Antiproliferative, apoptotic, and antimutagenic properties of stem bark and seed fractions of Polyalthia cerasoides (Roxb.).

AIMS: The aim was to compare the anticancer and antimutagenic potency of Polyalthia cerasoides seeds and stem bark. AIM OF THE STUDY: The aim of this study was to investigate the antiproliferative, apoptotic, antioxidation to DNA, and antimutagenic activity of alcoholic (PS-1 and PS-3) and petroleum ether (PS-2 and PS-4) stem bark and seed fractions of P. cerasoides. METHODS: P. cerasoides stem bark and seeds were extracted with ethanol: water mixture (9:1 ratio v: v) and fractionated with petroleum ether. Fractions were investigated for antiproliferative effect using cell by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, a tetrazole assay (cell line used liver [HepG2] and cervical [HeLa] cancer cell lines), DNA damage protection using hydroxyl radical and antimutagenic effect using chromosome aberration test. RESULTS: PS-1 (IC50 10 µg/ml) and PS-3 (IC50 11 µg/ml) showed maximum antiproliferative activity against HepG2 cell lines, whereas, PS-1 (IC50 10 µg/ml), PS-2 (IC50 24 µg/ml), and PS-3 (IC50 11 µg/ml) showed better antiproliferative activity against HeLa cell lines. PS-3 and PS-4 were protective against oxidation to the supercoiled DNA molecule. Further, petroleum ether extract of both seed (PS-2) and stem bark (PS-4) showed good antimutagenicity as revealed by the less chromosomal aberrations compared to PS-1 and PS-3 fractions. CONCLUSIONS: This study demonstrated the beneficial effect of fractions against oxidation of DNA, antiproliferative, apoptotic, and antimutagenic activity. Probably, this property would be attributable by their phenolic and steroid constituents. Therefore, this plant could be used as a potential source of nutraceutical agents.

Dose assessment of bremsstrahlung induced by beta-emitting radioisotopes of uranium-238 series and lead in human tissues.

In the natural uranium-238 decay series, pure beta isotopes such as (234)Th, (234)Pa, (214)Pb, (214)Bi, (210)Pb and (210)Bi are released. The few lead isotopes such as (211)Pb, (212)Pb, (213)Pb and (215)Pb are good beta emitters. In certain nuclear reactions of reactor these isotopes are released. These beta isotopes have maximum beta energies, which induce the bremsstrahlung radiation. The bremsstrahlung component of these beta isotopes has been traditionally ignored in dosimetry calculations. The shapes of bremsstrahlung spectra are a basic ingredient in the understanding and quantification of beta-ray dosimetry. The bremsstrahlung spectra produced by these high-energy isotopes such as (234)Th, (234)Pa, (214)Pb, (214)Bi, (210)Pb, (210)Bi, (211)Pb, (212)Pb, (213)Pb and (215)Pb in bone, muscle and teeth are studied, and the computed spectral distributions are presented. The spectral shapes are primarily responsible for variations in the shapes of depth-dose distributions. They are intended to provide a quick and convenient reference for spectral shapes and to give an indication of the wide variation in these shapes. The evaluated beta bremsstrahlung dose as a function distance for the studied nuclides is also presented. The efficiency, intensity and dose rate of bremsstrahlung induced by beta isotopes of natural uranium-238 decay series and beta-emitting lead isotopes in human tissues such as brain, breast, heart, kidney, liver, muscle, pancreas and bone have also been studied in the present investigation. The values of bremsstrahlung dosimetric parameters are low for pancreas, but they are high for bone. For all studied tissues these parameters are high for (234)Pa, but low for (210)Pb.

Antiproliferative, apoptotic and antimutagenic activity of isolated compounds from Polyalthia cerasoides seeds.

Phytochemical investigation of the petroleum ether extract fraction of Polyalthia cerasoides seeds led to the isolation of two phytosterols (alpha-spinasterol and spinasterol) and a clerodane di-terpenoid. The structures of these compounds were elucidated using IR, (1)H-NMR, (13)C-NMR and Mass spectral analysis. Further, these compounds were tested for antiproliferative action against CACO-2 cell line and apoptotic action was determined by nuclear staining and DNA fragmentation analysis. The results showed that the compounds exhibited antiproliferative action at various concentrations with an IC(50) value of 28.6+/-4.34nM/ml, 57.7+/-6.81nM/ml and 60.0+/-7.10nM/ml for clerodane diterpenoid, spinasterol and alpha-Spinasterol respectively. Furthermore, the isolated compounds were screened for antimutagenic effect against methylmethane sulfonate (MMS) induced mutation. Phytosterols showed protective effect, whereas clerodane diterpenoid was less effective to MMS induced chromosomal aberrations. Our research contributes to the characterization of phytochemical constituents and to understand the ability of these compounds to antiproliferative and antimutagenic responses from the seed extracts.

Free radical scavenging, antioxidant enzymes and wound healing activities of leaves extracts from Clerodendrum infortunatum L.

Three successive extracts of Clerodendrum infortunatum L. leaves have been studied for their potential as antioxidants in 1,1-diphenyl-2-picrylhydrazyl (DPPH) model. The scavenging activity of ethanol extract was found to be high when compared to petroleum ether and chloroform extracts. Hence, it was selected to evaluate the beneficial properties using in vitro and in vivo models. The antioxidant and its protective effects against CCl(4) induced oxidative stress in rats were significantly high. Further, to validate the traditional therapeutic claim, wound healing activity of the plant extracts was also carried out. Among the three extracts tested the petroleum ether and ethanol extracts exhibited a significant response. The presence of high antioxidant and pharmacological properties correlates to the total phenolic contents in the plant Clerodendrum infortunatum L.

Hypolipidemic and antioxidant efficacy of dehydrated onion in experimental rats.

Hypolipidemic and antioxidant potency of a dehydrated onion product was evaluated in experimental rats maintained for 6 weeks at 5 and 10% dietary levels. Serum cholesterol especially low-density lipoprotein was significantly reduced by dietary dehydrated onion in hypercholesterolemic rats. This was associated with an increase in high density lipoprotein cholesterol. Blood triglyceride concentration in hypercholesterolemic rats was lower in onion supplemented diet group. Glutathione, ascorbic acid and α-tocopherol in the blood of hypercholesterolemic rats were higher in onion treatment, while lipid peroxides were lower. Hepatic α-tocopherol concentration was higher in rats maintained on onion diets, while lipid peroxides were reduced. Thus, this study has proved significant cholesterol lowering and antioxidant effect of dehydrated onion product.

Antimicrobial activity of flavanoid sulphates and other fractions of Argyreia speciosa (Burm.f) Boj.

Antimicrobial activity of flavanoid sulphates and different fractions of A. speciosa root was studied against bacteria, fungi and Mycobacterium tuberculosis H37 Rv sensitive strain by in vitro and in vivo assays. Flavanoid sulphates such as quercetin 3'7 di-O methyl 3- sulphate and kaempferol 7-O methyl 3-sulphate were isolated from the n-butanol fraction of 80% methanolic extract of the plant. The structures of the isolated flavanoids were confirmed by spectral studies. Ethyl acetate (EAAS) fraction and flavanoid sulphates inhibited the growth of M. tuberculosis Rv sensitive strain at MIC values 50 and 25 microg/ml, respectively. Ethanolic fraction (EtAS) showed significant inhibition of gram positive organism with a MIC of 31.25 microg/ml. More inhibition was observed with a less MIC (2 microg/ml) for flavanoid sulphates against Klebsiella pneumoniae, a gram negative organism and it is almost comparable with the standards. Interestingly, chloroform fraction alone exhibited significant antifungal activity with a MIC of 100 microg/ml. A synergistic effect between flavanoids sulphates and commercially available antitubercular drugs was observed with FIC index of 0.443 +/- 0.245, 0.487 +/- 0.247 for isoniazid and 0.468 +/- 0.333, 0.417 +/- 0.345 for rifampicin, whereas EAAS fraction showed partial synergistic effect. A synergistic effect was observed for EAAS fraction and flavanoids sulphates with FIC index < 0.5 with antibiotics. Hemolysis assay on RBCs suggested that EAAS and flavanoids sulphates exhibited least cellular toxicity to erythrocytes as compared to chloramphenicol. In vivo studies in mice infected with K. pneumoniae demonstrated that on day 10 post treatment of different fractions and isolated compounds of A. speciosa, about 60% of the animals treated with EAAS, 70% of animals treated with flavanoids sulphates and 40% of animals treated with EtAS were survived.

Protective effect of dietary capsaicin on induced oxidation of low-density lipoprotein in rats.

An animal study was carried out to examine the beneficial influence of the known hypocholesterolemic spice principle-capsaicin on the susceptibility of low-density lipoprotein to oxidation in normal and hypercholesterolemic condition. In rats rendered hypercholeterolemic by maintaining them on a cholesterol-enriched diet for eight weeks, inclusion of capsaicin (0.015%) in the diet, produced significant hypocholesterolemic effect. Oxidation of low-density lipoprotein was induced either by copper ion in vitro after its isolation, or by ferrous ion in vivo in experimental rats under either normal or hypercholesterolemic situation and the beneficial effect of dietary capsaicin on the same was evaluated. LDL oxidation was measured by the thiobarbituric acid reactive substances (TBARS) formed and relative electrophoretic mobility of oxidized LDL. Dietary capsaicin was found to be protective to the LDL oxidation in vitro in the case of normal rats as indicated by reduction in TBARS by more than 40%. In the case of LDL isolated from hypercholesterolemic rats the extent of copper induced LDL oxidation was significantly lower than that of LDL isolated from normal rats. Dietary capsaicin did not make any difference in the extent of LDL oxidation in vitro in hypercholesterolemic rats. Ferrous ion induced in vivo oxidation of LDL was 71% lower in capsaicin fed normal rats. In high cholesterol feeding, Fe-induced in vivo oxidation of LDL was 73% lower, while the same was still marginally lower in capsaicin fed hypercholesterolemic rats. Hepatic lipid peroxidation was significantly decreased by dietary capsaicin in normal rats. While a significantly decreased level of lipid peroxidation was observed in hypercholesterolemic rats compared to normal rats, the same was not significantly altered by dietary capsaicin. Results suggest that dietary spice principle capsaicin is protective to LDL oxidation both in vivo and in vitro under normal situation, while in hypercholesterolemic situation where the extent of LDL oxidation is already lowered, capsaicin does not offer any further reduction.