Abstract
Plants of the genus Teucrium (Lamiaceae or Labiatae family) are known historically for their medicinal value. Here, we identify and characterize the anticancer potential of T. mascatense and its active compound, IM60, in human cancer cells. The anti-proliferative effect of a T. mascatense methanol extract and its various fractions were analyzed in MCF-7 and HeLa cells in a dose- and time dependent manner. The dichloromethane fraction (TMDF) was observed to be the most effective with cytotoxicity against a more expanded series of cell lines, including MDA-MB-231. A time and dose-dependent toxicity profile was also observed for IM60; it could induce rapid cell death (within 3 h) in MCF-7 cells. Activation of caspases and PARP, hallmarks of apoptotic cell death pathways, following treatment with TMDF was demonstrated using western blot analysis. Inversion of the phosphatidylserine phospholipid from the inner to the outer membrane was confirmed by annexin V staining that was inhibited by the classical apoptosis inhibitor, Z-VAK-FMK. Changes in cell rounding, shrinkage, and detachment from other cells following treatment with TMDF and IM60 also supported these findings. Finally, the potential of TMDF and IM60 to induce enzymatic activity of caspases was also demonstrated in MCF-7 cells. This study, thus, not only characterizes the anticancer potential of T. mascatense, but also identifies a lead terpenoid, IM60, with the potential to activate anticancer cell death pathways in human cancer cells.
Highlights
Cancer is the second major cause of mortality worldwide, responsible for an estimated 9.6 million deaths in 2018, and accounting for one out of every six deaths [1]
The initial screening was limited to two types of human cancer cell lines: MCF-7, a breast cancer cell line [43], and HeLa, a cervical carcinoma cell line [44]
After 24 h of treatment, TMME and two of its organic fractions prepared by using dichloromethane and n-hexane solvents (TMDF and TMHF), were observed to be effective against MCF-7 cell line by inducing ≥20% inhibition of cell proliferation at a concentration of 250 μg/mL
Summary
Cancer is the second major cause of mortality worldwide, responsible for an estimated 9.6 million deaths in 2018, and accounting for one out of every six deaths [1]. This burden is expected to rise from. The economic burden of cancer is no less, where only in the US, it was estimated to be nearly $1.16 trillion in 2010 alone [3]. Molecules 2019, 24, 977 compounds for cancer therapy is widely prevalent, with more than 60% of clinically approved anticancer drugs being derivatives of medicinal plants [4,5].
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