Abstract
The present work reports the anticancer, antioxidant, lipo-protective, and anti-HIV activities of phytoconstituents present in P. hysterophorus leaf. Dried leaf samples were sequentially extracted with nonpolar and polar solvents. Ethanol fraction showed noticeable cytotoxic activity (81–85%) in SRB assay against MCF-7 and THP-1 cancer cell lines at 100 μg/ml concentration, while lower activity was observed with DU-145 cell line. The same extract exhibited 17–98% growth inhibition of HL-60 cancer cell lines in MTT assay, showing concentration dependent response. Ethanol extract caused 12% reduction in mitochondrial membrane potential and 10% increment in sub G1 population of HL-60 cell lines. Several leaf fractions, namely, ethyl acetate, ethanol, and aqueous fractions exhibited considerable reducing capability at higher concentrations. Most of the extracts demonstrated appreciable (>75%) metal ion chelating and hydroxyl radical scavenging activities at 200 µg/ml. All the extracts except aqueous fraction accounted for about 70–80% inhibition of lipid peroxidation in rat liver homogenate indicating protective response against membrane damage. About 40% inhibition of reverse transcriptase (RT) activity was observed in hexane fraction in anti-HIV assay at 6.0 µg/ml concentration. The study showed that phytochemicals present in P. hysterophorus leaf have considerable potential as cytotoxic and antioxidant agents with low to moderate anti-HIV activity.
Highlights
Identification of novel therapeutic agents as new drugs for alleviation of the human suffering from cancer and other degenerative diseases is of prime concern [1, 2]
This brings changes in the mitochondrial membrane that results in an opening of the mitochondrial permeability transition pore (MPT), loss of mitochondrial transmembrane potential (ΔΨm), and release of proapoptotic proteins from the intermembrane space into the cytosol [9]
The dried residues were dissolved in DMSO for determination of anticancer, antioxidant, and anti-HIV activities, while for lipid peroxidation inhibition (LPOI) studies the residues were dissolved in respective solvents
Summary
Identification of novel therapeutic agents as new drugs for alleviation of the human suffering from cancer and other degenerative diseases is of prime concern [1, 2]. It is generally believed that chemotherapeutic agents in the treatment of cancer cells induce apoptosis. Apoptosis results from the activation of caspases, the cysteine proteases, in response to different cell death stimuli via extrinsic and/or intrinsic pathways [6, 7]. Intrinsic pathway is triggered due to the release of cytochrome c in the cytosol from mitochondria which results in the formation of a multiprotein complex apoptosome and leads to activation of caspase 3, 6, and 9 [8]. Present work was undertaken to evaluate the anticancer, antioxidant, lipo-protective, and anti-HIV activities of various P. hysterophorus leaf extracts
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