Urease inhibitory activity of ursane type sulfated saponins from the aerial parts of Zygophyllum fabago Linn.

Five ursane type sulfated saponins have been isolated from the aerial parts of Zygophyllum fabago Linn. (locally called Chashum). The urease inhibitory effects of these compounds have been investigated for the first time as well as their molecular docking studies have also been carried out to check the structure-activity relationship. The IC50 values of these compounds could not be found due to paucity of the samples. The molecular docking studies were performed only for the most active compound mono sodium salt of 3ß,23-di-O-sulfonyl-23-hydroxyurs-20(21)-en-28-oic acid 28-O-[ß-D-glucopyranosyl] ester (Zygofaboside A; 1).

Estimation of anti-inflammatory, antinociceptive and antioxidant activities of Arctium minus (Hill) Bernh. ssp. minus.

ETHNOPHARMACOLOGICAL RELEVANCE: Arctium minus (Hill) Bernh. ssp. minus (Asteraceae) leaves are used to alleviate rheumatic pain, against fever and sunstroke with externally application in Turkish folk medicine. AIM OF THE STUDY: To evaluate the anti-inflammatory, antinociceptive and antioxidant activities of aqueous and ethanol extracts prepared from the leaves of Arctium minus ssp. minus. MATERIALS AND METHODS: The ethanolic and aqueous extracts from the leaves of Arctium minus ssp. minus were evaluated in mice for anti-inflammatory activity using carrageenan-induced hind paw edema model and for antinociceptive activity using p-benzoquinone-induced abdominal contractions test. Moreover, the antioxidant power of the extracts has been determined by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and flow injection analysis-luminol chemiluminescence (FIA-CL). In addition, the total phenolic content in both extracts was determined with spectrophotometric method. RESULTS: Our results showed that only the ethanol extract exhibited a dose-dependent anti-inflammatory activity ranging between 11.1 and 23.6% at 200mg/kg dose as well as displayed a significant antinociceptive activity without inducing any gastric damage. Although, both extracts were shown to possess significant DPPH radical-scavenging activity, that of aqueous extract was found to have more pronounced activity. In FIA-CL system, the ethanol extract was shown to possess a significant scavenger activity against H(2)O(2) while the aqueous extract was much more potent antioxidant activity against HOCl-luminol CL than ethanol extract. CONCLUSION: According to our results, it was concluded that Arctium minus ssp. minus contains potent natural antioxidants. In this study, in vivo experimental results have also supported the folk medicinal utilization of Arctium minus ssp. minus.

Bioassay-guided isolation of anti-inflammatory and antinociceptive principles from a folk remedy, Rhododendron ponticum L. leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: Rhododendron ponticum L. (Ericaceae) is used for the treatment of inflammatory diseases and to alleviate rheumatic pain and against toothache in Turkish traditional medicine. AIM OF THE STUDY: To evaluate the anti-inflammatory and antinociceptive effects of Rhododendron ponticum leaves using in vivo models, and isolation and chemical characterization of the biologically active constituents through bioassay-guided fractionation procedures. MATERIAL AND METHODS: Carrageenan-induced hind paw edema model was used for anti-inflammatory activity and p-benzoquinone induced abdominal contractions model for the antinociceptive activity assessment. RESULTS: The ethylacetate fraction displayed marked anti-inflammatory (28.4-40.7% inhibition) and antinociceptive (50.7% inhibition) effects as compared to reference compounds. Through bioassay-guided fractionation and isolation procedures flavonol glycosides [a mixture of hyperoside and isoquercitrin (1) and quercitrin (2)] along with one flavanone glycoside [6-C-glycosylnaringenin (3)] were isolated as the active ingredients of ethylacetate extract against carrageenan-induced edema and p-benzoquinone-induced writhes and their structures were elucidated by spectral techniques. 1 and 2 also showed a significant anti-inflammatory activity against 12-O-tetradecanoyl-13-acetate (TPA)- induced mouse ear edema model. CONCLUSION: Results of the present study supported the utilization of the plant in Turkish folk medicine and revealed that flavones are the major anti-inflammatory and antinociceptive principles of the leaves.

Antioxidant activities of some Lamiaceae plant extracts.

The antioxidant activities of four Lamiaceae plants, Salvia viridis L., Salvia multicaulis Vahl, Stachys byzantina C. Koch and Eremostachys laciniata (L.) Bunge have been determined by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) as well as by flow injection analysis-luminol chemiluminescence (FIA-CL). All extracts were shown to possess a significant scavenger activity against DPPH free radical and an inhibitory effect on H2O2- or HOCl-luminol chemiluminescence. The extracts scavenged 50% of DPPH radical ranging in the following descending order: Salvia viridis > Stachys byzantina > Salvia multicaulis > Eremostachys laciniata. The most potent extract on H2O2-induced peak chemiluminescence was that of Salvia viridis and on HOCl-induced peak chemiluminescence was that of Stachys byzantina. The results concluded that the extracts have a potential source of antioxidants of natural origin.

Anti-ulcerogenic lignans from Taxus baccata L.

Four lignan type compounds, lariciresinol, taxiresinol, isolariciresinol and 3-demethyl-iso-lariciresinol, were isolated from the heartwood of Taxus baccata L. (Taxaceae) growing in Turkey through chromatographic techniques. In vivo anti-ulcerogenic potency of these compounds was investigated on ethanol-induced ulcerogenesis model in rats at two different doses, 50 and 100 mg/kg. All compounds were shown to possess significant anti-ulcerogenic activity at both doses. However, the effect of taxiresinol was the most prominent.

Bioactivity of Lignans from Taxus baccata.

Three lignan derivatives, (-)-taxiresinol (1), (-)-3'-demethylisolariciresinol-9'-hydroxyisopropylether (2) and (-)-3-demethylisolariciresinol (3), previously isolated from the heart-wood of Taxus baccata L. (Taxaceae) were investigated for cytotoxicity against the Oncology Cell Line Panel (breast, colon, ovary, prostate, lung and a normal adult bovine aortic endothelial cell line) as well as for antimicrobial activities. Besides, a chloroform-soluble portion of the ethanol extract from the heartwood of T. baccata was also tested for antimicrobial activities. Compounds 1 - 3 did not demonstrate much cytotoxic potency according to the reference drug etoposide. With the exception of compound 2, the other two lignans (1 and 3) and the chloroform extract were shown to possess antifungal activity, whereas only the chloroform extract exhibited antibacterial activity against Pseudomonas aeruginosa.

Anti-inflammatory and antinociceptive activity of taxoids and lignans from the heartwood of Taxus baccata L.

Four taxoids (taxusin, baccatin VI, baccatin III and 1beta-hydroxybaccatin I) and five lignans (lariciresinol, taxiresinol, 3'-demethylisolariciresinol-9'-hydroxyisopropylether, isolariciresinol and 3-demethylisolariciresinol) were isolated from the heartwood of Taxus baccata L. (Taxaceae) growing in Turkey through chromatographic techniques. In vivo anti-inflammatory and antinociceptive activity of these compounds were investigated. All the compounds were shown to possess significant antinociceptive activity against p-benzoquinone-induced abdominal contractions, while only lignan derivatives significantly inhibited carrageenan-induced hind paw edema in mice.

Anti-inflammatory and antinociceptive activity assessment of plants used as remedy in Turkish folk medicine.

Ethanolic and aqueous extracts from seven plant species used in Turkish traditional medicine were evaluated for in vivo anti-inflammatory and antinociceptive activities; Helleborus orientalis Lam. roots and herbs, Juglans regia L. leaves, Laurocerasus officinalis Roemer leaves, Nerium oleander L. dried and fresh flowers and leaves, Rhododendron ponticum L. leaves, Rubus hirtus Walds. et Kit aerial parts and Rubus sanctus Schreber aerial parts and roots. All the plant extracts, except the aqueous extract of Rubus hirtus, were shown to possess significant antinociceptive activity in varying degrees against p-benzoquinone-induced abdominal contractions in mice. However, only the ethanolic extracts of Helleborus orientalis roots, Juglans regia leaves, Laurocerasus officinalis leaves, Nerium oleander dried and fresh flowers, and Rhododendron ponticum leaves exhibited potent anti-inflammatory activity against carrageenan-induced hind paw edema model in mice without inducing any gastric damage. Results of the present study confirmed the folkloric claim that all the selected materials to possess potent antinociceptive and anti-inflammatory activity.