Raghuveer Irchhaiya

Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives.

A new series of betulinic acid derivatives have been synthesized by introducing heterocyclic ring between C-2 and C-3 positions of betulinic acid. Further modifications were also carried out by reduction of C-20(29) unsaturated bond and substitution of C-28 carboxyl group by ester and amide linkage to enhance the selectivity. Compound 11 resulted in IC(50) of 2.44, 2.5, and 2.7 microg/ml on MIAPaCa, PA-1, and SW620 cancer cell lines, respectively. Compound 38 resulted in IC(50) of 0.67 microg/ml on MIAPaCa cell line.

1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity.

A number of 1-propargyl-1,8-naphthyridine-3-carboxamide derivatives (15-35) have been synthesized and screened for their in vitro cytotoxicity and anti-inflammatory activity. Compounds 22, 31 and 34 have shown high cytotoxicity against a number of cancer cell lines, while compound 24 showed significant anti-inflammatory activity.

Niosomes: a potential tool for novel drug delivery

Vesicular drug delivery system are novel means to improve the bioavailability of the encapsulated drug along with numerous advantages over conventional drug delivery systems. Liposomes were first in such type of delivery systems but it was not so successful due to their numerous drawbacks. Niosomes or non ionic surfactant vesicles are formed from self assembly of hydrated surfactant monomers. They are formulated by non ionic surfactants but various ionic amphiphiles like di cetyl phosphate, sodium deoxycholate and stearylamine etc. are also incorporated inorder to achieve a stable vesicular suspension by inducing negative or positive charge. The most striking feature of such delivery system is that it can be used to encapsulate both hydrophobic as well as hydrophilic drug. The emphasis of this type of vesicular drug delivery system is placed over the slow release of drug in a controlled manner, resulting into sustained activity, reduced toxicity, protection of active moiety, targeting, modification in distribution profile of drugs and enhancing the bioavailability of encapsulated drug. This article summarizes the merits of niosomal drug delivery system over conventional drug therapy, its structural components, factors affecting its formation, method of preparation, evaluation techniques, therapeutic applications and patents.

Synthesis of functionalized amino acid derivatives as new pharmacophores for designing anticancer agents

A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines. Compound 6 has shown interesting cytotoxicity (IC50 = 5.67 μm) in ovarian cancer, while compound 10 exhibited promising cytotoxicity in ovarian (IC50 = 6.1 μm) and oral (IC50 = 4.17 μm) cancers. These compounds could be of use in designing new anti-cancer agents.

Anticancer and immunomodulatory activities of novel 1,8-naphthyridine derivatives

A number of 1,8-naphthyridine derivatives (22–62) have been synthesized and screened for their in vitro cytotoxicity against eight tumors and two non-tumor cell lines. Halogen substituted 1,8-naphthyridine-3-caboxamide derivatives showed potent activity with compound 47 having IC50 of 0.41 and 0.77 μM on MIAPaCa and K-562 cancer cell lines, respectively while, compound 36 had IC50 of 1.19 μM on PA-1 cancer cell line. However, one of the unsubstituted 1,8-naphthyridine-C-3’-heteroaryl derivative 29 showed potent cytotoxicity with IC50 of 0.41 and 1.4 μM on PA-1 and SW620 cancer cell lines, respectively. These compounds were also evaluated for anti-inflammatory activity as suggested by downregulation of proinflammaotory cytokines.

Anticonvulsant and muscle relaxant activity of the ethanolic extract of stems of Dendrophthoe falcata (Linn. F.) in mice

Objective: To investigate the anticonvulsant and muscle relxant activity of ethanolic extract of stems of Dendrophthoe falcata in mice. Materials and Methods: The ethanolic extract of stems of D. falcata (100, 300 and 500 mg/kg, p.o.) was studied for its anticonvulsant effect on maximal electroshock-induced seizures and muscle relaxant activity at the same dose level using rota rod and traction test in mice. Results: Preliminary phytochemical analysis revealed presence of proteins, carbohydrates, glycosides, steroids, triterpenes, flavonoids, tannins and phenolic compounds. D. falcata ethanolic extract (DFEE) (100, 300 and 500 mg/kg, p.o.) significantly (P<0.001) inhibited seizures induced by MES, reduced the duration of Hind limb tonic extensor phase (HLTE) and a decline in motor coordination. Conclusion: The ethanolic extract possesses anticonvulsant activity and muscle relaxant activity.

Phytochemical analysis, exploration of antidiabetic and antioxidant potential of Anthocephalus cadamba (Roxb.)

http://dx.doi.org/10.21276/IJRDPL.227 8-0238.2017.6(6).2800-2805 ABSTRACT: The most common disease nowadays is diabetes. In a fast-changing world, many means to treat diabetes naturally are explored by experts and clinicians today. Continuing use of insulin and other oral hypoglycemic agent creates undesirable side-effects, consequentially, unrestrained increase in blood sugar as well as complications associated with heart diseases; diabetics may have to face. To evade such glitches, herbal medications has superior advantages. As an alternative of using allopathic formulations, it is thus, gainful to use ayurvedic preparations for healthier regulation of diabetes mellitus. Current research was thus taken on to explore the antidiabetic and antioxidant activities of crude extracts and pure compound obtained from the bark of Anthocephalus cadamba. The methanolic extract exhibited promising antidiabetic and antioxidant activity. Grounded on these results, the methanolic extract was fractionated on a silica gel column chromatography in a bioassay-led fractionation resulting in one known isolate, cadambine showing potent anti-diabetic activity, more than that of the positive control, glibenclamide. The results indicated that Anthocephalus cadamba methanolic extract (ACME) and the isolated compound (Cadambine) are potential natural agents to control diabetes. Alloxan significantly induced hyperglycemia; Oral administration of test samples for 14 days caused a significant decrease in blood glucose levels. The possible mechanism by which ACME mediated its antidiabetic effect could be by potentiation of pancreatic secretion of insulin from existing β-cells of islets in the extract treated animals. ⇑ Corresponding author at: Himanshu Pratap Singh, Department of Pharmaceutical Sciences, Faculty of Health Sciences, Sam Higignbottom University of Agriculture, Technology and Sciences, Allahabad211007, India Email: princehimanshusingh@rediffmail.com