Scutellarin(Scutellarin) - 药物靶点：IDH1_在研适应症：肝细胞癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Scu

靶点

IDH1

作用机制

IDH1抑制剂(细胞质异柠檬酸脱氢酶[NADP]抑制剂)

治疗领域

肿瘤消化系统疾病

在研适应症

肝细胞癌

非在研适应症-

原研机构

中国中医科学院

在研机构

中国中医科学院

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

结构

分子式C21H18O12

InChIKeyDJSISFGPUUYILV-ZFORQUDYSA-N

CAS号27740-01-8

关联

2

项与 Scutellarin 相关的临床试验

ChiCTR2100048583 / Suspended临床4期IIT

Homocysteine, inflammatory factors, safety study of scutellarin for injection in patients with acute cerebral infarction - a single center, randomized, open label clinical trial

开始日期2021-07-19

申办/合作机构

云南省第一人民医院

ITMCTR2100005042 / Suspended临床4期IIT

Homocysteine, inflammatory factors, safety study of scutellarin for injection in patients with acute cerebral infarction - a single center, randomized, open label clinical trial

开始日期2021-07-19

申办/合作机构

云南省第一人民医院

100 项与 Scutellarin 相关的临床结果

登录后查看更多信息

100 项与 Scutellarin 相关的转化医学

登录后查看更多信息

100 项与 Scutellarin 相关的专利（医药）

登录后查看更多信息

572

项与 Scutellarin 相关的文献（医药）

2025-01-01·JOURNAL OF ETHNOPHARMACOLOGY

Scutellaria baicalensis ameliorates allergic airway inflammation through agonism and transcriptional regulation of TAS2Rs

Article

作者: Liu, Yanxia ; Liu, Kaiyang ; Xu, Zhenzhen ; Ren, Yue ; Zhang, Yanling ; Qiao, Liansheng ; Wang, Shifeng

ETHNOPHARMACOLOGICAL RELEVANCE:

Scutellaria baicalensis Georgi (SCB, Huangqin) is a traditional medicinal plant used to treat fever and respiratory diseases. SCB has a good therapeutic effect on asthma and anti-inflammation in traditional clinic use. However, the molecular mechanism and targets of SCB in treating asthma are still unclear.

AIM OF THE STUDY:

Combining transcriptomic analysis and in vitro experimental validation, this study aimed to reveal the molecular mechanism and targets of SCB in treating asthma.

MATERIALS AND METHODS:

The anti-asthmatic effects of SCB and its active components, scutellarin and oroxylin A, were evaluated in ovalbumin (OVA)-induced rats by analysis of pulmonary function and pathology. The signaling pathways in rat pulmonary tissue were analyzed using transcriptomics and protein interaction network analysis. Calcium mobilization assay and molecular docking were utilized to discover the active compounds from SCB with agonism activity of type 2 taste receptors (TAS2Rs). The anti-asthmatic effect and transcriptional regulation of TAS2Rs regulated by SCB and its active components were analyzed in vitro.

RESULTS:

Extracts of SCB (ESB), scutellarin, and oroxylin A ameliorated airway function and inflammation in OVA-induced rats. The anti-asthma mechanism of ESB, scutellarin and oroxylin A was highly related to immune and taste transduction pathways based on transcriptomic analysis, especially the TAS2Rs signaling pathway. ESB was the direct agonist of TAS2R4 and TAS2R14 with EC₅₀ of 209.1 and 217.2 μg/mL based on calcium mobilization assay, respectively. Baicalein was the main active component for TAS2R4 agonism activity, and scutellarin and oroxylin A had weak agonism activity of TAS2R4 and TAS2R14 through calcium mobilization assay and molecular docking. However, scutellarin and oroxylin A significantly upregulated the gene expression of Tas2r108 (the mouse ortholog of the TAS2R4) in lung tissue. ESB, scutellarin, and oroxylin A inhibited LPS-induced lactate dehydrogenase release and gene expression of TNF through transcriptional regulation of TAS2R4 and TAS2R14 on bronchial epithelial cells. ESB and oroxylin A ameliorated IgE-induced β-hexosaminidase release and gene expression of Il4 and Tnf and upregulated gene expression of Tas2r108.

CONCLUSION:

These results provided new insight into the anti-asthmatic mechanism of SCB and active components, scutellarin and oroxylin A, through agonism and transcriptional regulation of TAS2Rs to ameliorate allergic airway inflammation.

2025-01-01·JOURNAL OF ETHNOPHARMACOLOGY

Exploratory research on the effective chemical basis of tanreqing injection for treating acute lung injury: In vivo, in vitro and in silico

Article

作者: Zang, Yi ; Feng, Bo ; Xie, Like ; Xu, Zhijian ; Li, Jia ; Shi, Yulong ; Zhu, Weiliang ; Tian, Xiaoting ; Kan, Weijuan ; Wang, Yangyang ; Zhang, Xuemei ; Lin, Chenxuan ; Tang, Bixi

ETHNOPHARMACOLOGICAL RELEVANCE:

Sepsis-induced acute lung injury (ALI) presents with significant morbidity and mortality in clinical settings. Tanreqing Injection (TRQI) has been clinically recommended for the treatment of ALI; however, the specific active chemical constituents remain unidentified.

AIM OF THE STUDY:

This study aimed to elucidate the potential pharmacologically active components and the underlying mechanisms of TRQI in the treatment of sepsis-induced ALI.

MATERIALS AND METHODS:

High-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) techniques were employed to identify the effective chemical constituents of TRQI. Additionally, an in vitro study was conducted using Raw264.7 macrophage cells stimulated with lipopolysaccharide (LPS) to evaluate the inhibitory effects of TRQI. An acute lung injury model produced by LPS was intraperitoneal injection in mice to assess the ALI-inhibitory effect of TRQI. The lung's pathological characteristics were examined using hematoxylin and eosin staining. Enzyme-linked immunosorbent assay (ELISA) and QPCR were performed to confirm the pharmaceutical effect. Network pharmacology was employed for mechanistic exploration, incorporating GO, and PPI analyses of targets. Src inhibitor and JNK agonist used to investigate the dependence of associated signaling pathways.

RESULTS:

Combining pharmacokinetic characteristics, lung first-pass effect and anti-inflammatory effects, the main components of TRQI for treating sepsis induced ALI were narrowed down to seven compounds: chlorogenic acid, scutellarin, wogonoside, oroxyloside, oroxylin A and baicalein. Network pharmacology indicated that Src/JNK signaling pathway, may be the main regulatory pathway for treatment of actue lung injury. Next by using Src inhibitor, Src inhibition partly diminished the protective effects of TRQI in LPS-injected mice. Pretreatment with JNK agonist anisomycin abolished the protective effects of lung injury in vivo.

CONCLUSIONS:

TRQI is injected, the seven compounds could be presented in vivo, which can improve ALI by inhibiting Src-JNK signaling.

2024-12-01·Natural products and bioprospecting

Current advances on the therapeutic potential of scutellarin: an updated review

Review

作者: Du, Guanhua ; Xie, Yifei ; Lu, Yang ; Zhang, Li ; Sun, Guotong ; Yang, Shiying ; Zhang, Wen ; Tao, Yue

Abstract:

Scutellarin is widely distributed in Scutellaria baicalensis, family Labiatae, and Calendula officinalis, family Asteraceae, and belongs to flavonoids. Scutellarin has a wide range of pharmacological activities, it is widely used in the treatment of cerebral infarction, angina pectoris, cerebral thrombosis, coronary heart disease, and other diseases. It is a natural product with great research and development prospects. In recent years, with in-depth research, researchers have found that wild scutellarin also has good therapeutic effects in anti-tumor, anti-inflammatory, anti-oxidation, anti-virus, treatment of metabolic diseases, and protection of kidney. The cancer treatment involves glioma, breast cancer, lung cancer, renal cancer, colon cancer, and so on. In this paper, the sources, pharmacological effects, in vivo and in vitro models of scutellarin were summarized in recent years, and the current research status and future direction of scutellarin were analyzed.Graphical Abstract

100 项与 Scutellarin 相关的药物交易

登录后查看更多信息