Acharya Balkrishna , Meenakshi Panwar , Sakshi Mishra , Vidushi Kala , Vedpriya Arya , Anurag Dabas
{"title":"A mechanistic review on Zanthoxylum species for anti-inflammatory and analgesic potentials","authors":"Acharya Balkrishna , Meenakshi Panwar , Sakshi Mishra , Vidushi Kala , Vedpriya Arya , Anurag Dabas","doi":"10.1016/j.prmcm.2024.100553","DOIUrl":"10.1016/j.prmcm.2024.100553","url":null,"abstract":"<div><h3>Introduction</h3><div>In Traditional Chinese Medicine (TCM), <em>Zanthoxylum</em> species are valued for their analgesic and anti-inflammatory effects, relieving pain and controlling inflammation. The study aimed to provide insight into how <em>Zanthoxylum</em> species reduce inflammation and pain by targeting molecular pathways and regulating immune responses.</div></div><div><h3>Methods</h3><div>A structured literature search on PubMed, ScienceDirect, and Google Scholar using targeted keywords yielded a broad selection of sources, which were refined to include 104 articles and 50 books from 1978 to 2023 based on strict criteria. Data extraction focused on identifying bioactive compounds and synthesizing insights into the therapeutic mechanisms of <em>Zanthoxylum</em> species, particularly the key pathways involved.</div></div><div><h3>Results</h3><div>Only 13 of the 33 traditionally used species were shown to be effective in analgesic responses, and only two were employed in treating inflammation ailments. In comparison, 18 species were found to have both anti-inflammatory and analgesic properties. Furthermore, 16 species exhibited anti-inflammatory and analgesic potential in various in-vitro/in-vivo studies. Only ten species studied had anti-inflammatory responses, two had analgesic activity, and four had both anti-inflammatory and analgesic responses. Bioactive compounds like zanthoxylumamides, zanthoaustrones C, tetrahydrobungeanol, decarene, and zanthoxylumamide B exhibit anti-inflammatory effects through MyD88, IRF3, MAPK, and NF-κB pathways. Additionally, the alkaloid benzophenanthridine and essential oils from various plant parts provide analgesic effects by reducing writhing and flinching responses.</div></div><div><h3>Discussion</h3><div>Modern studies support the traditional use of <em>Zanthoxylum</em> species for inflammation and pain, highlighting anti-inflammatory and analgesic effects via key pathways and suggesting further clinical validation for safety and efficacy.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100553"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142748716","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}
Feng Li , Yilei Dong , Guangrui Wang , Zishan Huang , Wenting Song , Xiaoyu Zheng , Peng Zhang , Mingjiang Yao
{"title":"Exploring the pharmacological mechanism of Tongluo Qingnao formula in treating acute ischemic stroke: A combined approach of network pharmacology, molecular docking and experimental evidences","authors":"Feng Li , Yilei Dong , Guangrui Wang , Zishan Huang , Wenting Song , Xiaoyu Zheng , Peng Zhang , Mingjiang Yao","doi":"10.1016/j.prmcm.2024.100550","DOIUrl":"10.1016/j.prmcm.2024.100550","url":null,"abstract":"<div><h3>Introduction</h3><div>Tongluo Qingnao (TLQN) Formula is a patent Traditional Chinese Medicine injection designed for the treatment of Acute Ischemic Stroke (AIS) and associated complications. Previous researches had shown promising potential of TLQN in treating ischemic brain edema. This study aimed to reveal specific mechanisms of TLQN in treating AIS by bioinformatics analysis and following confirmatory experiments.</div></div><div><h3>Methods</h3><div>HPLC was used to analyze the active ingredients of TLQN. Network Pharmacology and Molecular Docking were introduced to screen treatment targets and pathways. And then middle cerebral artery occlusion and reperfusion (MCAO/R) model was established in rats to verify the therapeutic effect of TLQN in neurological deficit score, cerebral infarction size, HE staining, TUNEL staining, and proteins expression related to inflammation, apoptosis and the PI3K-AKT signaling pathway.</div></div><div><h3>Results</h3><div>Seven main active ingredients were contained in TLQN. Network pharmacology identified IL-6 and IL-1β as the key targets, and PI3K-AKT as the critical pathway. Molecular Docking analysis indicated that the constituents of TLQN demonstrated a high affinity for crucial targets. TLQN could significantly reduce neurological deficits, pathological lesions and apoptosis caused by AIS. Western blotting results indicated that TLQN can activate the PI3K-AKT signaling pathway, inhibit the expression of pro-apoptotic proteins bax, Caspase-3 and inflammatory factors IL-6, IL-1β.</div></div><div><h3>Discussion</h3><div>TLQN has a therapeutic effect on AIS, and these results highlight the therapeutic effects of TLQN on AIS by activating PI3K-AKT signaling pathway to inhibit inflammation and apoptosis.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100550"},"PeriodicalIF":0.0,"publicationDate":"2024-11-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142703333","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":"Effect of Eriobotrya japonica L. (Chinese medicinal plant) on the regulation of lipid metabolism in atherosclerosis-induced mice and in HepG-2 cells","authors":"Imane Mokhtari , Dragan Milenkovic , Souliman Amrani , Hicham Harnafi","doi":"10.1016/j.prmcm.2024.100552","DOIUrl":"10.1016/j.prmcm.2024.100552","url":null,"abstract":"<div><h3>Background</h3><div>Hyperlipidemia and related metabolic disorders are the main cause of nonalcoholic fatty liver diseases, atherosclerosis and cardiovascular complications. Loquat (<em>Eriobotrya japonica</em>) leaf infusion is an innovative formula derived from Traditional Chinese medicine, known for its therapeutic properties against a number of ailments including inflammation, diabetes and hyperlipidemia.</div></div><div><h3>Aim of the study</h3><div>This study was designed to identify the active compounds of an aqueous extract of <em>E. japonica</em> leaves (ELE) and to investigate its effect on hyperlipidemia and related metabolic complications in high-fat high-sucrose diet-fed mice as well as to elucidate the possible underlying mechanisms.</div></div><div><h3>Materials and Methods</h3><div>Mice were fed a high-fat high-sucrose diet for 3 months and treated with the ELE at doses of 50 mg/kg and 100 mg/kg. Lipids in plasma, liver, adipose tissue, bile and feces were quantified using enzymatic kits. Liver steatosis and oxidative status were highlighted by measuring AST, ALT, ALP, MDA, SOD and catalase activities as well as monitoring of lipid droplets in histological sections. The identification and quantification of possible active compounds were carried out using the HPLC-DAD method. The underlying mechanisms were predicted by <em>in silico</em> study and confirmed by quantifying the expression of the principal involved proteins including PCSK-9, CYP7A1 and p-AMPK in HepG2 cells.</div></div><div><h3>Results</h3><div>The ELE restored lipid metabolism and improved liver histological structures. It also reduced oxidative stress by lowering MDA levels and activating SOD and catalase enzymes. The ELE prevented hepatic steatosis and corrected transaminases profile. HPLC analysis reveals seven phenolic compounds, with ferulic acid being the major one. The extract and its identified phenolic compounds upregulated the expression of CYP7A1 and p-AMPK while downregulated the expression of PCSK-9 in HepG2 cells. The ELE appears to be nontoxic in mice (LD<sub>50</sub>>5000 mg/kg) and in HepG2 cells at pharmacologically active doses.</div></div><div><h3>Conclusion</h3><div>the ELE could be considered as a source of active biomolecules to produce phytotherapeutics drugs or dietary supplements to treat hyperlipidemia and related cardio-metabolic diseases.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100552"},"PeriodicalIF":0.0,"publicationDate":"2024-11-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142703334","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}
Juan Leonardo , Purnawan Pontana Putra , Trina Ekawati Tallei , Fatimawali Fatimawali , Nurpudji Astuti Taslim , Raymond Rubianto Tjandrawinata , Vincent Lau , Saad Mustafa , Miguel A Prieto , Fahrul Nurkolis
{"title":"Unraveling biomolecules, antidiabetic and antioxidants properties of DelitesTM via pharmacoinformatics and in vitro investigation","authors":"Juan Leonardo , Purnawan Pontana Putra , Trina Ekawati Tallei , Fatimawali Fatimawali , Nurpudji Astuti Taslim , Raymond Rubianto Tjandrawinata , Vincent Lau , Saad Mustafa , Miguel A Prieto , Fahrul Nurkolis","doi":"10.1016/j.prmcm.2024.100551","DOIUrl":"10.1016/j.prmcm.2024.100551","url":null,"abstract":"<div><h3>Introduction</h3><div>Type 2 diabetes (T2D) remains a global health burden characterized by insulin resistance and chronic hyperglycemia, often exacerbated by oxidative stress, leading to severe complications. Despite the efficacy of pharmacological treatments such as metformin, their side effects and costs highlight the need for alternative therapies. Delites™ (Chong Cao Ling Zhi Xiang Tang), a multi-herbal formulation, presents a promising solution with its bioactive compounds including Apocynin, Curcumin, and Quercetin, which are hypothesized to target T2D pathways.</div></div><div><h3>Methods</h3><div>This study employed pharmacoinformatics, in vitro assays, and molecular dynamics simulations to evaluate the antidiabetic and antioxidative properties of Delites™. Metabolomic profiling using Ultra-High-Performance Liquid Chromatography coupled with High-Resolution Mass Spectrometry identified active compounds, while <em>in silico</em> docking analyzed interactions with T2D-related proteins (<em>e.g</em>., KCNJ11, TCF7L2). Enzyme inhibition assays measured alpha-glucosidase and alpha-amylase activity, and antioxidant potential was assessed using ABTS inhibition.</div></div><div><h3>Results</h3><div>Delites™ demonstrated significant enzyme inhibition (EC<sub>50</sub> < metformin), strong binding affinity to T2D proteins (e.g., Sachaliside 2: -9.4 kcal/mol with TCF7L2), and antioxidant activity comparable to Trolox (EC<sub>50</sub>: 54.44 mg/mL). Molecular dynamics confirmed stable interactions of its compounds with target proteins, while network pharmacology highlighted multi-target potential against diabetes-related pathways.</div></div><div><h3>Discussion</h3><div>The findings underline Delites™ as a multi-target therapeutic candidate for T2D management. Its ability to inhibit carbohydrate-hydrolyzing enzymes, interact strongly with key proteins, and mitigate oxidative stress positions it as a holistic alternative. However, further clinical trials are essential to validate these promising in vitro and <em>in silico</em> results, particularly its long-term efficacy and safety.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100551"},"PeriodicalIF":0.0,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142721284","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":"Protective effects of Bidens pilosa alleviates against alcohol—induced hepatic steatosis in rats: In vivo studies and in silico analysis","authors":"Melva Silitonga , Hudson Sidabutar , Hendro Pranoto , Adriana Yulinda Dumaria LumbanGaol , Feimmy Ruth Pratiwi Sipahutar","doi":"10.1016/j.prmcm.2024.100546","DOIUrl":"10.1016/j.prmcm.2024.100546","url":null,"abstract":"<div><h3>Background</h3><div>Steatosis has become the critical indicator of the higher alcohol exposure to liver injury. Traditional Chinese medicine, notably <em>Bidens pilosa</em>, is used as anti-inflammatory, antihyperglycemic, and hepatoprotective. This current study aimed to investigate the protective effect of <em>Bidens pilosa</em> leaves ethanolic extract (EEB) against alcohol induced hepatic steatosis.</div></div><div><h3>Methods</h3><div>Using the rat model of alcoholic hepatic steatosis (AHS), this study investigated EEB efficacy through the experimental analysis and in silico method. The animals received EEB at doses of 300 and 600 mg/kg for 42 days in the acute alcoholic experiment. Biochemical analysis and histopathological alteration are examined in alcohol-induced liver rats. Additionally, the pharmacological analysis, molecular docking and dynamic study were evaluated.</div></div><div><h3>Results</h3><div>The results indicated that the EEB has ameliorative effects against hepatic steatosis. It significantly improved hepatic histopathological change, the level of blood glucose, triglyceride, LDL and cholesterol in rats exposed to alcohol. Furthermore, the virtual screening study demonstrated the predominant compounds of EEB might regulate the top core targets linked to AHS, particularly AKT/PIK3CA, MAPK, and MTOR, respectively.</div></div><div><h3>Conclusion</h3><div>Thus, the preventive effect of EEB could be an underlying mechanism for the development of herbal medicine to treat AHS in clinical therapy.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100546"},"PeriodicalIF":0.0,"publicationDate":"2024-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142703312","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}
Van Hung Hoang , Thi Thanh Huong Le , Phu Hung Nguyen , Viet Hoang , Van Khang Pham , Thi Kieu Oanh Nguyen , Dinh Quang Hung Can
{"title":"Acorus gramineus extract decreases cancer stem cell properties and stimulates ROS signaling pathway in HepG2 hepatocellular carcinoma cells","authors":"Van Hung Hoang , Thi Thanh Huong Le , Phu Hung Nguyen , Viet Hoang , Van Khang Pham , Thi Kieu Oanh Nguyen , Dinh Quang Hung Can","doi":"10.1016/j.prmcm.2024.100548","DOIUrl":"10.1016/j.prmcm.2024.100548","url":null,"abstract":"<div><h3>Background</h3><div><em>Acorus gramineus</em> is called “Shi Chang Pu'” in Chinese and has been used in traditional Chinese medicine (TCM) for over 2,000 years. The records in the 'Shennong Bencao Jing' show that many species in the genus <em>Acorus</em> are used to treat various diseases in humans such as epilepsy, cardiovascular issues, abdominal pain, memory loss, etc. Several species of the genus <em>Acorus</em> have been demonstrated to exhibit antiproliferative effects against various cancer cell lines. This study aims to evaluate the inhitory effects of <em>Acorus gramineus</em> extract (AGE) on HepG2 liver cancer cells.</div></div><div><h3>Methods</h3><div>The inhibitory effect of AGE on HepG2 cell proliferation was assessed using the MTT assay. Migration was analyzed using the wound healing technique. The 3D culture technique was employed to evaluate tumorsphere formation and the invasive potential of cancer cells. Real-time PCR was used for mRNA expression analysis. Changes in the expression levels of CD44 protein and ROS were analyzed using fluorescence staining techniques. Chemical compounds of AGE were identified using UPLC-QToF-MS.</div></div><div><h3>Results</h3><div>The results indicate that AGE exhibits potent inhibitory activity against cell proliferation, with an IC50 value of 34.1 mg/mL. AGE significantly inhibited both the formation and growth of tumorspheres in 3D cultures, reducing both their number and size. Additionally, AGE was found to suppress the invassion of cancer cells. AGE regulated the downregulation of stem cell-related markers including NANOG, SOX2, OCT4, and ALDH. AGE was also shown to increase the production of reactive oxygen species (ROS) within cells by activating genes involved in ROS signaling pathways, which may lead to a decrease in cell proliferation, migration, and invasion, as well as a reduction in cancer stem cell properties. Finally, 58 compounds present in AGE were identified by UPLC-QtoF-MS analysis, and Mulberrofuran K, Akebonoic acid, and Shancilin were evaluated for their affinity with protein markers related to liver cancer stem cells.</div></div><div><h3>Conclusion</h3><div>This study is the first report on the inhibitory activity of AGE against cancer stem cell characteristics in HepG2 cells, highlighting the potential of this plant species as an anti-liver cancer agent.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100548"},"PeriodicalIF":0.0,"publicationDate":"2024-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142703311","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}
Hui su , Jun Dong , Luyao Liu , Zechen Yan , Rujie Zhuang , Guangxin Huang , Haipeng Xue , Zhanwang Xu , Yu Pan
{"title":"Gu Sui Bu (Drynaria fortunei J. Smith) prevents osteoporosis in ovariectomized rats by inhibiting pyroptosis through NLRP3/GSDMD/CASPASE-1","authors":"Hui su , Jun Dong , Luyao Liu , Zechen Yan , Rujie Zhuang , Guangxin Huang , Haipeng Xue , Zhanwang Xu , Yu Pan","doi":"10.1016/j.prmcm.2024.100544","DOIUrl":"10.1016/j.prmcm.2024.100544","url":null,"abstract":"<div><div>Traditional Chinese medicine Gu Sui Bu (<em>Drynaria fortunei J. Smith</em>), has the effect of tonifying the kidneys and strengthening bone. There are many modern studies on the anti-osteoporosis pharmacological mechanism of Gu Sui Bu (<em>Drynaria fortunei J. Smith</em>) but no reports on the pharmacological mechanism of Gu Sui Bu (<em>Drynaria fortunei J. Smith</em>) improving cell pyroptosis and anti-osteoporosis have been found.</div></div><div><h3>Aim</h3><div>This study aims to verify the changes in cellular standard indicators in postmenopausal osteoporosis, thereby revealing the participating mechanism of pyroptosis and the intervention effect of Gu Sui Bu (<em>Drynaria fortunei J. Smith)</em> .</div></div><div><h3>Methods</h3><div>Gu Sui Bu (<em>Drynaria fortunei J. Smith</em>) subjected to UHPLC-Q-Orbitrap-MS/MS analysis, and the OVX rat model was constructed in vivo as the research object. It was divided into sham operation group (SHAM), ovariectomized osteoporosis model group (OVX) and Gu Sui Bu (<em>Drynaria fortunei J. Smith</em>) group (TFRD-L, TFRD-H). After 3 months of modeling, the medication group was treated with Gu Sui Bu (<em>Drynaria fortunei J. Smith</em>) and the samples were collected after 12 weeks of intervention. ELISA was used to detect the levels of Caspase-1, NLRP3, GSDMD, IL-1β, and IL-18 in rat serum; the right femur was taken for Micro-CT large bone microstructure scanning and femoral BMD detection; the femur was subjected to rat histopathology HE, TRAP staining; immunohistochemistry and immunofluorescence staining of rat histopathology were performed. WB and PCR were used to observe the expression of Osteoblasts and pyroptosis-related indicators Caspase-1, NLRP3, GSDMD and RUNX2, IL-1β, and IL-18.</div></div><div><h3>Results</h3><div>UHPLC-Q-Orbitrap-MS/MS analysis the main compounds in Gu Sui Bu (<em>Drynaria fortunei J. Smith)</em> samples were identified. These 9 chemical components are Palmitic acid, Fisetin, Caffeic acid, Naringin, Rutin, Uridine, Cafestol, Astilbin . Rat Micro-CT, The results of HE staining and TRAP showed that compared with the rats in the OVX group, the number of bone trabeculae in the rats in the <em>Gu Sui Bu (Drynaria fortunei J. Smith)</em> medication group (TFRD-L, TFRD-H) increased, became wider and thicker, and the bone density increased. Continuity increases and bone lacunae decrease. Rat serum ELISA, femoral tissue immunohistochemistry, immunofluorescence staining and WB, PCR showed that compared with the OVX group, Caspase-1, NLRP3, The expression levels of GSDMD and inflammation were reduced (p<0.05), and the expression of osteogenic marker RUNX2 was reduced and increased (p<0.05).</div></div><div><h3>Conclusion</h3><div>The traditional Chinese medicine Gu Sui Bu (<em>Drynaria fortunei J. Smith)</em> can improve the bone density of ovariectomized osteoporosis model rats and significantly enhance the bone microstructure. At the same time, it reduced the expres","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100544"},"PeriodicalIF":0.0,"publicationDate":"2024-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142702784","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":"In silico and in vivo evaluations of fisetin and fisetin-loaded nanosuspension on monoamine oxidase inhibition in Aβ(25–35) induced dementia in mice model","authors":"Siti Zaidathul Iman Zolkiffly , Mizaton Hazizul Hasan , Siti Azma Jusoh , Ashok Kumar Janakiraman , Sathesh Kumar Sukumaran , Noreen Husain , Yuslina Zakaria , Hanish Singh Jayasingh Chellammal","doi":"10.1016/j.prmcm.2024.100547","DOIUrl":"10.1016/j.prmcm.2024.100547","url":null,"abstract":"<div><h3>Background</h3><div>Amyloid beta (Aβ) plaques on the extracellular matrix and intracellular neurofibrillary tangles comprise the key indicative pathology of Alzheimer's disease (AD). Fisetin, an antioxidant bioactive compound having pharmacotherapeutic effects is applied by traditional Chinese medicine (TCM) such as <em>Toxicodendron vernicifum</em> (Chinese lacquer tree), <em>Cotinus coggygria Scop</em>, Gan Shuang granulates and formula of <em>Acacia catechu</em>-<em>Scutellariae Radix</em>. Nevertheless, fisetin has constraints such as low oral bioavailability, insignificant aqueous solubility and high hepatic metabolisms.</div></div><div><h3>Objective</h3><div>This investigation aimed to envisage the effects of fisetin and its optimised nanoformulation on Aβ<sub>(25–35)</sub> desirous neurotoxicity in mice through deciphering inhibitory actions against monoamine oxidase A and B (MAO-A and B) enzymes following molecular docking.</div></div><div><h3>Methods</h3><div>Molecular docking with MAO-A and B enzymes were accomplished by AMDock's integrated AutoDock Tools (ADT) scripts. For <em>in vivo</em> studies, fisetin nanosuspension was prepared by nanoprecipitation method and evaluated for standard characterization. 10 and 20 mg/kg of fisetin and 10 mg/kg of fisetin nanosuspension were given once daily to mice for 21 days. On the 15th day, the mice were challenged with Aβ<sub>(25–35)</sub> by intracerebroventricular injection (ICV) and behavioural tests (open field and elevated plus maze) were performed on the 20th day. Biochemical and histology were examined in brain tissues.</div></div><div><h3>Results</h3><div>Fisetin docked to the catalytic positions of MAO-A and B, unveiling good binding scores and molecular interactions with amino acid residues for inhibition activities. Fisetin nanosuspension has average particle size (225.4 ± 2.95 nm) with low polydispersity index (0.19) and standard zeta potential (-19.13 ± 1.17 mV). Findings showed that fisetin increased locomotor activity and reduced anxiety-like behaviour. Fisetin and its nanosuspension significantly reduced the concentration of MAO-A (<em>P <</em> 0.01) and MAO-B enzymes suggesting a potential neuroprotection effect in Aβ peptide-induced amnesia in mice.</div></div><div><h3>Conclusion</h3><div>Fisetin with optimized bioavailability, effectively exhibits neuroprotection through molecular interactions of MAO enzymes. Further investigations affidavits the neuroprotection through bidirectional pathways related to biogenic amines and their deamination on Aβ stress conditions.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100547"},"PeriodicalIF":0.0,"publicationDate":"2024-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142657243","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}
Zhong-mou Zhang , Tian-tian Zuo , Ming-hui Chen , Cai-xia Zang , Yong-jian Wang , Ya-dan Wang , Shuang-cheng Ma
{"title":"Progress on Tripterygium wilfordii Hook f. as a treatment option for neurodegenerative diseases","authors":"Zhong-mou Zhang , Tian-tian Zuo , Ming-hui Chen , Cai-xia Zang , Yong-jian Wang , Ya-dan Wang , Shuang-cheng Ma","doi":"10.1016/j.prmcm.2024.100545","DOIUrl":"10.1016/j.prmcm.2024.100545","url":null,"abstract":"<div><h3>Introduction</h3><div>Neurodegenerative diseases are becoming increasingly widespread as the global population ages. Although neurodegenerative diseases have received continued attention from researchers, there are currently no drugs that can reverse the progression of these diseases. <em>Tripterygium wilfordii</em> Hook f., a traditional form of Chinese medicine, has been widely used to treat many diseases due to its numerous bioactivities and shows considerable potential for the improvement of neurodegenerative diseases.</div></div><div><h3>Methods</h3><div>Articles for this review were searched on Pubmed, Scifinder, CNKI and Web of Science. Keyword included “<em>Tripterygium wilfordii</em> and neurodegenerative disease,” “triptolide and neurodegenerative disease,” “celastrol and neurodegenerative disease,” and “tripchlorolide and neurodegenerative disease.” 178 articles were initially retrieved and 119 articles were cited finally.</div></div><div><h3>Results</h3><div>In this study, we summarize the progress of <em>T. wilfordii</em>, especially its bioactive components such as triptolide, celastrol and tripchlorolide for the treatment of neurodegenerative diseases and review the therapeutic mechanisms involved. This article provides reference guidelines for the use of <em>T. wilfordii</em> to treat neurodegenerative diseases.</div></div><div><h3>Discussion</h3><div>The bioactive components like triptolide, celastrol, tripchlorolide and others extracted from <em>T. wilfordii</em> has enormous potential in the treatment of neurodegenerative diseases. However, the vague pathogenic mechanisms underlying neurodegenerative diseases, as well as toxicity and side effects of <em>T. wilfordii</em> on clinical use still exist. Further research is needed to investigate these issues.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100545"},"PeriodicalIF":0.0,"publicationDate":"2024-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142703310","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}
Mei Wang , Wendi Huang , Juan Huang , Jingshan Shi , Nanqu Huang , Yong Luo
{"title":"Traditional Chinese medicine in Alzheimer's disease: From the perspective of GSK-3β and Tau hyperphosphorylation","authors":"Mei Wang , Wendi Huang , Juan Huang , Jingshan Shi , Nanqu Huang , Yong Luo","doi":"10.1016/j.prmcm.2024.100543","DOIUrl":"10.1016/j.prmcm.2024.100543","url":null,"abstract":"<div><h3>Introduction</h3><div>Alzheimer's disease (AD) accounts for the majority of dementia cases, characterized by a gradual decline in memory and cognitive functions. Traditional Chinese medicine (TCM) has a long history of treating AD and has proposed a series of causes, pathogenesis and treatment methods, and has extremely rich experience in the treatment of AD. TCM believes that deficiency of the spleen, which is the main organ for the body to absorb nutrients, is one of the important causes of AD. Which coincides with the theory that AD is type 3 diabetes in recent years. Therefore, effectively regulating the common targets of AD and diabetes is a potential strategy for treating spleen deficiency type AD.</div></div><div><h3>Method</h3><div>By conducting an in-depth search in PubMed and China National Knowledge Infrastructure (CNKI), using the keywords \" Traditional Chinese Medicine\", \"Alzheimer's Disease\", \"GSK-3β\", \"Tau Protein\" and \"Tau Hyperphosphorylation\". Ultimately, 92 papers were included for review.</div></div><div><h3>Result</h3><div>Glycogen synthase kinase 3 beta (GSK-3β) plays a significant role in the pathogenesis of AD, and numerous <em>in vitro</em> and <em>in vivo</em> experiments have demonstrated that Chinese medicine monomers and compounds can inhibit its activity, reducing the hyperphosphorylation of Tau.</div></div><div><h3>Discussion</h3><div>TCM can affect the activity of GSK-3β through various pathways, thereby reducing the hyperphosphorylation of Tau protein and improving the cognitive function of AD. These studies highlight the potential of TCM in treating AD, but further basic and clinical research is still required to validate their safety and efficacy. It is expected that our review will yield novel insights and a scientific foundation for investigating the underlying mechanisms of AD and developing novel anti-AD therapeutics.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100543"},"PeriodicalIF":0.0,"publicationDate":"2024-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142657351","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}