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At least 145 records · Page 8Linked to original sources
PubMed2006

Rumex induratus leaves: interesting dietary source of potential bioactive compounds.

The phenolic compounds of Rumex induratus leaves were determined by HPLC-DAD-MS/MS-ESI. The results revealed a profile composed of 19 compounds: caffeoyl-hexoside, two p-coumaroyl-hexoside isomers, feruloyl-hexoside, sinapoyl-hexoside, 6-C-hexosyl-quercetin, 8-C-hexosyl-luteolin, 6-C-hexosyl-luteolin, 6-C-hexosyl-apigenin, 3-O-hexosyl-quercetin, 3-O-rutinosyl-quercetin, 7-O-hexosyl-diosmetin, 3-O-rutinosyl-isorhamnetin, 7-O-(acetyl)-pento-hexosyl-diosmetin, 6-C-hexosyl-genkwanin, and four unidentified O-glycosyl-C-glycosylflavones. The quantification of the identified phenolics by HPLC-DAD showed 6-C-hexosyl-luteolin as the main compound. Organic acid composition was determined by HPLC-UV, revealing a high content of oxalic acid. R. induratus was also investigated for its capacity to act as a scavenger of DPPH and superoxide radicals. Good antioxidative results were obtained against both radicals. Unlike other species of the genus Rumex, R. induratus did not present any anthraquinone derivative.

Anthraquinones↗
PubMed2000

Bioactive compounds and 1,3-Di[(cis)-9-octadecenoyl]-2-[(cis,cis)-9, 12-octadecadienoyl]glycerol from Apium graveolens L. seeds.

Bioassay-directed isolation and purification of the hexane extract of Apium graveolens L. seeds led to the characterization of three compounds: beta-selinene (1), 3-n-butyl-4,5-dihydrophthalide (2) and 5-allyl-2-methoxyphenol (3). The structures of these compounds were established by using (1)H and (13)C NMR spectral methods. Compounds, 1-3 demonstrated 100% mortality on fourth-instar Aedes aegyptii larvae at 50, 25, and 200 microg mL(-)(1), respectively, in 24 h. Also, 2 inhibited the growth of Candida albicans and Candida kruseii at 100 microg mL(-)(1). It inhibited both topoisomerase-I and -II enzyme activities at 100 microg mL(-)(1). Compound 2 displayed 100% mortality at 12.5 and 50 microg mL(-)(1), respectively, when tested on nematodes, Panagrellus redivivus and Caenorhabditis elegans. The triglyceride, 1,3-di[(cis)-9-octadecenoyl]-2-[(cis,cis)-9, 12-octadecadienoyl]glycerol (4) and 3 were isolated for the first time from A. graveolens seeds, although 4 was not biologically active.

Apiaceae↗
PubMed1994

Structural studies on bioactive compounds. 23. Synthesis of polyhydroxylated 2-phenylbenzothiazoles and a comparison of their cytotoxicities and pharmacological properties with genistein and quercetin.

A series of polyhydroxylated 2-phenylbenzothiazoles 3 has been prepared by demethylation of the precursor methoxylated 2-phenylbenzothiazoles 9. The key step in the construction of the benzothiazole nucleus involves a Jacobson cyclization of methoxylated thiobenzanilides 8. The target compounds inhibit WiDr human colon tumor cells and MCF-7 human mammary tumor cells in vitro with IC50 values in the low micromolar range, but the activity against MCF-7 cells is not related to estrogen receptor-binding affinity. None of the compounds showed selective cytotoxicity against Abelson virus-transformed ANN-1 cells encoded with the pp120gag-abl tyrosine kinase compared with the parental 3T3 line. Compounds were only marginally inhibitory to the EGF receptor-associated protein tyrosine kinase from a membrane preparation of A431 cells. The most active compound was 4,6-dihydroxy-2-(4-hydroxyphenyl)benzothiazole (3b) which has the same overall hydroxyl substitution pattern as genistein (1a). The compounds were weakly cytotoxic for an EGF receptor, overexpressing cell line HN5, but when tested for differential toxicity against the EGF receptor tyrosine kinase or the PDGF receptor tyrosine kinase in a standard mitogenesis assay utilizing human fibroblasts, no discrimination was observed. In this assay, the compounds inhibited DNA synthesis when added to cells during S phase. This suggests that inhibition could not be interpreted in terms of tyrosine kinase inactivation but more likely as a relatively broad specificity for the ATP-binding domain of other kinases such as thymidine kinase.

3T3 Cells↗
PubMed1989

Studies on bioactive compounds. 13. Synthesis and lack of growth-inhibitory properties of cyclohexane-1,2,4-triol 1,2-diesters, which resemble ring C of the phorbol ester molecule.

It has been suggested that ring C of biologically active phorbol esters is an essential structural feature of the pharmocophore which confers activity on these compounds. In this study the hypothesis has been tested that compounds which resemble ring C of the phorbol ester molecule mimic the ability of phorbol esters to inhibit cell growth at nontoxic concentrations. All four diastereoisomers of (+/-)-1,2-di-O-octanoylcyclohexane-1,2,4-triol have been prepared from cyclohexen-4-ol and tested for growth-inhibitory and cytotoxic properties. The phorbol ester 12-O-tetradecanoylphorbol 13-acetate inhibited the growth of A549 human lung carcinoma cells by 50% at a concentration of 0.2 nM and exerted cytotoxicity at concentrations of greater than 1 microM. Diacylglycerols are the physiological ligands and activators of protein kinase C, the receptor via which phorbol esters are thought to mediate their effects. The diacylglycerols 1-oleoyl-2-acetylglycerol and 1,2-dioctanoylglycerol and the cyclohexanetriol diesters inhibited the growth of A549 cells only at concentrations of 10(-5) to 10(-4) M, at which they were also cytotoxic. A computer-assisted analysis of the goodness of fit between the cyclohexanetriol diesters and ring C of the phorbol moiety revealed possible energetic grounds for conformational dissimilarities. The results suggest that activation of protein kinase C alone is probably not sufficient to reproduce phorbol ester induced growth arrest in A549 cells and that the cyclohexanetriol diesters may lack pivotal elements of the phorbol ester pharmacophore.

Cell Division↗
PubMed1989

Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cell line.

A series of 2,4-diamino-5-aryl-6-ethylpyrimidines embracing basic substituents in the 5-aryl ring was synthesized and evaluated for inhibitory activity against rat liver dihydrofolate reductase (DHFR). Maximal enzyme inhibition was observed for compounds bearing a benzylamino (19) or N-alkylbenzylamino substituent (29 and 30) in the 4-position of the phenyl ring and a nitro group in the 3-position, the corresponding 3-amino, 3-azido, or unsubstituted analogues proving only weakly active or inactive as DHFR inhibitors. Selected compounds were also screened in vivo against a methotrexate-resistant tumor, the M5076 murine reticulosarcoma, and antitumor activity in general paralleled activity against DHFR, the (3,4-dichlorobenzyl)amino analogue 26 proving the least toxic compound to exhibit significant antitumor activity. The X-ray crystal structure of the ethanesulfonic acid salt of the N-methylbenzylamino compound 29 has been determined to facilitate future molecular modeling studies in this new series of DHFR inhibitors.

Animals↗