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Curvularin derivatives from hydrothermal vent sediment fungus Penicillium ***-50 guided by molecular networking and their antiinflammatory activity

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chinese Journal of Natural medicines 2025年第1期23卷 119-128页

作者： Chunxue Yu Zixuan Xia Zhipeng Xu Xiyang Tang Wenjuan Ding Jihua Wei Danmei Tian Bin Wu Jinshan Tang Institute of traditional chinese Medicine and Natural Products College of Pharmacy/Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drug Research/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Ministry of Education (MOE) of China Jinan University School of traditional chinese Materia Medica Shenyang Pharmaceutical University Ocean College Zhejiang UniversityZhoushan Campus

Guided by molecular networking, nine novel curvularin derivatives（1-9） and 16 known analogs（10-25） were isolated from the hydrothermal vent sediment fungus Penicillium sp. HL-50. Notably, compounds 5-7 represented a hybrid of curvularin and purine. The structures and absolute configurations of compounds 1-9 were elucidated via nuclear magnetic resonance（NMR） spectroscopy, X-ray diffraction, electronic circular dichroism（ECD） calculations,13C NMR calculation, modified Mosher's method, and chemical derivatization. Investigation of anti-inflammatory activities revealed that compounds 7-9, 11, 12, 14, 15, and 18 exhibited significant suppressive effects against lipopolysaccharide（LPS）-induced nitric oxide（NO）production in murine macrophage RAW264.7 cells, with IC50values ranging from 0.44 to 4.40μmol·L-1. Furthermore, these bioactive compounds were found to suppress the expression of inflammation-related proteins, including inducible NO synthase（i NOS）, cyclooxygenase-2（COX-2）, NLR family pyrin domain-containing protein 3（NLRP3）, and nuclear factor kappa-B（NF-κB）. Additional studies demonstrated that the novel compound 7 possessed potent antiinflammatory activity by inhibiting the transcription of inflammation-related genes, downregulating the expression of inflammation-related proteins, and inhibiting the release of inflammatory cytokines, indicating its potential application in the treatment of inflammatory diseases.

关键词： Anti-inflammatory activity Curvularin derivatives Molecular networking Penicillium sp. HL-50

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Analysis of the anti-T2DM components in dichloromethane fraction of Schisandra sphenanthera and its mechanism

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traditional Medicine Research 2025年第1期10卷 27-43页

作者： Shi-Bo Feng Hai-Hui Jiang Hui-Li Kang Yi Jiang Hua-Wei Zhang Xiao-Mei Song Yu-Ze Li Wen-Li Huang Dong-Dong Zhang Chong Deng School of Pharmacy Shaanxi University of Chinese MedicineXianyang 712046China School of Pharmacy and Shaanxi Qinling application development and engineering Center of chinese Herbal Medicine Shaanxi University of Chinese MedicineXianyang 712046China Key laboratory for Research and development of“Qin Medicine”of Shaanxi Administration of traditional chinese Medicine Xianyang 712046China Shaanxi Key laboratory of Research and application of“Taibai Qi Yao” Xianyang 712046China

Background:The type 2 diabetes mellitus(T2DM)pharmacodynamic study of various parts of Schisandra sphenanthera was conducted in the previous stage,and it was found that dichloromethane extracted part(SDP)had a significant hypoglycemic ***,the components of SDP were analyzed,and the specific mechanism of its anti-T2DM was ***:We used a high-fat,high-sugar diet in combination with streptozotocin to induce a T2DM rat model,and the model rats were divided into two groups according to body weight and blood ***,oral glucose tolerance test,fasting blood glucose,low density lipoprotein cholesterol,superoxide dismutase,insulin,glycated hemoglobin,total cholesterol,nonesterified free fatty acids,alanine aminotransferase,high-density lipoprotein cholesterol,aspartate aminotransferase,malondialdehyde,and glutathione peroxidase were measured,organ indices were calculated,and pathological sections of pancreas and liver were *** 16S rRNA V3–V4 region of intestinal flora was sequenced to explore the effect of SDP on biochemical indicators and intestinal *** on the above indicators,the anti-T2DM mechanism of SDP in Schisandra sphenanthera was ***:After six weeks of administration,the biochemical indices of diabetic rats were diminished compared to the control *** SDP could significantly increase the gut microbialα-diversity index,resulting in significant changes in the flora of T2DM rats,with increased richness and diversity,reduced harmful flora,and significantly back-regulated the levels of acetic acid,propionic acid,and butyric ***:SDP can improve the symptoms associated with elevated blood glucose,dyslipidemia,elevated fasting insulin levels,and damaged glucose tolerance in *** against T2DM may be through the control of intestinal flora to normalize and exert anti-diabetic effect;its main active components may be lignans and terpenoids.

关键词： Schisandra sphenanthera T2DM intestinal flora HPLC

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Highly anticipated natural diterpenoids as an important source of new drugs in 2013-2023

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chinese Chemical Letters 2025年第1期36卷 119-136页

作者： Yingjie Wang Peng Tang Wenchao Tu Qi Gao Cuizhu Wang Luying Tan Lixin Zhao Hongye Han Liefeng Ma Kouharu Otsuki Weilie Xiao Wenli Wang Jinping Liu Yong Li Zhajun Zhan Wei Li Xianli Zhou Ning Li School of traditional chinese Materia Medica Key Laboratory of Innovative Traditional Chinese Medicine for Major Chronic Diseases of Liaoning provinceKey Laboratory for TCM Material Basis Study and Innovative Drug Development of Shenyang CityShenyang Pharmaceutical UniversityShenyang 110016China Key laboratory of Medicinal Chemistry for Natural Resource Ministry of EducationYunnan Characteristic Plant Extraction LaboratoryYunnan Key Laboratory of Research and Development for Natural ProductsSchool of Pharmacy and School of Chemical Science and TechnologyState Key Laboratory for Conservation and Utilization of Bio-Resources in YunnanYunnan UniversityKunming 650091China School of Pharmacy Nantong UniversityNantong 226001China School of Pharmaceutical Sciences Jilin UniversityChangchun 130021China State Key laboratory of Bioactive Substance and Function of Natural medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China College of Pharmaceutical Sciences Zhejiang University of TechnologyHangzhou 310014China Faculty of Pharmaceutical Sciences Toho UniversityFunabashiChiba 274-8510Japan School of Life Science and engineering Southwest Jiaotong UniversityChengdu 610031China

This review covers the structures of diterpenoids,including chain(72),monocyclic(9),labdane-type(67),clerodane-type(127)abietane-type(716),ent-kaurane-type(89),grayanane-type(331),ingenanetype(55),tigliane-type(154),daphnane-type(237),and aconitine-type diterpene alkaloids(265)with rich biological activities reported in *** the drugs in clinical use or under clinical investigation of diterpenoids and leading compounds were summarized.

关键词： Natural diterpenoids Structures Bioactivities Druggability Leading compounds New drugs

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Astragali Radix-Notoginseng Radix et Rhizoma medicine pair prevents cardiac remodeling by improving mitochondrial dynamic balance

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chinese Journal of Natural medicines 2025年第1期23卷 54-63页

作者： Pingping Lin Hong Chen Zekun Cui Boyang Yu Junping Kou Fang Li Jiangsu Key laboratory of TCM Evaluation and Translational Research Research Center for Traceability and Standardization of TCMs School of Traditional Chinese PharmacyChina Pharmaceutical University

Astragali Radix(AR) and Notoginseng Radix et Rhizoma(NR) are frequently employed in cardiovascular disease treatment. However, the efficacy of the AR-NR medicine pair(AN) in improving cardiac remodeling and its underlying mechanism remains unclear. This study aimed to evaluate AN's cardioprotective effect and potential mechanism on cardiac remodeling using transverse aortic constriction(TAC) in mice and angiotensin II(Ang II)-induced neonatal rat cardiomyocytes(NRCMs) and fibroblasts in vitro. High-performance liquid chromatography-quadrupole-time of flight tandem mass spectrometry(HPLC-Q-TOF-MS/MS) characterized 23 main components of AN. AN significantly improved cardiac function in the TAC-induced mice. Furthermore, AN considerably reduced the serum levels of N-terminal pro-B-type natriuretic peptide(NT-pro BNP), cardiac troponin T(CTn-T), and interleukin-6(IL-6) and mitigated inflammatory cell infiltration. Post-AN treatment, TAC-induced heart size approached normal. AN decreased cardiomyocyte cross-sectional area and attenuated the upregulation of cardiac hypertrophy marker genes(ANP, BNP, and MYH7) in vivo and in ***, AN alleviated collagen deposition in TAC-induced mice. AN also reduced the expression of fibrosis-related indicators(COL1A1 and COL3A1) and inhibited the activation of the transforming growth factor-β1(TGF-β1)/mothers against decapentaplegic homolog 3(Smad3) pathway. Thus, AN improved TAC-induced cardiac remodeling. Moreover, AN downregulated p-dynamin-related protein(Drp1)(Ser616) expression and upregulated mitogen 2(MFN-2) and optic atrophy 1(OPA1) expression in vivo and in vitro, thereby restoring mitochondrial fusion and fission balance. In conclusion, AN improves cardiac remodeling by regulating mitochondrial dynamic balance, providing experimental data for the rational application of chinese medicine prescriptions with AN as the main component in clinical practice.

关键词： Astragali Radix−Notoginseng Radix et Rhizoma medicine pair Cardiac fibrosis Cardiac hypertrophy Mitochondrial dynamics Transforming growth factor-β1/Smad3 pathway

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Promotion of chronic wound healing by plant-derived active ingredients and research progress and potential of plant polysaccharide hydrogels

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chinese Herbal medicines 2025年第1期17卷 70-83页

作者： Ru Yan Yanhong Wang Weinan Li Jialin Sun School of Pharmacy Heilongjiang University of Chinese Medicine Key laboratory of Basic and application Research of Beiyao Ministry of Education Heilongjiang University of Chinese Medicine Department of Medicine Heilongjiang Minzu College Postdoctoral Research Station Heilongjiang University of Chinese Medicine

Wound healing is a complex biochemical *** use of herbal medicine in wound healing not only carries forward the wisdom of traditional medicine,with its anti-inflammatory and immune-regulating effects,but also reflects the direction of modern biopharmaceutical technology,such as its potential in developing new biomaterials like *** article first outlines the inherent structural properties of healthy skin,along with the physiological characteristics related to chronic wounds in patients with diabetes and ***,the article delves into the latest advancements in clinical and experimental research on the impact of active constituents in herbal medicine on wound tissue regeneration,summarizing existing studies on the mechanisms of various herbal medicines in the healing of diabetic and burn ***,the paper thoroughly examines the application and mechanisms of plant polysaccharide hydrogels containing active herbal compounds in chronic wound *** primary objective is to provide valuable resources for the clinical application and development of herbal medicine,thereby maximizing its therapeutic *** also represents the continuation of traditional medical wisdom,offering new possibilities for advancements in regenerative medicine and wound care.

关键词： active ingredient herbal medicine hydrogel polysaccharides in traditional herbal medicine wound healing

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Discovery and bioassay of disubstituted β-elemene-NO donor conjugates:synergistic enhancement in the treatment of leukemia

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chinese Journal of Natural medicines 2023年第12期21卷 916-926页

作者： ZHU Junlong JIANG Xiaoying LUO Xinyu GAO Yuan ZHAO Rui LI Junjie CAI Hong DANG Xiawen YE Xiangyang BAI Renren XIE Tian School of Pharmacy Hangzhou Normal UniversityHangzhou 311121China Key laboratory of Elemene Class Anti-cancer chinese medicines Engineering Laboratory of Development and Application of Traditional Chinese MedicinesCollaborative Innovation Center of Traditional Chinese Medicines of Zhejiang ProvinceHangzhou Normal UniversityHangzhou 311121China

Natural products are essential sources of antitumor *** such molecule,β-elemene,is a potent antitumor compound extracted from Curcuma *** the present investigation,a series of novel 13,14-disubstituted nitric oxide(NO)-donorβelemene derivatives were designed,withβ-elemene as the foundational compound,and subsequently synthesized to evaluate their therapeutic potential against ***,the derivative labeled as compound 13d demonstrated a potent anti-proliferative activity against the K562 cell line,with a high NO *** vivo studies indicated that compound 13d could effectively inhibit tumor growth,exhibiting no discernible toxic ***,a significant tumor growth inhibition rate of 62.9%was observed in the K562 xenograft tumor mouse *** accumulated data propound the potential therapeutic application of compound 13d in the management of leukemia.

关键词： Antitumor activity Chronic myeloid leukemia β-elemene Nitric oxide donor Structural modification

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An Empathic Pain-Regulated Neural Circuit

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Neuroscience Bulletin 2022年第12期38卷 1613-1616页

作者： Xiumin Xue Qian Wang Zhihui Huang Yongjie Wang School of Pharmacy Hangzhou Normal UniversityHangzhou 311121China Key laboratory of Elemene Class Anti-Cancer chinese medicines Engineering Laboratory of Development and Application of Traditional Chinese MedicinesCollaborative Innovation Center of Traditional Chinese Medicines of Zhejiang ProvinceHangzhou Normal UniversityHangzhou 311121China

Empathy is a general term in psychology that refers to the correct understanding of the feelings and emotions of others,so as to achieve mutual understanding,care,and *** behavior is common in rodents[1],and various e... 详细信息

关键词： mutual harmony happiness

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Loss of C9orf72 in Microglia Drives Neuronal Injury by Enhancing Synaptic Pruning in Aged and Alzheimer’s Disease Mice

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Neuroscience Bulletin 2022年第3期38卷 327-330页

作者： Mengmeng Wang Yuanyuan Jiang Zhihui Huang School of Pharmacy Hangzhou Normal UniversityHangzhou311121China Key laboratory of Elemene Class Anti-Cancer chinese medicines Engineering Laboratory of Development and Application of Traditional Chinese MedicinesCollaborative Innovation Center of Traditional Chinese Medicines of Zhejiang ProvinceHangzhou Normal UniversityHangzhou311121China

Many diseases are caused by the expansion of simple sequence repeats scattered throughout the human genome;they are defined as repeat expansion *** size of the repeat unit ranges from trinucleotides(the vast majority)to tetranucleotides,pentanucleotides,hexan cleotides,and even dodecanucleotides[1].Expansions of the hexanucleotide GGGGCC in the C9orf72 gene are the most frequent genetic cause of amyotrophic lateral sclero・sis(ALS)and frontotemporal dementia(FTD)[2].In addition to ALS and FTD,C9orf72 repeat expansions may also be associated with Alzheimer's disease(AD),since the rate of such expansions in AD cases(0.57%)is higher than normal(0.11%)[3].However,the exact role of C9orf72 in AD is still unclear.

关键词： C9orf72 Alzheimer diseases

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Astrocyte-Derived Saturated Lipids Mediate Cell Toxicity in the Central Nervous System

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Neuroscience Bulletin 2022年第6期38卷 699-702页

作者： Yiming Qian's Mengmeng Wang Jianhong Dong Yuanyuan Jiang Zhihui Huang School of Pharmacy Hangzhou Normal UniversityHangzhou 311121China Key laboratory of Elemene Class Anti-Cancer chinese medicines Engineering Laboratory of Development and Innovation Center of Traditional Chinese Medicines of Application of Traditional Chinese MedicinesCollaborative Zhejiang ProvinceHangzhou Normal UniversityHangzhou 311121China

Astrocytes,the most abundant cells in the central nervous system(CNS),have a variety of functions such as providing nutrients for neurons,facilitating the formation and functioning of synapses,pruning synapses through phagocytosis,and maintaining homeostasis[1].As a response to CNS injury and disease,quiescent astrocytes are transformed into reactive astrocytes,which usually can be divided into two types:Al and A2[2].Al astrocytes help to drive the death of neurons and oligodendrocytes in neurodegenerative disorders by producing a large number of inflammatory factors and secreted toxins,while A2 astrocytes protect neurons via releasing many neurotrophic factors[3].

关键词： homeostasis cytes releasing

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Sodium-Calcium Exchanger-3 Plays Critical Roles in Pain"Wind-up"

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Neuroscience Bulletin 2023年第5期39卷 869-872页

作者： Lin Lin Xiumin Xue Zhihui Huang Yongjie Wang School of Pharmacy Hangzhou Normal UniversityHangzhou 311121ZhejiangChina Key laboratory of Element Class Anti-Cancer chinese medicines Engineering Laboratory of Development and Application of Traditional Chinese MedicinesCollaborative Innovation Center of Traditional Chinese Medicines of Zhejiang ProvinceHangzhou Normal UniversityHangzhou 311121ZhejiangChina

Chronic pain,broadly described as pain lasting longer than 3 months,is a classic example of gene-environment interaction[1].A couple of types of chronic pain have also been shown to have complex heritable properties with a polygenic component[2].Quantitative Sensory Testing(QST)is a formal variant of the sensory examination,including"static"sensory profiling and"dynamic"*** contributes to the prediction of vulnerable subpopulations and effective *** addition,a deficit in dynamic QST has been proposed as a predictor of chronic pain[3].

关键词： pain formal Wind

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