A Double-blind, Single-dose Escalation Study of SQ-001 Infusion at a Single Center to Characterize the PK Profiles of Major Sentinel Compounds, Astragaloside IV, Calycosin 7-O-beta-glucopyranoside, and Lobetyolin in the Plasma of Healthy Adult Volunteers in the United States

This is a single-center, double-blind, single-dose escalation study in healthy volunteers.

开始日期2018-10-03

申办/合作机构

丽珠医药集团股份有限公司

[+2]

100 项与黄芪甲苷相关的临床结果

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100 项与黄芪甲苷相关的转化医学

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100 项与黄芪甲苷相关的专利（医药）

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1,270

项与黄芪甲苷相关的文献（医药）

2025-01-01·BEHAVIOURAL BRAIN RESEARCH

Astragaloside IV plays a neuroprotective role by promoting PPARγ in cerebral ischemia-reperfusion rats

Article

作者: Shao, Baoping ; Jie, Kang ; Xin, Liu ; Ding, Yanping

BACKGROUND:

Cerebral ischemia-reperfusion injury (CIRI) usually occurs during the treatment phase of ischemic disease, which is closely related to high morbidity and mortality. Promoting neurogenesis and synaptic plasticity are effective neural recovery strategies for CIRI. Astragaloside IV (AS-IV) has been shown to play a neuroprotective role in some neurological diseases. In the current study, we evaluated the effect and possible mechanism of AS-IV in CIRI rats.

METHODS:

The middle cerebral artery occlusion reperfusion (MCAO/R) model was established in rats to simulate the occurrence of human CIRI. First, we determined the cerebral injury on the 1st, 3rd, 5th and 7th day after cerebral ischemia-reperfusion (I/R) surgery by neurological deficit detection, TTC staining, TUNEL staining and Western blot analysis. Furthermore, rats were pre administered with AS-IV and then subjected to cerebral I/R surgery. Brains were collected on the 3rd day to evaluate the neuroprotective effect of AS-IV.

RESULTS:

Our results showed that on the 3rd day after I/R, the neurological impairment score and infarct volume were highest, the levels of apoptosis and expression of Caspase3 and Bax reached the peak. AS-IV treatment apparently attenuated neurological dysfunction, reduced infarct volume and pathological damage, promoted the neurogenesis, and alleviated the pathological damage caused by cerebral I/R involved in thickening and blurring of synaptic membranes, reduction of microtubules and synaptic vesicles, and loss of synaptic cleft. Our study also showed that AS-IV promoted the transcription and expression of the peroxisome proliferators-activated receptors γ (PPARγ) and brain-derived neurotrophic factor (BDNF), increased the expression of phosphorylation of tyrosine kinase receptor B (TrkB) and downstream PI3K/Akt/mTOR pathway proteins. Notably, when GW9662, an inhibitor of PPARγ was administered with AS-IV, the neuroprotective effect of AS-IV was reduced.

CONCLUSIONS:

These findings suggested that AS-IV has neuroprotective function in CIRI rats, and its molecular mechanism may depend on the phosphatidylinositide 3-kinase (PI3K)/protein kinase B (PKB)/Akt signalling pathway activated by PPARγ. AS-IV could be an effective therapeutic drug candidate for CIRI treatment.

2025-01-01·JOURNAL OF ETHNOPHARMACOLOGY

A systematic UHPLC-Q-TOF-MS/MS-based strategy for analysis of chemical constituents and related in vivo metabolites of Buyang Huanwu decoction

Article

作者: Cao, Xiangyang ; Deng, Zhipeng ; Yan, Zhimin ; Yan, Yajuan ; Zheng, Guangzhen ; Peng, Daiyin ; He, Dongbing ; Yu, Yadong ; Li, Heng ; Shi, Yingying ; Tao, Mingtao ; Cheng, Siting ; Wang, Rong ; Xiong, Qingping

ETHNOPHARMACOLOGICAL RELEVANCE:

Buyang Huanwu Decoction (BYHWD), a traditional Chinese medicine, is one of the classic prescriptions for the treatment of ischemic stroke in clinical practice. It has the effects of tonifying qi, activating blood circulation, and promoting meridian circulation. However, its chemical analysis has not been clarified, which greatly hinders its further clinical application. Therefore, it is necessary to clarify the chemical constituents and metabolites profile of BYHWD in vivo.

AIM OF THE STUDY:

Characterizing the chemical basis of BYHWD in vitro, and combing studies of related metabolism in vivo to screen out the potential active components of BYHWD with pharmacological effects in vivo.

MATERIALS AND METHODS:

Twelve male rats weighed 200 ± 20 each were selected for the experiments. According to the fragmentation of different structural types of components and diagnostic ions, UHPLC-Q-TOF-MS/MS was used to classify and clarify the unknown components of BYHWD and identify the material basis of BYHWD in vitro. Then, rat plasma, tissues, feces, and urine were collected for analysis. Based on the similarity of MS responses (accurate molecular weight and secondary fragmentation) and chromatographic behavior (retention time), the in vivo prototype and metabolites were analyzed. Through the phase I and phase II metabolism law, a metabolite library was established to analyze the prototype-matched metabolites.

RESULTS:

A total of 121 in vitro compounds and 55 in vivo prototypes of BYHWD were identified, corresponding to 123 matched prototypes. It was mainly composed of flavonoids, triterpene saponins, nucleosides and lactones both in vitro and in vivo. Quercetin, ligustilide, astragaloside IV, calycosin, paeoniflorin and ferulic acid were the main prototypes and metabolites in plasma and urine.

CONCLUSION:

Quercetin, ligustilide, astragaloside IV, calycosin, paeoniflorin and ferulic acid were the main active ingredients of BYHWD.

2024-12-31·AUTOIMMUNITY

Astragaloside IV promotes the pyroptosis of airway smooth muscle cells in childhood asthma by suppressing HMGB1/RAGE axis to inactivate NF-κb pathway

Article

作者: Zhang, Jun ; Zhang, Huahong ; Hu, Chongwei ; Pan, Hangli ; Yang, Ke

Childhood asthma, a common chronic childhood disease, leads to high mortality and morbidity in the world. Airway smooth muscle cells (ASMCs) is a group of multifunctional cells that has been found to be correlated with the pathogenesis of asthma. Astragaloside IV (AS-IV) is a compound extracted from Astragalus membranaceus, which has the anti-asthmatic effect. However, the role of molecular mechanisms regulated by AS-IV in the biological processes of ASMCs in asthma remains unclear. Our current study aims to investigate the downstream molecular mechanism of AS-IV in modulating the aberrant proliferation and pyroptosis of ASMCs in asthma. At first, we determined that the viability of ASMCs could be efficiently suppressed by AS-IV treatment (200 μM). Moreover, AS-IV promoted the pyroptosis and suppressed PDGF-BB-induced aberrant proliferation. Through mechanism investigation, we confirmed that AS-IV could suppress high mobility group box 1 (HMGB1) expression and prevent it from entering the cytoplasm. Subsequently, AS-IV blocked the interaction between HMGB1 and advanced glycosylation end product-specific receptor (RAGE) to inactivate NF-κB pathway. Finally, in vivo experiments demonstrated that AS-IV treatment can alleviate the lung inflammation in asthma mice. Collectively, AS-IV alleviates asthma and suppresses the pyroptosis of AMSCs through blocking HMGB1/RAGE axis to inactivate NF-κB pathway.

项与黄芪甲苷相关的新闻（医药）

2022-09-29

·蒲公英Ouryao

【中检院】9月最新对照品停用通知！

来源：中检院整理：wangxinglai20049月28日停用通知：各有关单位，现停止使用以下化学对照品:对照品名称：黄芪甲苷对照品批号：110781-202118特此通知。9月27日停用通知：各有关单位，现停止使用以下化学对照品:对照品名称：甲基丙烯酸二甲氨基乙酯对照品批号：190272-202001特此通知。往期信息（建议收藏）8月22日停用通知：各有关单位，现停止使用以下化学对照品:对照品名称：骨化三醇对照品批号：100995-202102特此通知。8月18日停用通知：各有关单位，现停止使用以下化学对照品:对照品名称：苯甲酰次乌头原碱对照品批号：111796-201906特此通知。主要内容：2022年至今中检院已发布了7期国家药品标准物质供应情况，截止至2022年09月共计有65个对照品即将过期，以下是具体信息整理：截止8月过期品种24个：截止9月过期品种41个：

2022-09-26

·BioSpace

Creative Enzymes Announces the Start of Year-End Promotion on Its Kosher Certified Products

Creative Enzymes, a professional enzyme provider located in New York, USA, is always hammering away at research and trials in order to provide customers with enzyme services and products with its greatest effort. Creative Enzymes today announced extensive savings on the full range of Kosher Certified Products in its year-end promotion, which runs until December 29, 2022. Kosher Certification is the stamp of kosher approval by a rabbinic agency verifying checked products ingredients, production facility, and actual production to ensure that all ingredients, derivatives, tools and machinery have no trace of non-kosher substances. The Kosher Certified symbol assures consumers that both the actual product and its production adhere to all Kosher Law requirements. The promotion will enable biologists to save money on premium Kosher-certified products. Creative Enzymes provides the following featured Kosher certified products: Epimedium Extract Epimedium extract, also known as horny goat weed extract, has been used to treat male erectile dysfunction, which enhances sperm production, stimulates nervous sensation, and indirectly promotes sexual desire. Lotus Leaf Extract Lotus leaf extract can significantly reduce serum cholesterol levels of glycerol and glycerol, and plays a role in regulating blood lipid health. Astragalus Extract Astragalus extract astragaloside has been used to promote the discharge of urine, lower blood pressure, and increase endurance. Maca Root Extract Maca root extract powder contains several biologically active components that may help enhance physical energy and endurance. Bilberry Extract Bilberries are rich in anthocyanosides, proanthocyanidins, resveratrol, flavors, and tannins that inhibit cancer cell development and inflammation. Capsicum Extract Capsaicin in capsicum consists of anti-inflammatory and antioxidant effects. Rosemary Extract Rosemary extract reveals growing popularity among certain food producers due to its ability to act as a natural preservative. Native Roxburgh Superoxide Dismutase Superoxide dismutase (SOD) catalyzes the dismutation of superoxide radicals to hydrogen peroxide and molecular oxygen. SOD plays a critical role in the defense of oxygen radicals. “This promotion is definitely a unique offer. For many years, we have been committed to providing our customers with cost-effective and high-quality services and products. We are pleased to offer our customers widely discounted prices on most of our products and are fully aware that only high-quality products can reward their support and trust,” said Creative Enzymes’s Chief Scientist. About Creative Enzymes Creative Enzymes is a remarkable supplier and manufacturer in the enzymology field. Equipped with advanced technology platforms, Creative Enzymes is able to offer high-quality and professional services to customers. Its products and services have been widely used institutionally for academia and industrially for pharmaceuticals. Contact Address: Shirley, NY 11967, USA Email: contact@creative-enzymes.com

2022-08-29

·生物探索

ERMM：新冠治疗，西医效果好还是中医效果好？

摘要：目前，中国的新冠大流行已基本得到控制，但该流行病仍在世界其他国家肆虐。中医药（Traditional Chinese medicine，TCM）与西医（western medicine，WM）一起为抗击疫情做出了巨大贡献。中国新冠患者的中医药应用率高达92%，一些中药如金花清肝颗粒、连花清瘟胶囊/颗粒和血必净注射液用于治疗新冠患者，并已被临床证明是有效的。疫情发展已3年，中医和西医在治疗新冠的效果如何？2022年，武汉大学和广东疾病预防控制中心研究团队在Expert Reviews in Molecular Medicine发表题为“A systematic review of outcomes in COVID-19 patients treated with western medicine in combination with traditional Chinese medicine versus western medicine alone”的研究成果（图1）[1]。研究结果表明在新冠的临床治疗方面，中西医结合治疗的效果显著优于西医治疗。图1 研究成果（图源：[1]）研究人员通过汇总2021年2月10日之前已发表文献的数据，系统比较新冠患者中西医结合（integrated Chinese with western，ICW）与WM治疗的结果，并确定新冠患者的ICW治疗是否具有更好的临床结果。在数据来源方面：研究人员使用新冠肺炎、中药和疗效相关的关键词检索了PubMed、Embase、Cochrane Central Register of Controlled Trials（CENTRAL）、中国临床试验注册中心、中国生物医学文献数据库（Chinese Biomedical Literature Database，CBM）、中国知网（China National Knowledge Infrastructure，CNKI）和万方数据库（图2）。其中，包括所有对新冠患者进行ICW或WM治疗的随机对照（randomised controlled，RC）和非随机对照（non-randomised controlled，NRC）临床试验，分析有效率、治愈率、加重率、病毒核酸转阴率、发热、咳嗽、乏力等症状缓解率和缓解时间，胸部CT及白细胞数（white blood cells，WBCs）和新冠患者的淋巴细胞（lymphocytes，LYM）指标。图2 研究结果（图源：[1]）表1 评价研究的特征与指标数据来源：[1]∣制表：生物探索编辑团队注：指标分为三类，即综合指标、症状指标和血液指标。综合指标包括有效率（①）、病毒核酸转阴率(②)、恶化率(③)和治愈率(④)；症状指标包括发热缓解率或时间（⑤）、咳嗽缓解率或时间（⑥）、乏力缓解率或时间（⑦）和胸部CT改善率（⑧）；血液指标包括WBC量（⑨）和LYM量（⑩）。对于定性和定量数据，分别以比率风险（ratio risk，RR）和加权平均差（weighted mean difference，WMD）作为统计分析的指标。RevMan 5.4用于使用固定效应和随机效应模型进行荟萃分析和森林图。Cochrane偏倚风险工具（RoB 2.0）用于评估纳入的RC试验的偏倚风险，而非随机干预研究的偏倚风险用于评估NRC试验的偏倚风险。研究发现： 1综合指标：较WM组，ICW的有效率高、临床治愈率高、恶化率低该研究包括16项研究，共有1645名确诊的新冠患者，其中实验组895名患者接受ICW治疗，而对照组750名患者接受WM治疗。综合指标中，ICW组有效率较高（RR=1.24），临床治愈率（RR=1.27）较高，恶化率较低（RR=0.36），但病毒核酸转阴率无统计学差异（RR=1.20）。 2症状指标：较WM组，ICW组的症状缓解更好在症状指标中，ICW组的发热缓解率更高（RR=1.24），发热缓解时间更短（WMD=-1.49），咳嗽缓解率（RR=1.38）和虚弱缓解率（RR=1.45）更高，减少咳嗽缓解时间（WMD=-1.61）和虚弱缓解时间（WMD=-1.50）和胸部CT结果改善更好（RR=1.19）。 3血液指标方面：较WM组，ICW组的血液指标恢复更优血液指标方面，ICW组患者血液中白细胞数量显著回升（WMD=0.35），血液中LYM的恢复更明显（WMD=0.23）。疫情爆发早期，20%的新冠患者会迅速出现非典型间质性肺炎、急性呼吸窘迫综合征和多器官功能障碍等严重疾病表现，其中近10%的患者最终会死亡。幸运的是，这种疾病演变的病理机制正在逐渐被揭示。研究表明，以广泛的内皮损伤、补体诱导的凝血和全身性微血管疾病为特征的过度免疫反应在疾病进展中起关键作用。通过观察因新冠死亡的患者的肺、脾、肝、心、肾、甲状腺和睾丸的组织病理学变化，发现患者的高炎症和修复状态并存，高炎症状态引起病理改变，包括凝血状态、微血栓形成、纤维化和血管生成等过程。因此，有必要对疾病症状严重的患者进行早期治疗，以预防多器官纤维化。根据以往的经验，在治疗疾病方面中西医结合通常可以取得不错的效果。2003年，在SARS治疗期间，发生了与使用西药皮质类固醇有关的一些不良事件。一些接受大剂量皮质类固醇治疗的SARS幸存者在治疗后出现股骨头坏死。根据循证医学报告，应用中药有助于有效降低皮质类固醇的日平均使用剂量。广东省中医院发现在不使用糖皮质激素和抗病毒药物的情况下，中医药在SARS疾病的早、中、重、恢复期作为主要治疗手段，是可行和安全的。在以往ICW的应用中，黄芩素、葛根素、没食子酸等36种中药单体活性成分和黄芪甲苷和其他25种中药复方活性成分，如玉屏风散、补肺汤和补阳还五汤以及这些药用化合物可通过转化生长因子-β降低炎症因子的表达，调节氧化还原平衡，诱导肺成纤维细胞凋亡，阻断纤维化进程。1/Smad、磷脂酰肌醇-3-激酶/Akt和核红细胞2相关因子2/谷胱甘肽或其他通路，表明具有良好的抗肺纤维化活性，可有效改善纤维化症状，延缓疾病进展。这或许可以解释为什么ICW治疗比WM治疗具有更好的治疗效果。因此，中医药尤其是复方在预防和治疗纤维化方面具有良好的临床应用前景，但应开展更多相关的临床试验，以治疗新冠中重度患者。以往新发传染病的治疗经验，如SARS和H1N1，已经证明ICW治疗比单纯的WM治疗具有更好的效果，本研究也得出了类似的结论。汇总的16项研究通过荟萃分析系统分析了ICW和WM治疗在三大类（即总体指标、症状指标和血液指标）之间的差异。结果表明，中西医联合用药在更好地控制患者病情恶化、提高治愈率和修复新冠患者免疫力方面发挥了显著作用。SARS、H1N1和COVID-19的治疗经验都表明，中药与西药有互补作用。中医药能够经受住与新出现的流行病作斗争的挑战。因此，开展更多这样的实践和进一步的研究，对促进中医药的发展是很有价值的。有理由推测中医药或其他传统医学，可以帮助我们在未来对抗新出现的流行病。撰文|文竞择排版|文竞择 End 参考资料：[1]Yu R, Zhang S, Zhao D, et al. A systematic review of outcomes in COVID-19 patients treated with western medicine in combination with traditional Chinese medicine versus western medicine alone. Expert Rev Mol Med. 2022 Jan 6;24:e5. doi: 10.1017/erm.2021.35. PMID: 34986905; PMCID: PMC8795778. 本文系生物探索原创，欢迎个人转发分享。其他任何媒体、网站如需转载，须在正文前注明来源生物探索。往期精选围观 WHO：全球新增新冠病例下降25% 热文北极暖化比全球快4倍，冰川融化释放致命病毒和细菌？人类是最大的元凶...... 热文感染新冠病毒两年后，这些疾病风险仍然增加！热文徐开骋口中的“酒后乱性”有无科学依据？酒精：这个锅我不背！热文慢性病高发，原来是饮食不对？每日少吃一克盐，竟可拯救数百万人！点击“阅读原文”，了解更多~

100 项与黄芪甲苷相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
心绞痛	申请上市	中国	贵州景峰注射剂有限公司	2014-12-29

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ESC2018	N/A	左心室功能不全	-	Astragaloside IV	窪製鏇範廠鏇鏇鬱觸夢(艱廠淵構衊淵襯醖艱鏇) = 艱醖鹹積繭齋壓蓋網範膚繭艱選鏇艱膚膚鹹襯 (餘選醖鹹蓋選簾鑰窪蓋 ) 更多	-	2018-08-27
				Astragaloside IV	窪製鏇範廠鏇鏇鬱觸夢(艱廠淵構衊淵襯醖艱鏇) = 襯鹽顧鏇膚壓艱窪窪觸膚繭艱選鏇艱膚膚鹹襯 (餘選醖鹹蓋選簾鑰窪蓋 ) 更多