Extraction, GC-MS Evaluation and Anti-epileptic Potential of Seeds Ethanolic Extract of Putranjiva roxburghii Wall.

BACKGROUND: Putranjiva roxburghii Wall is traditionally known to cure many pathological conditions including epilepsy. OBJECTIVE: The present study is aimed at determining bioactive compounds in ethanolic extract of Putranjiva roxburghii test extract (PRTE) seeds by GCMS analysis and to assess its antiepileptic potential using various experimental models of epilepsy. METHODS: The ethanolic extract of seeds of Putranjiva roxburghii was subjected to GC-MS analysis to detect the bioactive phytoconstituents. Acute oral toxicity of the extract was performed using OCED guideline 420. Pentylenetetrazol (PTZ) kindling model of epilepsy and Maximal electroshock epilepsy (MES) model of epilepsy were used to determine anti-epileptic potential. RESULTS: The GC-MS analysis of the extract revealed the presence of 20 phytoconstituents. The major phytoconstituents included n-Propyl heptyl ether (25.25%), 5-Ethyl hydantoin (8%), octadec- 9-enoic acid (16.25%) and 1, 2-Benzene dicarboxylic acid (11.86%). The PRTE (50 mg/kg and 100 mg/kg) afforded a significant and dose-dependent protection against PTZ-induced kindling epilepsy and MES induced epilepsy (p<0.001 and p<0.01). CONCLUSION: Based on the above findings, it is evident that Putranjiva roxburghii seeds contain biologically active compounds. It can also be concluded that the extract possesses anti-epileptic potential.

Nano-Based Therapy for Treatment of Skin Cancer.

BACKGROUND: According to the World Health Organization, skin cancer is the most common malignancy for the population. Conventional skin cancer treatment includes surgery and chemotherapy, but many of the chemotherapeutic agents used present undesirable properties. There are a number of patents on topical nano formulation like nanoparticle (US9757453; US9457041), liposomes (US2018177726 (A1), has been covered in this review in the treatment of skin cancer. METHODS: Encapsulated drugs are advantageous due to such properties as high stability, better bioavailability, controlled drug release, a long blood circulation time, selective organ or tissue distribution, a lower total required dose, and minimal toxic side effects. Today, researchers are constantly developing new formulations to meet unmet needs in the delivery of therapeutic agents for cancer therapy and diagnosis, respectively. RESULTS: Of particular interest here are lipid-based nanoformulations that are formulated from varieties of lipid and other chemical components that act collectively to overcome biological barriers, in order to preferentially accumulate in or around disease-target cells for the functional delivery of therapeutic agents. The article deals with the recent development of nano-sized topical lipid formulation approaches to treat skin cancer. CONCLUSION: We focus especially on the topical lipid formulation approaches combined with chemotherapy, a field which specialises in target specificity, drug release control, and realtime monitoring with the goal being to diminish unwanted side effects and their severity, achieving a cheaper treatment and a generally more efficient chemotherapy.

Nano-carriers for the Treatment of Tuberculosis.

BACKGROUND: Nano size based drug delivery systems are an emerging technique with the potential to develop new strategies involving handling of drugs at the nanometer scale. There are many nano-based drug delivery systems that have been extensively reported as drug carriers for the treatment of tuberculosis. METHODS: There are numerous nano sized drug delivery systems like lipid nanoparticles, polymeric micelle, carbon nanotubes and polymeric nanoparticles that have been reported for a long time to treat diseases. There are a number of drawbacks in conventional TB dosage forms such as the development of multiple drug resistance, resulting in intolerable toxicity and high drug dose required. So, to overcome the drawbacks of conventional therapy, there is a need for a new drug delivery system with an aim to reduce the side effects of drug treatment. Nano-sized based drug delivery systems have considerable potential for the treatment of tuberculosis. These delivery systems have several advantages like high stability, high loading capacity, the feasibility of incorporation of both hydrophilic and hydrophobic drugs, and feasibility of variable routes of administration, and prolonged drug release from the matrix. These advantages enable enhanced drug solubility, bioavailability, reduced dosing frequency, high targeting, and may resolve the problem of non adherence to prescribed therapy, which is one of the major obstacles in the control of tuberculosis epidemics. CONCLUSION: This article gives an exhaustive review of patents and research papers published over the years on the challenges, the current treatment therapy of the disease faces, and potential advantages of nano sized formulations to offer more effective treatment and prevention for tuberculosis.

Synthesis and in vitro antimicrobial activity of novel N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class.

In this study, a series of novel 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a-g) and 1,3,4-oxadiazole (7a-g, 8) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (-) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5-100 µg/mL in DMSO. It has been observed that triazolo-thiadiazole derivatives are found to be more active than 1,3,4-oxadiazole derivatives against all pathogenic bacterial and fungal strains.

Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation.

A number of 5-(4-substituted phenyl)-2-(substituted benzylsulfanyl)-4-(substituted phenyl)-6-methyl-1,4-dihydro-5-pyrimidine carboxamides (1-30) were designed and synthesized keeping in view the structural requirements as suggested in the pharmacophore model for antihypertensive activity. All the synthesized compounds were tested for antihypertensive activity by non-invasive blood pressure (NIBP) measurements (tail-cuff method) in rats. Almost all the tested compounds displayed considerable decrease in the blood pressure as compared to control. Thirteen compounds showed significant antihypertensive activity comparable to the standard drug nifedipine.

Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid.

The significance of this study was to prepare various isoniazid derivatives by introducing the isoniazid core into several molecules to explore the possibilities of some altered biological activities. Series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (3a-g) and 1,3,4-oxadiazole (4a-g and 5) derivatives of isoniazid were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models.

Synthesis, anticonvulsant and toxicity screening of newer pyrimidine semicarbazone derivatives.

A number of N-(4,6-substituted diphenylpyrimidin-2-yl) semicarbazones (4a-t) were synthesized and tested for their anticonvulsant activity against the two seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). All the synthesized compounds possessed the four essential pharmacophoric elements for good anticonvulsant activity. Most of the compounds displayed good anticonvulsant activity with lesser neurotoxicity. To assess the unwanted effects of the compounds on liver, estimation of enzymes and proteins was carried out.