Archives of Pharmacal Research最新文献

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2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition 2-杰拉尔基-1-甲氧基赤藓霉素II通过AMPK激活和AKT抑制减轻肝细胞中的脂质积聚和炎症。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-10-02 DOI: 10.1007/s12272-023-01464-z
Yiyuan Xi, Soeun Kim, Thi Thanh Thuy Nguyen, Phil Jun Lee, Jujia Zheng, Zhuofeng Lin, Namki Cho
{"title":"2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition","authors":"Yiyuan Xi,&nbsp;Soeun Kim,&nbsp;Thi Thanh Thuy Nguyen,&nbsp;Phil Jun Lee,&nbsp;Jujia Zheng,&nbsp;Zhuofeng Lin,&nbsp;Namki Cho","doi":"10.1007/s12272-023-01464-z","DOIUrl":"10.1007/s12272-023-01464-z","url":null,"abstract":"<div><p>A growing proportion of the global adult and pediatric populations are currently affected by nonalcoholic steatohepatitis (NASH), leading to rising rates of liver fibrosis and hepatocellular carcinoma without effective pharmacotherapy. Here, we investigated whether 2-geranyl-1-methoxyerythrabyssin II (GMET), isolated from <i>Lespedeza bicolor</i>, could alleviate lipid accumulation and inflammatory responses in a NASH model. GMET exhibited potent in vitro and in vivo effects against lipid accumulation and attenuated inflammatory responses without cytotoxicity. Mechanistically, GMET inhibits acetyl-CoA carboxylase (ACC), sterol regulatory element-binding proteins-1c (SREBP1), and mammalian target of rapamycin (mTOR), and activates PPARα by activating AMP-activated kinase (AMPK), leading to the alleviation of lipid accumulation. In addition, GMET suppresses the NF-κB pathway by activating AMPK and inhibiting the activated protein kinase B (AKT)/IκB-kinase (IKK) pathway, leading to the inhibition of the inflammatory response in hepatocytes. All these protective effects of GMET on lipid accumulation and inflammation in vivo and in vitro were largely abolished by co-treatment with dorsomorphin, an AMPK inhibitor. In conclusion, GMET alleviated lipid accumulation and inflammation to preserve normal hepatocyte function in steatohepatitis. Thus, GMET is a novel potential multi-targeting compound to improve steatohepatitis.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 9-10","pages":"808 - 824"},"PeriodicalIF":6.7,"publicationDate":"2023-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41092977","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Exploring new histone deacetylase 6 inhibitors and their effects on reversing the α-tubulin deacetylation and cell morphology changes caused by methamphetamine 探索新的组蛋白脱乙酰酶6抑制剂及其逆转甲基苯丙胺引起的α-微管蛋白脱乙酰化和细胞形态变化的作用。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-30 DOI: 10.1007/s12272-023-01467-w
Sunil K. Gupta, Khan Hashim Ali, Sooyeun Lee, Young Ho Seo
{"title":"Exploring new histone deacetylase 6 inhibitors and their effects on reversing the α-tubulin deacetylation and cell morphology changes caused by methamphetamine","authors":"Sunil K. Gupta,&nbsp;Khan Hashim Ali,&nbsp;Sooyeun Lee,&nbsp;Young Ho Seo","doi":"10.1007/s12272-023-01467-w","DOIUrl":"10.1007/s12272-023-01467-w","url":null,"abstract":"<div><p>Indazole-based HDAC6 inhibitors with novel zinc-binding modifications were synthesized and evaluated to determine their potential to inhibit HDAC6. The analogs were subjected to a histone deacetylase (HDAC) enzyme assay, which led to identification of compounds <b>3a</b> and <b>3b</b>. Both compounds demonstrated higher potency and selectivity as HDAC6 inhibitors with IC<sub>50</sub> values of 9.1 nM and 9.0 nM, respectively, and highlighted the importance of the hydroxamic acid moiety for binding to Zn<sup>2+</sup> inside the catalytic pocket of HDAC enzymes. In the neuroblastoma SH-SY5Y cell line, both compounds efficiently acetylated α-tubulin but not histone H3 at a low concentration of 0.5 µM. Moreover, compounds <b>3a</b> and <b>3b</b> effectively reversed the deacetylation of α-tubulin caused by methamphetamine in the SH-SY5Y cell line, suggesting the potential usefulness of HDAC6 selective inhibition in restoring blood brain barrier integrity by reversing methamphetamine-induced deacetylation.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 9-10","pages":"795 - 807"},"PeriodicalIF":6.7,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41103610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Artemongolins A–K, undescribed germacrane-guaiane sesquiterpenoid dimers from Artemisia mongolica and their antihepatoma activities 沙蒿中的Artemonglins A-K、未描述的germacrane guaiane倍半萜二聚体及其抗肝癌活性。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-28 DOI: 10.1007/s12272-023-01466-x
Chong Shang, Yun-Bao Ma, Yuan Wang, Xiao-Feng He, Tian-Ze Li, Ji-Jun Chen
{"title":"Artemongolins A–K, undescribed germacrane-guaiane sesquiterpenoid dimers from Artemisia mongolica and their antihepatoma activities","authors":"Chong Shang,&nbsp;Yun-Bao Ma,&nbsp;Yuan Wang,&nbsp;Xiao-Feng He,&nbsp;Tian-Ze Li,&nbsp;Ji-Jun Chen","doi":"10.1007/s12272-023-01466-x","DOIUrl":"10.1007/s12272-023-01466-x","url":null,"abstract":"<div><p>Artemongolins A<b>–</b>K (<b>1–11</b>), which are undescribed sesquiterpenoid dimers, were obtained from <i>Artemisia mongolica</i> and characterized through comprehensive spectral data, including HRESIMS, IR, 1D and 2D NMR, and ECD calculations. The absolute configurations of compounds <b>1</b>, <b>4</b>, and <b>7</b> were undoubtedly determined by a single-crystal X-ray crystallography. Artemongolins A<b>–</b>K (<b>1–11</b>) featured a rare 5/7/5/5/5/10 hexacyclic system composed of a germacrene and a guaianolide by a fused 2-oxaspiro[4,4]nonane-1-one ring system. Antihepatoma evaluation against three human hepatoma cell lines demonstrated that the most active compounds <b>5</b> and <b>6</b> displayed inhibitory activity with IC<sub>50</sub> values of 88.6 and 57.0 (HepG2), 59.1 and 26.4 (Huh7), and 67.5 and 32.5 (SK-Hep-1) <i>µ</i>M, respectively.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 9-10","pages":"782 - 794"},"PeriodicalIF":6.7,"publicationDate":"2023-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41095025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Anti-osteoporosis effects of triterpenoids from the fruit of sea buckthorn (Hippophae rhamnoides) through the promotion of osteoblast differentiation in mesenchymal stem cells, C3H10T1/2 沙棘果实中三萜类化合物通过促进间充质干细胞C3H10T1/2的成骨细胞分化而发挥的抗骨质疏松作用。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-26 DOI: 10.1007/s12272-023-01468-9
Da Eun Lee, Kun Hee Park, Joo-Hyun Hong, Seon Hee Kim, Ki-Moon Park, Ki Hyun Kim
{"title":"Anti-osteoporosis effects of triterpenoids from the fruit of sea buckthorn (Hippophae rhamnoides) through the promotion of osteoblast differentiation in mesenchymal stem cells, C3H10T1/2","authors":"Da Eun Lee,&nbsp;Kun Hee Park,&nbsp;Joo-Hyun Hong,&nbsp;Seon Hee Kim,&nbsp;Ki-Moon Park,&nbsp;Ki Hyun Kim","doi":"10.1007/s12272-023-01468-9","DOIUrl":"10.1007/s12272-023-01468-9","url":null,"abstract":"<div><p>In a previous study, we discovered that the ethanolic extract of sea buckthorn (<i>Hippophae rhamnoides</i>) fruits exhibited anti-osteoporosis effects both in vitro and in vivo. Through bioassay-guided fractionation, we identified the hexane fraction (HRH) as the active fraction, which was further fractionated using preparative HPLC. Among the resulting six fractions, HRHF4 showed significant activity. In the present study, we focused on the bioassay-guided isolation of bioactive compounds from the HRHF4 fraction. We successfully identified the active HRHF43 fraction, which led us to the isolation of potential bioactive compounds (<b>1–6</b>). The chemical structures of these compounds were determined using NMR data, LC-MS analysis, and HR-ESI-MS data as four triterpenes, ursolic acid (<b>1</b>), uvaol (<b>2</b>), oleanolic aldehyde (<b>3</b>), and ursolic aldehyde (<b>4</b>), together with two fatty acids, methyl linoleate (<b>5</b>) and ethyl oleate (<b>6</b>). To evaluate the efficacy of promoting osteoblast differentiation and the expression of mRNA biomarkers related to osteogenesis, we tested the isolated compounds in the mouse mesenchymal stem cell line, C3H10T1/2. Alkaline phosphate staining demonstrated that triterpenes (<b>1–4</b>) displayed osteogenic activity. Particularly noteworthy, ursolic aldehyde (<b>4</b>) exhibited the most potent effect, showing an 11.2-fold higher activity at a concentration of 10 μg/mL compared to the negative control. Moreover, ursolic aldehyde (<b>4</b>) upregulated the gene expression of bone formation-related biomarkers, including Runx2, Osterix, Alp, and Osteopontin. These findings suggest that the fruit extract of <i>H. rhamnoides</i> may have potential as a nutraceutical for promoting bone health, with ursolic aldehyde (<b>4</b>) identified as an active constituent.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 9-10","pages":"771 - 781"},"PeriodicalIF":6.7,"publicationDate":"2023-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41112552","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Multifaceted roles of mitochondrial dysfunction in diseases: from powerhouses to saboteurs 线粒体功能障碍在疾病中的多方面作用:从权力机构到破坏者。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-26 DOI: 10.1007/s12272-023-01465-y
Surapriya Surendranath Prabhu, Aathira Sujathan Nair, Saiprabha Vijayakumar Nirmala
{"title":"Multifaceted roles of mitochondrial dysfunction in diseases: from powerhouses to saboteurs","authors":"Surapriya Surendranath Prabhu,&nbsp;Aathira Sujathan Nair,&nbsp;Saiprabha Vijayakumar Nirmala","doi":"10.1007/s12272-023-01465-y","DOIUrl":"10.1007/s12272-023-01465-y","url":null,"abstract":"<div><p>The fact that mitochondria play a crucial part in energy generation has led to the nickname “powerhouses” of the cell being applied to them. They also play a significant role in many other cellular functions, including calcium signalling, apoptosis, and the creation of vital biomolecules. As a result, cellular function and health as a whole can be significantly impacted by mitochondrial malfunction. Indeed, malignancies frequently have increased levels of mitochondrial biogenesis and quality control. Adverse selection exists for harmful mitochondrial genome mutations, even though certain malignancies include modifications in the nuclear-encoded tricarboxylic acid cycle enzymes that generate carcinogenic metabolites. Since rare human cancers with mutated mitochondrial genomes are often benign, removing mitochondrial DNA reduces carcinogenesis. Therefore, targeting mitochondria offers therapeutic options since they serve several functions and are crucial to developing malignant tumors. Here, we discuss the various steps involved in the mechanism of cancer for which mitochondria plays a significant role, as well as the role of mitochondria in diseases other than cancer. It is crucial to understand mitochondrial malfunction to target these organelles for therapeutic reasons. This highlights the significance of investigating mitochondrial dysfunction in cancer and other disease research.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 9-10","pages":"723 - 743"},"PeriodicalIF":6.7,"publicationDate":"2023-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41096445","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Review on pharmacological effects of gastrodin 天麻素药理作用研究进展。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-25 DOI: 10.1007/s12272-023-01463-0
Guirong Xiao, Rong Tang, Nan Yang, Yanhua Chen
{"title":"Review on pharmacological effects of gastrodin","authors":"Guirong Xiao,&nbsp;Rong Tang,&nbsp;Nan Yang,&nbsp;Yanhua Chen","doi":"10.1007/s12272-023-01463-0","DOIUrl":"10.1007/s12272-023-01463-0","url":null,"abstract":"<div><p><i>Gastrodia elata</i> Blume is a well-known traditional Chinese medicine that is mainly used to treat diseases related to the nervous system, such as stroke, epilepsy, and headache. Gastrodin is the main bioactive component of <i>Gastrodia elata</i> Blume, and studies have shown that it has extensive pharmacological activity. This narrative review aims to systematically review relevant studies on the pharmacological effects of gastrodin to provide researchers with the latest and most useful information. Studies have shown that gastrodin has prominent neuroprotective effects and can treat or improve epilepsy, Tourette syndrome, Alzheimer’s disease, Parkinson’s disease, emotional disorders, cerebral ischemia-reperfusion injury, cognitive impairment, and neuropathic pain. Gastrodin can also improve myocardial hypertrophy, hypertension, and myocardial ischemia-reperfusion injury. In addition, gastrodin can mitigate liver, kidney, and bone tissue damage caused by oxidative stress and inflammation. In short, gastrodin is expected to treat many diseases, and it is worth investing more effort in research on this compound.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 9-10","pages":"744 - 770"},"PeriodicalIF":6.7,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41106272","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Hyperoside attenuates pyrrolizidine alkaloids-induced liver injury by ameliorating TFEB-mediated mitochondrial dysfunction 金丝桃苷通过改善TFEB介导的线粒体功能障碍来减轻吡咯烷酮生物碱诱导的肝损伤。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-21 DOI: 10.1007/s12272-023-01460-3
Jie Xu, Aizhen Xiong, Xunjiang Wang, Xing Yan, Yilin Chen, Xuanling Ye, Zhengtao Wang, Lili Ding, Li Yang
{"title":"Hyperoside attenuates pyrrolizidine alkaloids-induced liver injury by ameliorating TFEB-mediated mitochondrial dysfunction","authors":"Jie Xu,&nbsp;Aizhen Xiong,&nbsp;Xunjiang Wang,&nbsp;Xing Yan,&nbsp;Yilin Chen,&nbsp;Xuanling Ye,&nbsp;Zhengtao Wang,&nbsp;Lili Ding,&nbsp;Li Yang","doi":"10.1007/s12272-023-01460-3","DOIUrl":"10.1007/s12272-023-01460-3","url":null,"abstract":"<div><p>Pyrrolizidine alkaloids (PAs) are potent hepatotoxins that can cause liver damage. Hyperoside (Hyp), a natural flavonoid, can be extracted from medicinal plants. Hyp displays hepatoprotective activity in various liver diseases. However, the potential effect and mechanism of action of Hyp in ameliorating PA-induced liver injury remain obscure. This study aimed to explore the protective effect of Hyp against PA-induced hepatotoxicity and its underlying mechanism. We established an in vitro model of PAs in mouse primary hepatocytes and developed a mouse model of acute PA toxicity to investigate the protective effect of Hyp. We found that Hyp notably attenuated PA-induced hepatotoxicity. RNA-sequencing showed that the beneficial effect of Hyp against PA-induced hepatotoxicity was associated with the transcription factor EB (TFEB)-peroxisome proliferator-activated receptor-γ coactivator-1-α (PGC1α) pathway. Our results confirmed that both the autophagy-lysosomal pathway and mitochondrial biogenesis were induced by Hyp through TFEB nuclear translocation in PA-induced liver injury. Furthermore, we demonstrated that activation of the mechanistic target of rapamycin complex 1 (mTORC1) by MHY 1485 decreased TFEB nuclear translocation and abrogated the protective effect of Hyp against PA-induced liver injury in mice. In contrast, inhibition of mTORC1 activity increased the level of TFEB and reduced hepatotoxicity induced by PAs in mouse livers. Likewise, Hyp-induced TFEB activation was validated in vitro. In conclusion, Hyp can activate the TFEB-mediated autophagy-lysosomal pathway and mitochondrial biogenesis through inhibition of mTORC1 activity, alleviating the liver injury induced by PAs, thus suggesting the potential value of Hyp in the treatment of PA-induced hepatotoxicity.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 8","pages":"694 - 712"},"PeriodicalIF":6.7,"publicationDate":"2023-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41102997","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Effects of CYP2D6 and CYP2C19 genetic polymorphisms and cigarette smoking on the pharmacokinetics of tolperisone CYP2D6和CYP2C19基因多态性及吸烟对托培酮药代动力学的影响。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-20 DOI: 10.1007/s12272-023-01462-1
Ji-Young Byeon, Chang‑Keun Cho, Pureum Kang, Se-Hyung Kim, Choon-Gon Jang, Seok-Yong Lee, Yun Jeong Lee
{"title":"Effects of CYP2D6 and CYP2C19 genetic polymorphisms and cigarette smoking on the pharmacokinetics of tolperisone","authors":"Ji-Young Byeon,&nbsp;Chang‑Keun Cho,&nbsp;Pureum Kang,&nbsp;Se-Hyung Kim,&nbsp;Choon-Gon Jang,&nbsp;Seok-Yong Lee,&nbsp;Yun Jeong Lee","doi":"10.1007/s12272-023-01462-1","DOIUrl":"10.1007/s12272-023-01462-1","url":null,"abstract":"<div><p>Tolperisone, a muscle relaxant used for post-stroke spasticity, is metabolized to its main metabolite by CYP2D6 and to a lesser extent by CYP2C19 and CYP1A2. We investigated the effects of <i>CYP2D6</i> and <i>CYP2C19</i> genetic polymorphisms and cigarette smoking on tolperisone pharmacokinetics. A 150 mg oral dose of tolperisone was given to 184 healthy Korean subjects and plasma concentrations of tolperisone were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). A 3.14-fold significant increase in AUC<sub>0–∞</sub> was observed in the <i>CYP2D6*10/*10</i> group compared with the <i>CYP2D6*wt/*wt</i> group, whereas a 3.59-fold increase in AUC<sub>0–∞</sub> was observed in CYP2C19PMs compared to CYP2C19EMs. Smokers had a 38.5% decrease in AUC<sub>0–∞</sub> when compared to non-smokers. When these effects were combined, <i>CYP2D6*10/*10</i>-CYP2C19PM-Non-smokers had a 25.9-fold increase in AUC<sub>0–∞</sub> compared to <i>CYP2D6*wt/*wt</i>-CYP2C19EM-Smokers. Genetic polymorphisms of <i>CYP2D6</i> and <i>CYP2C19</i> and cigarette smoking independently and significantly affected tolperisone pharmacokinetics and these effects combined resulted in a much greater impact on tolperisone pharmacokinetics.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 8","pages":"713 - 721"},"PeriodicalIF":6.7,"publicationDate":"2023-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41098822","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Androgen receptor and hyaluronan-mediated motility receptor as new molecular targets of baicalein: new molecular mechanisms for its anticancer properties 雄激素受体和透明质酸介导的运动受体作为黄芩素的新分子靶标:其抗癌特性的新分子机制。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-09-10 DOI: 10.1007/s12272-023-01461-2
Mingyue Jiang, Suman Poudel, Kyung Song
{"title":"Androgen receptor and hyaluronan-mediated motility receptor as new molecular targets of baicalein: new molecular mechanisms for its anticancer properties","authors":"Mingyue Jiang,&nbsp;Suman Poudel,&nbsp;Kyung Song","doi":"10.1007/s12272-023-01461-2","DOIUrl":"10.1007/s12272-023-01461-2","url":null,"abstract":"<div><p>Natural compounds known as phytochemicals have served as valuable resources for the development of new anti-cancer drugs and treatment of malignancies. Among these phytochemicals, baicalein is an emerging anti-tumor flavonoid obtained from <i>Scutellaria baicaleinsis</i> (Lamiaceae), but its underlying mechanisms of action and molecular targets have not yet been completely elucidated. Here, we identified new mechanisms for the anti-tumor activities of baicalein, providing evidence that hyaluronan-mediated motility receptor (HMMR) and androgen receptor (AR) are new molecular targets of baicalein in human cancer cells. We observed that HMMR, known to be highly associated with poor prognosis in a wide range of human cancers, was substantially downregulated by baicalein at mRNA and protein levels. Reporter assays further revealed that the suppression of HMMR by baicalein might occur through a transcriptional regulatory mechanism with the participation of Egr-1, E2F3α, and serum response factor (SRF). We also found that baicalein significantly inhibits androgenic responses in hormone-responsive prostate cancer cells, indicating that this might be attributed to the downregulation of AR promoter activity by baicalein. Additionally, baicalein markedly induced the expression of tumor suppressive miR-30C, which might be partly involved in baicalein-mediated autophagy and anti-cancer effects. Overall, our study sheds light on new diverse mechanisms of the anti-cancer effects exhibited by baicalein, implying that baicalein could be a potential therapeutic agent against human cancers and function as an inhibitor of HMMR and AR.</p></div>","PeriodicalId":8287,"journal":{"name":"Archives of Pharmacal Research","volume":"46 8","pages":"679 - 693"},"PeriodicalIF":6.7,"publicationDate":"2023-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10199766","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Au–Ag bimetallic nanoparticles using Korean red ginseng (Panax ginseng Meyer) root extract for chemo-photothermal anticancer therapy 使用韩国红参根提取物合成Au-Ag双金属纳米颗粒,用于化学光热抗癌治疗。
IF 6.7 3区 医学
Archives of Pharmacal Research Pub Date : 2023-08-17 DOI: 10.1007/s12272-023-01457-y
Gayeon Lee, You Jeong Lee, Yeon-Jeong Kim, Youmie Park
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