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The nano-drug delivery system utilizing the ligand functionalized nanoparticles have a tremendous application in cancer therapeutics. The present study was aimed to fabricate the p-Coumaric acid-loaded aptamer (ligand) conjugated starch nanoparticles (Apt-p-CA-AStNPs) for effective treatment of triple-negative breast cancer (MDA-MB-231). The FT-IR spectrum stipulated the presence of functional groups associated with para-Coumaric acid (p-CA) and amino starch (AS) in p-CA-AStNPs. Further, the conjugation of aptamer in p-CA-AStNPs was confirmed by agarose gel electrophoresis. Transmission electron microscopic analysis revealed that the synthesized Apt-p-CA-AStNPs were less agglomerated. The zeta size analyzer displayed the average particle size as 218.97 ± 3.07 nm with ȥ-potential −29.2 ± 1.35 mV, and PDI 0.299 ± 0.05 for Apt-p-CA-AStNPs. The drug encapsulation and loading efficiencies were 80.30 ± 0.53% and 10.35 ± 0.85% respectively for Apt-p-CA-AStNPs. Apt-p-CA-ASNPs showed a rapid and bursting release in the initial five hours of the experiment in pH 5.4. A significant change was found in their cytotoxic efficacy between the samples: p-CA, p-CA-AStNPs, and Apt-p-CA-AStNPs. Among the tested samples, Apt-p-CA-AStNPs caused higher cytotoxicity in MDA-MB-231 cells through ROS regulation, nuclear damage, mitochondrial membrane potential, and apoptosis-related protein expressions. Overall, these results proved that Apt-p-CA-AStNPs were efficiently inhibited the MDA-MB-231 cells by regulating apoptosis.

Polydatin (POL) is an ingredient of many herbal medications and has pharmacological properties. The present study aimed to determine the antitumor potential of Polydatin loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (POL-PLGA-NPs) against the cancerous KB cell line. We evaluated the efficiency of synthesized nanoparticles on cell proliferation and apoptosis markers, in addition to the generation of reactive oxygen species (ROS) and its potential to induce damages on the mitochondrial membrane. Morphological changes in the cells (damage to DNA incurred due to cell lysis) were observed under Ethidium Bromide and Acridine orange staining techniques. The results evidenced the loss of cell viability, increased ROS, altered lipid peroxidation levels, increased DNA damage and loss of mitochondrial membrane potential in target cancerous KB cells. Further, immunoblot analysis quantified the expression of caspases-3, -9 and poly(ADP-ribose) polymerase (PARP) also supports the cell damage. Thus, the findings of the study suggested that POL-PLGA-NPs effectively induced oxidative stress by initiating cellular damage leading to apoptosis in KB cells.

The present study was aimed to green synthesis and characterization of zinc oxide nanoparticles (ZnONPs) from Aspergillus niger, which was evaluated for their antioxidant, antimicrobial and anticancer activity. The synthesised NPs were characterized by various analytical techniques such as UV–VIS Spectroscopy, FT-IR, XRD, DLS, SEM, and TEM. It was confirmed through the UV–Vis spectrophotometer; corresponding peaks were identified at 390 nm. The green synthesised ZnONPs were characterized by FT-IR studies to reveal the functional group attributed to the formation of ZnONPs. Morphological size of ZnONPs was 80–130 nm found through characterization by DLS, SEM, and TEM. Furthermore, the green synthesised ZnONPs showed potent antioxidant (ABTS and DPPH assay) antimicrobial activity against human pathogenic bacterial strains such as Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa, and Enterobacter aerogenes. In addition, the green synthesised ZnONPs showed the dose-dependent cytotoxicity and apoptotic features in human hepatocellular carcinoma cells (HepG2). The overall findings of the study suggested that A. niger had a potential for the biosynthesis of ZnONPs as an alternative biomaterial for future therapeutic application as an antioxidant, antimicrobial and anticancer compound.

Allium hirtifolium (A. hirtifolium), a member of the Amaryllidaceae family, is generally known as Persian shallot. It usually grows in hilly areas and took place in most of Persian cuisine. The parts of A. hirtifolium used in folk medicine and recently the constituents have been identified and documented. The compounds present in A. hirtifolium possess various beneficial biological effects such as antibacterial, antioxidant and antidiabetic. Naringenin is the major compound found among all flavonoids with diverse pharmacological activities. In addition, the constituents present in this plant plays various roles in modulating signaling pathways to prevent cancer, diabetes and heart diseases. Thus, A. hirtifolium and the compounds present in this plant may be promising candidate for various disease due to its wide pharmacological activities. In this review, we discussed pharmacological activities and disease prevention activities of A. hirtifolium by its modulating role of biochemical and molecular mechanisms.

The present study was aimed to investigate the chemopreventive potential of troxerutin on 1,2-dimethylhydrazine (DMH) induced rat colon carcinogenesis by evaluating the antioxidant and lipid peroxidation (LPO) status. Rats were randomly divided into six groups. Group I rats served as control. Group II rats received troxerutin (50 mg/kgb.w., p.o.) for 16 weeks. Groups III-VI rats received subcutaneous injections of DMH (20 mg/kgb.w., s.c.) once a week, for the first 4 weeks. In addition to DMH, groups IV-VI rats received troxerutin at the doses of 12.5, 25 and 50 mg/kgb.w., respectively. In DMH treated rats, our results showed decreased activities of antioxidants and increased levels of LPO in the liver. Moreover, LPO and antioxidants in the colon were found to be significantly diminished in DMH the treated rats. Furthermore, enhanced activity of colonic vitamin C and vitamin E levels were observed in DMH alone treated rats (group III), which was significantly reversed on troxerutin supplementation. Troxerutin at the dose of 25 mg/kgb.w. had shown profound beneficial effects by exhibiting near normal biochemical profile and well-preserved colon histology as compared to the other two tested doses (12.5 and 50 mg/kgb.w.). These findings suggest that troxerutin could serve as a novel agent for colon cancer chemoprevention.

We investigated the chemopreventive effect of p-methoxycinnamic acid (p-MCA), an active phenolic acid of rice bran, turmeric, and Kaemperfia galanga against 1,2-dimethylhydrazine-induced rat colon carcinogenesis. Male albino Wistar rats were randomly divided into six groups. Group 1 consisted of control rats that received a modified pellet diet and 0.1% carboxymethyl cellulose. The rats in Group 2 received a modified pellet diet supplemented with p-MCA [80 mg/kg body weight (b.wt.) post-orally (p.o.)] everyday. The rats in Groups 3-6 received 1,2-dimethylhydrazine (DMH) (20 mg/kg b.wt.) via subcutaneous injections once a week for the first 4 weeks; additionally, the rats in Groups 4, 5 and 6 received p-MCA at doses of 20, 40 and 80 mg/kg b.wt./day p.o., respectively, everyday for 16 weeks. The rats were sacrificed at the end of the experimental period of 16 weeks. The DMH-treated rats exhibited an increased incidence of aberrant crypt foci (ACF) development; an increased crypt multiplicity; decreased concentrations of tissue lipid peroxidation markers such as thiobarbituric acid reactive substances (TBARS), conjugated dienes (CD) and lipid hydroperoxides (LOOH); decreased levels of tissue enzymic antioxidants such as superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione reductase (GR); and decreased levels of non-enzymic antioxidants such as reduced glutathione (GSH) and vitamins C, E and A in the colon. Supplementation with p-MCA significantly reversed these changes and significantly inhibited the formation of ACF and its multiplicity. Thus, our findings demonstrate that p-MCA exerts a strong chemopreventive activity against 1,2-dimethylhydrazine-induced colon carcinogenesis by virtue of its ability to prevent the alterations in DMH-induced circulatory and tissue oxidative stress and preneoplastic changes. p-MCA was more effective when administered at a dose of 40 mg/kg b.wt. than at the other two doses tested.

Colon cancer is one of the most common cancers in both men and women. The present study is an effort to unravel the anticarcinogenic effects of rosmarinic acid (RA) in 1,2-dimethylhydrazine (DMH)-induced rat colon carcinogenesis. Administration of DMH induces multiple tumors in the rat colon, which mimics human colon cancer.Male Wistar rats were divided into six groups and fed a high-fat diet. Group 1 served as control, group 2 rats were given RA [5 mg/kg body weight (b.w.)] orally every day for a total period of 30 weeks, and groups 3–6 were given weekly injections of DMH (20 mg/kg b.w. subcutaneous) once a week in the groin for the first 15 weeks. In addition to DMH, groups 4–6 received RA at a dose of 5 mg/kg b.w. during the initiation and postinitiation stages, and also throughout the entire study period. Colon tissues were examined histologically; further, the extent of oxidative stress was assessed by measuring lipid peroxidation and antioxidant levels in the colonic mucosa of rats.Macroscopic and microscopic tumors were identified in all the groups that received DMH. The results revealed that supplementation with RA significantly inhibited the tumor formation and tumor multiplicity in DMH-treated rats. RA supplementation to DMH-administered rats significantly reduced the cell proliferation markers, namely, argyrophilic nucleolar organizing regions as well as proliferative cell nuclear antigen labeling index. In addition, RA supplementation reduces the expressions of tumor necrosis factor-α, interlukin-6, and cyclooxygenase-2, and modulates the expression of p65.The above findings clearly underline the chemopreventive efficacy of RA against DMH-induced colon carcinogenesis.