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从合成到药理活性:乳香酸的旅程。

The journey of boswellic acids from synthesis to pharmacological activities.

机构信息

Department of Pharmacognosy and Medicinal Plants, Faculty of Pharmacy, Al-Azhar University, Cairo, 11884, Egypt.

Department of Biochemistry, Faculty of Pharmacy, Badr University in Cairo (BUC), Badr City, 11829, Cairo, Egypt.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2024 Mar;397(3):1477-1504. doi: 10.1007/s00210-023-02725-w. Epub 2023 Sep 23.

Abstract

There has been a lot of interest in using naturally occurring substances to treat a wide variety of chronic disorders in recent years. From the gum resin of Boswellia serrata and Boswellia carteri, the pentacyclic triterpene molecules known as boswellic acid (BA) are extracted. We aimed to provide a detailed overview of the origins, chemistry, synthetic derivatives, pharmacokinetic, and biological activity of numerous Boswellia species and their derivatives. The literature searched for reports of B. serrata and isolated BAs having anti-cancer, anti-microbial, anti-inflammatory, anti-arthritic, hypolipidemic, immunomodulatory, anti-diabetic, hepatoprotective, anti-asthmatic, and clastogenic activities. Our results revealed that the cytotoxic and anticancer effects of B. serrata refer to its triterpenoid component, including BAs. Three-O-acetyl-11-keto-BA was the most promising cytotoxic molecule among tested substances. Activation of caspases, upregulation of Bax expression, downregulation of nuclear factor-kappa B (NF-kB), and stimulation of poly (ADP)-ribose polymerase (PARP) cleavage are the primary mechanisms responsible for cytotoxic and antitumor effects. Evidence suggests that BAs have shown promise in combating a wide range of debilitating disease conditions, including cancer, hepatic, inflammatory, and neurological disorders.

摘要

近年来,人们对利用天然物质治疗多种慢性疾病产生了浓厚的兴趣。从乳香树 Boswellia serrata 和 Boswellia carteri 的树胶树脂中提取出了一种五环三萜分子,称为乳香酸(BA)。我们旨在详细概述多种乳香树及其衍生物的起源、化学、合成衍生物、药代动力学和生物学活性。文献中报道了乳香树和分离出的乳香酸具有抗癌、抗菌、抗炎、抗关节炎、降血脂、免疫调节、抗糖尿病、保肝、抗哮喘和致突变活性。我们的结果表明,乳香树的细胞毒性和抗癌作用与其三萜类成分,包括乳香酸有关。在测试的物质中,三-O-乙酰-11-酮-BA 是最有前途的细胞毒性分子。细胞毒性和抗肿瘤作用的主要机制是激活半胱天冬酶、上调 Bax 表达、下调核因子-κB(NF-κB)和刺激多聚(ADP-核糖)聚合酶(PARP)裂解。有证据表明,乳香酸在对抗多种衰弱性疾病方面具有潜力,包括癌症、肝脏、炎症和神经疾病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b1f0/10858840/10d5d6ee102f/210_2023_2725_Fig1_HTML.jpg

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