Natural products as a crucial source of anti-inflammatory drugs: recent trends and advancements

Natural active molecules are key sources of modern innovative drugs. Particularly, a great amount of natural active molecules have been reported to possess promising therapeutic effects on inflammatory diseases, including asthma, rheumatoid arthritis, hepatitis, enteritis, metabolic disorders and neurodegenerative diseases. However, these natural active molecules with various molecular structures usually exert anti-inflammatory effects through diversiform pharmacological mechanisms, which is necessary to be summarized systematically. In this review, we introduced the current major anti-inflammatory natural active molecules based on their chemical structures, and discussed their pharmacological mechanisms including anti-inflammatory molecular signaling pathways and potential target proteins, which providing a referential significance on the development of novel anti-inflammatory drugs, and also revealing new therapeutic strategies for inflammatory diseases.

An Explorer of Chemical Biology of Plant Natural Products in Southwest China,Xiaojiang Hao

Xiaojiang Hao,who obtained Master Degree from Kunming Institute of Botany(KIB),Chinese Academy of Sciences(CAS)in 1985,and Doctor in Pharmacy degree in Pharmacy from Institute for Chemical Research,Kyoto University,in 1990,was born in Chongqing in July,1951.In 1991,he returned to KIB,CAS,as an Associate professor and served as the chair of the Department of Phytochemistry.In 1994,he was promoted to a full professor at the current institute.He served as the Deputy Director of KIB and the Director of Open Laboratory of Phytochemistry from 1995 to 1997,and the Director of KIB from 1997 to 2005.Professor Hao has published more than 450 peer-reviewed SCI papers,which have been cited over 6000 times.He has obtained one PCT patent and 23 patents in China.Due to his tremendous efforts,one candidate drug,phenchlobenpyrrone,has entered the Phase II clinical trail for the treatment of Alzheimer’s disease.Moreover,he won the First Prize of Natural Sciences in Yunnan Province for three times,and Ho Leung Ho Lee Fund Science and Technology Innovation Award in 2017.

Natural Products as Potential Leads Against Coronaviruses: Could They be Encouraging Structural Models Against SARS-CoV-2?

New coronavirus referred to SARS-CoV-2 has caused a worldwide pandemic(COVID-19)declared by WHO.Coronavirus disease 2019(COVID-19)is an infectious disease with severe acute respiratory syndrome caused by coronavirus-2(SARS-CoV-2).SARS-CoV-2 is akin to SARS-CoV,which was the causative agent of severe acute respiratory syndrome(SARS)in 2002 as well as to that of Middle East respiratory syndrome(MERS)in 2012.SARS-CoV-2 has been revealed to belong to Coronaviridiae family as a member ofβ-coronaviruses.It has a positive-sense single-stranded RNA with the largest RNA genome.Since its genomic sequence has a notable similarity to that of SARS-CoV,antiviral drugs used to treat SARS and MERS are now being also applied for COVID-19 treatment.In order to combat SARS-CoV-2,many drug and vaccine development studies at experimental and clinical levels are currently conducted worldwide.In this sense,medicinal plants and the pure natural molecules isolated from plants have been reported to exhibit significant inhibitory antiviral activity against SARS-CoV and other types of coronaviruses.In the present review,plant extracts and natural molecules with the mentioned activity are discussed in order to give inspiration to researchers to take these molecules into consideration against SARS-CoV-2.

Antimicrobial and antioxidant properties of medicinal plants used by the Bentian tribe from Indonesia

Some selected medicinal plants used by Bentian tribe from Indonesia were evaluated for potential antimicrobial and antioxidant properties.The leaves stem bark and root of the plants were extracted with n-hexane,ethyl acetate and ethanol to give respective extracts.Antimicrobial activity against Propionibacterium acnes and Candida albicans was determined by an agar well diffusion method.Antioxidant activity was assayed by the DPPH radical scavenging activity mechanism.The results showed that n-hexane,ethyl acetate and ethanol extracts of Cananga odorata,ethanolic extract of Chromolaena odorata,and ethanolic extracts of Hyptis capitata and Ampelocissus cinnamomeae displayed good activity against P.acnes at 25–400μg/well of the extracts tested.The n-hexane and ethanol extracts of Chromolaena odorata and H.capitata,and the n-hexane,ethyl acetate and ethanol extracts of Cananga odorata displayed more activity against C.albicans than others at 25–400μg/well of the extracts tested.The most antioxidant activities against DPPH were displayed by the ethanol extracts of Ficus variegata stem bark,Leucosyke quadrinerva root and Clausena excavata leaves exhibiting 91%,91%and 86%inhibition,respectively.The present results showed potential of some medicinal plants used by Bentian tribe from Indonesia as natural anti-microbial and anti-oxidant and potentially anti-inflammatory agents.

Strategies on biosynthesis and production of bioactive compounds in medicinal plants

Medicinal plants are a valuable source of essential medicines and herbal products for healthcare and disease therapy.Compared with chemical synthesis and extraction,the biosynthesis of natural products is a very promising alternative for the successful conservation of medicinal plants,and its rapid development will greatly facilitate the conservation and sustainable utilization of medicinal plants.Here,we summarize the advances in strategies and methods concerning the biosynthesis and production of natural products of medicinal plants.The strategies and methods mainly include genetic engineering,plant cell culture engineering,metabolic engineering,and synthetic biology based on multiple“OMICS”technologies,with paradigms for the biosynthesis of terpenoids and alkaloids.We also highlight the biosynthetic approaches and discuss progress in the production of some valuable natural products,exemplifying compounds such as vindoline(alkaloid),artemisinin and paclitaxel(terpenoids),to illustrate the power of biotechnology in medicinal plants.

Click chemistry and natural products

The 2022 Nobel Prize in Chemistry was awarded to American scientists Carolyn Bertozzi,K.Barry Sharpless,and Danish scientist Morten P.Merdahl for their contributions to the development of click chemistry and bioorthogonal chemistry.

Screening and identifying natural products with SARS-CoV-2 infection inhibitory activity from medicinal fungi

The coronavirus disease of 2019(COVID‐19),a global pandemic caused by the severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2),can result in severe health complications.In addition to physical preventative measures,pharmaceutical intervention is also crucial.Numerous natural products from medicinal fungi have shown promise as potential antiviral drugs and may serve as a source of effective components with antiviral activity against SARS‐CoV‐2 and other coronaviruses.In this study,we developed a workflow that integrates viral infection inhibition assays at both cellular and molecular levels,as well as molecular separation and characterization,to screen and identify natural products with antiviral activity.Using this workflow,we screened 167 extracts extracted from 36 medicinal fungi using optimized extraction methods.We assessed the antiviral effects of these extracts by measuring their ability to inhibit SARS‐CoV‐2 infection and receptor binding domain‐human angiotensin‐converting enzyme 2(RBD‐hACE2)binding in vitro.Following charge‐and size‐based characterization of the active compounds through filtration and chromatographic fractionation,mass spectrometry characterization of the fractionated compounds revealed that the active components are polysaccharides and determined their monosaccharide residue composition.Our findings provide new insights into the antiviral potential of natural products and their screening strategies and may contribute to the development of effective antiviral therapeutics against COVID‐19 and other diseases.

Control of autoimmune arthritis by herbal extracts and their bioactive components

Autoimmune diseases such as rheumatoid arthritis (RA) cause significant morbidity and loss of productivity. Many potent conventionally used drugs are available for these diseases, but their prolonged use is accompanied by severe adverse effects besides a high cost.Therefore, there is an unmet need for effective but less expensive medications for RA and other autoimmune diseases. Natural plant products belonging to the traditional systems of medicine, such as the traditional Chinese medicine and Indian Ayurvedic medicine, offer a vast and promising resource in this regard. However, herbal medicinal products are often poorly characterized for their composition as well as mechanisms of action. We review here the results of our systematically performed studies aimed at defining the anti-arthritic activity of three herbal extracts, namely, modified Huo-luo-xiao-ling dan (HLXL), Celastrus aculeatus Merr., and polyphenolic fraction of green tea (Camellia sinensis), as well as a purifiedcompound Celastrol, a bioactive component of Celastrus. Specifically, we examined the effects of these herbal products on the immunological, biochemical and molecular biological effector pathways in autoimmune arthritis. We have also reviewed here related studies on these herbal products by other investigators. Taken together, we suggest further testing of these herbal products in RA patients.

Research Progress on the Natural Anti-peptic Ulcer Chemical Structures

Natural products provide an important original source of structural diversity for finding new compounds as anti-peptic ulcer drugs. The present review highlights some recent advances on gastro-protective flavonoids, terpenes, alkaloids, steroids, phenylpropanoids,glycosides and chromenes from natural herbs or traditional medicinal plants, and helps us analyze the structure-activity relationship(SAR) of natural products in healing of peptic ulcer for further drug development.

Natural Products Potential and Scope for Modern Cancer Research

In the present time Natural products are considered to be symbols of protection in comparison to the synthetic product that are regarded as unsafe to human life and environment. Although a large number of synthetic drugs are being added to the world of present pharmacopoeia, but still no system of medicine in the world has been able to solve all the health problems, which include diseases like Cancer. Therefore the search for innovative therapeutic constituents from plants is genuine and urgent. In India, there is an ocean of knowledge about medicinal plants and rich medicinal flora, but still only a few pearls have been searched as therapeutic agents. There are large numbers of original plants left which have not been investigated thoroughly from modern scientific view or their healing values have not been known. Thus there is an insistent need for systematic phytochemical examination of those plants which have not been investigated scientifically. More research can be done to investigate the unknown and unexplored potential of plants. Further analysis of plants (active compounds) can be carried out by way of making use of different analytical methods such as HPTLC, HPLC, NMR and UV spectrophotometer analysis or computer based drug designing.

Synthesis of Cytotoxic Sinapyl Alcohol Derivatives fromLigularia nelumbifolia

Total synthesis of two cytotoxic natural products, nelumol A (1) and nelumal A (2), were carried out by two different paths. 4-O-Benzyl substitute analogues 26 and 27, as well as the 4-O-(2-methyl-butenyl) derivatives 29 and 30 were also synthesized for a SAR investigation. 1 and 2 were also measured on different tumor cell line.

Thai traditional medicine development:The proposed development model of modern Thai traditional medicine

The development of modern traditional medicine in developing countries is facing challenges,and a potential solution was proposed to resolve these problems.Developing countries are trapped in the vicious circle of the natural product development in the modern scientific paradigm.The application of the ethno research strategy is described to resolve these problems.First,Folk Traditional medicine knowledge inquiry is explored,testified and verified similar to R&D practice in modern biomedicine.

Delineating the role of phytocompounds against anti-bacterial drug resistance–An update

Antibacterial resistance developed by bacteria due to the unlimited use of antibiotics has posed a challenge for human civilization.This kind of problem is not limited to India only,but it is a global concern.Nowadays,many treatments and medicines for bacterial diseases have been developed.However,they possess some drawbacks.Therefore,the alternative medicine has been used to target the drug resistant mechanisms and such medicines have less side effects which is becoming necessary.Natural products have traditionally or historically been of importance for the development of antibacterial agents and are also known to overcome bacterial drug resistance by directly targeting the drug resistance mechanisms in bacteria.In recent years,researchers have also focused on new drug discovery from plant-based research.They have looked on various phytocompounds as antibacterial agents.In the current review,we report various classes of secondary metabolites such as phenolic compounds,flavonoids,alkaloids,saponins,terpenes,quinones,and some essential oils that have been used as an antibacterial agent.In addition,we also discuss several mechanisms behind bacterial multi-drug resistance that are used during bacterial pathogenesis.

Allelopathy of Medicinal Plants: Current Status and Future Prospects in Weed Management

An attempt has been made in this article to accumulate and elucidate the literatures about the allelopathic potentiality of medicinal plants, and its role on the development of bio-herbicides for eco-friendly weed management strategies to conserve bio-diversity and ecological balance. This review paper has been prepared by comprehensive studies of various published research articles, books and proceedings available in the world literature. The farmers of different countries use several weed management techniques in order to minimize the deleterious effect of weeds. Among them most commonly used practice is application of herbicides due to its high efficacy and cost effectiveness, less time-consuming nature, flexibility and easy accessibility, and more rapid out return. Although use of synthetic herbicides in the crop fields has increased the crop production as well as the productivity by reducing the weed infestation, over time it causes a number of environmental hazards. Hence, to avoid these detrimental effects of synthetic herbicide, a lot of efforts have been dedicated by the researchers to search the novel natural plant products mainly allelochemicals and try to apply them as a tool for the development of bio-degradable natural herbicides. This paper intended to reflect the current state of allelopathic medicinal plants and their potentiality to develop eco-friendly and natural product-based herbicides for sustainable agriculture, and to invite further debate on this issue.

Recent advances in research on natural product inhibitors of SREBPs

Sterol regulatory element-binding proteins(SREBPs)are a class of cholesterol-sensitive transcription factors that play important roles in lipid metabolism.Natural product inhibitors of SREBPs have been shown to inhibit the synthesis of free fatty acids and cholesterol,promote the burning of brown fat,and relieve insulin resistance by inhibiting different links during the synthesis,cleavage,and transport of SREBPs,thereby improving obesity,diabetes,atherosclerosis,and other metabolic diseases and disorders.There are numerous Chinese herbal medicines with verified efficacy in the treatment of metabolic diseases,including Coptis chinensis Franch.and Pueraria peduncularis Grah.for diabetes,Pueraria peduncularis Grah.,Epimedium brevicornum Maxim.,and Panax ginseng C.A.Meyer for osteoporosis,and Nelumbo nucifera Gaertn.and Poria cocos(Schw.)Wolf.for obesity.Present-day research on the mechanisms underlying the activity of traditional Chinese medicine has indicated that certain chemical components of these traditional preparations can be used to treat metabolic diseases by inhibiting SREBPs.Progress in the research on natural product SREBP inhibitors is continuing apace,and the mechanisms of action of certain small molecules have become well established.In this study,we review recent progress in the research on natural small-molecule inhibitors of SREBPs,including flavonoids,saponins,triterpenoids,and alkaloids,which we hope will provide a useful reference for future research and development of drugs for the treatment of metabolic diseases.

The Effect of the Extracts of Endophytic Fungi on Pancreatic a-Amylase Activity

Inhibitors of pancreatic a-amylase offer an effective strategy to lower the levels of postprandial hyperglycemia by controlof starch breakdown. Among 86 fungal endophytes isolated from 15 medicinal plants Aspergillus terreus-AFl04S, Aspergillusegypticus-HT166S and Penicillium sp.-CC200 exhibited strong pancreatic amylase inhibitory potential were selected. Endophyteswere subjected to ethyl acetate extraction and tested for a-amylase inhibition, in order to assess and evaluate their inhibitory potentialon pancreatic a-amylase. Analysis showed concentration dependent enzyme inhibition up to 83% with half inhibition （IC50） valuesfor less 25 mg.mL1, which is lower than acarbose as control. It was observed 3-fold increasing of Vmax and maintenance Km atcontrol level in the presence of extracts A. terreus-AFl04S and Penicillium sp.-CC200, while in presence of extract A.egypticus-HT166S Km was doubled, and Vmax was maintained at the control level. Kinetic studies allow proposing the competitivemode of a-amylase inhibition by extracts A. egypticus-HT166S and uncompetitive inhibition by extracts A, terreus-AFl04S andPenicillium sp.-CC200.

Exploitation of Pangolins (Pholidota, Mammalia) by Communities Living in and around the Tayna Nature Reserve (RNT) North Kivu, Democratic Republic of Congo (DRC)

Pangolin exploitation has recently increased in diverse forms such as bushmeat consumption;species or parts trade, medical use. This species is protected in Democratic Republic of Congo (DRC) and worldwide, unfortunately it is threatened by numerous human actions. The purpose of this study was to determine the profiles of actors using pangolins, the reasons for pangolin exploitation and its products and their use within the local community in and surrounding the reserve. We carried out surveys in the households of hunters, farmers and people practicing other professions in 12 villages, located within the Tayna Nature Reserve (RNT) and surroundings areas. Two interview techniques were used: the individual interview and the participatory diagnostic technique. During one month of data collection, 175 respondents were interviewed. Respondents had diverse profiles according to sex, age, education level and ethnicity. Men were more represented as actors in pangolin exploitation (71.70%) than women (28.30%);the most represented age interval was 20 - 30 years. The education level is distinct amongst respondents: illiterate (37%), primary school (32.4%) and graduate from university (2.9%). An average number of respondents are motivated to consume pangolin as meat obtained by hunting at 50%. The main reason for its consumption is preference (44%) and habit (33%). The scales are pangolin derivatives most recognized by local people and widely used in the pharmacopoeia. Consequently, pangolin protection needs some rigorous measures to reinforce the current law implementation.

Inhalation therapy for pulmonary fibrosis:chemical medicines and herbal medicines

Pulmonary fibrosis(PF)is a chronic,progressive,and irreversible pulmonary interstitial disease with unclear pathogenesis.Currently,there are few treatment options for managing PF.Inhalation therapy,as a routine treatment for respiratory diseases,is being used to study the treatment of PF.Some herbal medicines and their active ingredients have been reported to have anti-PF effects.This review aims to provide an overview of the latest developments in inhalation therapy,focusing on the utilization of chemical medicines and herbal medicines for the treatment of PF in both clinical practice and basic research.The inhalation of chemical drugs such as pirfenidone,nintedanib,N-acetylcysteine,and interferon-γhas been shown to demonstrate anti-PF effects.Additionally,the inhalation of various natural products derived from herbal medicines,encompassing polyphenols,alkaloids,flavonoids,saponins,terpenoids,and herbal extracts,contributes to the therapeutic management of PF through diverse mechanisms.The inhalation of both chemical and herbal medicines presents promising advantages in the treatment of PF.Further clinical trials are required to investigate the effectiveness,safety,and mechanism of action of inhalation therapy utilizing natural products derived from herbal medicines.

基于雨课堂与SPOC嵌合的天然药物化学混合式教学研究

为进一步深化天然药物化学教学改革,尝试打造雨课堂与SPOC嵌合的天然药物化学智慧课堂,实施混合式教学。打造的智慧课堂可以同时发挥雨课堂与SPOC的优势,活跃课堂气氛,调动学生的学习积极性,帮助其将课堂知识与科研工作衔接起来,培养科研思维。

基于课程思政的《天然药物化学》教学实践

《天然药物化学》是西昌学院动物科学学院制药工程专业的专业基础课,也是一门具丰富课程思政元素的课程。为达到“立德树人”、培养“德才兼备”的社会主义接班人与建设者的目的,本课程深入挖掘课程思政元素,实施“三全育人”方式,将思想政治教育融入课堂教育之中,增强了学生对阐释中(彝)医药的科学内涵的热情、民族自信心与自豪感,调动了学生的学习积极性与主动性。同时,教学内容强调“厚基础、强实践,理实结合与学科交叉”,即:理论教学贯彻由浅入深、循序渐进的教学理念;实践教学贯彻应用性的教学理念,加强基础知识与动手能力的培养;而学科交叉强调基于凉山彝医药独特应用的药效物质基础研究以及与动物医药的学科交叉,从而提升了教学效果。因此,笔者总结近年来本课程基于课程思政的教学实践,供同行参考。