Bakrim Saad, Benkhaira Nesrine, Bourais Ilhame, Benali Taoufiq, Lee Learn-Han, El Omari Nasreddine, Sheikh Ryan A, Goh Khang Wen, Ming Long Chiau, Bouyahya Abdelhakim
Molecular Engineering, Biotechnologies and Innovation Team, Geo-Bio-Environment Engineering and Innovation Laboratory, Polydisciplinary Faculty of Taroudant, Ibn Zohr University, Agadir 80000, Morocco.
Laboratory of Microbial Biotechnology and Bioactive Molecules, Department of Biology, Faculty of Sciences and Techniques, University Sidi Mohamed Ben Abdellah, Fez 1975, Morocco.
Antioxidants (Basel). 2022 Sep 27;11(10):1912. doi: 10.3390/antiox11101912.
Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmasterol has been examined via in vitro and in vivo assays and molecular docking for its various biological activities on different metabolic disorders. The findings indicate potent pharmacological effects such as anticancer, anti-osteoarthritis, anti-inflammatory, anti-diabetic, immunomodulatory, antiparasitic, antifungal, antibacterial, antioxidant, and neuroprotective properties. Indeed, stigmasterol from plants and algae is a promising molecule in the development of drugs for cancer therapy by triggering intracellular signaling pathways in numerous cancers. It acts on the Akt/mTOR and JAK/STAT pathways in ovarian and gastric cancers. In addition, stigmasterol markedly disrupted angiogenesis in human cholangiocarcinoma by tumor necrosis factor-α (TNF-α) and vascular endothelial growth factor receptor-2 (VEGFR-2) signaling down-regulation. The association of stigmasterol and sorafenib promoted caspase-3 activity and down-regulated levels of the anti-apoptotic protein Bcl-2 in breast cancer. Antioxidant activities ensuring lipid peroxidation and DNA damage lowering conferred to stigmasterol chemoprotective activities in skin cancer. Reactive oxygen species (ROS) regulation also contributes to the neuroprotective effects of stigmasterol, as well as dopamine depletion and acetylcholinesterase inhibition. The anti-inflammatory properties of phytosterols involve the production of anti-inflammatory cytokines, the decrease in inflammatory mediator release, and the inhibition of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Stigmasterol exerts anti-diabetic effects by reducing fasting glucose, serum insulin levels, and oral glucose tolerance. Other findings showed the antiparasitic activities of this molecule against certain strains of parasites such as (in vivo) and on promastigotes and amastigotes of the (in vitro). Some stigmasterol-rich plants were able to inhibit , , and at low doses. Accordingly, this review outlines key insights into the pharmacological abilities of stigmasterol and the specific mechanisms of action underlying some of these effects. Additionally, further investigation regarding pharmacodynamics, pharmacokinetics, and toxicology is recommended.
豆甾醇是一种属于四环三萜类的不饱和植物甾醇。它是最常见的植物甾醇之一，存在于多种天然来源中，包括许多植物的植物脂肪或油类。目前，已通过体外和体内试验以及分子对接研究了豆甾醇对不同代谢紊乱的各种生物活性。研究结果表明其具有强大的药理作用，如抗癌、抗骨关节炎、抗炎、抗糖尿病、免疫调节、抗寄生虫、抗真菌、抗菌、抗氧化和神经保护特性。事实上，来自植物和藻类的豆甾醇通过触发多种癌症中的细胞内信号通路，在癌症治疗药物开发中是一种有前景的分子。它作用于卵巢癌和胃癌中的Akt/mTOR和JAK/STAT信号通路。此外，豆甾醇通过下调肿瘤坏死因子-α（TNF-α）和血管内皮生长因子受体-2（VEGFR-2）信号，显著破坏人胆管癌中的血管生成。豆甾醇与索拉非尼联合使用可促进乳腺癌中caspase-3活性并下调抗凋亡蛋白Bcl-2的水平。确保降低脂质过氧化和DNA损伤的抗氧化活性赋予了豆甾醇在皮肤癌中的化学保护活性。活性氧（ROS）调节也有助于豆甾醇的神经保护作用，以及多巴胺耗竭和乙酰胆碱酯酶抑制。植物甾醇的抗炎特性包括产生抗炎细胞因子、减少炎症介质释放以及抑制诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）。豆甾醇通过降低空腹血糖、血清胰岛素水平和口服葡萄糖耐量发挥抗糖尿病作用。其他研究结果显示了该分子对某些寄生虫菌株的抗寄生虫活性，如（体内）以及对（体外）前鞭毛体和无鞭毛体的活性。一些富含豆甾醇的植物能够在低剂量下抑制、和。因此，本综述概述了豆甾醇药理能力的关键见解以及其中一些作用的具体作用机制。此外，建议对药效学、药代动力学和毒理学进行进一步研究。
