Web of Science and Scopus. Hecogenin, a steroidal sapogenin found abundantly in the leaves of Agave genus species such as, Agave sisalana, Agave cantala, Agave aurea and many more. This phytosteroid (hecogenin) is used as initial material for the synthesis of steroidal drugs in the pharmaceutical industry. Hecogenin has exhibited potential role in the management of a number of disorders such as inflammation, arthritis, cancer, gastric ulcer, cardiotonic and larvicidal activity. In this review, we have summarized the saponins and sapogenins present in the Agave species and pharmacological roles of hecogenin with their mechanism of action.
ABSTRACT
Nyctanthes arbor-tristis (Oleaceae) popularly known as “Parijat” is a plant of great importance in India. It iswidely used in Ayurvedic medicines. Each part of this plant has some medicinal value. It possesses extensivemedicinal uses, viz., antipyretic, anti-inflammatory, anthelmintic, sedative effect, laxative, and expectorant, inrheumatism. The present review aims to perform a detailed compilation of work done on this plant mainly asa source of the antioxidant and anticancer agent as well as various pharmacological properties from 1987 totill date. All these activities possessed by plants are due to the presence of multiple phytochemicals which canact as a source of active pharmacological agents. Crude extracts, as well as pure compounds like 4-hydroxyhexahydrobenzofuran-7-one, 6β-hydroxyloganin, and Arbortristoside A from seeds, a polysaccharide fromleaves, and Naringenin from the stem, are reported for its anticancer and antioxidant properties. The need ofthe hour is to provide scientific validation of ethnomedicinal use of this plant. The present study can be usedto highlight the need for research and potential development of natural therapeutic products with lesser sideeffects.
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The genus Carpesium plants contain many kinds of sesquiterpenes. Up to now, more than 201 sesquiterpene compounds have been isolated and identified, including 86 germacranolides, 30 eudesmanolides, 29 guaianolides, 23 sesquiterpene dimers, 9 pseudoguaianes, 9 carabranolides, 7 xanthanolides, 6 sesquiterpenes without lactone, 1 eremophilane and 1 tricyclo dodecane sesquiterpene. The reported sesquiterpenes possess a series of pharmacological properties, such as anti-tumor, anti-inflammatory, antibacterial, antiparasitic, insecticidal, and antiviral activities. This paper summarizes the 201 chemical structures and biological activities of sesquiterpenes in genus Carpesium, and provides the scientific basis for the further development and utilization.
Subject(s)
Anti-Bacterial Agents , Anti-Inflammatory Agents , Asteraceae/chemistry , Lactones , Molecular Structure , Phytochemicals/pharmacology , Sesquiterpenes/pharmacologyABSTRACT
Rhinacanthus nasutus is the shrubs of Acanthacesa of Rhinacanthus nasutus. It has been used as traditional Zhuang medicine for thousands of years, with antipyretic and alexipharmic, antibacterial and anti-inflammatory, antiasthmatic and expectorant effects. Modern pharmacological studies have shown that R. nasutus has been used for treatment of various diseases, including pneumonia, gastritis and hepatitis. In addition, naphthoquinone esters isolated from this plant exhibits antitumor, antiviral, antifungal, and immunomodulatory activities, with a high application value. Scholars at home and abroad have isolated a variety of compounds from R. nasutus, including 20 naphthoquinones, organic acids, lignans, alkaloids and other structural types of components. Among them, naphthoquinones have a variety of biological activities. Up to now, there are no systematic and comprehensive report on the chemical constituents and pharmacological effects of naphthoquinones. In this review, we summarized the chemical constituents of naphthoquinones with pharmacological activity, finding that R. nasutus and naphthoquinones have a great potential to be developed as a traditional Chinese medicine for tumors, diabetes, nonalcoholic fatty liver, which can provide an important scientific basis for defining the pharmacodynamic basis of the pharmacological activities and a reference for further research and comprehensive utilization of Zhuang medicine of Rhinacanthus nasutus.