Chemical composition and protective role of Pulicaria undulata (L.) C.A. Mey. subsp. undulata against gastric ulcer induced by ethanol in rats.

Pulicaria undulata subsp. undulata (Family; Asteraceae) is a medicinal plant used to treat inflammation. The objective of this study is to explore the protective effect of the ethanol extract of P. undulata subsp. undulata aerial parts against ethanol induced gastric ulcer in rats. The chemical composition of plant extract, the unsaponifiable matter and the fatty acid methyl esters were analyzed. The biological evaluation was carried out through measuring ulcer indices, oxidative stress markers, certain marker enzymes, inflammatory index and the histopathological assessment of the stomach in rats. The total unsaponifiable matter (94.29%) and the fatty acid methyl ester (82.96%) content were identified. Gastric ulcer recorded significant increase in gastric volume and lesion counts (p < 0.0001). Drastic changes in all biochemical parameters under investigation were observed. Protection with plant extract reversed the action of ethanol by variable degrees of improvement in comparison with the reference drug. The presence of carbohydrates and proteins that acted as a mucilage lining the stomach inner wall give its protective action. In conclusion, P. undulata subsp. undulata succeeded to have anti-ulcerative protective effect. The measured biomarkers served as a good mirror to predict gastric ulcer and the presence of carbohydrates, protein and fibers present in the plant extract acted as a mucilage lining the inner intestinal wall and protect against ethanol induced gastric ulcer. Future study will be carried out to identify the biologically active compounds responsible for plant protection against the gastric ulcer.

Phytochemical composition, protective and therapeutic effect on gastric ulcer and α-amylase inhibitory activity of Achillea biebersteinii Afan.

Three sesquiterpene lactones [two germacranolides (micranthin and sintenin) and one guaianolide (4ß,10α-dihydroxy-5ß,7ß,8ßH-guaia-1,11(13)dien-12,8α-olide)] and four derivatives of 3-methoxy flavones (santin, quercetagetin-3,6,3'-trimethyl ether, quercetagetin-3,6-dimethyl ether, and 5,7 dihydroxy 3,3',4'-trimethoxy flavone) were isolated from the ethyl acetate extract (EAE) of the aerial parts of Achillea biebersteinii Afan. (Asteraceae). Evaluation of protective and therapeutic effects of EAE against ethanol-induced gastric ulcer in rats was carried. Antiulcer activity evaluation was done through measuring ulcer indices, stomach acidity, gastric volume and lesion counts. Oxidative stress markers; malondialdehyde, glutathione and superoxide dismutase were also estimated. The work was extended to determine the histopathological assessment of the stomach. Gastric ulcer exhibited a significant elevation of the ulcer index and oxidative stress markers. The extract attenuated these increments and recorded protective and therapeutic effects against gastric ulcer. Hyperglycaemia increases the mucosal susceptibility to ulcerogenic stimuli and predisposes gastric ulceration. In vitro α-amylase inhibitory assay was applied to evaluate the post prandial antihyperglycaemia activity. The result showing that the EAE has the ability to reduce starch-induced postprandial glycaemic excursions by virtue of potent intestinal α-amylase inhibitory activity. These findings demonstrated the remarkable potential of A. biebersteinii as valuable source of antiulcer agent with post prandial hyperglycaemia lowering effect.

Flavone composition and antihypercholesterolemic and antihyperglycemic activities of Chrysanthemum coronarium L.

Five flavones were isolated from Chrysanthemum coronarium L., four of which were isolated for the first time from the genus Chrysanthemum. Two were the flavonoid aglycones 5,7-dihydroxy-3,6,4'-trimethoxyflavone (1) and scutellarin-6,7-dimethyl ether (2). A new flavonoid glycoside, apigenin-7-O-[2"(6'''-O-beta-D-acetylglucopyranosyl)]-6"-O-acetylglucopyranoside (3), along with two known ones, i. e. apigenin-7-O-(2"-O-beta-D-glucopyranosyl)-beta-D-glucopyranoside (4) and 6-methoxy quercetin-7-O-beta-D-glucopyranoside (5), were identified. Structures were elucidated by NMR and MS. The therapeutic value of petroleum ether, ethyl acetate, and methanol extracts, respectively, in rats suffering from hypercholesterolemia--as a consequence of high-fat diet-and hyperglycemia--as a consequence of hypercholesterolemia and low doses of streptozotocin--was investigated through determination of biochemical markers and histopathology. The ethyl acetate and methanol extracts showed remarkable results, followed by the petroleum ether extract.

Preliminary in vitro and in vivo evaluation of antidiabetic activity of Ducrosia anethifolia Boiss. and its linear furanocoumarins.

Aim. Ducrosia anethifolia is used as flavoring additive. There have been little detailed phytochemical reports on this genus and the antidiabetic activity of this plant is not yet evaluated. Method. Structure of compounds was deduced by spectroscopic analyses. Preliminary in vitro evaluation of the antidiabetic activity of crude extract and its furanocoumarins was carried out ( α -amylase, α -glucosidase, and ß -galactosidase). The in vivo activity was investigated by measuring some oxidative stress markers. Biomarkers of liver injury and kidney were also determined. Results. Eight linear furanocoumarins, psoralen, 5-methoxypsoralen, 8-methoxypsoralen, imperatorin, isooxypeucedanin, pabulenol, oxypeucedanin methanolate, oxypeucedanin hydrate, and 3-O-glucopyranosyl- ß -sitosterol, were isolated. All compounds were reported for the first time from the genus Ducrosia except pabulenol. The blood glucose level, liver function enzymes, total protein, lipid, and cholesterol levels were significantly normalized by extract treatment. The antioxidant markers, glucolytic, and gluconeogenic enzymes were significantly ameliorated and the elevated level of kidney biomarkers in the diabetic groups was restored. The compounds showed inhibitory activity in a concentration dependant manner. Imperatorin and 5-methoxypsoralen showed the most potent inhibiting power. Conclusion. D. anethifolia extract showed hypoglycemic, hypolipidemic, and antioxidant effect as well as ameliorating kidney function. This extract and some linear furanocoumarins exhibited carbohydrate metabolizing enzymes inhibitory effect.

Antiviral activity of Aloe hijazensis against some haemagglutinating viruses infection and its phytoconstituents.

Evaluation of the antiviral activities of flowers, flower-peduncles, leaves, and roots of Aloe hijazensis against haemagglutinating viruses of avian paramyxovirus type-1 (APMV-1), avian influenza virus type A (AI-H5N1), Newcastle disease virus (NDV), and egg-drop syndrome virus (EDSV) in specific pathogen free (SPF) chicken embryos were carried out. Extract of the flowers and leaves showed relatively higher activity than the extracts of other plant parts. Thirteen compounds were isolated from both the flowers and flower-peduncles of A. hijazensis. The isolated compounds were classified into: five anthraquinones; ziganein, ziganein-5-methyl ether, aloesaponarin I, chrysophanol, aloe-emodin, one dihydroisocoumarin; feralolide, four flavonoids; homoplantaginin, isoorientin, luteolin 7-glucuronopyranoside, isovitexin, one phenolic acid; p-coumaric acid, the anthrone; barbaloin together with aloenin. Eleven compounds were attributed to the flowers and seven to the flower-peduncles. Homoplantaginin and luteolin 7-glucuronopyranoside are reported here for the first time from Aloe spp. To the best of our knowledge, this is the first report on the chemical composition and biological activity of those plant parts.

New bioactive compounds from Aloe hijazensis.

The chemical constituents and biological activities of leaves and roots of Aloe hijazensis, collected in Saudi Arabia, are reported here for the first time. Twenty-two compounds were obtained, among them eight hydroxyquinones: aloe-emodin (1), emodin (2), chrysophanol (3), aloesaponarin II 3-methyl ether (4), ziganein (5), ziganein-5-methyl ether (6a), aloesaponarin I (7) and chrysophanein (8), the dihydro-isocoumarin feralolide (9), 4,7-dichloro-quinoline (10), the triterpene lupeol (11), the anthrone aloin (12), three aloenin derivatives, aloenin (13) ethylidene-aloenin (14), and aloenin B (15), four flavonoids, quercetin (16), kaempferol (17) cosmosiin (18) and isovitexin (19), and cinnamic acid (20) and two further analogues, caffeic acid (21) and ferulic acid (22). While 15 of the isolated compounds were found in the leaves, 12 were isolated from roots of the plant. Compounds 6a and 10 are reported as new natural constituents, while the compounds 4, 5, 8, and 18 are reported here for the first time from Aloe spp. The structures of the compounds were deduced by intensive studies of their UV, NMR, MS data and by comparison with related structures. The biological activity of plant extracts was studied against various microbial strains, and potent anti-bacterial and anti-fungal activities were found. [image omitted] [image omitted].

Humoral and cellular immune responses induced in mice by purified iridoid mixture that inhibits penetration of Schistosoma mansoni cercariae upon topical treatment of mice tails.

When tested for possible blocking effect on the cercarial, serine proteinase, elastase (CE) activity, an iridoid mixture extracted from leaves of Citharexylum quadrangular abolished 31% of the enzyme activity at final concentration 15 microg. When formulated in jojoba oil and applied to mice tails followed by infection with Schistosoma mansoni cercariae, the iridoid mixture blocked cercarial penetration and caused significant reducetion (94%; P < 0.05) in worm burden in treated mice in comparison to controls. Also, immunomodulatory effects of iridoid mixture, iridoid-treated S. mansoni worm homogenate on mice were studied by measuring IgG and IgM levels against E. coli lysates (ECL), solube S. mansoni worm antigenic preparation (SWAP) and cancer bladder homogenates (CBH) as antigens by ELISA. Cellular immune responses were studied by calculating mean percent of CD4+, CD8(+)-T, B-mesenteric lymph node cells (MLNC) and CD4+, CD8(+)-T thymocytes by direct immunofluorescence staining in treated mice as compared to untreated homogenate given mice or untreated mice. Injecting mice with serial dilutions of iridoid mixture resulted in fluctuation, peaks and troughs, in both IgG and IgM responses against the above mentioned antigens. 1st and 2nd immunizations with iridoid mixture treated homogenate resulted in significantly elevated (P < 0.05). IgM and IgG levels against the 3 used antigens in comparison with sera from control mice. Immunized mice with homogenate treated with iridoid mixture showed a significant increase (P < 0.05) in CD4+T thymocytes, a non significant increase in CD8+T thymocytes, a significant increase (P < 0.05) in CD4+T lymphocytes (MLNC) and a non significant increase in CD8+ T- and B-lymphocytes (MLNC) compared with mice immunized with untreated homogenate or non-injected normal mice.

Pharmacologically active ellagitannins from Terminalia myriocarpa.

A new ellagitannin, methyl (S)-flavogallonate (14) along with fourteen known compounds, gallic acid, methyl gallate, ethyl gallate, 2,3-di-O-[( S)-4,5,6,4',5',6'-hexahydroxybiphenyl-2,2'-diyldicarbonyl]-(alpha/beta)-D-glucopyranose (4), vitexin, isovitexin, orientin, iso-orientin, kaempferol 3-O-beta-D-rutinoside, rutin, neosaponarin, ellagic acid, flavogallonic acid (13), and (alpha/beta)-punicalagin (15) have been isolated from the leaves of Terminalia myriocarpa Heurck. Protective effect of the major and structurally related compounds 4, 13, 15 and the new compound 14 against CCl 4 -induced hepatotoxicity has been evaluated and compared, using adult male rats weighing 200-250 g. Serum levels of glutamic oxaloacetic transaminase (GOT), glutamic pyruvic transaminase (GPT), lipid peroxide and nitric oxide production were significantly increased by administration of CCl 4 to rats and then reduced significantly only by treatment with compounds 4, 14 and 15 in a dose-dependent manner. Comparison of the protective properties of these compounds showed that compound 14 is more potent than compound 15 than 4 and that compound 13 has a non-significant effect at the used two dose levels.