Nephrotoxic effects of Valeriana wallichii

Aminoglycosides are the commonly used antibiotics against Gram negative bacteria. Their clinical applications are limited due to nephrotoxic side effects. Therefore, the current study was undertaken in an attempt to increase the use of these drugs without causing nephrotoxicity by exploring the nephroprotective effects of a medicinal plant with high flavonoid contents and strong antioxidant properties, namely Valeriana wallichii. A daily dose of 200mg/kg of the extract derived from V. wallichii was employed for a period of three weeks. The results obtained revealed that co-therapy of extract with gentamicin protected some changes in renal functions; however, failed to provide a complete protection as assessed by biochemical, physiological and histological parameters. It can be concluded from the current findings that V. wallichii failed to deliver protective effects against gentamicin induced renal damage in spite of strong flavonoid contents and antioxidant properties

Isolation of flavonoides from Artemisia macrocephala anticholinesterase activity: isolation, characterization and its in vitro anticholinesterse activity supported by molecular docking

In this study the flavonoids isolated from Artemisia macrocephala were screened out for anticholinesterase activity. The isolated flvanoids were characterized by HNMR, NOESY, COSY, HMBC, HSQC and mass spectroscopy. The compounds [1-4] in appropriate quantities were isolated from chloroform fraction using gravity column chromatography by eluting ethyl acetate/n-hexane solvent system. The flavonoids were characterized and resulted in the form of mono substituted methoxy flavones to tri substituted flavones. Ellman's assay techniques were used to find out enzyme inhibition. Operating environment [MOE] software was used for molecular docking studies. Compounds [1], [2] and [3] showed 88.42+/-2.76, 84.50+/-1.60 and 90.16+/-2.98 percent inhibition of the acetyl cholinesterase [AChE] respectively at 1000µg/mL concentrations with IC50 value 165, 60, 65µg/mL respectively which were comparable to that of standard galanthamine. While for butyryl cholinesterase [BChE], [1], [2] and [3] showed 91.63+/-4.32, 81.03+/-3.53 and 87.69+/-2.84 percent inhibitions respectively at 1mg/mL as compared to the standard galanthamine which caused 96.50+/-2.41 percent inhibition at the same concentration. Whereas, compound [4] exhibited moderate activity for both the enzymes. Molecular docking studies confirmed the experimental AChE and BChE inhibitory activities of the test samples by their virtue of multiple interactions with target enzymes. The results confirm that the specie has biologically active constituents that are more useful for the management of several neurodegenerative ailments like ataxia, Parkinson's disease, Alzeimer's disease and some other types of dementia

Parasiticidal and brine shrimp cytotoxicity potential of crude methanolic extract of rind of Punica granatum Linn against round worms and tape worms

Rind of Punica granatum is traditionally used for anthelmintic purposes. The current work describes the possible anthelmintic activity of crude methanolic extract of Punica granatum [Pg. Cr] against round worms [Ascaridia galli] and the tape worms [Raillietina spiralis]. Brine shrimp cytotoxicity is also performed. Brine shrimp cytotoxic activity was tested using different concentrations [1000µg/ml, 100µg/ml and 10µg/ml] of Pg.Cr. In vitro anthelmintic activity of Pg. Cr was determined against the parasites using albendazole and piperazine citrate as st and ard anthelmintic drugs in concentration 10 mg/ml. LC50 value for Brine shrimp cytotoxicity was 189.44+/-28µg/ml. In test concentration of 40mg/ml of the Pg. Cr, Raillietina spiralis was paralyzed in 23 minutes. However, for parasiticidal activity [death of the parasite], it took less time [40 minutes] as compared to st and ard Albendazole. Time taken for death of the parasite Raillietina spiralis, in concentration 40 mg /ml, is 40 min. While st and ard drugs took more time to kill the Raillietina spiralis. Pg. Cr took 19 minutes to paralyze the Ascaridia galli at concentration 40 mg/ml whereas; it took 48 minutes for to kill the parasite Ascaridia galli. The current work confirms the traditional use of rind of Punica granatum as anthelmintic against Raillietina spiralis and Ascaridia galli. Results of brine shrimp cytotoxicity assay warrant for the isolation of cytotoxic compounds. List of abbreviation: Pg. Cr = Crude methanolic extract of Punica granatum

Acute toxicity and antispasmodic activities of achillea wilhelmsii C. Koch

Since Achillea wilhelmsii is used as antispasmodic in traditional medicine, we conducted our current work to investigate its rationale on scientific grounds. Acute toxicity studies of crude methanol extract of Achillea wilhelmsii [Aw. CMeOH] is also performed. Effect of Aw. CMeOH and its fractions were tested on isolated sections of rabbits' jejunum at test concentrations 0.01, 0.03, 1.0, 3.0, 5.0 and 10mg/ml. The test extracts, in similar concentrations, were also tested on KCl-induced contractions. Calcium chloride curves were constructed for those fractions which relaxed KCl induced contractions in the absence and presence of the test samples to investigate its possible mode of action through calcium channels. Aw. CMeOH tested positive for flavonoids, saponins, tannins, glycosides, terpenoids, sterols, phenols, carbohydrates and proteins. LD[50] for acute toxicity studies is 2707 +/- 12.6 mg/kg. Mean EC[50] values for Aw. CMeOH on spontaneous and KCl-induced contractions are 3.41 +/- 0.18 [2.56-3.8, n=6] and 0.68 +/- 0.05 [0.6-0.85, n=6] mg/ml, respectively. Respective EC[50] values for n-hexane fraction on spontaneous and KCl-induced contractions are 3.06 +/- 0.08 [2.8-3.3, n=6] and 1.68 +/- 0.8 [1.4-1.9, n=6] mg/ml, respectively. Corresponding EC[50] [mg/ml] values for chloroformic, ethylacetate and aqueous fractions of Achillea wilhelmsii on spontaneous rabbits' jejunum preparations are 4.8 +/- 0.2 [4.41-5.63, n=6], 5.07 +/- 0.15 [4.7-5.58, n=6] and 5.2 +/- 0.13 [4.91-5.64, n=4], respectively. Constructing calcium chloride curves, in the presence of 0.1 mg/ml of Aw. CMeOH, mean EC[50] value [log molar [Ca[++]]] is-1.98 +/- 0.03 [-1.89-2.05, n=6] vs. control EC50 [log molar [Ca[++]]]-2.41 +/- 0.02 [-2.32-2.44, n=6]. Mean EC50 value [log molar [Ca[++]]] for 0.3 mg/ml n-hexane fraction is-1.76 +/- 0.05 [-1.70 -1.93, n=6] vs. control EC50 [log molar [Ca[++]]] value-2.18 +/- 0.07 [-2.0-2.46, n=6]. While in the presence of chloroformic fraction [3 mg/ml], mean EC50 [log molar [Ca[++]]] value is -2.4 +/- 0.1 [-2.78 - 2.9, n=6] vs. control EC50 [log molar [Ca[++]]] value-2.70 +/- 0.05 [-2.5-2.8, n=6]. Mean EC50 value [log molar [Ca[++]]] for ethyl acetate fraction [1 mg/ml] is-1.94 +/- 0.07 [-1.75-2.05, n=6] vs. control EC50 [log molar [Ca[++]]] value-2.69 +/- 0.04 [-2.57-2.79, n=6]. Mean EC50 [log molar [Ca[++]]] value for residual aqueous fraction [3 mg/ml] is-1.8 +/- 0.3 [-1.71-1.84, n=6] vs. control EC50 [log molar [Ca++]] -2.6 +/- 0.04 [-2.59-2.76, n=6]. Whereas, the verapamil [0.1 micro M] EC[50] value [log molar [Ca[++]]] is-1.7 +/- 0.1 [-1.6-1.8, n=6] vs. control EC50 value [log molar [Ca[++]]]- 2.4 +/- 0.09 [-2.3-2.47, n=6]. The present research work confirms that the intestinal relaxation effect of Achillea wilhelmsii is supporting its traditional use as antispasmodic. The plant species can be a source for calcium antagonist[s], which can preferably be isolated from n-hexane fraction