A novel polyherbal formulation containing thymoquinone attenuates carbon tetrachloride-induced hepatorenal injury in a rat model

Objective: To evaluate a novel polyherbal formulation (BSVT) containing the standardized extracts from the leaves of Boerhavia diffusa, Solidago virgaurea, Vitex negundo, and thymoquinone in CCl4 induced hepatorenal toxicity in rats. Methods: A total of 36 rats were divided into six groups including normal control, CCl4 (2 mL/kg, i.p.), CCl4 (2 mL/kg, i.p.) + Cystone? (750 mg/kg p.o.), CCl4 (2 mL/kg, i.p.) + BSVT (25 mg/kg, p.o.), CCl4 (2 mL/kg, i.p.) + BSVT (50 mg/kg, p.o.), and CCl4 (2 mL/kg, i.p.) + BSVT (100 mg/kg, p.o.). All treatments were given for four weeks. Serum levels of aspartate transaminase, alanine transaminase, alkaline phosphatase, cholesterol, total protein, serum urea, blood urea nitrogen and creatinine were assessed. Superoxide dismutase, malondialdehyde, and glutathione peroxidase were evaluated in tissue homogenate. The histopathological study of liver and kidney tissues was also done. Results: Aspartate transaminase, alanine transaminase, alkaline phosphatase, cholesterol, serum urea, blood urea nitrogen and creatinine were significantly elevated (P<0.001) while total protein was considerably reduced in the CCl4 group as compared to the normal control (P<0.001), which indicated hepatorenal toxicity. In addition, superoxide dismutase and glutathione peroxidase activities were significantly decreased (P<0.001) while malondialdehyde levels were increased markedly (P<0.001). Treatment with BSVT formulation recovered these parameters towards a normal level in a dose-dependent manner. Conclusions: BSVT formulation ameliorates the hepatorenal toxicity in a dose-dependent manner. Furthermore, clinical studies are required to confirm its efficacy.

Studies on new substituted pyridazinones: synthesis and biological evaluation

We report herein the synthesis and pharmacological evaluation of a new series of 6-aryl-2-(imidazol-1-yl/1,2,4-triazol-1-yl)-2-methyl-4,5-dihydro-(2H)-pyridazin-3-one (3a-j) as potential anticonvulsant and antitubercular agents. The title compounds were prepared by reacting 6-aryl-4,5-dihydro-(2H)-pyridazin-3-one (2a-e) with formaldehyde and secondary cyclic amine imidazole or 1,2,4-triazole as per Mannich reaction. Anticonvulsant activity of pyridazinone derivatives was tested at 50 mg.kg-1 dose level against maximal electroshock (MES), isoniazid (INH, 250 mg.kg-1) and pentylenetetrazole (PTZ at 80 mg.kg-1) induced seizure methods. Phenytoin sodium (25 mg.kg-1) and sodium valproate (100 mg.kg-1) were used as reference drugs for comparison purpose. In-vitro antitubercular activity was tested by Microplate Alamar Blue assay (MABA) method and the results were compared with clinically used antitubercular agents such as INH, Pyrazinamide (PZA) and Streptomycin (STM). None of the screened compounds were found to be neurotoxic at a dose level of 100 mg.kg-1. All the screened compounds (3a-j) significantly reduced the MES, INH and PTZ induced convulsions and thus showed good anticonvulsant activity. The minimum inhibitory concentration (MIC) of the title compounds against M. tuberculosis ranged from 1.6 µg/mL to 6.25 µg/mL in comparison to INH, PZA (3.125 µg/mL) and STM (6.25 µg/mL) which indicated good antitubercular activity.

Phytochemistry and potential therapeutic actions of Boswellic acids:A mini-review

The pentacyclic triterpenic acids isolated from the oleo gum resin of various Boswellia species are collectively called as Boswellic acids (BA). The oleo gum resin obtained from Indian variety i.e. Boswellia serrata (Family–Burseraceae) is commonly known as Salai guggal. The resin fraction of Salai guggal is rich in Boswellic acids and its essential oil is composed of a mixture of mono, di and sesquiterpenes while gum fraction chiefly con-tains pentose and hexose sugars. This oleo-gum resin is quite popular among traditional practitioners of traditional Chinese and Indian Systems of medicine owing to their wide range of useful biological properties such as anti-inflammatory, anti-arthritic, anti-rheumatic, anti-diarrheal, anti-hyperlipidemic, anti-asthmatic, anti-cancer, anti-microbial anti-fungal, anti-complementary and analgesic activity, etc. It has been used as a herbal medicine since the prehistoric time to cure acute and chronic ailments including in-flammatory diseases. Phytochemical investigation of this herbal medicine lead to iden-tification of Boswellic acids which are found to be novel, potent, specific anti-inflammatory agents due to non-redox inhibition of 5-lipoxygenase (5-LO) enzyme. However, the other important targets of Boswellic acids also include topoisomerases, angiogenesis, and cytochrome p450 enzymes. This review is a sincere attempt to discuss and present the current status of therapeutic potential, phytochemical as well as phar-macological profile of Boswellic acids primarily obtained from B. serrata.

Synthesis and in vivo Anti-inflammatory and Analgesic activities of Oxadiazoles clubbed with Benzothiazole nucleus.

The aim of the present work is to synthesize and evaluate the anti-inflammatory and analgesic activity of 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3-benzathiazole derivatives. In the present investigation, a series of 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3-benzathiazole derivatives (3a1-3a9) were synthesized by condensing benzothiazolyl carboxyhydrazide and appropriate aryl acids in the presence of phosphorous oxychloride. Structures of synthesized compounds were established on the basis of IR, 1H NMR, and Mass spectroscopy. All the synthesized compounds were screened for their in-vivo anti-inflammatory and analgesic activities at the dose of 50 mg/kg and 10 mg/kg po. The biological result shows that some compounds were good in their anti-inflammatory and analgesic actions.

Pharmacognostical and phytochemical analysis of Lepidium sativum L. seeds.

Objective of the present study was to carry out the physicochemical and phytochemicals standardization of Lepidium sativum Lseeds to establish the standard pharmacognostical parameters of this valuable medicinal plant. Many standardization parameters of Lepidium sativum were analyzed. Standard method was adopted for the preliminary phytochemicals screening. Analysis of pesticides residues, aflatoxin & heavy metals were also performed. The sections of seeds were prepared for quantitative microscopic parameters. The air dried powdered plant material was subjected for determination of physicochemical standardizations like ash value, Extractive value and fluorescence nature of the powder drug using light of short and longwavelength of 254nm and 366nm respectively. Phytochemical screening was performed for the identification of phytoconstituents in the plant which was helpful in the development of analytical profile. The morphological and microscopic examinations of drug were revealed the presence of endosperm cell which are polygonal in shape and contain alerone grains and oil droplet, cell of testa, yellow colouring matter and starch grains. Preliminary phytochemical screening showed the presence of carbohydrates, phenolic compounds, flavonoids, alkaloids, proteins, saponins and lipids in the drug extract and flourescence nature of drug was confirmed by fluorescence analysis in different solvent. Concentrations of heavy metals,ash value and extractive value were determined and found within acceptable Pharmacopoeial limits. Pesticides residues and aflatoxins were also determined but not detected in the tested samples. The physicochemical and phytochemical standards which are outcome of this research may be utilized as substantial data for identification and standardization of L. sativum seed.

Synthesis and in vivo Anti-inflammatory and Analgesic activities of Oxadiazoles clubbed with Benzothiazole nucleus.

The aim of the present work is to synthesize and evaluate the anti-inflammatory and analgesic activity of 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3-benzathiazole derivatives. In the present investigation, a series of 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3-benzathiazole derivatives (3a1-3a9) were synthesized by condensing benzothiazolyl carboxyhydrazide and appropriate aryl acids in the presence of phosphorous oxychloride. Structures of synthesized compounds were established on the basis of IR, 1H NMR, and Mass spectroscopy. All the synthesized compounds were screened for their in-vivo anti-inflammatory and analgesic activities at the dose of 50 mg/kg and 10 mg/kg po. The biological result shows that some compounds were good in their anti-inflammatory and analgesic actions.

Pharmacognostical and phytochemical analysis of Lepidium sativum L. seeds.

Objective of the present study was to carry out the physicochemical and phytochemicals standardization of Lepidium sativum L seeds to establish the standard pharmacognostical parameters of this valuable medicinal plant. Many standardization parameters of Lepidium sativum were analyzed. Standard method was adopted for the preliminary phytochemicals screening. Analysis of pesticides residues, aflatoxin & heavy metals were also performed. The sections of seeds were prepared for quantitative microscopic parameters. The air dried powdered plant material was subjected for determination of physicochemical standardizations like ash value, Extractive value and fluorescence nature of the powder drug using light of short and long wavelength of 254nm and 366nm respectively. Phytochemical screening was performed for the identification of phytoconstituents in the plant which was helpful in the development of analytical profile. The morphological and microscopic examinations of drug were revealed the presence of endosperm cell which are polygonal in shape and contain alerone grains and oil droplet, cell of testa, yellow colouring matter and starch grains. Preliminary phytochemical screening showed the presence of carbohydrates, phenolic compounds, flavonoids, alkaloids, proteins, saponins and lipids in the drug extract and flourescence nature of drug was confirmed by fluorescence analysis in different solvent. Concentrations of heavy metals,ash value and extractive value were determined and found within acceptable Pharmacopoeial limits. Pesticides residues and aflatoxins were also determined but not detected in the tested samples. The physicochemical and phytochemical standards which are outcome of this research may be utilized as substantial data for identifica-tion and standardization of L. sativum seed.

Synthesis, characterization and biological evaluations of some 5-(substituted amino alkyl)-2-{(1, 3- benzothiazole-2-yl)}-thiazolidine-4 one Mannich bases as potent antibacterial agents.

Novel Mannich bases of 5-(substituted amino alkyl)-2-{(1, 3 benzothiazole-2-yl)}-thiazolidine-4 one, are synthesized by amination at 5th position of thiazolidine ring of 2-{(1, 3 benzothiazole-2-yl)}-thiazolidine-4 one using formaldehyde and various secondary amines. The synthesized compounds have been characterized by physico-chemical and spectral analysis and screened for their in- vitro antibacterial activity against various strains of bacteria.

A Review on Candesartan: Pharmacological and Pharmaceutical Profile.

Candesartan is classified as an angiotensin II receptor type 1 antagonist. Angiotensin II receptor type 1 antagonists are widely used in treatment of diseases like hypertension, heart failure, myocardial infarction and diabetic nephropathy. Candesartan is an orally active lipophilic drug and possesses rapid oral absorption. It causes reduction in blood pressure and is used in treatment of hypertension. It is also used in the treatment of congestive heart failure and given as prophylaxis to reduce the severity and duration of migraine. Candesartan cilexetil, a prodrug of Candesartan, is available in the market under the trade names- Blopress®, Atacand®, Amias® and Ratacand®. Candesartan is also available in a combination formulation with a low dose thiazide diuretic, invariably hydrochlorothiazide, to achieve an additive antihypertensive effect. This paper reviews the pharmacological and pharmaceutical properties of Candesartan. Candesartan could be an attractive target for the generic industries.

Pharmacological and Pharmaceutical Profile of Valsartan: A Review.

Angiotensin II Receptor type 1 antagonists have been widely used in treatment of diseases like hypertension, heart failure, myocardial infarction and diabetic nephropathy. Their beneficial effects are related to inhibition of Angiotensin II by blockade of AT1 receptor. Valsartan is an orally active Angiotensin II receptor type 1 antagonist which causes reduction in blood pressure and is used in treatment of hypertension. It was first developed by Novartis and has a wide market in the developed and the developing countries. It is also available in combination with other antihypertensive drugs. It is a lipophilic drug and possesses moderate onset of action than other drugs of the same category. The drug is a very good target for the generic industries. This review evaluates the pharmacological properties of Valsartan and its efficacy and tolerability in the treatment of patients with hypertension. A brief discussion has also been made on the current and future aspects of the drug in the market.