Novel Synthetic Indazoles Abrogate Angiogenesis in Erlich Ascites Tumor Bearing Mice.

Background: Indazoles are known for their anti-cancer properties.

Objective: The current investigation was on the synthesis and evaluation of novel indazole derivatives for their anticancer properties.

Methods: A series of novel indazoles were synthesized and characterized by IR, NMR and LCMS.

Comprehensive Nutritional Analysis, Antioxidant Activities, and Bioactive Compound Characterization from Seven Selected Cereals and Pulses by UHPLC-HRMS/MS.

Cereals and pulses comprise the largest proportion in a typical Indian diet plate. This research mainly focuses on determining the nutritional composition, bioactive compound characterization, and antioxidant activities of seven selected cereals and pulses. The total carbohydrate content was high in unripe banana (67.

Group IIA secreted phospholipase A inhibition by elemolic acid as a function of anti-inflammatory activity.

Human group IIA secreted phospholipase A2 (GIIA) is a key enzyme in inflammatory reactions, worsening the condition of several chronic inflammatory diseases. The natural inhibitors of GIIA potentially block the production of inflammatory mediators. In the present study, elemolic acid, a triterpenoid from Boswellia serrata inhibited the GIIA enzyme in a concentration-dependent manner with IC value of 5.

Novel 3-(3, 5-difluoro-4-hydroxyphenyl)-1-(naphthalen-2-yl) prop-2-en-1-one as a potent inhibitor of MAP-kinase in HeLa cell lines and anti-angiogenic activity is mediated by HIF-1α in EAC animal model.

In the present investigation, we synthesized chalcone bearing naphthalene compound d1, and on the basis of H-NMR, C NMR, and LC-MS data we had specified the structure of the synthesized compound. The resultant compound d1 was assessed for their antiproliferative action against human cancer cell lines (HeLa, HCT116, HT29, MDA-MB-231, MCF-7, and SKBR3). The IC range was estimated at 5.

Musa acuminata lectin exerts anti-cancer effects on HeLa and EAC cells via activation of caspase and inhibitions of Akt, Erk, and Jnk pathway expression and suppresses the neoangiogenesis in in-vivo models.

In the present study aimed to purify the lectin from the sap of Musa acuminata pseudostem and elucidate the apoptotic and angiogenic molecular mechanism in both in-vitro and in-vivo model. Mannose specific lectin was purified by using mannose affinity column chromatography and analyzed by RP-HPLC, SDS-PAGE, and PAS staining method. Furthermore, the protein was identified by MALDI-MS/MS.

Angiosuppressive effects of bio-fabricated silver nanoparticles synthesis using Clitoria ternatea flower: an in vitro and in vivo approach.

Biosynthesis of silver nanoparticles (CTNP's) by Clitoria ternatea flower in the aqueous extract was investigated. Synthesized nanoparticles were characterized by using UV-Visible spectroscopy, followed by DLS, Zeta potential, XRD, FTIR, SEM, and AFM. The biocompatibility nature of CTNP's was determined using erythrocytes model system.

Angio-Suppressive Effect of Partially Purified Lectin-like Protein from Musa acuminata pseudostem by Inhibition of VEGF-Mediated Neovascularization and Induces Apoptosis Both In Vitro and In Vivo.

Lifestyle and nutritional changes have contributed much to the somatic genetic changes which have concurrently led to an increase cancer in humans. Hence the plant-based and nutritional involvements block oncogenic transformation are in good demand. We evaluate Phloem exudates of the dietary plant, Musa acuminate pseudostem, the initial domesticated plant species with the effective lectin activity for its functional role against the tumor development and its mechanism of action.

Synthesis of new coumarin tethered isoxazolines as potential anticancer agents.

A series of new coumarin tethered isoxazolines (7a-l) were synthesized and evaluated for their cytotoxic potency against human melanoma cancer cell line (UACC 903) as well as fibroblast normal cell line (FF2441). Preliminary results revealed that some of these coumarin tethered isoxazolines 7b, 7c, 7f and 7j exhibited significant antiproliferative effect against human melanoma cancer (UACC 903) with IC values of 8.8, 10.

Anti-cancer and anti-angiogenic effects of partially purified lectin from Praecitrullus fistulosus fruit on in vitro and in vivo model.

Praecitrullus fistulosus, belonging to the family of Cucurbitaceae is a tropical vegetable and medicinal plant, grown and consumed extensively in subtropical countries, including the subcontinent India. However, there are limited reports on the medicinal properties of the plant and need to be explored. The lectin identified from the fruit sap of Praecitrullus fistulosus, named as PfLP, possesses potent agglutinating activity against trypsinized rabbit erythrocytes and exhibited its functional role against tumor progression, on in vitro &in vivo models.

Synthesis, Characterization of 4-Anilino-6,7-Dimethoxy Quinazoline Derivatives as Potential Anti-Angiogenic Agents.

Background: Quinazolines are a big family of heterocyclic compounds with anti-cancer properties.

Objective: The latest investigation was on synthesis, characterization of novel 4-anilinoquinazoline derivatives for their anti-angiogenic effect.

Method: A series of novel 4-anilino-6,7-dimethoxy quinazoline derivatives were synthesized and characterized using 1H, 13C NMR, FT-IR and LC-MS techniques.

Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice.

Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-1,7-dimethyl-2-propyl-1H,3H-2,5-bibenzo[d]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC50 >50 μM).

MADD is a downstream target of PTEN in triggering apoptosis.

Mitogen-activated kinase activating death domain containing protein (MADD) is abundantly expressed in cancer cells and necessary for maintaining cancer cell survival. However, this survival function of MADD is dependent upon its phosphorylation by protein kinase B (Akt). The tumour suppressor PTEN (phosphatase and tensin homolog deleted on chromosome 10) is a lipid phosphatase that negatively regulates the phosphatidylinositol 3-kinase (PI3K)-Akt signaling pathway.

Akt-phosphorylated mitogen-activated kinase-activating death domain protein (MADD) inhibits TRAIL-induced apoptosis by blocking Fas-associated death domain (FADD) association with death receptor 4.

MADD plays an essential role in cancer cell survival. Abrogation of endogenous MADD expression results in significant spontaneous apoptosis and enhanced susceptibility to tumor necrosis factor alpha-related apoptosis-inducing ligand (TRAIL)-induced apoptosis. However, the regulation of MADD function is largely unknown.

Nanodisc-incorporated hemagglutinin provides protective immunity against influenza virus infection.

Every year, influenza virus infection causes significant mortality and morbidity in human populations. Although egg-based inactivated viral vaccines are available, their effectiveness depends on the correct prediction of the circulating viral strains and is limited by the time constraint of the manufacturing process. Recombinant subunit vaccines are easier to manufacture with a relatively short lead time but are limited in their efficacy partly because the purified recombinant membrane proteins in the soluble form most likely do not retain their native membrane-bound structure.

Pro-apoptotic activity of imidazole derivatives mediated by up-regulation of Bax and activation of CAD in Ehrlich Ascites Tumor cells.

In this study we report that, imidazole derivatives can induce apoptosis in Ehrlich ascites tumor (EAT) cells, which is clearly evident from annexin-V staining, flow cytometric analysis of cell cycle phase distribution and DNA fragmentation. Delineating further into molecular mechanisms leading to apoptosis of EAT cells, we observed that imidazole derivatives induce tumor cell death by the up-regulation of proto-oncoprotein Bax, release of cytochrome c from the mitochondria which activates caspase-3 and activated caspase-3 activates CAD (Caspase Activated DNase) causes DNA fragmentation. The status of Bcl-2 remains unaltered in EAT cells, and the under expression of Bcl-2 and up-regulation of Bax resulted in the increase of Bax: Bcl-2 ratio suggesting that Bcl-2 family involved in the control of apoptosis.