Pharmacological Research - Modern Chinese Medicine最新文献

{"title":"In-vitro modulation of glucose and lipid metabolism by Lentinula edodes extracts in obesity and type 2 diabetes models","authors":"Jasmeet Kaur ,&nbsp;Farheen Azad ,&nbsp;Anish Murtaja Alam Khan ,&nbsp;Mohd. Farzaan ,&nbsp;Javed Ahmad ,&nbsp;Humaira Farooqi ,&nbsp;Kailash Chandra ,&nbsp;Bibhu Prasad Panda","doi":"10.1016/j.prmcm.2024.100540","DOIUrl":"10.1016/j.prmcm.2024.100540","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Lentinula edodes</em> (shiitake mushroom) has been integral to Traditional Chinese Medicine (TCM) for centuries, with its cultivation dating back to the Song dynasty (960–1127) in China. Traditionally valued for its immune-boosting properties, L. <em>edodes</em> is now being studied for its potential in managing metabolic disorders like obesity and type 2 diabetes. This study examines the effects of L. <em>edodes</em> fruiting body extract on key metabolic pathways related to glucose metabolism and lipid regulation.</div></div><div><h3>Methods</h3><div>Fruiting body extracts of <em>Lentinula edodes</em> including water, ethanolic, methanolic, and hydroalcoholic (50:50, 75:25, 25:75) were tested on L6 myoblasts. The study evaluated glucose uptake, GLUT4 expression, p-AMPK activation, and gene expression levels of PPARγ, AMPK, UCP-1, and FASN. Comparisons were made with control groups and standards like berberine and insulin.</div></div><div><h3>Results</h3><div>The hydroalcoholic extracts (50:50 and 75:25) significantly enhanced glucose uptake (<em>p</em> &lt; 0.001) and GLUT4 translocation, similar to the effects of insulin (<em>p</em> &lt; 0.0001) and berberine (<em>p</em> &lt; 0.0001). These extracts also upregulated p-AMPK (<em>p</em> &lt; 0.0001) and UCP-1 expression (7.621), indicating improved insulin sensitivity and thermogenic activity. Additionally, these extracts differentially regulated PPARγ and FASN, suggesting a complex interaction with lipid metabolism. Notably, FASN expression was highly upregulated in water extract (37.792), indicating potential implications for fatty acid synthesis and storage.</div></div><div><h3>Discussion</h3><div><em>Lentinula edodes</em> shows significant potential as a functional food for managing obesity and diabetes, supporting traditional TCM practices with modern scientific evidence. The study suggests that L. <em>edodes</em> can modulate key metabolic pathways such as glucose uptake, AMPK signalling, PPARγ regulation, and upregulation of FASN and UCP-1, making it a promising natural therapeutic agent. Further research, including clinical trials, is necessary to confirm these benefits in humans and explore the underlying mechanisms.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100540"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142593703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Xylopia parviflora (A. rich.) benth. Mitigates anxiety behavior and chronic mild stress-induced depression-like behavior in mice: The involvement of biogenic amine neurotransmitters, cyclooxygenase-2 and stress biomarkers in its antidepressant activity","authors":"Abdullahi A. Murtala ,&nbsp;Elijah O. Oyinloye ,&nbsp;Farouk A. Oladoja ,&nbsp;Samuel M. Fageyinbo ,&nbsp;Holiness A. Olasore ,&nbsp;Luqman O. Ogunjimi ,&nbsp;Akinyinka A. Alabi ,&nbsp;Wasiu E. Olooto ,&nbsp;Oluwatosin O. Soyinka ,&nbsp;Abayomi S. Faponle ,&nbsp;Oluwatoyin O. Shonde ,&nbsp;Luqmon E. Osipitan ,&nbsp;Emmanuel O. Kasumu ,&nbsp;Olusola O. Joseph ,&nbsp;Emmanuel O. Olaniran ,&nbsp;Esther F. Olatunji","doi":"10.1016/j.prmcm.2024.100541","DOIUrl":"10.1016/j.prmcm.2024.100541","url":null,"abstract":"<div><h3>Background</h3><div><em>Xylopia parviflora</em> is a novel botanical in Modern Chinese Medicine that contains bioactive constituents including alkaloids, flavonoids, and terpenoids, which are the pharmacologically active components in various Chinese herbal formulations such as Coptis chinensis (alkaloid-rich herbs), Ginkgo biloba (flavonoid-rich herbs) and Artemisia annua (terpenoid-rich herbs).</div></div><div><h3>Objective</h3><div>This investigation sought to evaluate the anxiolytic and antidepressant-like effects of the hydroethanol leaf extract of <em>Xylopia parviflora</em> using mouse models. We elucidated the roles of noradrenaline, serotonin, cyclooxygenase-2, and reactive oxidative species in mediating its antidepressant effects, providing a fresh perspective on the pharmacological activity of <em>Xylopia parviflora</em>.</div></div><div><h3>Methods</h3><div>The acute toxicity of XPE was assessed following OECD guideline 420. Established behavioral tests were used to evaluate the anxiolytic (including the hole-board, open field, elevated plus maze, and light/dark exploration assessments) and antidepressant (encompassing the forced swim and tail suspension tests) effects of the extract. Mice received treatments of distilled water (10 mL/kg, serving as the negative control), fluoxetine (20 mg/kg, acting as the reference medication), and XPE (at doses of 50, 100, and 200 mg/kg). The concentrations of noradrenaline, serotonin, and COX-2 within the brain tissue were quantified using ELISA kits. The levels of antioxidant biomarkers were evaluated using standardized commercial assay kits.</div></div><div><h3>Results</h3><div>The oral/intraperitoneal LD50 for the extract was established at 2000 mg/kg. In the behavioral assessments designed to measure anxiolytic effects, XPE significantly mitigated anxiety levels in mice, as evidenced by an increase in exploratory behaviors (including head dips, sectional crossings, general square crossings, rearing, and assisted rearing) and an increased time spent in the brightly illuminated compartments. Concerning the antidepressant evaluations, XPE significantly reduced depression-like behaviors in mice, which was indicated by an increased latency to immobility and a decrease in the duration of immobility. XPE was found to modulate noradrenaline and serotonin transmissions, attenuate oxidative species, and inhibit COX-2 activity.</div></div><div><h3>Conclusion</h3><div>The findings above demonstrate that <em>Xylopia parviflora</em> possesses anxiolytic and antidepressant-like activities. The antidepressant property of XPE, as revealed in this study, may be attributable to the enhancement of biogenic amines (specifically noradrenaline and serotonin), the suppression of oxidative species, and the inhibition of COX-2 activity.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100541"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142657242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Virtual screening and lead optimization of Desmostachya bipinnata-derived FGFR inhibitors for oral squamous cell carcinoma management","authors":"Nitya Krishnasamy ,&nbsp;Ramya Ramadoss ,&nbsp;Swarnalakshmi Raman","doi":"10.1016/j.prmcm.2024.100534","DOIUrl":"10.1016/j.prmcm.2024.100534","url":null,"abstract":"<div><h3>Background</h3><div>Oral cancer remains a major global health challenge with limited therapeutic options, highlighting the need for novel treatments. Phytochemicals derived from <em>Desmostachya bipinnata (Db),</em> a plant used in traditional Chinese medicine for its anti-inflammatory and analgesic properties, have demonstrated potential anti-cancer effects. However, their mechanisms of action, particularly in targeting Fibroblast Growth Factor Receptor (FGFR) in oral cancer, are not well characterized.</div></div><div><h3>Objective</h3><div>This study aimed to leverage in-silico drug design methodologies to identify bioactive compounds from <em>Db</em> with potential FGFR-inhibiting activity for the treatment of oral cancer.</div></div><div><h3>Methodology</h3><div>An MTT assay was conducted using KB cell lines to evaluate cytotoxic effects, while thirty-eight phytochemicals from <em>Db</em> were screened through in silico approaches for their pharmacokinetics, toxicity, and drug-likeness. Molecular docking studies were performed to assess binding affinities to the FGFR protein. The biological activity and toxicity of the compounds were predicted to prioritize candidates for further investigation.</div></div><div><h3>Results</h3><div>Fourteen compounds were identified as promising candidates based on their drug-like properties, favourable pharmacokinetic profiles, significant FGFR binding affinities, and predicted anti-cancer activity. These compounds also demonstrated potential for oral bioavailability and central nervous system penetration, supporting their candidacy for further drug development. Notably, the traditional use of <em>Desmostachya bipinnata</em> in TCM emphasizes its role in enhancing overall vitality and immune function, which may synergize with the identified FGFR-inhibiting properties in the context of oral cancer treatment</div></div><div><h3>Conclusion</h3><div>The phytochemicals from Desmostachya bipinnata exhibit significant potential as FGFR-targeted therapeutic agents for oral cancer. Further experimental validation and optimization of these lead compounds could contribute to the development of novel, effective treatments for oral cancer and related conditions</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100534"},"PeriodicalIF":0.0,"publicationDate":"2024-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142587426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploration of the key active ingredients and mechanisms of Sparganii Rhizoma-Curcumae Rhizoma compatible formulation against human colorectal cancer through network pharmacology and in vitro experiments","authors":"Hongyan Lin ,&nbsp;Dongxuan Ai ,&nbsp;Xinling Wang ,&nbsp;Shuaijun Cui ,&nbsp;Xinghong Li ,&nbsp;Bangmei Ye ,&nbsp;Lingyu Ruan ,&nbsp;Jing Xu ,&nbsp;Liqun Wang","doi":"10.1016/j.prmcm.2024.100532","DOIUrl":"10.1016/j.prmcm.2024.100532","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Sparganii Rhizoma</em>-<em>Curcumae Rhizoma</em> (SR-CR) formulation may offer an effective treatment for human colorectal cancer (CRC). However, the active ingredients and underlying mechanisms of this herbal formulation remain unclear.</div></div><div><h3>Methods</h3><div>This study integrates network pharmacology, molecular docking and experimental verification to identify key active ingredients and elucidate the mechanisms of SR-CR in CRC treatment.</div></div><div><h3>Results</h3><div>Twenty-three active components of SR-CR were identified using the TCMSP, UniProt and Gene Cards databases. These components were associated with 178 targets, of which 118 are directly related to CRC. Protein-protein interaction (PPI) network analysis identified protein kinase B (AKT) 1, epidermal growth factor receptor (EGFR), SRC, Bcl2 and CASP3 as core anti-CRC targets. Gene Ontology (GO) and KEGG pathway analyses were performed on these 178 intersecting targets, and the results showed that these targets are involved in EGFR tyrosine kinase inhibitor resistance and AGE-RAGE signaling pathway in diabetic complications. At the same time, five compounds, including bisdemethoxycurcumin, formononetin, β-sitosterol, stigmasterol and hederagenin, were selected based on the target number of effective components and tested for cytotoxicity against human CRC cell lines HT-29, HCT-8 and HCT-116 <em>in vitro</em>. The results showed that bisdemethoxycurcumin exhibited significant anti-proliferative activity against HCT-116 cells. Molecular docking results indicated that bisdemethoxycurcumin effectively binds with AKT, EGFR, Bcl-2 and CASP3. Further pharmacological experiments demonstrated that bisdemethoxycurcumin inhibits HCT-116 cell proliferation and migration via inhibiting EGFR-AKT pathway, and induces apoptosis by up-regulating Bcl-2 expression.</div></div><div><h3>Discussion</h3><div>Based on our study, inhibiting the EGFR-AKT pathway and upregulating Bcl2 may be one of the mechanisms by which SR-CR inhibits the growth of CRC. The main active ingredients of SR-CR include bisdemethoxycurcumin, formononetin, β-sitosterol, stigmasterol and hederagenin, which may exert anti-colon cancer activity by targeting the regulation of AKT, EGFR, Bcl-2 and CASP3. However, we need more <em>in vitro</em> and <em>in vivo</em> evidence to confirm this conclusion. This study lays the foundation for further research on the pharmacological mechanism of SR-CR in the treatment of CRC.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100532"},"PeriodicalIF":0.0,"publicationDate":"2024-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142553556","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hypoglycemic and antihyperglycemic effects of Abelmoschus esculentus and Alchornea cordifolia in normal and alloxan-induced diabetic rats","authors":"Barnabé Lucien Nkono Ya Nkono ,&nbsp;Adjia Hamadjida ,&nbsp;Damolai Gounkagou ,&nbsp;Fidèle Ntchapda ,&nbsp;Sélestin Sokeng Dongmo ,&nbsp;Pierre Kamtchouing","doi":"10.1016/j.prmcm.2024.100531","DOIUrl":"10.1016/j.prmcm.2024.100531","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Background&lt;/h3&gt;&lt;div&gt;&lt;em&gt;Abelmoschus esculentus&lt;/em&gt; and &lt;em&gt;Alchornea cordifolia&lt;/em&gt; are commonly used in Traditional Chinese Medicine (TCM) to treat several diseases. &lt;em&gt;Abelmoschus esculentus&lt;/em&gt; is used to treat infertility and menorrhagia, while &lt;em&gt;Alchornea cordifolia&lt;/em&gt; is used for the treatment of venereal diseases, cough, and diarrhoea. However, very few studies assessed the antidiabetic effects of these plants. Therefore, this study aimed to investigate the hypoglycemic and antihyperglycemic effects of aqueous extract of &lt;em&gt;A. esculentus&lt;/em&gt; fruits and &lt;em&gt;A. cordifolia&lt;/em&gt; leaves.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Material and Methods&lt;/h3&gt;&lt;div&gt;Fresh Abelmoschus esculentus fruits and the powder from the dried leaves of &lt;em&gt;Alchornea cordifolia&lt;/em&gt; leaves were prepared by maceration in the aqueous phase (200 mg/100 mL and 50 mg/100 mL respectively) for 24 h, then filtered and concentrated in an oven at 45 °C. Diabete was induced to male Wistar rats by a single intraperitoneal injection of alloxan (150 mg kg&lt;sup&gt;−1&lt;/sup&gt;, b.w). Rats with a blood glucose level greater than or equal to 200 mg/dL were selected, divided into groups and were daily administered orally with either aqueous extracts of &lt;em&gt;A. esculentus&lt;/em&gt; at 30 mg kg&lt;sup&gt;−1&lt;/sup&gt; (AEAE30) or &lt;em&gt;A. cordifolia&lt;/em&gt; at 400 mg kg&lt;sup&gt;−1&lt;/sup&gt; (AEAC400) for 14 consecutive days. For comparison, acarbose (100 mg kg&lt;sup&gt;−1&lt;/sup&gt;), glibenclamide (5 mg kg&lt;sup&gt;−1&lt;/sup&gt;), and 500 mg kg&lt;sup&gt;−1&lt;/sup&gt; metformin (Glucophage) were administered orally as reference drugs. Moreover, insuline was also used as a positive control and administered intraperitoneally at a dose of 5 IU/kg. Then, blood glucose levels, oral glucose tolerance test, oral maltose tolerance club, body weight and hemoglobin were assessed. For evaluation of the aqueous extracts in the intestinal transit, imodium (2mg kg&lt;sup&gt;−1&lt;/sup&gt;, p.o) and fructine (5 mg kg&lt;sup&gt;−1&lt;/sup&gt;, p.o) were used as a positive control to determine the spasmolytic and laxative activities, respectively. The histopathological study of the liver, kidney, pancreas, testis, epididymis, and seminal vesicle was also carried out using the hematoxyline &amp; eosin (H&amp;E) technique.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;div&gt;AEAE30 and AEAC400 significantly reduced (&lt;em&gt;P&lt;/em&gt; &lt; 0.001) fasting blood glucose (FBG) levels and significantly prevented (&lt;em&gt;P&lt;/em&gt; &lt; 0.001) postprandial glycemia in AI-db rats following oral glucose tolerance test (OGTT) and oral maltose tolerance test (OMTT) in alloxan-induced diabetic rats (AI-db). In normoglycemic and insulin-resistant (IR) rats, AEAE30 significantly prevented the post-prandial blood glucose level during the OGTT (&lt;em&gt;P&lt;/em&gt; &lt; 0.01) only in normoglycemic rats. At the end of treatment, AEAE30 significantly reduced the relative weight of the liver (&lt;em&gt;P&lt;/em&gt; &lt; 0.01) and significantly increased (&lt;em&gt;P&lt;/em&gt; &lt; 0.001) the relative weight of the testes and pancreas while AEAC400 significantly increased the ","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100531"},"PeriodicalIF":0.0,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142657241","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Clinical formulation Zhigan Oral Liquid intervenes in alcoholic liver injury by regulating the intestinal flora and PI3K⧵AKT⧵NF-κB pathway","authors":"Yahong Zhao (赵亚红) ,&nbsp;Dongyang Li (李东阳) ,&nbsp;Shengchao Wang (王胜超) ,&nbsp;Wenxia Zhao (赵文霞) ,&nbsp;Zhenling Zhang (张振凌) ,&nbsp;Hongwei Zhang (张宏伟) ,&nbsp;Ruisheng Wang (王瑞生) ,&nbsp;Yafang Hou (侯娅芳) ,&nbsp;Meng Zhao (赵萌)","doi":"10.1016/j.prmcm.2024.100537","DOIUrl":"10.1016/j.prmcm.2024.100537","url":null,"abstract":"<div><h3>Introduction</h3><div>Zhigan Oral Liquid (ZOL) was developed from the empirical formulation of Professor Zhao Wenxia, a nationally renowned practitioner of Chinese medicine, and it has been used in Chinese medicine for many years for the effective treatment of alcoholic liver damage (ALD). However, the interventional mechanism of action of the dosage indications for different stages of ALD pathogenesis is not clear.</div></div><div><h3>Methods</h3><div>The main chemical components of ZOL were qualitatively analyzed by ultra-high performance liquid chromatography (UHPLC-Q-Orbitrap HRMS) in tandem with quadrupole electrostatic field orbital well high resolution mass spectrometry and quantitatively analyzed by high-performance liquid chromatography (HPLC). Network pharmacological analysis was performed to predict the targets and pathways of the potential pharmacodynamic components. The pharmacodynamic effects and potential target mechanisms were verified in a murine model of ALD. To observe the effect of ZOL on the intestinal flora, 16s rDNA sequencing was performed on ALD mice.</div></div><div><h3>Results</h3><div>ZOL can achieve alcohol detoxification by increasing the activity of ALDH and other detoxification enzymes and can intervene in the process of alcoholic liver injury and liver fibrosis by regulating the alcohol-induced bacterial dysbiosis, increasing the level of antioxidants, and inhibiting the activation of the PI3KAKTNF-κB signaling pathway. Kakkalide, Luteolin, Puerarin, tectoridin, and dihydromyricetin are related to the flavonoids that may be the main pharmacodynamic components that exert their medicinal effects.</div></div><div><h3>Conclusions</h3><div>The findings have significant implications for the development of Empirical treatments for alcoholic liver injury. Furthermore, the study contributes to promoting development and utilization of new dosage forms of hospital preparations by emphasizing the composition identification and animal experimental efficacy of ZOL. Overall, this study provides valuable insights into establishing an alcohol-induced liver injury model, and demonstrates the potential of ZOL as a common treatment for alcoholic liver injury a rich source.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100537"},"PeriodicalIF":0.0,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142657353","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Green synthesis of Au nanoparticles by Scutellaria barbata extract for chemo-photothermal anticancer therapy","authors":"Yinchuan Wang ,&nbsp;Jia Chen ,&nbsp;Yifan Bo ,&nbsp;Jiacheng Chen ,&nbsp;Yuan Liu ,&nbsp;Zhanglong Li ,&nbsp;Changyuan Yu ,&nbsp;Jiahui Liu ,&nbsp;Shihui Wang","doi":"10.1016/j.prmcm.2024.100536","DOIUrl":"10.1016/j.prmcm.2024.100536","url":null,"abstract":"<div><h3>Introduction</h3><div>The combination of photothermal therapy and chemotherapy has emerged as a promising strategy for cancer treatment. The green synthesis of gold nanoparticles (Au NPs) using extracts from traditional Chinese medicine <em>Scutellaria barbata D. Don</em> (Scu) has revealed an economical, sustainable, and eco-friendly approach for the outstanding anticancer activities.</div></div><div><h3>Methods</h3><div>Scu extract was mixed with HAuCl₄ solution to fabricate Scu-Au NPs. The synthesis process was optimized by varying the reaction temperature, reaction time, and HAuCl₄ concentration. The changes in the components of Scu before and after synthesis were analyzed using the 3,5-dinitrosalicylic acid (DNS) reduction test, the rutin colorimetric method, and the Folin–Ciocalteu method. The morphology, size, and structure of Scu-Au NPs were characterized by TEM, DLS, XRD, and XPS. The photothermal characteristics induced by near-infrared (NIR) irradiation were assessed by continuously monitoring the temperature elevation. The anticancer activity and mechanisms of Scu-Au NPs were investigated using MTT assay, cell uptake studies, ROS level detection, cell apoptosis and necrosis assays, flow cytometry analysis, intracellular Caspase-3 protein activity fluorescence detection, and Western blot analysis on A549, 4T1, and RAW264.7 cells.</div></div><div><h3>Results</h3><div>Scu-Au NPs were successfully fabricated using Scu extract as a reducing agent. The Scu-Au NPs were spherical with a size of 50 nm. During the synthesis process, the levels of reducing sugars, flavonoids, and polyphenols in the Scu extract decreased by 80.8%, 54.3%, and 70.1%, respectively. Scu-Au NPs demonstrated excellent photothermal responsiveness, thermostability, and biocompatibility. For chemo-photothermal anticancer therapy, the cytotoxicity of Scu-Au NPs on 4T1 cells reached approximately 85% upon exposure to 808 nm NIR irradiation. The anticancer activity was attributed to the induction of apoptosis and necrosis, achieved by increasing intracellular ROS levels, causing cell cycle arrest at the S phase, and modulating the expression of apoptosis-related proteins.</div></div><div><h3>Discussion</h3><div>Our synthesized Scu-Au NPs exhibit favorable photothermal conversion characteristics, demonstrating excellent therapeutic efficacy and safety for cancer treatment.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100536"},"PeriodicalIF":0.0,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142593702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"From tradition to evidence-base: Leveraging TCM human use experience in modern drug development","authors":"Lu Lu ,&nbsp;Shihao Ni ,&nbsp;Xingling He ,&nbsp;Yusheng Huang ,&nbsp;Xingling Chen ,&nbsp;Zhongqi Yang","doi":"10.1016/j.prmcm.2024.100535","DOIUrl":"10.1016/j.prmcm.2024.100535","url":null,"abstract":"<div><h3>Introduction</h3><div>Traditional Chinese medicines (TCM) have been used in China for hundreds, and in some cases, thousands of years, accumulating substantial clinical experience known as \"TCM Human Use Experience.\" These medicines are also widely used in modern medical institutions, presenting the challenge of leveraging this extensive experience and applying modern evidence-based medicine and pharmaceutical methods for the scientific research and development of new drugs from ethnic medicines.</div></div><div><h3>Methods</h3><div>A literature and regulatory search was conducted using PubMed, Web of Science, CNKI, and relevant national databases (CDE, FDA, PMDA, EMA) to collect peer-reviewed studies and policies on TCM human use experience and its integration into modern drug development. In total, 112 articles and regulations were reviewed, with 12 excluded due to irrelevance to empirical TCM applications.</div></div><div><h3>Results</h3><div>Our review identifies the methodological challenges and innovations necessary for integrating TCM into the modern medical landscape. We propose a systematic approach for the collection and analysis of TCM clinical data, including the establishment of a standardized database for TCM human use experience, the translation of TCM concepts into modern medical practices, and ensuring efficacy, safety, and regulatory compliance through rigorous data methodologies.</div></div><div><h3>Discussion</h3><div>Our findings advocate for a balanced approach that respects the rich heritage of TCM while embracing contemporary scientific and clinical standards. This integration has the potential to enrich global healthcare with diverse, evidence-based treatment options, significantly contributing to the broader acceptance and integration of TCM into global healthcare systems.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100535"},"PeriodicalIF":0.0,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532920","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological relevance of taraxasterol: A review","authors":"Olabisi Tajudeen Obafemi ,&nbsp;Ademola Olabode Ayeleso ,&nbsp;Blessing Ariyo Obafemi ,&nbsp;Olusola Bolaji Adewale ,&nbsp;Benjamin Olusola Omiyale ,&nbsp;Sogolo Lucky Lebelo ,&nbsp;Monde McMillan Ntwasa","doi":"10.1016/j.prmcm.2024.100533","DOIUrl":"10.1016/j.prmcm.2024.100533","url":null,"abstract":"<div><h3>Introduction</h3><div>Taraxasterol is a pentacyclic triterpenoid which was first discovered from the roots of <em>Taraxacum officinale</em>. However, it is generally found in the <em>Taraxacum</em> genus (Pugongying in Chinese). It has been reported to possess several medicinal properties, and modulate several biochemical and metabolic signaling pathways as a means of exerting its pharmacological effects. Even though some biological effects have been ascribed to taraxasterol, it is still being explored for more therapeutic benefits. This review aimed to highlight the relevance of taraxasterol as an antidiabetic, anti-cancer, anti-inflammatory and an antioxidant agent.</div></div><div><h3>Methods</h3><div>Articles for this review were searched on Scopus, Nature, SpringerLink and PubMed databases. The keywords used for the search were “taraxasterol pharmacology”, “taraxasterol antioxidant”, “taraxasterol cancer”, “taraxasterol biosynthesis” and “taraxasterol antidiabetic”. Relevance and report of distinct mechanisms of action were considered in the selection.</div></div><div><h3>Results</h3><div>This review underlines the therapeutic potential of taraxasterol in cancer and diabetes conditions, while also highlighting its anti-inflammatory and antioxidant effects. Some specific biochemical pathways that are modulated due to the pharmacological effect of taraxasterol were diagrammatically represented.</div></div><div><h3>Conclusions</h3><div>It is hoped that this review would stimulate interest in taraxasterol by focusing on its pharmacological relevance, specific mechanisms of action and pharmacokinetics. This might facilitate its eventual development into drug and adoption into treatment regimen of various diseases.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100533"},"PeriodicalIF":0.0,"publicationDate":"2024-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532919","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phytochemistry, antioxidant and anti-diabetic activities of Sterculia villosa in-vitro","authors":"Debarupa Hajra,&nbsp;Anirban Chouni,&nbsp;Santanu Paul","doi":"10.1016/j.prmcm.2024.100530","DOIUrl":"10.1016/j.prmcm.2024.100530","url":null,"abstract":"<div><h3>Objective</h3><div>As ongoing research continues, many anti-diabetic agents still have a multitude of side effects which is the reason why more and more people resort to traditional medicines such as Traditional Chinese Medicine (TCM). There are many Therapeutic Species of <em>Sterculia</em> spp. that are commonly used in TCM practices. Here, we have studied one of such TCM herbal plants, namely <em>Sterculia villosa</em> Roxb. (Chinese: 绒毛苹婆), for its anti-diabetic potential. In this way, the study intends to assess its effectiveness and examine its suitability as a raw natural medicine for diabetes management in traditional medicine.</div></div><div><h3>Method</h3><div><em>In-vitro</em> anti-diabetic property was evaluated by <em>α</em>-amylase and <em>α</em>-glucosidase enzyme inhibition and glucose uptake assays. Metabolomic profiling by GC–MS was conducted to determine the probable phyto-constituents in <em>S. villosa</em>. These phyto-compounds were further subjected to <em>in-silico</em> molecular docking studies, identifying stigmasterol as the most potent anti-diabetic phyto-compound. Glucose uptake efficacy was estimated by a fluorescence microplate reader employing glucose analog, 2-NBDG. Molecular dynamic studies (MDS) were carried out with GROMACS to comprehend the protein-ligand binding stability.</div></div><div><h3>Results</h3><div>Stigmasterol showed enhanced enzyme inhibition for both <em>α-</em>amylase (IC₅₀ 23.84±1.37 μM) and <em>α-</em>glucosidase (IC₅₀ 39.56±1.5 μM). Line-weaver Burk plot revealed competitive and mixed modes of inhibition for <em>α-</em>amylase and <em>α-</em>glucosidase, respectively. The GC-–MS analysis identified 23 vital phyto-compounds present in the methanolic extract of the <em>S. villosa</em> leaves. Upon screening against crucial anti-diabetic proteins by <em>in-silico</em> molecular docking, stigmasterol followed by lupeol, Stigmasta-3,5-diene, and γ-sitosterol were found to be the most effective lead compounds. Stigmasterol also showed potent hypoglycaemic efficacy, as evidenced by augmentation of 2-NBDG glucose uptake in 3T3-L1 cells. The docking and simulation studies against four crucial anti-diabetic targets, <em>α-</em>amylase, <em>α-</em>glucosidase, GLUT 4, and IRS-1, predicted that stigmasterol exhibits a multi-pronged anti-diabetic activity mediated by <em>α</em>-amylase inhibition and activation of IRS1 pathway, simultaneously. The MDS studies highlighted that stigmasterol showed stable interactions with these four proteins, as evidenced by the RMSD, RMSF and hydrogen bond analysis.</div></div><div><h3>Conclusion</h3><div>The results of this study are intriguing, as they identify stigmasterol, sourced from the medicinal plant <em>S. villosa</em>, as a potential breakthrough in the field of diabetic remediation. This discovery paves the way for further research and development of stigmasterol as a more effective and safer treatment for diabetes.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100530"},"PeriodicalIF":0.0,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532921","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}