Anti-ulcerogenic activity and isolation of the active principles from Sambucus ebulus L. leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: Sambucus ebulus L. has a very prominent place in Turkish folk medicine. Leaves of the plant are practiced externally to relieve rheumatic pain, to treat abscess, for wound healing and internally against hemorrhoids and stomachache. In a previous work, aqueous extract of the leaves was shown to possess potent antiulcerogenic activity on water immersion and immobilization-induced stress ulcer model in rats. This study aims to investigate the antiulcerogenic activity profile of the plant on various in vivo peptic ulcer models and gastric biochemical parameters and through bioassay-guided processing to isolate the active constituent (s) and to elucidate its structure. MATERIALS AND METHODS: Among the subextracts obtained by successive solvent extractions from the MeOH extract of the leaves, the butanol subextract exerted significant antiulcerogenic activity against water-immersion and immobilization-induced stress ulcer model in rats as the bioassay model. This subextract was then subjected to successive chemical separation techniques (precipitation, column chromatography based on ion-exchange, silica gel and sephadex) and the activity of each fraction/subfraction was tested using the same bioassay model. After determination of active principles, further studies were performed on the active subextract by using various in vivo test models (ethanol-, serotonin-, pyloric ligation-induced ulcerogenesis) in rats as well as biochemical methods for the evaluation of antiulcerogenic potential. RESULTS: Bioassay-guided fractionation procedures yielded two flavonol glycosides as the active antiulcerogenic principles. The structures of these compounds were elucidated as isorhamnetin-3-O-monoglycoside and quercetin-3-O-monoglycoside by using (1)H, (13)C-NMR, and FAB-MS techniques. CONCLUSION: This study has proven the folkloric use of Sambucus ebulus leaves for the treatment of gastric ailments in Turkish folk medicine. The antiulcerogenic activity of the two flavonol glycosides isolated in the present study was not previously reported elsewhere.

In vitro isoflavonoid production and analysis in natural tetraploid Trifolium pratense (red clover) calluses

Isoflavones are polyphenolic phytoestrogens, predominantly found in leguminous plants. Trifolium pratense L., Fabaceae (red clover), is rich in isoflavones that possess estrogenic activity due to their similar molecular structure and effectiveness in preventing health conditions such as menopause, osteoporosis, cardiovascular disease, hypertension and hormone-dependent cancers. In this study, presence and amount of various phytoestrogens in the tetraploid plant and in the calluses derived from the plants were investigated. Calluses were generated from explants obtained from natural tetraploid T. pratense seedlings. The best callus formation was obtained from hypocotyl explants cultured in Phillips Collins and Gamborg B5 media containing different plant growth regulators. Flowers of plants and calluses were analysed for formononetin, biochanin A, genistein and daidzein contents using HPLC. In HPLC analysis, high levels of formononetin (0.249 µg/mg) were determined in natural tetraploid T. pratense flowers in addition to genistein and biochanin A. In calluses, highest isoflavone content (1.15 µg/mg formononetin) was observed in modified Gamborg B5 medium. Biochanin A content of calluses and the plant were found to be nearly the same. But formononetin and genistein contents of the calluses in this medium were found to be respectively 4.62 and 21.39 folds higher than the tetraploid plant.

An in vitro perspective to cholinesterase inhibitory and antioxidant activity of five Gentiana species and Gentianella caucasea.

The dichloromethane (DCM), ethyl acetate (EtOAc), and methanol extracts from the leaves, roots, and flowers of the five species of Gentiana (Gentiana asclepiadea, Gentiana cruciata, Gentiana olivieri, Gentiana septemfida, and Gentiana verna) and Gentianella caucasea were investigated for their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and antioxidant effect using 2,2-diphenyl-1-picrylhydrazyl radical scavenging, metal-chelation capacity, and ferric-reducing antioxidant power assays. Total phenol and flavonoid contents of the extracts were determined spectrophotometrically. The presence of some characteristic compounds found in Gentiana species (gentiopicroside, swertiamarin, isoorientin, isovitexin and vitexin) was analyzed in the extracts by thin layer chromatography. The flower DCM extract of G. verna exerted the highest inhibition against AChE (53.65 ± 1.03%), whereas the root EtOAc extract of G. cruciata was the most effective in BChE inhibition assay (50.72 ± 0.75%) at 100 µg ml⁻¹. The extracts of G. verna were also found to be more active in the antioxidant tests.

Anatomical investigations on root, stem, and leaf of Gentiana olivieri Griseb.

BACKGROUND: Gentiana olivieri Griseb. (Afat) (Gentianaceae), which has many bioactive compounds is used as antidiabetic, hepatoprotective, digestive aid, antidepressant, and antianemic in traditional medicine. MATERIALS AND METHODS: Root, stem, and leaf sections of G. olivieri were taken free hand or by sliding microtome and examined on light microscope. RESULTS: Anatomical characters of the species were observed to be similar to the usual features of Gentianaceae anatomy. CONCLUSION: Intraxylary phloem, which was primarily the distinguishing feature between Gentianoideae and Menyanthoideae sub-families was observed in G. olivieri roots.

Exploring the wound healing activity of Arnebia densiflora (Nordm.) Ledeb. by in vivo models.

ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Arnebia densiflora (Nordm.) Ledeb. (Boraginaceae), which is an endemic plant for Turkey, have been used for healing of wounds in folk medicine. The extract of the roots in olive oil and mostly the root barks was applied onto open wounds for rapid healing. AIM OF THE STUDY: To evaluate the wound healing activity of the roots, extracts were prepared with different solvents; hexane, chloroform, ethyl acetate and methanol, respectively from the roots of Arnebia densiflora. MATERIALS AND METHODS: Incision by using tensiometer and excision models were employed on mice and rats. RESULTS: Significant wound healing activity was observed with the ointment formulation prepared by using hexane extract at 1% concentration on the mentioned models. The results of histopathological examination supported the outcome of both incision and excision wound models. The wound healing effect was comparatively evaluated with a reference ointment Madecassol. CONCLUSION: The experimental data demonstrated that Arnebia densiflora displayed remarkable wound healing activity.

Antiviral and antimicrobial assessment of some selected flavonoids.

In the current study, the results of antibacterial, antifungal, and antiviral activity tests of four flavonoid derivatives, scandenone (1), tiliroside (2), quercetin-3,7-O-alpha-L-dirhamnoside (3), and kaempferol-3,7-O-alpha-L-dirhamnoside (4), are presented. Antibacterial and antifungal activities of these compounds were tested against Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Klebsiella pneumoniae, Acinetobacter baumannii, Staphylococcus aureus, Bacillus subtilis, and Enterococcus faecalis, as well as the fungus Candida albicans by a micro-dilution method. On the other hand, both DNA virus Herpes simplex (HSV) and RNA virus Parainfluenza-3 (PI-3) were employed for antiviral assessment of the compounds using Madin-Darby bovine kidney and Vero cell lines. According to our data, all of the compounds tested were found to be quite active against S. aureus and E. faecalis with MIC values of 0.5 microg/ml, followed by E. coli (2 microg/ml), K. pneumoniae (4 microg/ml), A. baumannii (8 micro/g/ml), and B. subtilis (8 microg/ml), while they inhibited C. albicans at 1 microg/ml as potent as ketoconazole. However, only compound 3 displayed an antiviral effect towards PI-3 in the range of 8-32 microg/ml of inhibitory concentration for cytopathogenic effect (CPE).

Anti-inflammatory and antinociceptive potential of Maclura pomifera (Rafin.) Schneider fruit extracts and its major isoflavonoids, scandenone and auriculasin.

The aqueous, ethanolic and chloroform extracts and two prenylated isoflavones: scandenone (I) and auriculasin (II), isolated from the fruits of Maclura pomifera (Rafin.) Schneider, were investigated for their in vivo anti-inflammatory and antinociceptive activity. For the anti-inflammatory activity, both carrageenan-induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models and for the antinociceptive activity, p-benzoquinone-induced abdominal constriction test were used. Scandenone, the chloroform and the ethanolic extracts were shown to possess antinociceptive activity and anti-inflammatory activity on carrageenan-induced hind paw edema model at 100 mg/kg dose. The same compound and the extract were also found to be highly active in (TPA)-induced mouse ear edema model whereas auriculasin and the H(2)O extract showed to be inactive in all of the assays.

Flavonoids with antinociceptive and anti-inflammatory activities from the leaves of Tilia argentea (silver linden).

Silver linden, Tilia argentea Desf. ex DC (Tiliaceae) leaves are used in the treatment of common cold and bronchitis. In order to evaluate this information, antinociceptive and anti-inflammatory activities of the two main flavonoid glycosides: kaempferol-3,7-O-alpha-dirhamnoside and quercetin-3,7-O-alpha-dirhamnoside isolated from the leaves, were investigated. For the antinociceptive activity, p-benzoquinone-induced writhing test and for the anti-inflammatory activity, carrageenan-induced hind paw edema model in mice were used. Both compounds were shown to possess potent antinociceptive and anti-inflammatory activity at 50 mg/kg dose, per os, without inducing any apparent acute toxicity as well as gastric damage.