Uncovering the anti-inflammatory and anti-angiogenesis activities of sinensetin orally administered to arthritic mice: synthesis, in vivo and in vitro evaluation.

IF 1.6 3区 医学 Q3 CHEMISTRY, APPLIED
Abdulmenem Bakkouri, Mun Fei Yam, Chong-Yew Lee
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引用次数: 0

Abstract

Sinensetin, a prominent flavone from Orthosiphon stamineus is a promising constituent for anti-rheumatoid arthritis. This study evaluated the oral anti-inflammatory and anti-angiogenic efficacy of sinensetin. In carrageenan-induced arthritic mice, oral sinensetin (25-100 mg/kg) significantly reduced paw edema with dose-correlated plasma kinetics, confirming functional oral bioavailability despite a delayed onset compared to intraperitoneal administration. Ex vivo rat aortic ring and in vitro human endothelial assays revealed that sinensetin robustly suppressed microvessel outgrowth and cell migration via VEGF downregulation. These findings demonstrate that sinensetin is an orally bioavailable agent capable of suppressing inflammation and angiogenesis.

揭示中药青藤素对关节炎小鼠的抗炎和抗血管生成活性:合成、体内和体外评价。
正虹吸管(Orthosiphon stamineus)中重要的黄酮类化合物——蛇鼻血素是一种很有前景的抗类风湿关节炎成分。本研究评价了鼻窦炎素的口服抗炎和抗血管生成作用。在卡拉胶诱导的关节炎小鼠中,口服鼻窦炎素(25-100 mg/kg)显著减少足跖水肿,并伴有剂量相关的血浆动力学,证实了功能性口服生物利用度,尽管与腹腔给药相比延迟了发病时间。离体大鼠主动脉环和离体人内皮细胞实验表明,紫丁香苷通过下调VEGF抑制微血管生长和细胞迁移。这些研究结果表明,青肠素是一种能够抑制炎症和血管生成的口服生物可利用剂。
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来源期刊
CiteScore
3.20
自引率
5.90%
发文量
47
审稿时长
2.3 months
期刊介绍: The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures. All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.
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