Vipin Kumar Garg

Thiazoles: having diverse biological activities

In the last few decades, a lot of work has been done on thiazole ring to find new compounds related to this scaffold to act as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective, and antitumor or cytotoxic drug molecules with lesser side effects. This review presents the up to date development on the design and development of different thiazole derivatives.

Role of fetuin-A in atherosclerosis associated with diabetic patients

Objectives  Fetuin‐A is a circulating glycoprotein, formed in the liver. It regulates bone remodelling and calcium metabolism. Fetuin‐A has adipogenic properties, so fat accumulation in the liver may be associated with higher levels of fetuin‐A. Fetuin‐A is an inhibitor of the phosphorylation of the insulin receptor tyrosine kinase.

Ocular inserts - Advancement in therapy of eye diseases.

The ocular insert represents a significant advancement in the therapy of eye disease. Ocular inserts are defined as sterile, thin, multilayered, drug-impregnated, solid or semisolid consistency devices placed into the cul-de-sac or conjuctival sac, whose size and shape are especially designed for ophthalmic application. They are composed of a polymeric support that may or may not contain a drug. The drug can later be incorporated as dispersion or a solution in the polymeric support. They offer several advantages as increased ocular residence and sustained release of medication into the eye. The insert includes a body portion sized to position within a lachrymal canaliculus of the eyelid. The inserts are classified according to their solubility as insoluble, soluble, or bioerodible inserts. The release of drug from the insert depends upon the diffusion, osmosis, and bioerosion of the drug, and this article is an attempt to present a brief about this newer drug delivery system.

Role of PPARg2 transcription factor in thiazolidinedione-induced insulin sensitization

Objectives  Adipose tissue is the key regulator of energy balance, playing an active role in lipid storage and metabolism and may be a dynamic buffer to control fatty acid flux. Peroxisome proliferator‐activated receptor gamma isoform‐2 (PPARg2), an isoform of the nuclear hormone receptor superfamily, has been implicated in almost all aspects of human metabolic alterations such as obesity, insulin resistance, type‐2 diabetes and dyslipidaemia. The PPARg2 isoform is highly present in adipose tissue where it functions as a thrifty phenotype, which promotes adipocyte differentiation and triglyceride storage. Thiazolidinediones, antidiabetic drugs, induce insulin sensitivity by controlling adipokines. The thiazolidinediones bind with PPARg2 in adipocytes and exert an agonist effect by enhancing adipogenesis and fatty acid uptake. Thiazolidinediones stimulate PPARg2, by which they down‐regulate tumour necrosis factor‐α, leptin, interleukin‐6 and plasminogen and also enhance insulin sensitivity. The aim of this work is to define role of PPARg2 transcription factor in thiazolidinedione‐induced insulin sensitization.

Wound-healing activity of ethanolic and aqueous extracts of Ficus benghalensis.

Wound healing is the process of repair that follows injury to the skin and other soft tissues. Following injury, an inflammatory response occurs and the cells below the dermis (the deepest skin layer) begin to increase collagen (connective tissue) production. Later, the epithelial tissue (the outer skin) is regenerated. There are three stages to the process of wound healing: inflammation, proliferation, and remodeling. Traditionally, Ficus benghalensis is used for wound healing. Since no detailed scientific data are available regarding the wound-healing activity of F. benghalensis, the present study was designed to explore the same. The wound-healing efficacy of ethanolic and aqueous extracts of F. benghalensis was evaluated in excision and incision wound models. The parameters studied include rate of wound contraction, period of complete epithelialization, and tensile strength of incision wound. Students t test was used to analyze the results obtained from the present study and P<0.05 was considered significant. Both the ethanolic and aqueous extracts of F. benghalensis were found to possess significant wound-healing activity, which was evidenced by decrease in the period of epithelialization, increase in the rate of wound contraction and skin-breaking strength. The present study has demonstrated that the ethanolic and aqueous extracts of F. benghalensis have properties that render them capable of promoting accelerated wound-healing activity compared with placebo control.

Protein tyrosine phosphatase 1B inhibitors as antidiabetic agents - A brief review.

Diabetes mellitus and obesity are one of the most common health issues spread throughout world and raised the medical attention to find the new effective agents to treat these disease state. Occurrence of the drug resistance to the insulin and leptin receptor is also challenging major issues. The molecules that can overcome this resistance problem could be effective for the treatment of both type II diabetes and obesity. Protein Tyrosine Phosphatase (PTP) has emerged as new promising targets for therapeutic purpose in recent years. Protein Tyrosine Phosphatase 1B (PTP 1B) act as a negative regulator of insulin and leptin receptor signalling pathways. Several approaches have been successfully applied to find out potent and selective inhibitors. This article reviews PTP 1B inhibitors; natural, synthetic and semi-synthetic that showed inhibition towards enzyme as a major target for the management of type II diabetes. These studies could be contributing the future development of PTP 1B inhibitors as drugs.

The target-specific transporter and current status of diuretics as antihypertensive.

The currently available diuretics increase the urinary excretion of sodium chloride by selective inhibition of specific sodium transporters in the loop of Henle and distal nephron. In recent years, the molecular cloning of the diuretic‐sensitive sodium transporters at distal convoluted tubule has improved our understanding of the cellular mechanisms of action of each class of diuretics. Diuretics are tools of considerable therapeutic importance. First, they effectively reduce blood pressure. Loop and thiazide diuretics are secreted from the proximal tubule via the organic anion transporter‐1 and exert their diuretic action by binding to the Na+‐K+‐2Cl− co‐transporter type 2 in the thick ascending limb and the Na+‐ Cl− co‐transporter in the distal convoluted tubule, respectively. Recent studies in animal models suggest that abundance of these ion transporters is affected by long‐term diuretic administration. The WHO/ISH guidelines point out that diuretics enhance the efficacy of antihypertensive drugs and will most often be a component of combination therapy.

Therapeutic Potential of Calendula officinalis

Calendula officinalis (Calendula), belonging to the family of Asteraceae, commonly known as English Marigold or Pot Marigold is an aromatic herb which is used in Traditional system of medicine for treating wounds, ulcers, herpes, scars, skin damage, frost-bite and blood purification. It is mainly used because of its various biological activities to treat diseases like analgesic, anti–diabetic, anti-ulcer and anti-inflammatory. It is also used for in gastrointestinal, gynecological, eye disease, skin injuries and in some cases of burn. Calendula oil is still medicinally used as, an anti-tumor agent, and a remedy for healing wounds. Plant pharmacological studies have suggested that Calendula extracts have antiviral, antigenotoxic properties in-vitro. In herbalism, Calendula in suspension or in tincture is used topically for treating acne, reducing inflammation, controlling bleeding, and soothing irritated tissue. Calendula is used for protection against the plague. In early American Shaker medicine, calendula was a treatment for gangrene. In addition to its first aid uses, calendula also acts as a digestive remedy. An infusion or tincture of the flowers, taken internally, is beneficial in the treatment of yeast infections, and diarrhea. An infusion of Calendula officinalis may also be used to treating bee stings, eye inflammations, boils and abscesses, varicose veins, eczema, and as a gargle for mouth sores or to relieve toothache. It improves the circulation of the blood & the lymphatic fluids and aids in elimination of toxins from the body. This plant is rich in many pharmaceutical active ingredients like carotenoids, flavonoids, glycosides, steroids and sterols quinines, volatile oil, and amino acid. The extract of this plant as well as pure compound isolated from it, have been demonstrated to possess multiple pharmacological activities such as anti-cytotoxic, hepato-protective and spasmolytic amongst others. Acute toxicity studies in rats and mice suggest that the extract is relatively nontoxic. Animal tests have demonstrated minimal skin irritation, and no sensitization or photo toxicity. Minimal ocular irritation was seen with one formulation and no irritation with others. Six saponins isolated from C. officinalis flowers were not mutagenic in an Ames test, and a tea derived from C. officinalis was not genotoxic in Drosophila melanogaster. Clinical testing of cosmetic formulations containing the extract elicited little irritation or sensitization. This review has explored the organoleptic, in-vitro and in-vivo pharmacological activities as well as description, cultivation and active chemical constituents of Calendula officinalis in order to existing information on this plant as well as highlighted its multi activity properties as a medicinal agent.