Newly Synthesized 3-Indolyl Furanoid Inhibits Matrix Metalloproteinase-9 Activity and Prevents Nonsteroidal Anti-inflammatory Drug-Induced Gastric Ulceration.

Indomethacin, a known nonsteroidal anti-inflammatory drug (NSAID) induces gastric inflammation, causing degradation of the extracellular matrix by specific matrix metalloproteinases (MMPs). We investigated the antiulcer efficacy of 3-indolyl furanoids ( and , i.e.

Assessment of superiority of HSP70-targeting aptamer-functionalized drug-nanocarrier over non-targeted commercially available counterpart in HCC therapy: in vitro and in vivo investigations and molecular modeling.

Aims: This research aims to compare the therapeutic potential of target-specific phosphorothioate backbone-modified aptamer L5 (TLS9a)-functionalized paclitaxel (PTX)-loaded nanocarrier (PTX-NPL5) that we formulated with that of non-targeted commercial formulation, protein albumin-bound nanoparticles of PTX, Abraxane® (CF) against hepatocellular carcinoma (HCC) through a myriad of preclinical investigations.

Main Methods: A variety of in vitro and in vivo assays have been executed to compare the therapeutic effects of the formulations under investigation, including the investigation of the degree of apoptosis induction and its mechanism, cell cycle analysis, the level of ROS production, and redox status, the morphological and histological characteristics of malignant livers, and in vivo imaging. The formulations were also compared concerning pharmacokinetic behaviors.

A Comparative Investigation of the Ability of Various Aptamer-Functionalized Drug Nanocarriers to Induce Selective Apoptosis in Neoplastic Hepatocytes: In Vitro and In Vivo Outcome.

Aptamers offer a significant promise to target various cancers including hepatocellular carcinoma (HCC), for their high affinity and ability to reach the target site(s), non-immunogenicity, and low cost. The targeting ability to neoplastic hepatocytes by the aptamer, TLS 9a with phosphorothioate backbone modification (designated as L5), has not been explored yet. Hence, we investigated the comparative potential of L5 with some other previously reported liver cancer cell-specific aptamers, conjugated on the surface of drug-nanocarriers.

Orcinol Glucoside Loaded Polymer - Lipid Hybrid Nanostructured Lipid Carriers: Potential Cytotoxic Agents against Gastric, Colon and Hepatoma Carcinoma Cell Lines.

Purpose: Orcinol glucoside (OG) - loaded nanostructured lipid carrier (NLC), coated with polyethylene glycol-25/55-stearate (PEG-25/55-SA), were explored for delivering OG to improve in vitro cytotoxicity against gastrointestinal tract (GIT), colon and hepatoma carcinoma cell lines. It is being expected that the PEGylated formulations would possess the sustainability in withstanding the adverse physiological extremities like the most significant metabolic activities and phase I / II enzymatic activities in the intestines.

Methods: NLCs were prepared using tristearin, oleic acid and PEG-25/55-stearate by hot homogenization-ultrasonic dispersion; characterized by DLS, TEM, SEM, AFM, entrapment efficiency and drug loading capacity studies.

Influence of Lipid Core Material on Physicochemical Characteristics of an Ursolic Acid-Loaded Nanostructured Lipid Carrier: An Attempt To Enhance Anticancer Activity.

The impact of saturation and unsaturation in the fatty acyl hydrocarbon chain on the physicochemical properties of nanostructured lipid carriers (NLCs) was investigated to develop novel delivery systems loaded with an anticancer drug, ursolic acid (UA). Aqueous NLC dispersions were prepared by a high-pressure homogenization-ultrasonication technique with Tween 80 as a stabilizer. Mutual miscibility of the components at the air-water interface was assessed by surface pressure-area measurements, where attractive interactions were recorded between the lipid mixtures and UA, irrespective of the extent of saturation or unsaturation in fatty acyl chains.

Anti-leukemic activity of Wattakaka volubilis leaf extract against human myeloid leukemia cell lines.

Ethnopharmacological Relevance: Wattakaka volubilis has been traditionally used in Ayurvedic medicine in India for treatment of several ailments such as bronchial asthma, inflammations, tumors, piles, leucoderma, application to boils, rat bite etc.

Aim Of The Study: The present study was designed to investigate anti-leukemic activity of the crude aqueous methanolic extract and to identify active compounds from the leaves of Wattakaka volubilis.

Materials And Methods: The leaves of Wattakaka volubilis were extracted with aqueous methanol.

Anti-inflammatory and anti-nociceptive activities of methanolic extract of the leaves of Fraxinus floribunda Wallich.

Fraxinus floribunda Wallich (Family-Oleaceae) is a wide green tree in the sub-alpine region of Sikkim, India. The methanolic extract of the leaves of Fraxinus floribunda (MEFF) at 100, 200 and 400 mg/kg/p.o was screened in rats for anti-inflammatory activity by acute-carrageenan induced paw edema, sub-acute cotton pellet induced granuloma and chronic Freund's adjuvant induced arthritis models.

Production and purification of a bioactive substance inhibiting multiple drug resistant bacteria and human leukemia cells from a salt-tolerant marine Actinobacterium sp. isolated from the Bay of Bengal.

Four marine actinobacteria tolerant to 200 g NaCl l(-1) were screened for antibacterial activity against eight patient-derived multiple drug resistant (MDR) bacteria. The active compound (MW 300.2, predicted molecular formula C(20)H(28)O(2)) from an actinobacterium, was inhibitory to three Gram-positive and three Gram-negative MDR bacteria, seven non-clinical Gram-positive, four Gram-negative bacteria and five fungi (MIC: 3.

Cytotoxic and apoptogenic effect of tea (Camellia sinensis var. assamica) root extract (TRE) and two of its steroidal saponins TS1 and TS2 on human leukemic cell lines K562 and U937 and on cells of CML and ALL patients.

The anticancer activity of di- and tri-terpenes and other polyphenolic compounds present in tea is already reported. We evaluated the cytotoxic and apoptogenic effect of tea root extract (TRE) and two of its steroidal saponins named as TS1 and TS2, on human cell lines and on cells from leukemic patients. It was found that TRE, TS1 and TS2 significantly decreased cell count and that TRE caused apoptosis, as confirmed morphologically by confocal microscopy and by flow-cytometric analysis using Annexin-V FITC and propidium iodide (PI).