ABSTRACT
Abstract In this study, sahandone (1) and a new diterpenoid named sahandol II (2) were isolated from the roots of Salvia chloroleuca Rech. f. & Aellen, Lamiaceae. The absolute configurations of compounds 1 and 2 were assigned by comparison of experimental electronic circular dichroism spectra and comparing with published data. Cytotoxic and apoptotic evaluation of the isolated compounds and the methanol crude extract and its subfractions including petroleum ether, dichloromethane, ethyl acetate, n-butanol and aqueous fraction on two human prostate cancer cell lines and a breast cancer cell lines, showed that non-polar and semi-polar subfractions had the potent cytotoxic effect on PC3 cells with the IC50 values of 24.19, 33.59, and 47.15 µg/ml, respectively. Sub-G1 peak in flow cytometry histogram of cells treated with petroleum ether, dichloromethane and ethyl acetate subfractions showed the induction of apoptosis. Change in the Bax/Bcl-2 ratio and cleavage of poly ADP-ribose polymerase were observed.
ABSTRACT
Most species of genus Artemisia L. (Compositae) are medicinal herbswith several uses in the folk medicine worldwide. In the present study, methanol extract of Artemisia santolina has been subjected for isolation of its metabolites along with evaluation of cytotoxic activity against Artemia salina larvae. The structures of the compounds determined by 1H-and 13C-NMR, HMQC, HMBC, 1H-1H COSY and Mass spectral analysis. Two sesquiterpenes, 1,5-dihydroxy- 4(15)eudesman-12,6-olid (artemin) (1), 2-hidroxy-2,6,10-trimethyl-7,10- oxide-3,11-dodecadien-5-one (2) and one flavonoid, 5,7,4'-trihydroxy-6,3'-dimethoxyflavone (jaceosidin) (3) have been successfully characterized. Cytotoxicity of the sesquiterpene lactone (1), was assessed on Artemia salina larvae and resulted in IC50 value of 6.44 µg/mL, which was more potent compared to the positive standard berberine hydrochloride (IC50 = 26 µg/mL). In this study, the separation and identification of two sesquiterpenes and one flavone from the aerial parts of A. santolina is described. Among them the compound artemin (1) showed a toxicity effect against A. salina nauplii.
La mayoriÌa de las especies del geÌnero Artemisia L. (Compositae) son hierbas medicinales con varios usos en la medicina popular en todo el mundo. En el presente estudio, el extracto metanoÌlico de Artemisia santolina ha sido sometido al aislamiento de sus metabolitos junto con la evaluacioÌn de la actividad citotoÌxica contra las larvas de Artemia salina. Las estructuras de los compuestos se determinaron mediante RMN 1H y 13C, HMQC, HMBC, 1H-1H COZY y anaÌlisis espectral de masas. Dos sesquiterpenos, 1,5-dihidroxi-4 (15) eudesman- 12,6-olid (artemin) (1), 2-hidroxi-2,6,10-trimetil-7,10-oÌxido-3,11-dodecadien-5-ona (2) y un flavonoide, 5,7,4'-trihidroxi-6,3'- dimetoxiflavona (jaceosidina) (3). Se evaluoÌ la citotoxicidad de la lactona sesquiterpeÌnica (1) en larvas de Artemia salina y resultoÌ en un valor de CI50 de 6,44 µg/ml, que era maÌs potente en comparacioÌn con el clorhidrato de berberina estaÌndar positivo (CI50 = 26 µg/ml). En este estudio se describe la separacioÌn e identificacioÌn de dos sesquiterpenos y una flavona de las partes aeÌreas de A. santolina. Entre ellos, el compuesto artemin (1) mostroÌ un efecto de toxicidad contra los nauplios de A. salina.
Subject(s)
Artemia/drug effects , Artemisia/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Flavonoids/analysis , Larva , Sesquiterpenes/analysisABSTRACT
Anti-proliferative properties have been reported for certain species of the genus Artemisia. In this study, we investigated the cytotoxic and apoptotic effects of n-hexane, CH2Cl2, EtOAc, n-BuOH and H2O fractions obtained from a crude methanol extract of A. armeniaca on two myeloid cell lines, apoptosis-proficient HL60 cells and apoptosis-resistant K562 cells; in addition, J774 cells were used as a control. Among the solvent fractions of A. armeniaca, the CH2Cl2 fraction was found to have the largest anti-proliferative effect on cancer cells. The IC50 values obtained using an MTS assay for the CH2Cl2 fraction were 75 and 130 µg/ml for HL-60 cells and K562, respectively. The control cells were not significantly affected by this fraction. A flow cytometry histogram of cells treated with the CH2Cl2 fraction of A. armeniaca revealed a sub-G1 peak. DNA fragmentation, increased protein levels of Bax and cleavage of the poly (ADP-ribose) polymerase (PARP) protein confirmed the induction of apoptosis in cells after a 48-h exposure to the CH2Cl2 fraction. Our results corroborate the cytotoxic and apoptotic effects of the CH2Cl2 fraction of A. armeniaca on K562 and HL-60 cancer cell lines.
ABSTRACT
Chemical investigation on the CH2Cl2 fraction of the Scutellaria litwinowii Bornm. & Sint., Lamiaceace, root extract for the first time resulted in the isolation of wogonin, and neobaicalein. These compounds were evaluated for their cytotoxicity towards HeLa cell lines and lymphocytes. Meanwhile, the role of apoptosis was explored in this toxicity. The cells were cultured in RPMI medium and incubated with different concentrations of isolated flavonoids. Cell viability was quantified by MTS assay. Apoptotic cells were determined using propidium iodide staining of DNA fragmentation by flow cytometry (sub-G1peak). Wogonin, and neobaicalein inhibited the growth of malignant cells in a dose-dependent manner. The IC50 values of 46.62 and 79.34 µM were, respectively, found for neobaicalein and wogonin against HeLa cells after 48 h of treatment. Neobaicalein induced a sub-G1 peak in the flow cytometry histogram of treated cells compared to control cells indicating that apoptotic cell death is involved in neobaicalein toxicity. Neobaicalein exerts cytotoxic and pro-apoptotic effects in HeLa cell lines and could be considered as a potential chemotherapeutic agent in cancer treatment.