摘要：
A chalcone-flavonone type biflavonoid, trichocladabiflavone A (1), along with eight known biflavonoids (2–9) were isolated from the 70% EtOH extract of Selaginella trichoclada. Their structures were elucidated by extensive spectroscopic analyses. Compound 1 was the first chalcone-flavonone type biflavonoid reported in the genus Selaginella. Moreover, compound 1 exhibited moderate cytotoxicity against DU145, MCF-7 and PC3 human cancer cell lines.
摘要：
Nonsmall-cell lung carcinoma (NSCLC) is one of the deadliest malignancies in the world. LncRNAs are confirmed to be involved in the progression of NSCLC. Meanwhile, lncRNA CRNDE is known to be upregulated in NSCLC; however, the mechanism by which CRNDE regulates the tumourigenesis of NSCLC remains unclear. To test the function of CRNDE in NSCLC, cell proliferation, invasion, and migration were investigated by colony formation and Transwell assays, respectively. qPCR and Western blotting were applied to test gene and protein levels. In addition, the relationship among CRNDE, miR-455-3p, and HDAC2 was explored by dual-luciferase and RIP assays. The data revealed that the expression of CRNDE was upregulated in NSCLC tissues, while miR-455-3p was downregulated. CRNDE knockdown inhibited the viability, migration and invasion of NSCLC cells or epidermal growth factor receptor gene (EGFR)-mutant NSCLC cells. Moreover, inhibition of miR-455-3p exhibited the opposite effect. CRNDE bound with miR-455-3p, and HDAC2 was found to be targeted by miR-455-3p. Meanwhile, miR-455-3p downregulation reversed the effect of CRNDE knockdown on NSCLC cell function. Furthermore, miR-455-3p notably inhibited the growth and invasion of NSCLC cells via downregulation of HDAC2. Knockdown of CRNDE attenuated NSCLC progression via modulation of the miR-455-3p/HDAC2 axis. Thus, those findings might provide a novel strategy against NSCLC.
摘要：
The folliculitis decalvans (FD) and lichen planopilaris (LPP) phenotypic spectrum combines biphasic features of FD and LPP. It is characterized by successive or concomitant occurrence of pustules, crusts, follicular tufts, perifollicular erythema, perifollicular scales, and cicatricial alopecia and includes mixed histologic features of both FD and LPP. Here, we report the case of a 33-year-old female patient with a 30-year history of FD-LPP phenotypic spectrum lesions.
作者机构：
[徐昕怡] School of Chinese Medicine, Hunan University of Chinese Medicine, Changsha, Hunan, 410208, China;[曹学帅] School of Medicine, Hunan University of Chinese Medicine, Changsha, Hunan, 410208, China;Department of Blood Transfusion, The Third Xiangya Hospital of Central South University, Changsha, Hunan, 410013, China;[Long Xi; 张国民] Graduate School, Hunan University of Chinese Medicine, Changsha, Hunan, 410208, China;[彭素娟] Department of Respiratory Medicine, The Second Affiliated Hospital of Hunan University of Chinese Medicine, Changsha, Hunan, 410005, China
通讯机构：
[Zhang Guomin] G;Graduate School, Hunan University of Chinese Medicine, Changsha, Hunan, 410208, China
作者机构：
湖南中医药大学 长沙 410208;湖南省中医药研究院 长沙 410006;湖南中医药大学第二附属医院 长沙 410005;[李鹏辉; 胥新元; 蔡媛; 彭艳梅] Hunan Academy of Traditional Chinese Medicine, Changsha, 410006, China;[孙瑜; 廖鑫] Hunan University of Chinese Medicine, Changsha, 410208, China, Hunan Academy of Traditional Chinese Medicine, Changsha, 410006, China
通讯机构：
[Peng, Y.] H;Hunan Academy of Traditional Chinese MedicineChina
关键词：
中药;灭菌;知识图谱
摘要：
中药应用形式多样，有饮片、生粉入药、提取物、中成药等，如何把控外源微生物污染，保障中药的安全性和有效性，选择适宜的灭菌技术是关键。本文通过检索中国知网、万方、维普、Web of Science自2001-2021年已发表的中药灭菌文献，应用可视化分析软件VOSviewer与CiteSpace对近20年来中药灭菌方法的应用现状与趋势进行分析。经过筛选，本研究共纳入文献322篇，收录中药灭菌相关文献载文量第一的期刊为《机电信息》；作者合作网络分析发现，中药灭菌领域主要形成了中国食品药品检定研究院和广州市药品检验所等核心研究团队；文献关键词显示，中药灭菌研究主要集中在辐照、微波、制备工艺、有效成分、干燥、指纹图谱等方面。本研究还深入探讨了不同灭菌技术的优缺点及其适宜范围，结合中药灭菌未来发展趋势进行深入分析，以期为研究者选择合适的灭菌方法提供参考。为进一步统筹推进中药灭菌科学发展，笔者提出中药灭菌未来需要紧密结合技术、设备和政策，才能更快推进中药现代化发展。
作者机构：
[Qiu, Huawei; Zhang, Li; Feng, Dongchan] Hainan Prov Hosp Tradit Chinese Med, Haikou 570203, Hainan, Peoples R China.;[Tang, Yan] Hunan Univ Chinese Med, Affiliated Hosp 2, Changsha 410005, Peoples R China.;[Wu, Dan] Hunan Univ Chinese Med, Hosp 1, Changsha 410005, Peoples R China.
通讯机构：
[Wu, D ] H;Hunan Univ Chinese Med, Hosp 1, Changsha 410005, Peoples R China.
关键词：
Acetaminophen;Bile acid;FXR;Liver injury;Structure-based Drug Design
摘要：
Abstract Based on structure-based drug design strategy, the optimal compound 2 (EC50=2.43 μM) has been designed and identified. Compound 2 revealed considerable activity on FXR, and exerts best therapeutic effects on alleviating acetaminophen-induced liver damages in this series by up-regulation of FXR-related gene expression in vivo. These results suggest that compound 2 is a promising FXR agonist suitable for further evaluation. Abstract Farnesoid X receptor (FXR) plays an important role in regulating glucolipid metabolism, detoxification, and inflammation in liver. Thus, FXR has huge potential on several liver diseases, including drug-induced liver injury, fibrosis, and fatty liver. In this study, we performed a structure-based drug design strategy to optimize the previous reported FXR agonist N-(2-methoxy-4-nitrophenyl)-2-((2-(2-oxopyrrolidin-1-yl)phenyl)amino)acetamide (1). After structure-based drug design, the optimal compound, 3-(2-((2-(2-oxopyrrolidin-1-yl)phenyl)amino)acetamido)benzoic acid (2, EC50=2.43 μM), was identified by displacing the potentially toxic nitro group of compound 1 with carboxylic acid to obtain new ionic bond with His294. Compound 2 revealed considerable activity on FXR, and exerts best therapeutic effects on alleviating acetaminophen-induced liver damages in this series by up-regulation of FXR-related gene expression in vivo. In summary, these results suggest that compound 2 is a promising FXR agonist suitable for further evaluation.
作者：
Wang Yan-fang;Deng Yan;Zhang Su-ying;Liu Dong;Luo Bin;...
期刊：
中国结合医学杂志,2022年28(12):1072-1080 ISSN：1672-0415
通讯作者：
Ai-jun Sun
作者机构：
[Ma Rui-lin; Wang Yan-fang; Deng Yan; Sun Ai-jun] Chinese Acad Med Sci & Peking Union Med Coll, Peking Union Med Coll Hosp, Dept Obstet & Gynecol, Beijing 100730, Peoples R China.;[Zhang Su-ying] Hunan Univ Chinese Med, Dept Obstet & Gynecol, Affiliated Hosp 2, Changsha 410001, Peoples R China.;[Luo Bin; Liu Dong] Sichuan Univ, West China Hosp 2, Key Lab Birth Defects & Related Dis Women & Child, Minist Educ, Chengdu 610041, Peoples R China.;[Wang Xue; Deng Miao] Hangzhou Womens Hosp, Dept Obstet & Gynecol, Hangzhou Matern & Child Hlth Care Hosp, Hangzhou 310008, Peoples R China.
通讯机构：
[Ai-jun Sun] D;Department of Obstetrics and Gynecology, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China
关键词：
Chinese medicine;Buxue Yimu Pills;gynecological anemia;network pharmacology;multi-target mechanism
摘要：
OBJECTIVE: To compare the clinical efficacy and safety of oral administration of Buxue Yimu Pills (BYP, ), ferrous sulfate (FS), and the combination of BYP and FS on gynecological anemia, and investigate the mechanisms using network pharmacology. METHODS: A randomized, controlled, multi-center clinical trial was conducted. Totally 150 patients with hemoglobin of 70-110 g/L due to gynecological conditions were recruited and randomized (using the block randomization method) into Buxue Yimu Pills group (24 g/d), oral iron group (FS Tablets, 0.9 g/d), and combined treatment group (BYP, 24 g/d plus FS Tablets, 0.9 g/d), 50 patients in each group. At the enrollment and 4-week treatment, complete blood count, serum iron indexes were evaluated. Adverse events, liver and renal functions, as well as blood coagulation were observed. Network pharmacology was conducted to identify the active ingredients and explore the potential mechanisms of BYP. RESULTS: Ten (20%) and 7 (14%) participants discontinued the therapy due to gastrointestinal symptoms in oral iron and combination treatment groups. All 3 groups showed elevated hemoglobin. The patients in the iron group exhibited typically elevated in serum iron and ferritin and decreased in total iron-binding capacity. No change in iron indexes was observed in BYP group. The patients in the combination treatment group neither showed significant changes in serum ferritin nor total iron-binding capacity. No significant adverse reactions were observed in the BYP group. The network pharmacology identified 27 bioactive compounds and 145 targets of BYP on gynecological anemia. Biological processes and pathways including regulation of inflammation, hormone, angiogenesis and hemostasis, response to decreased oxygen levels, effects on myeloma cell, and response to metal ions were identified. CONCLUSION: BYP contributes to the practical improvement on gynecological anemia potentially through multi-target mechanisms and optimized iron re-distribution. (Trial registration: No. NCT03232554).
摘要：
Abstract: Cantharidin (CTD) is the major component of anticancer drugs obtained from Mylabris Cichorii and has a good inhibitory effect on several cancers, including hepatocellular carcinoma (HCC) and breast cancer. However, due to its toxicity, oral administration can cause various adverse reactions, limiting its clinical application. The aim of this work was to design glycyrrhetinic acid (GA)- and/or folate (FA)-modified solid lipid nanoparticles (SLNs) for the encapsulation of CTD to target HCC. Four CTD-loaded SLNs (cantharidin solid lipid nanoparticles (CSLNs), glycyrrhetinic acid-modified cantharidin solid lipid nanoparticles (GA-CSLNs), folate-modified cantharidin solid lipid nanoparticles (FA-CSLNs), and glycyrrhetinic acid and folate-modified cantharidin solid lipid nanoparticles (GA-FA-CSLNs)) were prepared by the emulsion ultrasonic dispersion method, and their physicochemical parameters were determined (particle size and distribution, morphology, zeta-potential, entrapment efficiency, drug loading, and hemolysis). Additionally, the antitumor activities of the four SLNs were evaluated comprehensively by tests for cytotoxicity, cell migration, cell cycle, apoptosis, cellular uptake, competition suppression assay, and in vivo tumor suppression assay. Four SLNs showed spherical shapes and mean diameters in the range of 75–110 nm with size dispersion (PDI) within the range of 0.19–0.50 and zeta-potential approximately –10 mV. The entrapment efficiency of CTD in SLNs was higher than 95% for all tested formulations, and no hemolysis was observed. Compared to GA-CSLNs or CSLNs, GA-FA-CSLNs and FA-CSLNs showed stronger cytotoxicity on hepatocellular carcinoma cells (HepG2), and the cytotoxicity of GA-FA-CSLNs on hepatocyte cells (L-02) was remarkably reduced compared with other formulations. GA-FA-CSLNs and FA-CSLNs also increased the inhibition of HepG2 cell migration, and FA-CSLNs had the highest apoptosis rate. The cell cycle results indicated that HepG2 cells were arrested mainly in the S phase and G2/M phase. Analysis of competition inhibition experiments showed that GA and FA ligands had targeted effects on HepG2 cells. The in vivo tumor inhibition experiment showed that GA-FA-CSLNs and FA-CSLNs had excellent tumor inhibition ability—their tumor inhibition rates were 96.46% and 89.92%, respectively. Our results indicate that GA-FA-CSLNs and FA-CSLNs have a promising future in the therapeutic intervention of HCC. Keywords: cantharidin; solid lipid nanoparticles; glycyrrhetinic acid; folate; antitumor; liver-targeting
