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Anti-inflammatory germacrane-type sesquiterpene lactones from Vernonia sylvatica

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Chinese Journal of Natural Medicines 2024年第06期 568-576页

作者： WANG Min LI Han HU Bintao tang chunping XU Hui KE Changqiang XIE Zuoquan YE Yang YAO Sheng State Key Laboratory of Drug Research&Natural Products Research Center Shanghai Institute of Materia Medica Chinese Academy of Sciences University of Chinese Academy of Sciences School of Life Science and Technology Shanghai Tech University State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Zhongshan Institute for Drug Discovery Shanghai Institute of Materia Medica Chinese Academy of Sciences

Nine new germacranolides, sylvaticalides A-H（1–9）, and three known analogues（10–12） were isolated from the aerial part of Vernonia sylvatica. Their structures were established using comprehensive spectroscopic analysis, including high-resolution electrospray ionization mass spectroscopy（HR-ESI-MS） and 1D and 2D nuclear magnetic resonance（NMR） spectra. Their absolute configurations were determined by X-ray diffraction experiments. The anti-inflammatory activities of all isolated compounds were assessed by evaluating their inhibitory effects on the nuclear factor kappa B（NF-κB） pathway, which was activated by lipopolysaccharide（LPS）-stimulated human THP1-Dual cells, and the interferon-stimulated gene（ISG） pathway, activated by STING agonist MSA-2 in the same cell model. Compounds 1, 2 and 6 showed inhibitory effects on the NF-κB and ISG signaling pathways, with IC50values ranging from 4.12 to 10.57 μmol·L-1.

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Birhodomolleins D and E, two new dimeric grayanane diterpenes with a 3-O-2＇ linkage from the fruits of Rhododendron pumilum

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Chinese Chemical Letters 2018年第1期29卷 123-126页

作者： RuiZhang chunping tang Chang-Qiang Ke Sheng Yao Ge Lin Yang Ye State Key Laboratory of Drug Research and Natural Products Chemistry Department Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China University of Chinese Academy of Sciences Beijing 100049 China SIMM-CUHK Joint Research Laboratory for Promoting Globalization of Traditional Chinese Medicines between Shanghai Institute of Materia Medica Chinese Academy of Sciences and The Chinese University of Hang Kong Hang Kong SAR China School of Biomedical Sciences The Chinese University of Hang Kong Hang Kong SAR China School of Life Science and Technology ShanghaiTech University Shanghai 201210 China

Two new dimeric diterpenes, birhodomolleins D （1） and E （2）, were characterized from the fruits of Rhododendron pumilum. Their structures featured two grayanane diterpenes dimerized through an oxygen bridge locating at C-3 and C-2＇. They are the first examples of dimeric grayanane diterpenes with a 3-O-2＇ linkage from the Ericaceae family. Their structures were elucidated on the basis of comprehensive analysis of spectroscopic data.

关键词： Rhododendron pumilumEricaceaeDimeric diterpeneGrayananeBirhodomollein DBirhodomollein E

Traditional Chinese medicine extraction method by ethanol delivers drug-like molecules

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Chinese Journal of Natural Medicines 2019年第9期17卷 713-720页

作者： William G.Miao chunping tang Yang Ye Ronald J.Quinn Yunjiang Feng Griffith Institute of Drug Discovery(GRIDD) Griffith UniversityQueensland 4111Australia Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 201203China

Traditional Chinese Medicine(TCM)is an important reservoir for bioactive natural *** extraction methods by water decoction and wine tincture are an integral part of TCM and essential for their widely acknowledged *** this study,we selected 6 common TCMs that are rich in chemistry to investigate whether the TCM extraction methods deliver molecules with drug-like physical chemical *** TCM herbal materials were extracted by water,95%ethanol,and sequential hexane,d ichloromethane and *** extracts were analyzed by HPLC and^1H *** on one of the extracts yielded 32 compounds,their physical chemical properties were analyzed by Instant *** results showed that ethanol extraction,which mimics TCM wine tincture,delivered compounds with physical chemical properties compliant to Lipinski’s rule of 5.

关键词： Extraction Traditional Chinese medicine(TCM) Natural products Lipinski’s Ro5Physicochemical properties

Flavonoids from the roots and rhizomes of Sophora tonkinensis and their in vitro anti-SARS-CoV-2 activity

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Chinese Journal of Natural Medicines 2023年第1期21卷 65-80页

作者： LI Zhuo XIE Hang tang chunping FENG Lu KE Changqiang XU Yechun SU Haixia YAO Sheng YE Yang School of Chinese Materia Medica Nanjing University of Chinese MedicineNanjing 210023China State Key Laboratory of Drug Research and Natural Products Chemistry DepartmentShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China School of Pharmacy University of Chinese Academy of SciencesBeijing 100049China Drug Discovery and Design Center CAS Key Laboratory of Receptor ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced StudyUniversity of Chinese Academy of SciencesHangzhouChina

Acute respiratory infection caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)had caused a global pandemic since 2019,and posed a serious threat to global health *** Chinese medicine(TCM)has played an indispensable role in the battle against the *** components originated from TCMs were found to inhibit the production of SARS-CoV-23C-like protease(3CLpro)and papain-like protease(PLpro),which are two promising therapeutic targets to inhibit *** study describes a systematic investigation of the roots and rhizomes of Sophora tonkinensis,which results in the characterization of 12 new flavonoids,including seven prenylated flavanones(1−7),one prenylated flavonol(8),two prenylated chalcones(9−10),one isoflavanone(11),and one isoflavan dimer(12),together with 43 known compounds(13−55).Their structures including the absolute configurations were elucidated by comprehensive analysis of MS,1D and 2D NMR data,and time-dependent density functional theory electronic circular dichroism(TDDFT ECD)*** 12 and 51 exhibited inhibitory effects against SARS-CoV-23CLpro with IC_(50) values of 34.89 and 19.88μmol·L^(−1),repectively while compounds 9,43 and 47 exhibited inhibitory effects against PLpro with IC_(50) values of 32.67,79.38,and 16.74μmol·L^(−1),respectively.

关键词： Sophora tonkinensis Flavonoid Anti-SARS-CoV-2 activity SARS-CoV-23CLpro SARS-CoV-2 PLpro

基于TLR-4/NF-κB信号通路探究金花茶提取物对非酒精性脂肪肝的作用

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食品工业科技 2024年第20期45卷 349-360页

作者：陆少君蔡肇栩郭瑞雪谢群巧罗力唐春萍陈文健江涛肇庆市第一人民医院药学部广东省局部精准药物递药制剂工程技术研究中心广州市新药筛选模型系统建设与应用重点实验室广州新海医院广东药科大学实验动物中心中药学院食品科学学院

探讨金花茶提取物对非酒精性脂肪肝病（NAFLD）大鼠模型的改善作用及其机制。随机选取10只SD大鼠为空白组，剩余50只则灌服高糖高脂乳剂复制非酒精性脂肪肝模型，14d后造模大鼠按血清中总胆固醇（TC）水平随机分为模型组、辛伐他汀组（8... 详细信息

探讨金花茶提取物对非酒精性脂肪肝病（NAFLD）大鼠模型的改善作用及其机制。随机选取10只SD大鼠为空白组，剩余50只则灌服高糖高脂乳剂复制非酒精性脂肪肝模型，14d后造模大鼠按血清中总胆固醇（TC）水平随机分为模型组、辛伐他汀组（8mg/kg）及金花茶高、中、低剂量组（260、130、65mg/kg）。分组后连续给药6周，于末次给药前进行口服葡萄糖耐量试验（OGTT）并计算血糖曲线下面积（AUC），末次给药后采集血清及肝组织，检测血脂指标总胆固醇（TC）、三酰甘油（TG）、高密度脂蛋白（HDL-C）、低密度脂蛋白（LDL-C）及游离脂肪酸（FFA），肝脂指标TC及TG，肝功能指标谷丙转氨酶（ALT）及谷草转氨酶（AST），肝脏脂质过氧化指标丙二醛（MDA）及超氧化物歧化酶（SOD）；测定大鼠血清炎症因子指标白介素6（IL-6）、白介素8（IL-8）及肿瘤坏死因子（TNF-α）；检测血清胰岛素（FINS）并计算胰岛素抵抗指数（HOMA-IR）；HE染色法观察肝脏病理形态学变化并进行非酒精性脂肪肝病活动度积分（NAS）评分；测定肝组织中Toll样受体4（TLR-4）和核因子κB（NF-κB）的基因及蛋白的表达。结果表明：与模型组相比，金花茶药物组AUC、HOMA-IR及血清中FINS、TG、TC、LDL-C 、FFA、ALT、AST、IL-6、IL-8、TNF水平显著降低，HDL-C 水平明显升高（P＜0.05）；肝组织TG、TC、MDA中含量显著降低，SOD活性显著升高（P＜0.05）；肝脏脂肪肝病样变减轻，肝细胞形态异常及炎症浸润明显改善，NAS评分显著下降；TLR-4、NF-κB蛋白及mRNA表达降低，差异均有统计学意义（P＜0.05），其中以金花茶高剂量的改善效果最佳。综上所述，金花茶提取物可通过TLR-4/NF-κB信号通路来调节糖脂代谢紊乱，降低炎症反应和减轻炎症浸润，改善NAFLD大鼠肝脏病变。

关键词：非酒精性脂肪肝病金花茶脂质代谢 TLR-4/NF-κB信号通路

Atypical manifestations of acute coronary syndrome—throat discomfort:a multi-center observational study

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Frontiers of Medicine 2022年第4期16卷 651-658页

作者： Yanqing Fang Xiaoting Cheng Wenhui Peng Xueying Chen chunping tang Qiusheng Huang Sihai Wu Yibo Huang Fanglu Chi Matthew RNaunheim Huawei Li Bing Chen Yilai Shu ENT Institute and Department of Otorhinolaryngology Eye&ENT HospitalState Key Laboratory of Medical NeurobiologyFudan UniversityShanghai 200031China Institutes of Biomedical Sciences Fudan UniversityShanghai 200031China NHC Key Laboratory of Hearing Medicine Fudan UniversityShanghai 200031China Department of Cardiology Shanghai Tenth People’s HospitalSchool of MedicineTongji UniversityShanghai 200072China Department of Cardiology Zhongshan HospitalFudan UniversityShanghai Institute of Cardiovascular DiseasesNational Clinical Research Center for Interventional MedicineShanghai 200032China Department of Cardiology The First Affiliated HospitalNanjing Medical UniversityNanjing 210029China Department of Otolaryngology Affiliated Hospital of Jiangsu UniversityZhenjiang 212001China Department of Otorhinolarynogology The Second People’s Hospital of WuxiNanjing Medical UniversityWuxi 214002China Department of Otolaryngology-Head and Neck Surgery Massachusetts Eye and Ear InfirmaryHarvard Medical SchoolBostonMA 02114USA

To present the clinical characteristics and the misdiagnosis rate of acute coronary syndrome manifested primarily as throat discomfort,we conducted a multicentric and retrospective study in the cardiology and otorhinolaryngology *** of patients with primary complaint of throat discomfort,absence of chest pain at onset,and an ultimate diagnosis of acute coronary syndrome,as well as patients with pharyngitis(as controls)were collected from May 2015 to April *** patients’main manifestations were *** regression results showed that chest tightness,dyspnea,perspiring,and exertional throat symptoms were significantly associated with acute coronary syndrome,with odds ratios of 8.3(95%CI 2.2–31.5),10.9(95%CI 1.8–66.9),25.4(95%CI 3.6–179.9),and 81.2(95%CI 13.0–506.7).A total of 25(56.82%)out of 44 acute coronary syndrome patients,who were first admitted to the otorhinolaryngology department,were misdiagnosed,with a 12%(3/25)mortality *** discomfort can be the principal manifestation of acute coronary *** patients exhibit high misdiagnosis and mortality *** throat symptoms,chest tightness,perspiring,and dyspnea were important indicators of acute coronary syndrome in patients whose main complaint was throat *** awareness of this condition will result in prompt diagnosis and reduce morbidity and mortality.

关键词： acute coronary syndrome(ACS) throat discomfort(TD) throat pain cardiology departments non-cardiologic physicians

Flavonoids from the roots and rhizomes of Sophora tonkinensis and their in vitro anti-SARS-CoV-2 activity

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Chinese Journal of Natural Medicines 2023年第01期 65-80页

作者： LI Zhuo XIE Hang tang chunping FENG Lu KE Changqiang XU Yechun SU Haixia YAO Sheng YE Yang School of Chinese Materia Medica Nanjing University of Chinese Medicine State Key Laboratory of Drug Research and Natural Products Chemistry Department Shanghai Institute of Materia MedicaChinese Academy of Sciences Drug Discovery and Design Center CAS Key Laboratory of Receptor Research Shanghai Institute of Materia Medica Chinese Academy of Sciences School of Pharmacy University of Chinese Academy of Sciences School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced Study University of Chinese Academy of Sciences

Acute respiratory infection caused by severe acute respiratory syndrome coronavirus 2（SARS-CoV-2） had caused a global pandemic since 2019, and posed a serious threat to global health security. Traditional Chinese medicine（TCM） has played an indispensable role in the battle against the epidemic. Many components originated from TCMs were found to inhibit the production of SARS-CoV-2 3C-like protease（3CLpro） and papain-like protease（PLpro）, which are two promising therapeutic targets to inhibit SARS-CoV-2. This study describes a systematic investigation of the roots and rhizomes of Sophora tonkinensis, which results in the characterization of 12 new flavonoids, including seven prenylated flavanones（1-7）, one prenylated flavonol（8）, two prenylated chalcones（9-10）, one isoflavanone（11）, and one isoflavan dimer（12）, together with 43 known compounds（13-55）. Their structures including the absolute configurations were elucidated by comprehensive analysis of MS, 1D and 2D NMR data, and time-dependent density functional theory electronic circular dichroism（TDDFT ECD） calculations. Compounds 12 and 51 exhibited inhibitory effects against SARS-CoV-2 3CLpro with IC50values of 34.89 and 19.88 μmol·L-1, repectively while compounds 9, 43 and 47 exhibited inhibitory effects against PLpro with IC50values of 32.67, 79.38, and 16.74 μmol·L-1, respectively.

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The early risk stratification of the patients with acute chest pain

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Journal of Nanjing Medical University 2007年第6期21卷 363-366页

作者： chunping tang Yanrong Liu Qin Shen Zhijian Yang Jun Huang Ming Gui Chest Pain Emergency Department the First Affiliated Hospital of Nanjing Medical University＇ Nanjing 210029 Jiangsu Province China

Objective： This investigation was designed to stratify patients with acute chest pain based on their symptoms, electrocardiogram （ECG）, cardiac injury markers and the number of accompanying traditional risk factors（smoking, obesity, hyperlipemia, hypertension, diabetes）, and to assess the effect of the above factors to obtain a risk stratification for patients with chest pain. Methods： We identified 139 patients with acute chest pain, including 45 myocardiac infarction patients, 65 unstable angina patients and 29 chest pain patients without identified acute coronary syndrome（ACS） admitted to our Coronary Heart Center during December 2004 to February 2005. All patients accepted coronary angiography. All data was collected using questionnaires. Based on reported symptom, electrocardiogram （ECG）, cardiac injury markers and the number of the accompanying traditional risk factors, we stratified all patients into four groups： Group 1, patients with acute chest pain, ECG changes and abnormal cardiac injury biomarkers. Group 2, patients with acute chest pain and ECG changes（without abnormal cardiac injury biomarkers）. Group 3, patients with acute chest pain, normal ECG, normal cardiac injury biomarkers and 〉2 traditional risk factors. Group 4, patients with acute chest pain, normal ECG and normal cardiac injury biomarkers, but only ≤ 2 traditional risk factors. From this data we examined the difference of ACS incidence in the four groups. Results：After stratification the ACS incidence of the grouped patients in turn was 100%, 84%, 69.6% and 53.3%. The combination of early phase ECG and cardiac injury markers identified 70.9% patients with ACS（the specificity being 90.7%）. The mortality of group 3 was higher compared with group 4（69.6% vs 53.3%）, however the P value was more than 0.05 and didn＇ t show significant statistical difference. The correlation analysis found the number of the traditional risk factors had a significant positive correlation （r= 0.202, P = 0.044） with

关键词： acute chest pain risk stratification ECG cardiac injury markers

Observational study:efficacy of aspirin and low-molecular-weight heparin in the management of recurrent miscarriage

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Journal of Chinese Pharmaceutical Sciences 2024年第8期33卷 730-736页

作者： Yuehong tang Ting Wang Ai-e Cao Huizhi Lian chunping Qiu Department of Gynaecology and Obstetrics Hainan Obstetrics and Gynecology HospitalHaikou 570100HainanChina

In the present study,we aimed to assess the comparative efficacy of low-molecular-weight heparin(LMWH)in combination with low-dose aspirin for the management of recurrent miscarriage and scrutinize alterations in coagulation function following such treatment.A retrospective analysis was conducted on clinical data obtained from 97 patients with recurrent miscarriage treated at our institution from January 2019 to June *** were categorized into either the study or control groups based on the administration of *** control group comprised 48 patients treated solely with aspirin,while the study group included 49 patients treated with both LMWH and *** evaluations between the two groups encompassed pregnancy outcomes,coagulation function,adverse reactions,and blood loss during *** revealed a higher term birth rate in the study group(83.67%)compared to the control group(50%).Post-treatment,the study group exhibited lower prothrombin time,plasminogen activator inhibitor,and D-dimer levels than the control ***,the study group experienced fewer adverse reactions and reduced blood loss during delivery in comparison to the control group,demonstrating statistical significance(P<0.05).The combination of LMWH and low-dose aspirin exhibited noteworthy application in the management of recurrent *** therapeutic approach not only fostered the enhancement of coagulation function conducive to pregnancy but also diminished the incidence of adverse reactions observed with aspirin alone.

关键词： Recurrent miscarriage Low-molecular-weight heparin Aspirin Full production Coagulation function