lespenefril and kaempferol

Bauhinia forficata Link, commonly known as "cow's paw", is a native plant from South America. Its leaves are widely used in Brazilian folk medicine to treat diabetes and cardiovascular disorders. Although this species' biological potential has been extensively proven as an antidiabetic, anti-inflammatory and antioxidant agent, there is a lack of studies to evidence its action on the cardiovascular system.. This study was designed to investigate the vascular effects of B. forficata leaves preparations and its majority compound kaempferitrin, as well as its aglycone form kaempferol, in rat aortic rings of normotensive (NTR) and hypertensive (SHR) rats.. Aorta rings from NTR and SHR precontracted with phenylephrine were exposed to cumulative concentrations of B. forficata extract, fractions (1-50 μg/mL) and compounds (0.001-0.3 μg/mL). The mechanisms involved in the vasorelaxant effect of ethyl-acetate plus butanol fraction (EAButF) were also evaluated.. Although kaempferitrin is the most abundant compound found in both methanolic extract and EAButF, 24 minor phenolic compounds were identified in B. forficata leaves, including kaempferol. EAButF was the only with endothelium-dependent and independent vasorelaxant properties in both NTR and SHR. The incubation with L-NAME or ODQ completely blocked EAButF-induced vasorelaxation. On the other hand, the incubation with propranolol, atropine, indomethacin, glibenclamide or barium chloride did not change the vasorelaxant activity of EAButF (50 μg/mL). Nevertheless, the incubation with tetraethylammonium and 4-aminopyridine significantly influenced the EAButF activity. It was also shown that Ca. This study shows, for the first time, the vasorelaxant effect of EAButF from B. forficata leaves, an effect that may be attributed to the modulation of vascular tone through nitric oxide/soluble guanylate cyclase pathway, and potassium channels. The bioactive kaempferitrin and kaempferol seem to be important for the effects observed with the fraction. Finally, preparations obtained from the leaves of B. forficata may be interesting candidates for new or complementary strategies regarding cardiovascular diseases.

Topics: Animals; Aorta, Thoracic; Bauhinia; Brazil; Cardiovascular Diseases; Endothelium, Vascular; Hypertension; In Vitro Techniques; Kaempferols; Male; Medicine, Traditional; Nitric Oxide; Plant Extracts; Plant Leaves; Plants, Medicinal; Potassium Channels; Rats, Inbred SHR; Rats, Wistar; Vasodilator Agents

The tyrosinase inhibitory activity of ethanolic extract of kenaf (Hibiscus cannabinus L.) leaf was evaluated before and after subjecting it to far-infrared (FIR) irradiation. The main component of the extract was analyzed as kaempferitrin (kaempferol-3,7-O-α-dirhamnoside). Prior to FIR irradiation, no inhibitory activity of the extract was detected in a tyrosinase assay. However, after FIR irradiation for 1h at 60°C, significant tyrosinase inhibitory activity (IC(50)=3500 ppm) was observed in it. In HPLC analysis, derhamnosylation products (kaempferol, afzelin, and α-rhamnoisorobin) were detected. The inhibitory activity may be due to the existence of derhamnosylation products. This study demonstrated that FIR irradiation can be used as a convenient tool for deglycosylation of flavonoid glycoside.

Topics: Flavonoids; Hibiscus; Infrared Rays; Kaempferols; Mannosides; Monophenol Monooxygenase; Plant Extracts; Plant Leaves; Proanthocyanidins

Two novel derivatized peptides, designated as ixorapeptide I (1) and ixorapeptide II (2), in addition to 28 other known compounds, were isolated from the MeOH extract of Ixora coccinea using bioassay-guided fractionation. The structures of metabolites 1 and 2 were determined by interpretation of the spectroscopic data and Marfey's method. Compound 1 exhibited selective potency against Hep3B liver cancer cell line with an IC(50) value of 3.36 μg/mL, and compound 2 did not show notable cytotoxicity toward cancer cell lines but could inhibit superoxide anion generation and elastase release with IC(50) values of 0.21 and 0.27 μg/mL, respectively. Moreover, kaempferol and luteolin from this plant showed inhibition with IC(50) values of 3.55 and 2.56 μg/mL, respectively on platelet aggregation induced by collagen.

Topics: Cell Line, Tumor; Humans; Kaempferols; Luteolin; Magnetic Resonance Spectroscopy; Molecular Conformation; Pancreatic Elastase; Peptides; Platelet Aggregation Inhibitors; Rubiaceae; Structure-Activity Relationship; Superoxides

To study the biotransformation of kaempferitrin, a major chemical principle of the fruits of Siraitia grosvenori (Swingle) C. Jeffery, with human intestinal flora.. The kaempferitrin was incubated with human intestinal flora. The biotransformation products were isolated and purified by chromatographic methods and the structures were determined by spectroscopic techniques.. Kaempferitrin was converted into kaempferol 3-O-alpha-L-rhamnoside (afzelin, I) , kaempferol 7-O-alpha-L-rhamnoside (II), kaempferol (III) and p-hydroxybenzoic acid (IV) by human intestinal flora. rhamnoside (II), kaempferol (III) and p-hydroxybenzoic acid (IV) by human intestinal flora.. The structure of kaempferitrin can be biotransformatedly converted by human intestinal flora.

Topics: Bacteria; Biotransformation; Fruit; Humans; Intestines; Kaempferols; Mannosides; Momordica; Parabens; Plants, Medicinal; Proanthocyanidins