Characterisation of marrubenol, a diterpene extracted from Marrubium vulgare, as an L-type calcium channel blocker. (1/4)

1. The objective of the present study was to investigate the mechanism of the relaxant activity of marrubenol, a diterpenoid extracted from Marrubium vulgare. In rat aorta, marrubenol was a more potent inhibitor of the contraction evoked by 100 mM KCl (IC50: 11.8+/-0.3 microM, maximum relaxation: 93+/-0.6%) than of the contraction evoked by noradrenaline (maximum relaxation: 30+/-1.5%). 2. In fura-2-loaded aorta, marrubenol simultaneously inhibited the Ca2+ signal and the contraction evoked by 100 mM KCl, and decreased the quenching rate of fura-2 fluorescence by Mn2+. 3. Patch-clamp data obtained in aortic smooth muscle cells (A7r5) indicated that marrubenol inhibited Ba2+ inward current in a voltage-dependent manner (KD: 8+/-2 and 40+/-6 microM at holding potentials of -50 and -100 mV, respectively). 4. These results showed that marrubenol inhibits smooth muscle contraction by blocking L-type calcium channels.  (+info)

The in-vitro evaluation of antibacterial, antifungal and cytotoxic properties of Marrubium vulgare L. essential oil grown in Tunisia. (2/4)

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Molluscicidal and Mosquitocidal activities of the essential oils of Thymus capitatus Hoff. et Link. and Marrubium vulgare L. (3/4)

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Antiproliferative activity of Marrubium persicum extract in the MCF-7 human breast cancer cell line. (4/4)

AIM: Developing antitumor drugs from natural products is receiving increasing interest worldwide due to limitations and side effects of therapy strategies for the second leading cause of disease related mortality, cancer. METHODS: The antiproliferative activity of a methanolic extract from the aerial parts of Marrubium persicum extract was assessed with the MCF-7 breast cancer cell line using the MTT test for cell viability and cytotoxicity indices. In addition, antioxidant properties of the extract were evaluated by measuring its ability to scavenge free DPPH radicals. Moreover, the total phenolic and flavonoid content of the extract was determined based on Folin-Ciocalteu and colorimetric aluminum chloride methods. RESULTS: The findings of the study for the antiproliferative activity of the methanolic extract of M. persicum showed that growth of MCF-7 cells was inhibited by the extract in a dose and time dependent manner, where a gradual increase of cytotoxicity effect has been achieved setting out on 200 mug/mL concentration of the plant extract. The antioxidant assay revealed that the extract was a strong scavenger of DPPH radicals with an RC50 value of 52 mug/mL. The total phenolic and flavonoids content of the plant extract was 409.3 mg gallic acid equivalent and 168.9 mg quercetin equivalent per 100g of dry plant material. CONCLUSION: Overall, M. persicum possesses potential antiproliferative and antioxidant activities on the malignant MCF-7 cell line that could be attributed to the high content of phenolics and flavonoids, and therefore warrants further exploration.  (+info)