What is it about?
Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects.This review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products
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Why is it important?
The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.
Perspectives
Cucurbitacins belong to a group of triterpenes possessing an interesting chemical diversity on ring A and the side chain at C-17 and are reported mostly from the Cucurbitaceous family although a few have been isolated from other families. Apart from their famous bitter taste, they also display a wide range of significant biological and pharmacological effects, and of particular note is their cytotoxic and anticancer effects. For example, cucurbitacin B (1) displays anticancer effects towards the 59 NCI cancer cell lines namely seven breast cancer cells, six CNS cancer cells, seven colon cancer cells, six leukemia, nine lung cancer cells, eight melanoma cells, six ovarian cancer cells, two prostate cancer cells, and eight renal cancer cells. Most encouragingly, cucurbitacin B (1) possesses very potent activity towards 56 of the cancer cell lines, vide supra, with GI50 values below 100 nM. Similarly, cucurbitacin D (2) is also active towards the same 59 NCI cancer cell lines, vide supra, but are in general less active than cucurbitacin B (1).
Dr Maroof Ali
Xishuangbanna tropical botanical garden
Read the Original
This page is a summary of: Cucurbitacins as Anticancer Agents: A Patent Review, Recent Patents on Anti-Cancer Drug Discovery, August 2019, Bentham Science Publishers,
DOI: 10.2174/1574892813666181119123035.
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