Progress on pharmacological activities and hepatotoxicity of bavachinin / 药学实践杂志

Bavachinin is a dihydroflavone isolated from dried ripe fruits of Psoralea corylifolia L.，which has various pharmacological activities, such as anti-tumor, anti-virus, anti-diabetes, anti-inflammatory and neuroprotective, and good potential in clinical applications. With the increasing concern about the safety of P. corylifolia applications in clinical, the bavachinin has been found to be one of the main components causing liver injury. In this paper, the pharmacological activities and hepatotoxicity of bavachinin in the recent 20 years were reviewed, in order to provide reference for the further study and clinical application.

Research progress on triterpenoids of Betula plants / 药学学报

The secondary metabolites of plants are important sources of natural drugs. Betula plants have abundant pharmacological value, complex mechanism and wide applications, which are closely related to the triterpenoids of theirs. Triterpenoids in Betula species are mainly divided into dammarane-type, ocotillol-type, oleanane-type, lupane-type and cycloaltunane-type. The extracts of Betula species have varieties of activities such as anti-tumor, anti-inflammatory, anti-oxidant, anti-bacterial, etc. And the biosynthetic pathways of triterpenoids after 2,3-oxidosqualene are split into four branches of dammarenediol-II, lupeol, cycloartenol and amyrin according to the different oxidosqualene cyclases. This review summarizes the chemical constituents, pharmacological activities and biosynthetic pathways of triterpenoids in Betula plants. It provides a reference for the research and development of new drugs and the production of these triterpenoids in microbial cell factories by synthetic biology methods.

Progress on Pharmacological Effect of Terpinen-4-ol： A Review / 中国实验方剂学杂志

Terpine-4-ol is abundant in nature. As a cyclic monoterpenoid compound， terpine-4-ol is distributed in a variety of natural plants. It is the main component and the key active substance in many traditional Chinese essential oils， such as Melaleuca alba essential oil and coral ginger essential oil. Terpine-4-ol has anti-microbial， anti-tumor， insecticidal， anti-inflammatory， and other effects. It can treat cancer， as well as oral and cardiovascular diseases with great safety. In terms of antibacterial activity， terpine-4-ol can destroy bacterial cell walls， improve membrane permeability， and regulate bacterial migration， reproduction， and other related genes to inhibit bacterial activity. In terms of antifungal activity， terpine-4-ol can bind with ergosterol in fungal cell walls to cause fungal death. In terms of insecticidal activity， terpine-4-ol can inhibit Na+ and K+-ATPase activity and cause the death of the insect. In terms of anticancer activity， terpine-4-ol can regulate the expression of apoptosis-related proteins in cancer cells， so as to control the apoptosis of cancer cells. In this paper， the pharmacological activity and action mechanism of terpine-4-ol were reviewed to provide a reference for further research and utilization of terpine-4-ol.

Advances in medicinal research on tetrodotoxin / 药学实践杂志

Tetrodotoxin (TTX) is a neurotoxin found in puffer fish and other marine organisms. It has been used as an inhibitor of voltage-gated sodium channels (VGSCs), which could selectively bind to the α-subunit on the outer vestibule of VGSCs, preventing sodium ions from entering the channel, resulting in pharmacological activities. As a typical sodium channel blocker, TTX shows a significant analgesic effect. TTX could selectively block Na+ channels without affecting other ion channels, therefore it could reduce the probability of adverse reactions caused by commonly used antiarrhythmic drugs. In addition, TTX has a significant role in detoxification and prevention of renal failure, so TTX has great potential as a medicine. The structure and physicochemical properties, mechanism of action, pharmacological activities and preparations of tetrodotoxin have been reviewed in this paper, so as to provide a general support for the evaluation of its druggability and application in the field of pharmacy.

Research progress in chemical constituent and pharmacological activity of Punica granatum L / 中国药科大学学报

@#Punica granatum L.(pomegranate) is a medicinal plant belonging to the genus Punica Linn..The peel, seed, flower, leaf and root of P.granatum is widely used as traditional medicine in China.Phytochemical studies showed that the major chemical constituents of P.granatum were tannins, flavonoids, terpenes, alkaloids, phenolic acids, anthocyanins, fatty acids, etc.Biological studies on extracts and active ingredients of P.granatum show some bioactivities, such as antioxidant, hypoglycemic, anti-inflammatory, anti-tumor, antibacterial activities.Herein, the chemical constituents and pharmacological effects of different parts of pomegranate were reviewed, providing a theoretical basis for the further research and utilization of pomegranate.

UPLC-Q-TOF-MS/MS combined with network pharmacology for exploring antiinflammatory mechanism of Eurycoma longifolia / 南方医科大学学报

OBJECTIVE@#To explore the mechanisms that mediate the anti-inflammatory activity of Eurycoma longifolia.@*METHODS@#Kunming mouse models of xylene-induced ear swelling and lipopolysaccharide (LPS)-induced acute pneumonia were used to compare the anti- inflammatory activities of aqueous and ethanol extracts of Eurycoma longifolia. UPLC-Q-TOF-MS/MS was used to identify the chemical composition in the ethanol extract of Eurycoma longifolia, based on which the potential antiinflammatory targets of Eurycoma longifolia were screened using the databases including SwissADME, SwissTargetPrediction, and Genecards. The String database was used to generate the protein-protein interaction (PPI) network, and Cytoscape was used for network topology analysis and screening the core targets. The enrichment of the core targets was analyzed using Metascape database, the core components and targets were docked with Autodock software, and the docking results were visualized using Pymol software. In a RAW264.7 cell model of LPS-induced inflammation, the Griess reagent was used to measure NO level, and Western blotting was performed to detect the expression levels of MAPK1, JAK2, and STAT3 proteins to verify the anti- inflammatory mechanism of Eurycoma longifolia.@*RESULTS@#The ethanol extract (75%) of Eurycoma longifolia (ELE) was the active site, which contained a total of 37 chemical components. These chemical compounds and diseases had 541 targets, involving the JAK/STAT3, cAMP and other signaling pathways. Twelve indicator components were identified, which all showed good results of molecular docking with two core targets involved in the signaling pathways. In the cell validation experiment, treatment of the cells with low-, medium-, and high-dose ELE significantly reduced NO release in the cells, and ELE at the medium dose significantly decreased the cellular expressions of JAK2 and STAT3.@*CONCLUSION@#The anti-inflammatory activity of Eurycoma longifolia is attributed primarily to its active ingredients bitter lignin and alkaloids, which may regulate the JAK/STAT3 signaling pathway by targeting JAK2 and STAT3.

Research progress on chemical constituents and pharmacological activities of Viola plants / 中国中药杂志

There are 500 species of Viola(Violaceae) worldwide, among which 111 species are widely distributed in China and have a long medicinal history and wide varieties. According to the authors' statistics, a total of 410 compounds have been isolated and identified from plants of this genus, including flavonoids, terpenoids, phenylpropanoids, organic acids, nitrogenous compounds, sterols, saccharides and their derivatives, volatile oils and cyclotides. The medicinal materials from these plants boast anti-microbial, anti-viral, anti-oxidant and anti-tumor activities. This study systematically reviewed the chemical constituents and pharmacological activities of Viola plants to provide a basis for further research and clinical application.

α/Sulfono-γ-AA peptide hybrids agonist of GLP-1R with prolonged action both in vitro and in vivo

Peptides are increasingly important resources for biological and therapeutic development, however, their intrinsic susceptibility to proteolytic degradation represents a big hurdle. As a natural agonist for GLP-1R, glucagon-like peptide 1 (GLP-1) is of significant clinical interest for the treatment of type-2 diabetes mellitus, but its in vivo instability and short half-life have largely prevented its therapeutic application. Here, we describe the rational design of a series of α/sulfono-γ-AA peptide hybrid analogues of GLP-1 as the GLP-1R agonists. Certain GLP-1 hybrid analogues exhibited enhanced stability (t 1/2 > 14 days) compared to t 1/2 (<1 day) of GLP-1 in the blood plasma and in vivo. These newly developed peptide hybrids may be viable alternative of semaglutide for type-2 diabetes treatment. Additionally, our findings suggest that sulfono-γ-AA residues could be adopted to substitute canonical amino acids residues to improve the pharmacological activity of peptide-based drugs.

Research progress of Codonopsis Radix and prediction of its Q-markers / 中国中药杂志

Codonopsis Radix is a traditional tonic medicine commonly used in China, which has the effects of strengthening the spleen and tonifying the lung, as well as nourishing blood and engendering liquid. The chemical constituents of Codonopsis species are mainly polyacetylenes, alkaloids, phenylpropanoids, lignans, terpenoids and saponins, flavonoids, steroids, organic acids, saccharides, and so on. Modern pharmacological studies showed that Codonopsis Radix also has a variety of pharmacological effects such as enhancing body immunity, protecting gastrointestinal mucosa and resisting ulcers, promoting hematopoietic function, regulating blood sugar, and delaying aging. In this paper, the chemical constituents of Codonopsis species and the pharmacological effects of Codonopsis Radix were summarized, and on this basis, the quality markers of Codonopsis Radix were analyzed. It was predicted that lobetyolin, tangshenoside I, codonopyrrolidium A, and the oligosaccharides were the possible Q-markers of Codonopsis Radix. This paper will provide scientific references for the quality evaluation and profound research and the development of Codonopsis Radix.

Research advance on structure and function of amides in Zanthoxylum plants / 中国中药杂志

Zanthoxylum belongs to the Rutaceae family, and there are 81 Zanthoxylum species and 36 varieties in China. Most of the Zanthoxylum plants are used as culinary spice. In recent years, scholars in China and abroad have carried out in-depth research on Zanthoxylum plants, and found that the peculiar numbing sensation of Zanthoxylum plants originates from amides. It is also determined that amides are an important material basis for exerting pharmacological effects, especially in anti-inflammatory analgesia, anesthesia and other aspects. In this paper, 123 amides in 26 Zanthoxylum plants and their pharmacological activity that have been reported were summarized, which provided scientific reference for the clinical application of Zanthoxylum plants and the research and development of new drugs, and also facilitated the sustainable development and utilization of Zanthoxylum plant resources.

Metabólitos bioativos e atividades biológicas, tóxicas e farmacológicas de plantas ornamentais: uma revisão das espécies hydrangea macrophylla, euphorbia milii, dieffenbachia seguine e dracaena trifasciata / Bioactive metabolites and biological, toxic and pharmacological activities of ornamental plants: a review of the species hydrangea macrophylla, euphorbia milii, dieffenbachia seguine and dracaena trifasciata / Metabolitos bioactivos y actividades biológicas, tóxicas y farmacológicas de plantas ornamentales: una revisión de las especies hydrangea macrophylla, euphorbia milii, dieffenbachia seguine y dracaena trifasciata

As plantas ornamentais foram selecionadas pelo homem a partir de caracteres atraentes e começaram a ser cultivadas por sua beleza. São utilizadas frequentemente em arquitetura e paisagismo de espaços externos, porém, pode possuir princípios ativos que as tornam tóxicas e que podem causar danos a saúde como irritações na pele e mucosas. No Brasil há descritas diversas plantas de uso ornamental e que são consideradas tóxicas, dentre elas podemos destacar popularmente hortênsia, comigo-ninguém-pode, espada-de- são-jorge e a coroa-de-cristo e na literatura o envenenamento humano por essas plantas tóxicas quase não é documentado o que despertou interesse nessa revisão. Logo, esse estudo possui objetivo de revisar as bases de dados em busca de informações de atividades biológicas, tóxicas, farmacológicas e de metabólitos bioativos das espécies Hydrangea macrophylla, Euphorbia milii, Dieffenbachia seguine e Dracaena trifasciata. Para o compilado de dados deste artigo de revisão, foram utilizados 51 artigos que reuniram as condições de elegibilidade buscadas. Os artigos foram lidos na integra e os dados agregados em tabela ou texto. Esta revisão observou que a maioria dos ensaios aplicados nessas espécies foram de caráter toxicológico e objetivavam a busca de veículos para controle de doenças ocasionadas por vetores. Os ensaios demonstraram potencial tóxico preliminar, justificando os efeitos relacionados à intoxicação ou aos danos á saúde como irritações na pele e mucosas.

Ornamental plants were selected by man from attractive characters and began to be cultivated for their beauty. They are often used in architecture and landscaping of outdoor spaces; however, they may have active ingredients that make them toxic and that can cause health damage such as skin and mucous membrane irritations. In Brazil there are described several plants of ornamental use and that are considered toxic, among them we can highlight hortênsia, comigo-ninguém-pode, espada-de-são-jorge e a coroa-de- cristo, and in the literature the human poisoning by these toxic plants is hardly documented which aroused interest in this review. Therefore, this study aims to review the databases in search of information on biological, toxic, pharmacological activities and bioactive metabolites of the species Hydrangea macrophylla, Euphorbia milii, Dieffenbachia seguine and Dracaena trifasciata. To compile data from this review article, 51 articles were used that met the sought eligibility conditions. The articles were read in full and the data aggregated in a table or text. This review noted that most of the tests applied to these species were toxicological in nature and aimed to search for vehicles to control diseases caused by vectors. The trials demonstrated preliminary toxic potential, justifying the effects related to intoxication or damage to health such as skin and mucous membrane irritations.

Las plantas ornamentales fueron seleccionadas por el hombre a partir de caracteres atractivos y empezaron a cultivarse por su belleza. A menudo se utilizan en la arquitectura y el paisajismo de espacios exteriores; sin embargo, pueden tener principios activos que las hacen tóxicas y que pueden causar daños a la salud, como irritaciones de la piel y de las mucosas. En Brasil están descritas varias plantas de uso ornamental y que son consideradas tóxicas, entre ellas se destacan hortênsia, comigo-ninguém-pode, espada-de-são-jorge e a coroa-de- cristo, y en la literatura el envenenamiento humano por estas plantas tóxicas está poco documentado lo que despertó el interés en esta revisión. Por lo tanto, este estudio tiene como objetivo revisar las bases de datos en busca de información sobre las actividades biológicas, tóxicas, farmacológicas y metabolitos bioactivos de las especies Hydrangea macrophylla, Euphorbia milii, Dieffenbachia seguine y Dracaena trifasciata. Para recopilar los datos de este artículo de revisión, se utilizaron 51 artículos que cumplían las condiciones de elegibilidad buscadas. Los artículos se leyeron en su totalidad y los datos se agregaron en una tabla o texto. En esta revisión se observó que la mayoría de los ensayos aplicados a estas especies eran de naturaleza toxicológica y tenían como objetivo la búsqueda de vehículos para el control de enfermedades causadas por vectores. Los ensayos demostraron potencial tóxico preliminar, justificando los efectos relacionados con intoxicación o daños a la salud, como irritaciones de piel y mucosas.

Progress of research on the pharmacological effects and mechanisms of emodin / 中国药科大学学报

@#As an active hydroxyanthraquinone ingredient, emodin is abundant in Chinese medicine herbs, such as Rheum palmatum, Polygonum cuspidatum and Polygonum multiflorum.Modern pharmacological studies have shown that emodin has a variety of pharmacological activities including anti-tumor, anti-inflammatory and immunoregulatory, antibacterial and anti-viral effects, myocardial protection, neuroprotection, renal protection, bone protection, antifibrosis and so on, which indicate its high medicinal value and broad application prospects.This article aims to summarize the progress in the pharmacological activity and mechanism of action of emodin published in domestic and international journals over the last 5 years and highlight the potential targets and molecular signaling pathways linked with emodin, so as to provide some clues and references for further development and clinical application of emodin.

Pharmacological activities of berberine and strategies to improve its oral bioavailability / 药学学报

Berberine is a naturally occurring benzylisoquinoline alkaloid with a wide range of pharmacological activities, such as antibacterial, anticancer, hypolipidemic, antidiabetic and antidiarrheal. Although berberine has a wide range of curative effects, the extremely low bioavailability (< 1%) limits its clinical application. Pure berberine preparations have not yet been approved for any specific disease. The low oral bioavailability of berberine is mainly due to poor solubility caused by self-aggregation under acidic conditions, low permeability, P-glycoprotein (P-gp)-mediated efflux, and liver and intestine metabolism. To improve the oral bioavailability of berberine, researchers have adopted a variety of strategies, including the application of various nano-delivery systems, penetration enhancers and P-gp inhibitors, structural modifications, and development of berberine derivatives. Improving the oral bioavailability of berberine can improve the pharmacological activity of berberine, reduce the dosage, and then reduce the toxic and side effects. This review summarized the various pharmacological activities, metabolism progress and pharmacokinetic characteristics of berberine, the newly discovered berberine target intestinal microbiota and focused on the strategies to improve the oral bioavailability of berberine by improving solubility and permeability, inhibiting P-gp efflux, and structural modification. The research on berberine was prospected, which provided guidance for the in-depth study of berberine.

Research progress on chemical constituents and pharmacological activities of Blumea balsamifera / 中国药房

Blumea balsamifera belonging to Blumea of Compositae family is a perennial herb or subshrub ，which is the only source of Traditional Chinese medicine Aipian and ethnic medicine essential oil of B. balsamifera . B. balsamifera contains volatile oil，flavonoids，sesquiterpenoids，phenylpropanoids，etc.，and shows antibacterial ，anti-inflammatory，analgesic，treating burns and scalds，neuroprotective and antioxidant effects ，etc. In this paper ，the chemical constituents and pharmacological activities are summarized by reviewing the domestic and foreign research literatures ，and it is expected to provide a reference for the in-depth research and development and utilization of B. balsamifera .

Genus Tetrastigma: A review of its folk uses, phytochemistry and pharmacology / 中草药·英文版

The genus Tetrastigma belongs to the Vitaceae family and contains over 100 species. This paper reviewed folk uses, chemical constituents, pharmacological activities, and clinical applications of the medicinal plants in the genus Tetrastigma. In addition, the paper also discussed the current problems for the further studies. Up to now, more than 240 compounds were reported from the genus Tetrastigma, covering 74 flavonoids, 14 terpenoids, 19 steroids, 21 phenylpropanoids, 14 alkaloids and others constituents. Among them, flavonoids are the major and the characteristic chemical constituents in this genus. Modern pharmacological studies and clinical practice showed that the extracts and chemical constituents of Tetrastigma species possessed wide pharmacological activities including antitumor, antioxidative, hepatoprotective, antiviral, anti-inflammatory, and analgesic activities. The information summarized in this paper provides valuable clues for new drug discovery and an incentive to expand the research of genus Tetrastigma.

Phytochemical and pharmacological progress on Syringa oblata, a traditional Mongolian medicine / 中草药·英文版

Syringa oblata is a traditional Mongolian medicine mainly distributed in the Helan Mountains (the boundaries of Inner Mongolia and Ningxia, China) and the north of Yan Mountains (Aohan Qi, Inner Mongolia, China). It is clinically used to treat diseases caused by Heyi, such as heartache and heat pathogen in the heart. Phytochemical studies on S. oblata revealed the presence of iridoids, lignans, triterpenes, phenylpropanoids, phenylethanoids, and volatile components. Pharmacological investigations revealed a broad spectrum of bioactivities, such as antimicrobial, antioxidant, antiproliferative, and hepatoprotective effects. This article summarized the chemical components and pharmacological activities of S. oblata, providing a scientific rationale for its bioactive constituents, quality control, and utilization as an important medicine.

Research advances in chemical constituents and pharmacological activities of Dendrobium plants / 中国中药杂志

Dendrobii Caulis are commonly used tonic Chinese medicinal materials with a long history of application. As demonstrated by pharmacological results, the chemical constituents and the extracts of Dendrobii Caulis have anti-inflammatory, antibacte-rial, antioxidant, and anti-tumor effects, and can also regulate immunity, lower blood pressure, and regulate blood sugar. The active ingredients contained are widely concerned by scholars. This paper comprehensively summarized the chemical constituents and pharmacological activities of Dendrobium plants reported so far. The chemical constituents isolated from Dendrobium plants are mainly alkaloids, sesquiterpenoids, flavonoids, fluorenones, coumarins, bibenzyls, phenanthrenes, lignans, steroids, phenols, and polysaccharides. This paper is expected to provide a reference for further research, development, and utilization of Dendrobium plants.

Research progress on chemical constituents and pharmacological activities of Potentilla / 中国中药杂志

There are 200-500 species of Potentilla(Rosaceae) worldwide, among which 90 species are widely distributed in China and have a long history of ethnic medicinal use. According to our statistics, a total of 367 compounds have been isolated and identified from plants of this genus, including terpenoids, flavonoids, phenolic acids, tannins, and phenylpropanoids. The medicinal materials made from these plants mainly have antioxidative, blood sugar-lowering, anti-inflammatory, anti-tumor, cardiovascular system-protecting, neuroprotective, and hepatoprotective activities. This study systematically reviews the research progress on chemical constituents and pharmacological activities of Potentilla plants to provide a basis for further research and clinical application.

Research Progress of Quercetin in Treatment of Rheumatoid Arthritis / 中国实验方剂学杂志

Rheumatoid arthritis （RA） is a chronic and systemic autoimmune disease with aggressive and symmetrical polyarthritis as the main clinical manifestations. The exact pathogenesis is unknown. Its basic pathological changes include chronic inflammation of the joint synovium， increased joint cavity effusion， pannus formation， gradual cartilage damage and bone erosion， eventually leading to joint deformity and loss of function. It has been found that the onset and development of RA are related to heredity， environment and other factors. The drugs for RA mainly include non-steroidal anti-inflammatory drugs （NSAIDs）， corticosteroids， disease-modifying anti-rheumatic drugs （DMARDs） and biological agents. However， long-term use of these drugs can cause a variety of side effects and adverse reactions， such as myocardial infarction， peptic ulcer， poor wound healing， and liver and kidney dysfunction. In addition， natural medicines have a good application prospect because of their various pharmacological activities and few side effects. Quercetin is a flavonoid found in Morus alba and tetrandrine， with diverse pharmacological activities， including cardiovascular diseases， joint movement， tumor immunology and so on. Not only have the clinical trials shown good efficacy of quercetin， but the experimental studies have also proven that quercetin can improve RA by reducing inflammatory response， inhibiting the formation of synovial pannus， synovial hyperplasia， neutrophil NETs formation， osteoclast function， regulating Th17/Treg balance and other mechanism. In this article， we will briefly summarize the regulatory mechanism of quercetin and discuss the complexed effect of quercetin on rheumatoid arthritis.

Research Status and Comparison on Medicinal Plants of Callerya and Millettia in China / 中国实验方剂学杂志

The Leguminosae perennial vines of Callerya and Millettia have many species and wide distribution， not only can be used for medicines， but also they have ornamental and insecticidal effects. With increasing demand for Spatholobi Caulis， and the reserves of wild medicinal materials are on the verge of exhaustion， resulting in the increasing number of mixtures and substitutes in the market， which makes it urgent to study the origin of Spatholobi Caulis. By referring to related literature， there are three major origins of Spatholobi Caulis， including Callerya， Millettia and Spatholobus. Callerya is separated from Millettia， they are divided and united for many times， now the official website of Flora of China has accepted the revision of them as two genera. This paper intends to compare the chemical components and pharmacodynamic effects of Callerya and Millettia， aiming to explore the similarities and differences between the two genera， so as to determine the rationality and necessity of separating Callerya from Millettia. After comparing， it was found that the chemical composition and pharmacodynamic effects of the two genera were different， which supported the separation of Callerya from Millettia， and it was not recommended to mix use of them.