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Rhamnus crenata leaf extracts exhibit anti-inflammatory activity via modulating the Nrf2/HO-1 and NF-κB/MAPK signaling pathways

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Asian Pacific Journal of Tropical Biomedicine 2022年第10期12卷 430-436页

作者： Hyun Ji Eo Da Som Kim Gwang Hun Park Special Forest Resources Division Department of Forest Bio-ResourcesNational Institute of Forest ScienceSuwon 16631Korea Forest Medicinal Resources Research Center National Institute of Forest ScienceYeongju 36040Korea

Objective:To elucidate the potential anti-inflammatory mechanisms of Rhamnus crenata leaf extracts using RAW264.7 cells.Methods:We used 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay to measure cell viability.Nitric oxide(NO)production was measured using Griess reagent.Western blotting and RT-PCR assays were carried out for analyzing the protein and gene expressions of pro-inflammatory mediators,respectively.Moreover,PD98059(ERK1/2 inhibitor),SB203580(p38 inhibitor),SP600125(JNK inhibitor),and BAY11-7082(NF-κB inhibitor)were used to evaluate the anti-inflammatory mechanism of Rhamnus crenata leaf extract.Results:Rhamnus crenata leaf extracts significantly inhibited the production of the pro-inflammatory mediators such as NO,iNOS,COX-2,IL-1β,and TNF-αin lipopolysaccharide(LPS)-stimulated RAW264.7 cells.Rhamnus crenata leaf extracts also suppressed LPS-induced degradation of IκB-αand nuclear accumulation of p65,which resulted in the inhibition of NF-κB activation in RAW264.7 cells.Additionally,the extracts attenuated the phosphorylation of p38,ERK1/2,and JNK in LPS-stimulated RAW264.7 cells.Moreover,HO-1 expression induced by Rhamnus crenata leaf extracts was significantly downregulated by SB230580,PD98059,SP600125 and BAY11-7082.Conclusions:Rhamnus crenata leaf extract may upregulate HO-1 expression through inhibition of p38,ERK1/2,and NF-κB activation,which may contribute to the anti-inflammatory activity of the extracts.Rhamnus crenata leaf extracts may have great potential for the development of anti-inflammatory drugs to treat acute and chronic inflammatory diseases.

关键词： anti-inflammatory activity Heme oxygenase-1 Nrf2 Mitogen-activated protein kinase Nuclear factor kappa B Rhamnus crenata

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Extraction,Purification,and anti-inflammatory activity of Steroid Fraction from Physalis Alkekengi L.Var.Franchetii(Mast.)Makino

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World Journal of Traditional Chinese Medicine 2023年第2期9卷 167-177页

作者： Tian-Yi Xia Yi Wang Yan-Ni Yang Wu-Jing Wang Zi-He Ding Ren-Xing Zhong Ying Chen Wei Li Ming-Ming Peng Chuan-Qiu Li Li-Feng Shang Bing Liu Zhen-Yue Wang Chong-Rong Shi Zun-Peng Shu Guangdong Standardized Processing Engineering Technology Research Center of Traditional Chinese Medicine Guangdong Pharmaceutical UniversityGuangzhouP.R.China Department of Traditional Chinese Medicine Guangdong Pharmaceutical UniversityGuangzhouPR.China Guangdong Andao Medical Equipment Co.Ltd GuangzhouPR.China Department of Pharmacy Heilongjiang University of Chinese MedicineHeilongjiangPR.China Macao Association of Chinese Medicine(AIPPMCM) Macao SARPR.China

Objective: As a traditional medicinal plant listed in the Chinese Pharmacopeia, Physalis alkekengi L. var. franchetii(Mast.) Makino(PAF) has a long medicinal history and high economic value. PAF has immunomodulatory properties and can be used to treat acute lung injury and eczema.The aim of this study is to solve the problems of extraction and purification of active components from PAF. Materials and Methods: The solvent to be used for extraction and its concentration, the solid-to-liquid ratio, and extraction duration were investigated using a single-factor experiment.An orthogonal design(L_(9)[3^(4)]) was used to determine the optimum extraction conditions. After optimization, the sample’s concentrations and flow velocity, the eluents and their velocity, adsorption time, and the removed water volume were measured. The content of the five steroids in the sample was determined by high-performance liquid chromatography(HPLC). We also investigated the anti-inflammatory property of PAF calyxes before and after purification. Results: The optimum extraction and purification processes were determined by single-factor analysis.AB-8 was identified as the best macroporous adsorption resin for enrichment. After optimization, the average total steroid content was 71.83%,and the average recovery was 90% after purification. Among the five steroid components detected by HPLC, physalin F showed the highest content. Furthermore, the sample obtained after purification could significantly inhibit paw edema by egg whites induced. Conclusions: An environmentally-sustainable, efficient, and stable process was first optimized for enriching and purifying total steroids from PAF. The process has the potential for further development and utilization in the pharmaceutical industry.

关键词： anti-inflammatory activity extraction and optimization process physalins Physalis alkekengi L.var.francheti(Mast.)Makino steroids

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Three rare anti-inflammatory sesquiterpene lactones from Magnolia grandiflora

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Chinese Journal of Natural Medicines 2024年第3期22卷 265-272页

作者： XU Shuangyu ZHANG Feng TAO Linlan JIANG Yangming HUANG Tao LI Yanan HU Zhanxing YANG Jue HAO Xiaojiang YUAN Chunmao State Key Laboratory of Functions and Applications of Medicinal Plants Guizhou Medical UniversityGuiyang 550014China School of Pharmaceutical Sciences Guizhou Medical UniversityGuiyang 550025China Natural Products Research Center of Guizhou Province Guiyang 550014China State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201China

Four new sesquiterpene lactones(SLs)(1–4),along with a biosynthetically related SL(5),have been isolated from the leaves of Magnolia grandiflora.Magrandate A(1)is notable as the first C18 homogemarane type SL,featuring a unique 1,7-dioxaspiro[4.4]nonan-6-one core.Compounds 2 and 3,representing the first instances of chlorine-substituted gemarane-type SL analogs in natural products,were also identified.The structures of these isolates were elucidated through a combination of spectroscopic data analysis,electronic circular dichroism calculations,and X-ray single-crystal diffraction analysis.All isolates demonstrated anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 cells.Notably,3–5 showed a significant inhibitory effect on nitric oxide production,with IC50 values ranging from 0.79 to 4.73μmol·L^(−1).Additionally,4 and 5 exhibited moderate cytotoxic activities against three cancer cell lines,with IC50 values between 3.09 and 11.23μmol·L^(−1).

关键词： Magnolia grandiflora Sesquiterpene lactones Isolation and identification anti-inflammatory activity

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Isolation and microbial transformation of tea sapogenin from seed pomace of Camellia oleifera with anti-inflammatory effects

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Chinese Journal of Natural Medicines 2024年第3期22卷 280-288页

作者： SHEN Pingping JIANG Xuewa ZHANG Jingling WANG Jiayi Raj Richa LI Guolong GE Haixia WANG Weiwei YU Boyang ZHANG Jian State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 210009China Co-construction Collaborative Innovation Center for Chinese Medicine Resources Industrialization by Shaanxi&Education Ministry Shaanxi Province Key Laboratory of New Drugs and Chinese Medicine Foundation ResearchShaanxi University of Chinese MedicineXianyang 712046China School of Life Sciences Huzhou UniversityHuzhou 313000China Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine Nanjing 210046China Jiangsu Key Laboratory of TCM Evaluation and Translational Research China Pharmaceutical UniversityNanjing 211198China

In the current study,tea saponin,identified as the primary bioactive constituent in seed pomace of Camellia oleifera Abel.,was meticulously extracted and hydrolyzed to yield five known sapogenins:16-O-tiglogycamelliagnin B(a),camelliagnin A(b),16-O-angeloybarringtogenol C(c),theasapogenol E(d),theasapogenol F(e).Subsequent biotransformation of compound a facilitated the isolation of six novel metabolites(a1−a6).The anti-inflammatory potential of these compounds was assessed using pathogenassociated molecular patterns(PAMPs)and damage-associated molecular patterns molecules(DAMPs)-mediated cellular inflammation models.Notably,compounds b and a2 demonstrated significant inhibitory effects on both lipopolysaccharide(LPS)and high-mobility group box 1(HMGB1)-induced inflammation,surpassing the efficacy of the standard anti-inflammatory agent,carbenoxolone.Conversely,compounds d,a3,and a6 selectivity targeted endogenous HMGB1-induced inflammation,showcasing a pronounced specificity.These results underscore the therapeutic promise of C.oleifera seed pomace-derived compounds as potent agents for the management of inflammatory diseases triggered by infections and tissue damage.

关键词： Camellia oleifera Seed pomace Tea sapogenin Microbial transformation Damage-associated molecular patterns and Pathogen-associated molecular patterns anti-inflammatory activity

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Discovery of unusual phloroglucinol-triterpenoid adducts from Leptospermum scoparium and Xanthostemon chrysanthus by building blocks-based molecular networking

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Chinese Chemical Letters 2024年第6期35卷 353-357页

作者： Jinyan Zhang Fen Liu Qian Jin Xueyi Li Qiong Zhan Mu Chen Sisi Wang Zhenlong Wu Wencai Ye Lei Wang State Key Laboratory of Bioactive Molecules and Druggability Assessment Jinan UniversityGuangzhou 510632China Center for Bioactive Natural Molecules and Innovative Drugs and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs ResearchJinan UniversityGuangzhou 510632China College of Pharmacy Jinan UniversityGuangzhou 510632China

The first phloroglucinol-triterpenoid hybrids,myrtphlotritins A-E(1-5),were rapidly recognized and isolated from two species of Myrtaceae by employing the building blocks-based molecular network(BBMN)strategy.Compounds 1-5 featured new carbon skeletons in which phloroglucinol derivatives were coupled with lupane-and dammarane-type triterpenoids through different linkage patterns.Their structures and absolute configurations were elucidated by comprehensive analysis of spectroscopic data and quantum chemical calculations.Biosynthetic pathways for compounds 1-5 were proposed on the basis of the coexisting precursors.Guided by the biogenetic pathways,the biomimetic synthesis of compound 1 was also achieved.Additionally,compounds 2,3,and 5 exhibited potent antiviral activities against herpes simplex virus type-1(HSV-1)infection,and compounds 2 and 5 displayed significant anti-inflammatory activities on RAW264.7 cells.

关键词： Phloroglucinol-triterpenoid adduct Myrtaceae Building blocks-based molecular network Biomimetic synthesis antiviral activity anti-inflammatory activity

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anti-inflammatory activity of Mollugin on DSS-induced Colitis in Mice

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Current Medical Science 2020年第5期40卷 910-916页

作者： Juan LI Jin-ling ZHANG Xue-peng GONG Meng XIAO Yuan-yuan SONG Hui-fang PI Guang DU Department of Pharmacy Tongji HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China Department of Pharmacy The Central Hospital of XianningXianning 437100China School of Pharmacy Tongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China

We aimed to explore the anti-infammatory bactivity of mollugin extracted from Rubia cordifolia L,a traditional Chinese medicine,on dextran sulfate sodium(DSS)-induced ulcerative colitis(UC)in mice.Thirty C57BL/6 mice were divided into a control group(n=6),a model group(n=6),and three experimental groups(40,20,10 mg/kg of mollugin,n=6 each).DSS solution(3%)was given to mice in the model group and experimental groups from day 4 to day 10 to induce the mouse UC model.Mice in the experimental groups were intragastrically administrated mollugin from day 1 to day 10.Animals were orally given distilled water in the control group for the whole experiment time and in the model group from day 1 to day 3.The changes in colon pathology were detected by hematoxylin and eosin(HE)staining.Interleukin-1β(IL-1β)in the serum,and tumor necrosis factor-α(TNF-α)and interferon-γ(IFN)in the tissues were measured by enzyme linked immunosorbent assay.Expression levels of Toll-like receptor 4(TLR4)and myeloid differentiation factor 88 in the colon tissues were detected by immunohistochemistry.Results showed that mollugin could significantly reduce weight loss and the disease activity index in the DSS-induced UC mouse model.HE examinations demonstrated that mollugin treatment effectively improved the histological damage(Pinflammatory chemocytokines.

关键词： mollugin anti-inflammatory activity DSS-induced colitis

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Synthesis, antibacterial and anti-inflammatory activity of bis(indolyl)methanes

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Chinese Chemical Letters 2016年第1期27卷 16-20页

作者： Santhisudha Sarva Jayaprakash Soora Harinath Siva Prasad Sthanikam Selvarajan Ethiraj Mohanasrinivasan Vaithiyalingam Suresh Reddy Cirandur Department of Chemistry Sri Venkateswara University School of Biosciences and Technology VIT University

A series of bioactive bis（indolyl）methanes are synthesized by one-pot green reaction of indole with various substituted aldehydes by microwave irradiation under solvent free conditions. The antibacterial activity against Staphylococcus aureus and anti-inflammatory activity of the synthesized bis（indolyl）-methanes are evaluated in vitro and compared to standard drugs tetracycline and diclofenac,respectively. The majority of the compounds showed good antibacterial and anti-inflammatory activity.Interestingly, compounds 3j, 3i, 3k and 3g exhibited much higher anti-inflammatory activity than the standard diclofenac drug and thus qualify for clinical trials to be used as an anti-inflammatory compound.

关键词： Bis（indolyl）methanes Microwave irradiation antibacterial activity anti-inflammatory activity

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Synthesis and anti-inflammatory activity of 2-substituted-((N,N-disubstituted)-1,3-benzoxazole)-5-carboxamides

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药学学报 2010年第6期45卷 730-734页

作者： Reena M kiran G Rajyalakshmi G Venkateshwa Rao J Sarangapani M Department of Pharmaceutical Chemistry Talla Padmavati College of Pharmacy Department of Pharmaceutical Chemistry College of Pharmaceutical SciencesKakatiya University

A series of 2-substituted-((N,N-disubstituted)-1,3-benzoxazole)-5-carboxamides derivatives were synthesized by the reaction of 2-substituted-5-carbomethoxy benzoxazole with different secondary amines.The newly synthesized compounds were characterized on the basis of spectral(FT-IR,1H NMR,MS) & elemental analysis.All these compounds were screened for anti-inflammatory activity using carrageenan induced rat paw edema method.All of these compounds exhibited significant activity.Among the tested compounds Ve,Vg,Vf and Va were considered to have potent anti-inflammatory activity and was comparable with standard.

关键词： benzoxazole anti-inflammatory activity carrageenan

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Analysis of Lavandulyl Flavonoids from Sophora flavescens with antiinflammatory activity Based on Molecular Network Technology

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Medicinal Plant 2024年第2期15卷 1-5,14页

作者： Yan LIN Bo TU Shanggao LIAO Minghui HE Guizhou Provincial Higher Education Institutions Genuine Medicinal Materials Chronic Disease Prevention and Control Engineering Research Center College of PharmacyGuizhou Medical UniversityGuiyang 550025China

[Objectives]This study was conducted to screen lavandulyl flavonoids with anti-inflammatory activity from Sophora flavescens.[Methods]35 compounds were screened from traditional Chinese medicine S.flavescens using the nitric oxide(NO)anti-inflammatory activity model.[Results]Five components,8(xanthohumol),13(kurarinol),27(4-methoxysalicylic acid),28(b-resorcic acid)and 30(b-resorcic acid),exhibited significant anti-inflammatory activity,with IC 50 values of 5.99,4.76,6.96,3.41 and 5.22μM,respectively.Especially,8(xanthohumol)and 13(kurarinol)were typical lavandulyl flavonoids in S.flavescens,which were worth further exploration.Furthermore,UPLC-Q-Exactive and GNPS molecular networking technique were used for rapid analysis of lavandulyl flavonoids from S.flavescens.A total of 15 components were identified.[Conclusions]This work lays a theoretical foundation for further separation and analysis of lavandulyl flavonoids with anti-inflammatory activity from S.flavescens.

关键词： Sophora flavescens Molecular network anti-inflammatory activity Lavandulyl flavonoids

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Two New Quinazoline Derivatives from the Moss Endophytic Fungus Aspergillus sp. and Their anti-inflammatory activity

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Natural Products and Bioprospecting 2021年第1期11卷 105-110页

作者： Ning-Ning Wang Chun-Yu Liu Tian Wang Yue-Lan Li Ke Xu Hong-Xiang Lou Department of Natural Product Chemistry Key Lab of Chemical Biology of Ministry of EducationSchool of Pharmaceutical SciencesShandong UniversityJinan 250012China

Two new quinazoline derivatives versicomides E(1)and F(2),and 10 known compounds(3-12)were isolated from the moss endophytic fungus Aspergillus sp.Their structures were determined on the basis of extensive spectroscopic data analysis and ECD calculations.Among them,the compound 7(6-hydroxy-3-methoxyviridicatin)was first reported as a natural product.Inhibition on LPS-induced NO production in RAW 264.7 murine macrophages found that compounds 5,7 and 8 showed significant inhibitory effects on NO production,with IC50 values of 49.85,22.14 and 46.02μM respectively.

关键词： Endophytic fungus Quinazoline anti-inflammatory activity

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