Girisa Sosmitha, Parama Dey, Harsha Choudhary, Banik Kishore, Kunnumakkara Ajaikumar B
Cancer Biology Laboratory and DBT-AIST International Center for Translational and Environmental Research (DAICENTER), Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Guwahati, Assam 781039, India.
Explor Target Antitumor Ther. 2020;1(5):313-342. doi: 10.37349/etat.2020.00019. Epub 2020 Oct 30.
Cancer is one of the most dreadful diseases in the world with a mortality of 9.6 million annually. Despite the advances in diagnosis and treatment during the last couple of decades, it still remains a serious concern due to the limitations associated with currently available cancer management strategies. Therefore, alternative strategies are highly required to overcome these glitches. The importance of medicinal plants as primary healthcare has been well-known from time immemorial against various human diseases, including cancer. that belongs to Burseraceae family is one such plant which has been used to cure various ailments in traditional systems of medicine. This plant has diverse pharmacological properties such as antioxidant, antibacterial, antimutagenic, and antitumor which mostly owes to the presence of its active compound guggulsterone (GS) that exists in the form of Z- and E-isomers. Mounting evidence suggests that this compound has promising anticancer activities and was shown to suppress several cancer signaling pathways such as NF-κB/ERK/MAPK/AKT/STAT and modulate the expression of numerous signaling molecules such as the farnesoid X receptor, cyclin D1, survivin, caspases, HIF-1α, MMP-9, EMT proteins, tumor suppressor proteins, angiogenic proteins, and apoptotic proteins. The current review is an attempt to summarize the biological activities and diverse anticancer activities (both and ) of the compound GS and its derivatives, along with its associated mechanism against various cancers.
癌症是世界上最可怕的疾病之一，每年有960万人死于癌症。尽管在过去几十年中诊断和治疗取得了进展，但由于目前可用的癌症管理策略存在局限性，它仍然是一个严重的问题。因此，迫切需要替代策略来克服这些问题。自古以来，药用植物作为初级医疗保健手段，对包括癌症在内的各种人类疾病都具有显著疗效。橄榄科的一种植物就是这样一种在传统医学体系中被用于治疗各种疾病的植物。这种植物具有多种药理特性，如抗氧化、抗菌、抗诱变和抗肿瘤，这主要归功于其活性化合物古古甾酮（GS）的存在，它以Z型和E型异构体的形式存在。越来越多的证据表明，这种化合物具有良好的抗癌活性，并被证明可以抑制多种癌症信号通路，如NF-κB/ERK/MAPK/AKT/STAT，调节多种信号分子的表达，如法尼醇X受体、细胞周期蛋白D1、生存素、半胱天冬酶、HIF-1α、MMP-9、EMT蛋白、肿瘤抑制蛋白、血管生成蛋白和凋亡蛋白。本综述旨在总结化合物GS及其衍生物的生物活性和多种抗癌活性（体内和体外），以及其针对各种癌症的相关作用机制。
