Lupeol is a pharmacologically active pentacylic triterpenoid with several potential medicinal properties, found in the Chinese herb Sophora flavescens. The first total Synthesis was reported by Gilbert Stork.[1] Studies have shown that Lupeol is a powerful IL-4 Inhibitor, and can reduce cancer risk by as much as 20%. Lupeol and its derivatives demonstrated higher anti-inflammatory activity than the commonly used non-steroidal anti-inflammatory drug indomethacin. There is convincing evidence that Lupeol is a non-toxic but highly potent chemopreventative and chemotherapeutic agent. [2] Lupeol has also been found to have a contraceptive effect due to its inhibiting effect on the calcium channel of sperm (CatSper). [3]

MDS Labs has released several compounds from its innovative D+Q Senolytic counterpart, NEUROmergence, as individual supplements. One of these compounds is an extraction of Sophora flavescens, known as Ku Shen in traditional Chinese medicine. The lab experimented with various solvent screening methods before finding a technique that produced an extract rich in Lupeol.

“We wanted to partially isolate Lupeol, but not entirely for its anti-inflammatory and anti-cancer effects. The formulation we were developing needed a powerful, but selective CDK2, CDK4, and CDK6 inhibitor to better align NEUROmergence with Dasatinib.”

Lupeol is known as one of the most effective phytochemicals to inhibit the CDK family protein kinases.[4] “We were able to standardize to 38% Lupeol, but Western blotting revealed this wasn’t necessary to achieve its desired inhibitory properties, so we adjusted it to around 20%. As a result of this change, we were also measuring around 37% Oxymatrine.”

Oxymatrine, a phytosterol that is entirely unique to Sophora flavescens, is known to be anti-inflammatory, anticancer, antidiabetic, and antivirus, also demonstrates protective activities to the brain, liver, heart, lung, vascular, gastrointestinal, bone, kidney, and skin. The underlying anticancer activity of this compound may be involved anti-proliferation, invasion, migration, angiogenesis, epithelial-mesenchymal transition of cells, autophagy, especially apoptic cell deaths. [5]

“This might partially explain why the senolytic properties of NEUROmergence exhibited such a high level of effectiveness, while also demonstrating a better safety profile compared to Dasatinib during the testing process,” according to the lab. We are excited to release the compounds that were formulated specifically for NEUROmergence as individual supplements, allowing for a custom-tailored approach to healthy aging. These compounds are very unique in their own right and might provide substantial benefits for those who choose to take them.

Purchase NEUROmergence
Purchase Ku Shen Extract (250mg)

Citations:

[1] Stork G, Uyeo S, Wakamatsu T, Grieco P, Labovitz J (1971). “Total synthesis of lupeol”. Journal of the American Chemical Society. 93 (19): 4945. doi:10.1021/ja00748a068. https://doi.org/10.1021%2Fja00748a068

[2] Saleem M. Lupeol, a novel anti-inflammatory and anti-cancer dietary triterpene. Cancer Lett. 2009 Nov 28;285(2):109-15. doi: 10.1016/j.canlet.2009.04.033. Epub 2009 May 22. PMID: 19464787; PMCID: PMC2764818.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2764818/

[3] Mannowetz N, Miller MR, Lishko PV (May 2017). “Regulation of the sperm calcium channel CatSper by endogenous steroids and plant triterpenoids”. Proceedings of the National Academy of Sciences of the United States of America. 114 (22): 5743–5748. doi:10.1073/pnas.1700367114. PMC 5465908. PMID 28507119.
https://www.pnas.org/doi/full/10.1073/pnas.1700367114/

[4] Wang Y, Hong D, Qian Y, Tu X, Wang K, Yang X, Shao S, Kong X, Lou Z, Jin L. Lupeol inhibits growth and migration in two human colorectal cancer cell lines by suppression of Wnt-β-catenin pathway. Onco Targets Ther. 2018 Nov 9;11:7987-7999. doi: 10.2147/OTT.S183925. Retraction in: Onco Targets Ther. 2020 Aug 20;13:8371. doi: 10.2147/OTT.S276550. PMID: 30519040; PMCID: PMC6235339.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6235339/

[5] Duong Quang Huan, Nguyen Quang Hop, Ninh The Son (2009). “Oxymatrine: A current overview of its health benefits”. Faculty of Chemistry, Hanoi Pedagogical University 2 (HPU2), 32 Nguyen Van Linh, Xuanhoa, Phucyen, Vinhphuc, Viet Nam doi: 10.1016/j.canlet.2009.04.033
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6235339/