ABSTRACT
Traditionally mistletoes Dendrophthoe pentandra (L.) Miq known in Indonesia is to cure cough, hypertension, diabetes, cancer, ulcers, smallpox, diuretic, skin infection and after child-birth. The objective of this study was to evaluate the toxic effects at short and long term the Dendrophthoe pentandra ethanol extract in mice. In the acute test, the limit test dose of 40 g/kg of aqueous and hydroalcoholic extracts were administered orally to mice and then observed individually 2 h post-dosing and at least once daily for 14 days. Sub-chronic toxicity was evaluated after a daily oral administration of 420 mg/kg in a suspension of 2 % PGA for 90 days to Wistar rats. Animals were sacrificed and their organs were examined. The results showed LD50 values for acute toxicity at a dose of 17.78 and 12.59 g/kg which was comparable to a dose of 12.45 g/kg and 8.81 g/kg in rats. From the subchronic, the values of the parameters of hemoglobin, hematocrit, leukocytes, and erythrocytes index were still within the range of the reference. From histopathological examination value, the results revealed some abnormalities. Our results suggest the ethanol extract of Dendrophthoe pentandra have LD50 values which have practically not toxic but is not recommended to be used for a long periode.
ABSTRACT
The essential oils of three parts of the plant Alpinia malaccencis (Burm f.) (Zingiberaceae) collected from Sumedang, West Java Province has been studied. Determination of essential oil components from the rhizome, stem, and leaf of Alpinia malaccencis (Burm f.) was performed by confirmation of the linear retention index (LRI) and comparing the NIST library peak with data reported in the literature, the mass spectrum peaks with literature data. The essential oils obtained from rhizome, stem, and leaf of Alpinia malaccencis (Burm f.) by steam distillation was 1.22%, 0.25%, and 0.7%, (w/w), respectively. Rhizome oil composition was almost similar with stem oil with methyl cinnamate as the major component. Composition of leaf oil is different from rhizome and stem oil which dominated α-pinene (30.57%). The rhizome in doses 0.1 ml (47.09 %) had stronger locomotor inhibition activity compare than stem (26.97 %) and leaf oils (32.23 %) in doses 0.1 mL.
ABSTRACT
Xanthorrhizol (XNT) is one of major compounds from temulawak`s rhizome and its activity in several cancer cells is known. The aim of this study was to identify mechanism of xanthorrhizol from temulawak`s rhizome as an hERα inhibitor against breast cancer human cell lines. The cytotoxicity of XNT from temulawak`s rhizome on T47D human breast cancer cells lined by sulforhodamine B (SRB) method has been carried out, while molecular docking simulation and pharmacophore modelling methods were employed to predict mechanism of xanthorrhizol as hER inhibitor. Cytotoxicity studies showed that XNT of the isolated and standard had an IC50 100 and 55.50 μg/mL in T47D cells, respectively. Subsequently, molecular docking interaction showed that XNT might be able to compete with estradiol (E2) as a potential ERα inhibitor with the calculated binding free-energy of -8.2 kcal/mol, even the compound superimposed with tamoxifen (4-OHT). XNT formed hydrogen bonds with Arg394 and Glu353 as mention E2 and tamoxifen also formed same interaction with same residue and interacted hydrophobic bonds similar to 4-OHT with: Leu387, Leu384, Leu391, Phe404, L349, Leu346, Met388, and Leu525 of estrogen alpha Ligan Binding Domain (LBD), although 4-OHT indicated stronger hydrophobic when the tail of tamoxifen interacted with Tyr347, Asp351, Trp383 and Leu428. XNT missed two chemical features into HipHop models pharmacophore thus may result in reduced inhibitory activity against T47D compared than 4-OHT. The xanthorrhizol mechanism as a hER inhibitor is postulated as partial estrogen antagonist, is justifiable based on its competitive characteristic versus tamoxifen (OHT-200) which was located on the active side of HER-α.