Abstract
Bitter melon (Momordica charantia) has been used as traditional medicine for centuries. In many cases, whole extracts were used and the active component(s) responsible for the given activity is unknown. In this study, HEK293T and HCT116 cells treated with bitter melon seed extracts (BMSE), especially water (BMSE‐W) and 50% ethanol extracts, showed marked cytotoxicity. The cytotoxic activity in BMSE‐W was gathered in the unbound fractions when applied to various matrices, unaffected by digestion with trypsin and proteinase K, and eluted in total volume in size‐exclusion HPLC, suggesting small, organic nature of the active component(s). GC‐MS analysis of the active HPLC fractions identified methoxy‐phenyl oxime (MPO) and 2‐hydroxy‐2‐methyl‐ 2‐cyclopenten‐1‐one (2‐HMCP) as major components. Acetophenone oxime (AO), a structural homolog of MPO, exhibited similar cytotoxicity, but not 2‐hydroxy‐3‐methyl‐2‐ cyclopenten‐1‐one (3‐HMCP), a structural homolog of 2‐HMCP. Further studies showed acetophenone and methyl benzoate had no effect, indicating the oxime (C=N‐OH) functional group is essential. Increased PARP and actin cleavage, and chromatin condensation was seen in BMSE‐W and AO treated cells suggesting apoptosis as a potential cause for the cytotoxicity. In summary, this report identifies an oxime in BMSE as a cytotoxic factor and potential anticancer agent. Supported by NIH.
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