Sesamin, which was primarily extracted from Sesamum indicum L (sesame), is a natural lignan compound. Sesame seeds are traditionally known for their nutritional value and their property to restore liver and kidney health and for blood nourishment. While oxidative damage and inflammation are the common aetiology of many diseases, sesamin because of its anti-inflammatory and antioxidant properties is well known in their management. It acts by enhancing the antioxidant enzyme activity and limits the production of reactive oxygen species (ROS) and malondialdehyde (MDA).
Physicochemical properties of sesamin includes – white crystalline appearance with a molecular formula of C20H18O6 and a melting point of 120-121°C. Further studies showed that sesamin can degrade the free radicals in the body and thus exhibit their antioxidant activity. Inflammatory responses caused by physical trauma, pathogenic infection, allergic reactions etc. can be alleviated with the use of sesamin as it can reduce COX and PEG2 and block the release of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, etc.). Bai et al. used dextran sodium sulfate (DSS)-induced ulcerative colitis mice as a model and found that sesamin can enhance Nrf2-mediated protection against H2O2-induced oxidative stress in vitro and ease patients suffering from Ulcerative colitis (UC) a type of inflammatory bowel disease. It is also found to alleviate skin inflammation caused due to UV exposure. However, it was later studied that it is not sesamin itself that exhibits the antioxidant and anti-inflammatory effects, but its metabolites produced by the body.
The development of organic anticancer drugs or adjuvant therapies for cancer is in demand to avoid the adverse effects of chemotherapy. Considering this, many anticancer studies were done on sesamin and were proved to effectively inhibit various types of tumours. Although it is not as pharmacologically effective as the known anticancer drugs it can eventually be used as adjuvant therapy and is far less harmful to patients than chemotherapy. Through the above studies, it is found that sesamin plays an anticancer effect mainly by regulating the expressions of related proteins, promoting cell cycle arrest in the G1 phase, inhibiting the proliferation of cancer cells, and inducing apoptosis. On the other hand, fatty liver and other liver disorders can also be prevented with the use of sesamin due to its effective regulation of lipid metabolism disorders and lipid peroxidation.
In addition, the research on the structure-activity relationship(SAR) of sesamin is rarely reported. The SAR study can interpret the relationship between the chemical structure and physiological activities of the biologically active substance and then derive the structure of the target active site which can be used to design a new active substance structure. Interestingly, studies have found that the catechol groups in their metabolites play an important role in antioxidant and anti-inflammatory effects. This has proven to be pivotal for further research on the structure-activity relationship of sesamin, and its better application in clinical and new drug design.
Reference:
Yao Zhang, Fen Liu, Yan Lin, Linhai Li, Mingfeng Chen, Lin Ni, "A Comprehensive Review on Distribution, Pharmacological Properties, and Mechanisms of Action of Sesamin", Journal of Chemistry, vol. 2022, Article ID 4236525, 17 pages, 2022. https://doi.org/10.1155/2022/4236525
By Gauri Pillai
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