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Abstract
The bitter melon, Momordica charantia L., was once an important food and medicinal herb. Various studies have focused on the potential treatment of stomach disease with M. charantia and on its anti-diabetic properties. However, very little is known about the specific compounds responsible for its anti-inflammatory activities. In addition, the in vitro inhibitory effect of M. charantia on pro-inflammatory cytokine production by lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells (BMDCs) has not been reported. Phytochemical investigation of M. charantia fruit led to the isolation of 15 compounds (1−15). Their chemical structures were elucidated spectroscopically (one- and two-dimensional nuclear magnetic resonance) and with electrospray ionization mass spectrometry. The anti-inflammatory effects of the isolated compounds were evaluated by measuring the production of the pro-inflammatory cytokines interleukin IL-6, IL-12 p40, and tumor necrosis factor α (TNF-α) in LPS-stimulated BMDCs. The cucurbitanes were potent inhibitors of the cytokines TNF-α, IL-6, and IL-12 p40, indicating promising anti-inflammatory effects. Based on these studies and in silico simulations, we determined that the ligand likely docked in the receptors. These results suggest that cucurbitanes from M. charantia are potential candidates for treating inflammatory diseases.
Highlights
Inflammation is a beneficial host response to an external challenge or cellular injury that leads to the release of inflammatory mediators, finalizing the restoration of tissue function and structure [1]
Compound 1 was obtained as a white amorphous powder, with [α]D20 = −77.8 (c = 0.2, MeOH)
Using high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), the molecular formula was determined to be C33H54O4 from the positive-ion [M + Na]+ at m/z 537.3918. This is the first report of the nuclear magnetic resonance (NMR) assignment of this compound
Summary
Inflammation is a beneficial host response to an external challenge or cellular injury that leads to the release of inflammatory mediators, finalizing the restoration of tissue function and structure [1]. Inflammatory cells secrete increased amounts of nitric oxide (NO), prostaglandin E2, and cytokines (e.g., interleukin (IL)-1β, IL-6, IL12, and tumor necrosis factor-α (TNF-α)) to initiate the inflammatory process. These pro-inflammatory mediators can serve as targets to disrupt this mechanism therapeutically [2]. Acute inflammation is a rapid response in the early stage of inflammation that typically lasts from minutes to a few days It is usually beneficial for the host to initiate healing and promote tissue recovery. Our continued efforts to study biologically active compounds isolated from medicinal herbs led to the isolation of 15 cucurbitane-type terpenoids (1–15) from M. charantia fruit. We report the isolation, structure elucidation, and in vitro and in silico antiinflammatory activities of the isolated metabolites in lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells (BMDCs)
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