Esra Küpeli

A comparative study on the anti-inflammatory, antinociceptive and antipyretic effects of isoquinoline alkaloids from the roots of Turkish Berberis species

Roots and barks of various Berberis species are used as folk remedy for the treatment of various inflammatory diseases such as lumbago, rheumatism and to reduce fever. Six isoquinoline alkaloids namely berberine, berbamine, palmatine, oxyacanthine, magnoflorine, and columbamine were isolated as the main components of alkaloidal fraction from the roots of Turkish Berberis species and effects were studied using various in vivo models in mice. All alkaloids inhibited inflammations in varying degrees, among them berberine, berbamine and palmatine were shown to possess significant and dose-dependent inhibitory activity against serotonin-induced hind paw oedema both on oral and topical applications and acetic acid-induced increase in vascular permeability on oral administration. Moreover, these three alkaloids were also shown to possess dose-dependent antinociceptive activity, which assessed by using the model based on the inhibition of p-benzoquinone-induced writhing movements as well as antipyretic activity on FCA-induced increased rectal temperature on subacute administration. However, all alkaloids induced gastric lesions in varying degrees.

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.

Berberis crataegina DC. root exhibits potent anti-inflammatory, analgesic and febrifuge effects in mice and rats

Extracts obtained from the roots and barks of various Berberis species are used as folk remedy worldwide for the treatment of various inflammatory ailments including lumbago, rheumatism and to reduce fever. Effects of the extracts and fractions from the roots of Berberis crataegina DC. (Berberidaceae) were studied using various in vivo models of inflammation in mice and rats and observed potent inhibitory activity against carrageenan- and serotonin-induced hind paw oedema, acetic acid-induced increased vascular permeability, castor oil-induced diarrhoea, and Freunds complete adjuvant-induced (FCA) arthritis models. Through bioassay-guided fractionation berberine was isolated as the main active ingredient. Moreover, a dose-dependent analgesic activity was determined, which assessed by using the model based on the inhibition of acetic acid-induced writhing reflexes, as well as antipyretic activity on FCA-induced increased body temperature. Acute and subchronic toxicity studies were also performed.

Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives.

In this study new 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted benzal)hydrazone V derivatives were synthesized as analgesic and anti-inflammatory agents. The structures of compounds were elucidated by spectral and elemental analysis. Compounds Va, Vb and Vc were exhibited more potent analgesic activity than ASA. Also these derivatives demonstrated anti-inflammatory activity as well as standard compound indomethacin. Side effects of the compounds were examined on gastric mucosa. None of the compounds showed gastric ulcerogenic effect compared with reference nonsteroidal anti-inflammatory drugs (NSAIDs). On the basis of available data, the structure-activity relationship of V derivatives was also discussed.

Evaluation of in vivo Biological Activity Profile of Isoorientin

Anti-nociceptive, anti-inflammatory and gastroprotective activities of the known C-glycosyl flavonoid, isoorientin, were studied in rats and mice. For the anti-nociceptive activity assessment the p-benzoquinone-induced writing test, for the anti-inflammatory activity the carrageenan-induced hind paw edema model in mice, and for the gastroprotective activity the EtOH-induced ulcerogenesis model in rats were used. Isoorientin was shown to possess significant anti-nociceptive and anti-inflammatory activities at 15 mg/kg and 30 mg/kg doses, without inducing any apparent acute toxicity as well as gastric damage. However, the compound did not possess any significant gastroprotective activity against EtOH-induced ulcerogenesis.

Anti-inflammatory and antinociceptive activity of flavonoids isolated from Viscum album ssp. album.

Abstract Viscum album L. has been used in the indigenous systems of medicine for treatment of headache and some inflammatory diseases. In order to evaluate this information, antinociceptive and anti-inflammatory activities of the five flavonoids (5,7-dimethoxy naringenin or 4′,6′- dimethoxy chalcononaringenin) derivatives, isolated from the ethyl acetate fraction of the extract from V. album ssp. album, were investigated, namely 5,7-dimethoxy-flavanone-4′-O- β-ᴅ-glucopyranoside (1), 2′-hydroxy-4′,6′-dimethoxy-chalcone-4-O-β-ᴅ-glucopyranoside (2), 5,7-dimethoxy-flavanone-4′-O-[2″-O-(5‴-O-trans-cinnamoyl)-β-ᴅ-apiofuranosyl]-β-ᴅ-glucopyranoside (3), 2′-hydroxy-4′,6′-dimethoxy-chalcone-4-O-[2″-O-(5‴-O-trans-cinnamoyl)-β-ᴅ-apiofuranosyl]- β-ᴅ-glucopyranoside (4), 5,7-dimethoxy-flavanone-4′-O-[β-d-apiofuranosyl- (152)]-β-ᴅ-glucopyranoside (5). For the antinociceptive activity assessment the p-benzoquinone- induced writhing test and for the anti-inflammatory activity the carrageenan-induced hind paw edema model in mice were used. The ethyl acetate fraction in a dose of 250 mg/kg as well as compounds 2 and 5 in a 30 mg/kg dose were shown to possess remarkable antinociceptive and anti-inflammatory activities per os without inducing any apparent acute toxicity as well as gastric damage

Synthesis, Analgesic, and Anti-Inflammatory Activities of [6-(3,5-Dimethyl-4-Chloropyrazole-1-yl)-3(2H)-Pyridazinon-2-yl]Acetamides

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4-chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analgesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.

In vivo Anti-Inflammatory and Antinociceptive Activity Evaluation of Phenolic Compounds from Sideritis stricta

An acetone extract obtained from aerial parts of S. stricta Boiss. & Heldr. apud Bentham, its fractions and phenolic compounds were investigated for their in vivo anti-inflammatory and antinociceptive activities. For the anti-inflammatory activity and for the antinociceptive activity assessment, carrageenan-induced hind paw edema and p-benzoquinone-induced abdominal constriction tests were used, respectively. The acetone extract of the plant and its phenolic fraction exhibited potent inhibitory activity against both bioassay models in mice. From the active phenolic fraction a well-known phenylethanoid glycoside, verbascoside (acteoside) (1), and two flavonoid glycosides, isoscutellarein 7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-β-D-glucopyranoside (2) and isoscutellarein 7-O-[6‴-O-acetyl-β-D-allopyranosyl-(1→2)]-6‴-O-acetyl-β-d-glucopyranoside (3), were isolated. During phytochemical studies we also isolated a methoxyflavone, xanthomicrol (4), from the non-polar fraction. The structures of the isolated compounds were established by spectroscopic evidence (UV, IR, 1D- and 2D-NMR, MS). Although antinociceptive and anti-inflammatory activities of the phenolic components were found not significant in the statistical analysis, compounds 1 to 3 showed a notable activity without inducing any apparent acute toxicity as well as gastric damage. Furthermore, a mixture of flavonoid glycosides (2 + 3) exhibited a significant inhibitory effect in both models at a higher dose

Evaluation of Some Plants Used in Turkish Folk Medicine for Their Anti-inflammatory and Antinociceptive Activities

Abstract Ethanol and aqueous extracts obtained from 11 plant species from 11 families selected based on their use in Turkish folk medicine, including Isatis glauca. Aucher x Boiss. subsp glauca. (herb) (Brassicaceae), Tamus communis. L. (herb and root) (Dioscoreaceae), Rumex crispus. L. (herb) (Polygonaceae), Daphne oleoides. Schreber (aerial parts) (Thymeleaceae), Laurus nobilis. L. (leaves and seeds) (Lauraceae), Ranunculus tricophyllus. Chaix (herb) (Ranunculaceae), Anchusa azurea. Miller var. azurea. (herb) (Boraginaceae), Calluna vulgaris. L. (herb) (Ericaceae), Prunella vulgaris. L. (herb) (Lamiaceae), Scabiosa rotata. Bieb. (herb) (Dipsacaceae), and Arceuthobium oxycedri. (DC.) Bieb. (herb) (Loranthaceae), were evaluated for their in vivo. anti-inflammatory and antinociceptive activities. Among the plant extracts studied, the ethanol extracts of Laurus nobilis. seed and Calluna vulgaris. herb and the aqueous and ethanol extracts of Arceuthobium oxycedri. herb displayed significant anti-inflammatory activity using carrageenan-induced hind paw edema model in mice without inducing any gastric damage. The ethanol extracts of Isatis glauca. subsp. glauca., Calluna vulgaris., Laurus nobilis. (seeds) as well as the aqueous and ethanol extracts of Arceuthobium oxycedri. were also shown to possess significant antinociceptive activity in varying degrees against p.-benzoquinone-induced abdominal contraction test in mice.

Anti-Inflammatory and Antinociceptive Potential of Major Phenolics from Verbascum salviifolium Boiss.

The potential effects of flavonoids, phenylethanoid and neolignan glycosides from the aerial parts of Verbascum salviifolium Boiss. were studied in the p-benzoquinone-induced writhing reflex, for the assessment of the antinociceptive activity, and in carrageenan- and PGE1- induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced ear edema models in mice, for the assessment of the anti-inflammatory activity. Through bioassay-guided fractionation and isolation procedures ten compounds from the aqueous extract of the plant, luteolin 7-O-glucoside (1), luteolin 3′-O-glucoside (2), apigenin 7-O-glucoside (3), chrysoeriol 7-O-glucoside (4), β-hydroxyacteoside (5), martynoside (6), forsythoside B (7), angoroside A (8), dehydrodiconiferyl alcohol-9-O′-d-glucopyranoside (9) and dehydrodiconiferyl alcohol- 9′-O-β-d-glucopyranoside (10), were isolated and their structures were elucidated by spectral techniques. Results have shown that 1, 2, 3 and 5 significantly inhibited carrageenaninduced paw edema at a 200 mg/kg dose, while 1, 2 and 5 also displayed anti-inflammatory activity against the PGE1-induced hind paw edema model. However, all the compounds showed no effect in the TPA-induced ear edema model. The compounds 1 and 2 also exhibited significant antinociceptive activity