Quassinoids in Brucea javanica are potent stimulators of lipolysis in adipocytes

Abstract

Obesity is associated with a number of metabolic disorders. Lipolysis is the initial step in the metabolism of lipids stored in adipocytes and is therefore considered a therapeutic target for obesity. Quassinoids are unique terpenes found in plants of the Simaroubaceae family, which were recently reported to have lipolytic activity and to suppress weight gain. Brucea javanica is a plant employed in traditional medicines in Asia, which is known to contain various quassinoids. Here, we investigated the lipolytic activity of B. javanica extracts, and identified six quassinoids: brucein A, brucein B, brucein C, 3'hydroxybrucein A, brusatol, and bruceantinol, which represent the bioactive principals. The quassinoids contained in B. javanica demonstrated lipolytic activity at nanomolar concentrations, which were an order of magnitude lower than those of the previously reported quassinoids, suggesting that they may be useful for the treatment of obesity.

Medicinal Activities and Nanomedicine Delivery Strategies for Brucea javanica Oil and Its Molecular Components

“…There is also a significant opportunity to further explore how nanomedicine formulations of quassinoids might be used treat additional types of diseases, since quassinoids have been shown potentially useful in treating neurodegenerative diseases such as spinal muscular atrophy [82], in stimulating lipolysis in adipocyte cells that could be useful for combating obesity [83], in inhibiting insect pests [84], and in treating parasitic infections [85]. Since quassinoids are found in a wide range of plants, the nanomedicine delivery strategies discussed herein could be further explored to encapsulate various types of seed oils and purified quassinoids with distinct medicinal activities.…”

Metabolomic comparison between natural Huaier and artificial cultured Huaier

“…In addition, it has a good antiobesity effect and wound healing effect (Hwang et al, 2011; Park et al, 2017). Bruceantinol can stimulate the lipolysis of adipocytes and has an antitrypanosomal effect (Bawm et al, 2008; Lahrita et al, 2019). Cafestol protects the myocardium from Urotensin II‐induced cardiomyocyte hypertrophy, increases Caenorhabditis elegans fat oxidation and energy consumption through the DAF‐12‐dependent pathway and reduces inflammation, apoptosis and autophagy in hepatic ischemia–reperfusion injury (Farias‐Pereira et al, 2020; Hao et al, 2019; Ji, Wu, et al, 2020).…”

Evaluation on Antidiabetic Properties of Medicinal Plants from Myanmar

“…Triterpenoid glycosides having glucopyranosyl moiety are favorable for inhibiting PTP1B enzyme from E. prostrata [ 35 ]. Bitter-taste receptors of quassinoids may be a target as to induce lipolytic activity, the length of acyl side chain at 15-OH is important for the lipolytic activity of B. javanica [ 36 ].…”