acacetin and diosmetin

The aim of the present study was to investigate the interactions of the main components of. In vitro inhibition of drugs was assessed by incubating rat liver microsomes (RLMs) with a typical P450 3A enzyme substrate, midazolam, to determine their 50% inhibitory concentration (IC50) values. For the in vivo study, healthy male Sprague Dawley rats were consecutively administered acacetin or apigenin for 7 days at the dosage of 5 mg/kg after being randomly divided into 3 groups: Group A (control group), Group B (acacetin group) and Group C (apigenin group).. Among the five main components of. Acacetin and apigenin could inhibit the activity of the cytochrome P450 3A enzyme in vitro and in vivo, indicating that herbal drug interactions might occur when taking

Topics: Animals; Apigenin; Coumaric Acids; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Ferns; Flavones; Flavonoids; Glycosides; Male; Medicine, Traditional; Molecular Structure; Plant Roots; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

"Quelites" are edible plants that are part of the traditional agro-ecosystems in Mexico. These plants, despite their already known nutritional properties, are now considered neglected and underutilized species. With the objective of promoting their reinsertion in the markets and mainly, in daily diets, efforts have been made to study them from multidisciplinary approaches to demonstrate their beneficial properties. To generate evidence of an added health-promoting value that would encourage quelites consumption, in the present work, the anti-Helicobacter pylori activity of three representative quelite species, Anoda cristata (Alache), Cnidoscolus aconitifolius (Chaya), and Crotalaria pumila (Chepil), was tested. H. pylori is considered the etiological agent of gastritis, ulcer, and gastric cancer, and represents a public health problem in Mexico and worldwide. Aqueous (AQ) and dichloromethane-methanol (DM) extracts were obtained from the three species of quelites to investigate their effect on H. pylori growth and on two of its colonization factors (adherence and urease activity). DM extracts from Chaya, Chepil, and Alache exert the best inhibitory effect on bacterial growth, with minimum inhibitory concentrations of 62.5, 125, and 250 μg/mL, respectively. AQ and DM extracts inhibit bacterial adhesion by 30% to 50%. None of them has an effect on urease activity. The two flavonoids present in A. cristata, acacetin and diosmetin, inhibit H. pylori growth by ∼90% with 3.9 μg/mL. These results provide new information about the anti-H. pylori potential of three edible quelites, and give an added value, since their routine consumption may impact on the prevention and/or control of H. pylori-associated diseases.

Topics: Anti-Bacterial Agents; Crotalaria; Euphorbiaceae; Flavones; Flavonoids; Helicobacter Infections; Helicobacter pylori; Humans; Malvaceae; Mexico; Microbial Sensitivity Tests; Plant Extracts; Plants, Edible

Some studies refer that the entire plant of Anoda cristata is consumed as food and medicine; in particular for treating diabetes, inflammation, fever, cough, and wounds. The aim of this study was to establish the preclinical efficacy of Anoda cristata as hypoglycemic and/or antihyperglycemic agent using well-known animal models.. The acute toxicity was analyzed by the Lorke method. Acute hypoglycemic as well as oral glucose and sucrose tolerance tests were used to determine the hypoglycemic and antihyperglycemic action of Anoda cristata. Several preparations of the plant, including a mucilage (M), an aqueous (T-AE), a free mucilage aqueous (FM-AE), and an organic (OE) extracts, were tested in healthy and NA-STZ-hyperglycemic mice. Glibenclamide (15mg/kg), acarbose (5mg/kg ) and metformin (200mg/kg) were used as positive controls. The major compounds acacetin (1) and diosmetin (2), isolated from an infusion of the plant applying chromatographic methods, were evaluated as hypoglycemic agents using the same assays. The FM-AE was tested also in rats with metabolic syndrome induced by a high-fructose fed. Finally some assays were performed to determine the antioxidant capacity of the FM-AE in vitro.. The results demonstrated that the extracts and compounds from Anoda cristata were effective for reducing blood glucose levels in healthy and NA-STZ-hyperglycemic mice when compared with vehicle groups (p<0.05). The FM-AE exerted also positive effect over different biochemical parameters altered in rats with metabolic syndrome induced by a fructose diet. FM-AE has also antioxidant action effectively trapping ONOO(-) and ROO(•) radicals. The major flavonoids isolated from the plant, namely acacetin (1) and diosmetin (2), caused significant hypoglycemic effect and possessed antioxidant activity.. Anoda cristata is effective to diminish glucose levels in vivo and to ameliorate different disorders related with the metabolic syndrome in rats. According to the results, the efficacy of Anoda cristata preparations could be due to the presence of active principles with different mode of actions at the molecular level, including α-glycosidases inhibitors, insulin secretagogues, glucose entrapment and radical trapping agents.

Topics: Animals; Antioxidants; Blood Glucose; Diabetes Mellitus, Experimental; Flavones; Flavonoids; Free Radicals; Glycogen; Hyperglycemia; Hypoglycemic Agents; Insulin; Lipid Metabolism; Liver; Male; Malvaceae; Metabolic Syndrome; Mice, Inbred ICR; Phytotherapy; Plant Components, Aerial; Plant Preparations; Plants, Edible; Rats; Rats, Sprague-Dawley; Uric Acid

The leaves of Clerodendrum inerme (L.) Gaertn. have commonly been used in Thai traditional medicine for treatment of inflammatory diseases. However, the bioactive compounds responsible for the anti-inflammatory effect of leaves have not been yet determined. The objective of the present study was to isolate these bioactive compounds by bioassay-guided isolation technique and to determine the mode of action of isolated compounds in LPS-induced macrophages.. Anti-inflammatory effect of various fractions (hexane, ethyl acetate and water) of ethanol extract of C. inerme leaves was determined from the production of nitric oxide (NO) in RAW 264.7 macrophage stimulated with LPS. The mRNA and protein levels were determined also by real-time reverse transcription-polymerase chain reaction and western blot analysis, respectively. Leaf bioactive compounds were isolated by bioassay-guided fractionation technique using column chromatography.. The ethyl acetate fraction (EA) among solvent extracts provided the most potent inhibitory activity on NO production. Also, EA reduced the mRNA and protein expressions of inducible nitric oxide synthase (iNOS) in LPS-stimulated macrophages. Three known flavones, acacetin (1), hispidulin (2) and diosmetin (3), were isolated based on inhibition of NO production. Furthermore, hispidulin also inhibited PGE2 production as well as iNOS and cyclooxygenase-2 expressions via the blockade of NF-κB DNA-binding activity and JNKway.. Our results found acacetin (1), hispidulin (2) and diosmetin (3), were responsible for the anti-inflammatory properties of C. inerme leaves. We provide scientific evidence to support the usefulness of C. inerme leaves in traditional medicine for the treatment of inflammation-related diseases.

Topics: Animals; Anti-Inflammatory Agents; Biological Assay; Blotting, Western; Clerodendrum; Flavones; Flavonoids; Inflammation; Medicine, Traditional; Mice; Phytotherapy; Plant Extracts; Plant Leaves; RAW 264.7 Cells

To study the chemical constituents from the leaves of "Chuju" Chrysanthemum morifolium.. All compounds were separated and purified by column chromatography over silica gel, Sephadex LH-20 and preparative HPLC. Their structures were identified by spectral methods including 1H-NMR and 13C-NMR.. 21 compounds were isolated and identified as octa-cosyl alcohol (1), β-sitosterol (2), lupeol (3), α-amyrin (4), daucosterol (5), ineupatorolide B (6), syringin (7), chlorogenic acid (8), petasiphenol (9), physcion (10), acacetin (11), eupatilin (12), quercetin (13), diosmetin (14), luteolin (15), apigenin (16), apigenin- 7-O-β-D-glucopyranoside (17), quercetin-3-O-β-D-glucopyranoside (18), luteolin-7-O-β-D-gluco pyranoside (19), apigenin-7-O-β-D- neospheroside (20), and acacetin-7-O-β-D-glucoside (21).. Compounds 1-12, 18 and 20 are isolated from this plant for the first time. Compounds 10, 13, 14, 15 and 16 have shown strong antioxidant activities by DPPH · scavenging activity better than Vit C.

Topics: Antioxidants; Apigenin; Chlorogenic Acid; Chrysanthemum; Flavones; Flavonoids; Glucosides; Luteolin; Phenylpropionates; Phytochemicals; Plant Leaves; Plants, Medicinal; Quercetin; Sitosterols

To study the chemical constituents of Citrus medica fruit.. The fruit of Citrus medica was extracted with 95% EtOH, and the compounds were separated and purified by silica gel, RP-18 and Sephadex LH-20 column chromatography. The structures were identified by spectroscopic analysis.. A total of 16 compounds were isolated and identified, including methyl ferulic acid (1), dihydro-N-caffeoyltyramine (2) acacetin (3), β-ecdysterone (4), (-)-balanophonin (5), p-methoxy cinnamic acid (6), umbelliferone (7), ferulic acid (8), pyrocatechualdehyde (9), diosmetin (10), 4-methoxy salicylic acid (1), β-amyrin acetate (12), epigallocatechin (13), betulinic acid (14), lupeol (15) and nicotinamide (16).. All the compounds are isolated from the fruit of Citrus medica for the first time.

Topics: Caffeic Acids; Cinnamates; Citrus; Coumaric Acids; Flavones; Flavonoids; Fruit; Oleanolic Acid; Pentacyclic Triterpenes; Phytochemicals; Plants, Medicinal; Tyramine

Agents to control melanogenesis are in demand for the development of cosmetics to improve pigmentation disorders of skin and hair. In this study, we examined and evaluated the effects of flavonoids on melanogenesis in the melanogenic cells model, murine B16F10 melanoma cells. In the course of this study, we found that incubation of the cells in a medium containing 10 μM of the 4'-O-methylated flavonoids, diosmetin (4'-O-methylluteolin), acacetin (4'-O-methylapigenin) or kaempferide (4'-O-methylkaempferol), increased the melanin contents of the cells 3- to 7-fold higher than the control cells. The concentration-dependence test revealed that 20 μM acacetin showed the highest effect, up to 33-fold higher than the vehicle. On the other hand, the corresponding 4'-OH-type flavonoids, luteolin, apigenin and kaempferol, had a significantly smaller effect. Furthermore, by evaluating the melanogenic proteins, we found that the cells treated with 4'-O-methylated flavonoids showed higher tyrosinase activity, as well as upregulation of tyrosinase expression, preceded by activation of cAMP response element binding protein (CREB) and extracellular signal-regulated kinases types 1 and 2 (ERK1/2). These results indicate that the 4'-O-methyl group of flavonoids plays an important role in the induction of melanogenesis by activating its major signal transduction pathway through the upregulation of phospho-CREB in murine B16F10 melanoma cells.

Topics: Animals; Apigenin; Cell Line, Tumor; Extracellular Signal-Regulated MAP Kinases; Flavones; Flavonoids; Luteolin; Melanins; Melanoma, Experimental; Mice; Monophenol Monooxygenase