Synthesis, Antimicrobial and Antitubercular Activities of Some Novel Trihydroxy Benzamido Azetidin-2-one Derivatives

Purpose: To synthesize and characterize novel trihydroxy benzamido azetidin-2-one derivatives and screen them for antimicrobial and antitubercular activities.Methods: A series of novel 4-aryl-3-chloro-N-(3,4,5-trihydroxy benzamido)-2-azetidinones, 3a-o, were synthesized by reacting various Schiff bases of galloyl hydrazide, 2a-o, with chloroacetyl chloride in thepresence of dioxan and triethylamine. Schiff bases of galloyl hydrazide, 2a-o, were synthesized from galloyl hydrazide. The newly synthesized compounds were characterized by infrared spectroscopy (IR),mass spectroscopy (MS) and proton nuclear magnetic spectroscopy (1H NMR) and elemental analysis; they were also screened for in vitro antibacterial, antifungal and antitubercular activities. Ciprofloxacinand ketoconazole were used as reference standards for antibacterial and antifungal activities, respectively, while isoniazid was used as reference standard for antitubercular activity.Results: Compounds 3f, 3g and 3o with chlorophenyl group and compound 3k with 4-dimethyl amino phenyl group exhibited good antimicrobial activity. Also, compounds 3f, 3g, 3k and 3o showed antitubercular activity with minimum inhibitory concentration (MIC) values equivalent to the standard drug (isoniazid). MIC values of 3f, 3g, 3k and 3o were 0.76, 0.57.0.62 and 0.83 ìg/ml, respectively, while the MIC of isoniazid was 0.56.Conclusion: We report the successful synthesis, spectral characterization, as well as in vitro antimicrobial and antitubercular evaluation of a series of novel trihydroxy benzamido azetidin-2-one derivatives. The work shows the emergence of new antimicrobial and antitubercular compounds

Wound healing and anti-oxidant activities of the fruit pulp of limonia acidissima linn (rutaceae) in rats

Purpose: The fruits of Limonia acidissima Linn are used traditionally in India for the treatment of tumours, asthma, wounds, cardiac debility and hepatitis. The purpose of the present study was to evaluate the wound healing activity of the methanol extract of its fruit pulp (MELA) in incision, excision and dead-space wound models. Methods: Albino rats of either sex were divided into four groups, viz, wounded control, wounded rats administered standard drug, nitrofurazone (2 %), and wounded rats administered MELA 200 and 400 mg/kg, respectively. In incision wound model, wound breaking strength and epithelization period were evaluated, while in excision wound model, wound contraction was studied. In dead-space wound model, granulation tissue dry weight, hydroxyproline levels in dry granulation tissue, as well as superoxide dismutase (SOD) and catalase levels in wet granulation tissue were estimated. Granulation tissue was subjected to histopathological examination in order to determine whether there was healing by formation of collagen in the wound tissue in extract-treated animals.Results: Increased wound breaking strength, decreased epithelization period, increased wound contraction, increased granulation tissue weight and hydroxyproline concentration were observed in the various groups, compared with the control group. Also, increased activity of anti-oxidant enzymes, i.e., higher SOD and catalase levels, were seen in extract-treated groups when compared to controls. Wound healing activity was statistically significant (p < 0.001) in animals treated with 400 mg/kg of the extract. Conclusion: The methanol extract of L. acidissima possesses significant dose-dependant wound healing and anti-oxidant activities; this supports traditional claims for the plant as a wound healer.Keywords: Limonia acidissima, Wound healing, Antioxidant enzymes, Wound models, Hydroxyproline

IN VITRO CYTOTOXIC ACTIVITY OF ISOLATED COMPOUNDS FROM VIBURNUM PUNCTATUM BUCH-HAM EX D. DON

Objective: The main aim of the study was to screen the isolated compounds of Viburnum Punctatum for its in vitro anticancer activity and its percentage viability against HCT 15 (Human Colon Cancer Cells) Cell lines.Methods: Pet ether, Chloroform, Methanol and Aqueous extracts was prepared and assayed for the presence of phytochemicals. Two compounds were isolated from the methanol extract of Viburnum Punctatum by column chromatography such as ME1 (Quercetin) and ME2 (Kaemferol-3-glycoside) characterised by UV, IR, MS, 1H NMR and 13C NMR. The above isolated compounds were subjected to in vitro anticancer activity on HCT 15 cell lines was evaluated by Micro culture Tetrazolium (MTT) assay.Results: ME1 showed significant cytotoxic activity than the ME2 on HCT 15 cells with a percentage viability of 54.60 and 67.18 in the concentration of 10µg/ml and 50µg/ml respectively.Conclusion: On the basis of obtained results, ME1 and ME2 isolated from a methanolic extract of Viburnum Punctatum represent a new group of cytotoxic against HCT 15 Cell lines

Anthelmintic Activity of Extracts of Aerial Parts of Tephrosia spinosa (L.f.) Pres

Purpose: To determine the anthelmintic activity of Tephrosia spinosa (L.f.) Pres on Indian earth worms. Methods: Chloroform and methanol extracts of T. spinosa were investigated for anthelmintic activity in Indian earth worms (Pheretima posthuma) using albendazole (10 mg/ml) as standard reference and normal saline as control. The times to achieve paralysis and death of the worms were determined. Results: The aerial parts of T. spinosa (L.f.) Pres exhibited significant anthelmintic activity (p&lt;0.001) when compared with albendazole. Conclusion: Tephrosia spinosa has paralytic effect on Indian earth worms.Keywords: Tephrosia spinosa, Pheretima posthuma, Anthelmintic activity

Pharmacological In vivo test to evaluate the antidepressant activity of polyherbal formulation

The antidepressant effects of the polyherbal formulation (PF) (contain four extracts of medicinal plants namely: Nyctanthes arbortristis, Hippophae salcifolia, Ocimum tenuiflorum and Withania somnifera ) was examined by evaluating the extent of reduction of behavioural alterations and neurotransmitter in the rats stressed by forced swim test (FST). In the present study, compared with the model control group (FST), the altered behavioural parameters were attenuated significantly (P &lt; 0.05) in the group treated with the PF (100, 200 and 400 mg•kg−1), comparable with the standard drug treated group, Sertraline (10mg•kg−1). The PF and Sertraline significantly (P &lt; 0.05) increased the level of the neurotransmitter such as serotonin, dopamine, acetylcholine and noradrenalin whereas decreased the level of monoamine oxidase along with oxidant in the brain of the stressed rats. PF and Sertraline were also involved in the reduced oxidant and generated antioxidant in the stressed rats. The results indicated that polyherbal formulation exhibited significant antidepressant activity, as indicated by its ability to decrease force swim stress, induced immobility time in rats as well as restoring the biogenic amines to normal level that were altered by the swim induced stress in whole rat brain. Therefore, PF can be a potential candidate for treatment of depression as well as a potent antidepressant. However, further studies are required to substantiate the same