Ahsana Dar Farooq

Anticancer and antioxidant activities of methanol extracts and fractions of some Cameroonian medicinal plants.

OBJECTIVE To obtain a scientific basis of the use of plant-derived preparations by many rural people in Cameroon, for their primary health care needs in the treatment of diseases such as cancer. METHODS The antiproliferative effect of 11 plants methanol crude extracts on four cancer cells using sulforhodamine-B assay and their antioxidant activities using 1-diphenyl-2-picrylhydrazyl radical and nitric oxide radical scavenging ability were investigated. The Ekebergia senegalensis (E. senegalensis) and Protea elliotii (P. elliotii) extracts were selected based on their antioxidant and anticancer activities, and partition in hexane, dichloromethane, ethyl acetate, butanol and methanol was done. Each fraction was submitted to antioxidant and anticancer activities, and the effect of the dichloromethane fraction (the most antiproliferative fraction) on NCI-H460 cell cycle was determined by flow cytometry. RESULTS The most antiproliferative substances were found for the extracts from E. senegalensis, P. elliotii, Terminalia macroptera and Vitellaria paradoxa. Whereas the most antioxidant substances were found for the extracts from Cissus populnea, E. senegalensis, P. elliotii, Terminalia macroptera, Vitellaria paradoxa, and Gardenia aqualla. Dichloromethane fraction of P. elliotii was found to be highly antiproliferative to NCI-H460 cancer cells and showed S phase arrest cell cycle progression. Ethyl acetate n-butanol and methanol fractions showed quite strong antioxidant activity for both E. senegalensis and P. elliotii, as compared to that of gallic acid. CONCLUSIONS Overall, the antiproliferative and antioxidant activities of some of the extracts lend some support to their use in the traditional medicine of Adamawa Region, Cameroon to treat cancer.

Molecular Mechanism of Antiproliferation Potential of Acacia Honey on NCI-H460 Cell Line

Lung cancer is one of the leading causes of death worldwide. We investigated the molecular mechanism of antiproliferation potential of Acacia honey on NCI-H460 cells by cell cycle, viability, cytokines, calcium ion and gene expression analysis. Acacia honey inhibited cells proliferation, arrested G0/G1 phase, stimulated cytokines, calcium ion release as well as suppressed p53 and Bcl-2 expression in a dose-dependent manner. We proposed that the molecular mechanism of the antiproliferation potential of Acacia honey on NCI-H460 cell line is due to cell cycle arrest, stimulation of cytokines and calcium ion as well as downregulation of Bcl-2 and p53 genes.

Flavonoid and cardenolide glycosides and a pentacyclic triterpene from the leaves of Nerium oleander and evaluation of cytotoxicity

A pentacyclic triterpene, oleanderocioic acid, two flavonoidal glycosides, quercetin-5-O-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside and kaempferol-5-O-[α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside, and a cardenolide, oleandigoside, together with 11 known compounds, were isolated from the leaves of Nerium oleander. Their structures were elucidated on the basis of spectroscopic analysis. The growth inhibitory and cytotoxic activities of eight compounds were evaluated against the MCF-7 human breast cancer cell line using a sulforhodamine B assay. Three compounds, oleandrin, odoroside A and B were further assayed using a panel of 57 human cancer cell lines.

Acacia Honey Modulates Cell Cycle Progression, Pro-inflammatory Cytokines and Calcium Ions Secretion in PC-3 Cell Lines

Background: Prostate cancer is the most common malignancy in men and the second leading cause of cancer-related deaths. Honey has been proven to have a potentiality of being among the functional foods by both in vivo and in vitro studies. Aim: This study was primarily designed to provide evidence on the apoptotic role of acacia honey on PC-3 cell line. Methods: MTT and mitotic index assay were used to determine the anti-proliferative effects. Cell cycle analysis was conducted on flow cytometer using propidium iodide. Expression of pro-inflammatory cytokines [TNF α and IL 1β] and prostate specific antigen were determined by ELISA kits. Calcium ion level was analyzed by colorimetric method. Results: Our results show the anti-proliferative effects of acacia honey on NIH/3T3 and PC-3 cell lines with the IC 50 of 3.7 and 1.9% [v/v] respectively with simultaneous increase in the secretion of calcium ion and down regulation of prostate specific antigen. Significant [p < 0.05] dose-dependent modulation of G0/G1 phase was observed as compared with the control. However, there was an inverse relationship between TNF-α and IL-1β with latter being up regulated. Mitotic index of PC-3 cells decreased as the concentration of honey increases. Conclusion: Apoptotic role of acacia honey on PC-3 cell line may be due to modulation of G0/G1 phase, proinflammatory cytokines, calcium ions secretion and down regulation of prostate specific antigen in vitro.

Cytotoxic and antioxidant properties of phenolic compounds from Tagetes patula flower

Abstract Context: Tagetes patula Linn. (Asteraceae) (French Marigold) flowers are used by local practitioners for cancer treatment; however, it lacks scientific justification. Objective: Identification of bioactive compounds in T. patula flower for cytotoxic and growth inhibition in human cancer cell lines along with its antioxidant properties using chemical and cell based systems. Materials and methods: The T. patula flower methanol extract, its seven fractions, and three phenolic compounds including methyl protocatechuate (1), patuletin (2), and patulitrin (3) were evaluated using sulforhodamine-B assay against HeLa, HT-144, NCI-H460, MCF-7, PC-3, and SF-268 human cancer cell lines. In parallel, antioxidant activity was evaluated using chemical (DPPH·, deoxyribose, and lipid peroxidation assays) and cell-based chemiluminescence systems (human neutrophils and mice macrophages). Results: The methanol extract and ethyl acetate insoluble fraction exhibited cytotoxic and growth inhibitory effects against HeLa in which 2 exhibited highest cell growth inhibition (GI50: 0.6 ± 0.1 µg/ml) and cytotoxicity (LC50: 2.5 ± 0.1 µg/ml). It also scavenged LOO· (IC50: 6.5 ± 0.7 µg/ml) and (IC50: 27.5 ± 1.3 μg/ml) in chemical systems and human neutrophils, respectively. However, 1 preferably scavenged H2O2–Cl− (IC50: 0.5 ± 0.01 μg/ml) in mice macrophages. Discussion and conclusion: Compound 2 from T. patula flower exhibited both growth inhibitory and cytotoxic properties while 1 and 3 were only growth inhibitory against HeLa. 1–3 also displayed antioxidant properties implying its probable role in growth inhibition/cytotoxic action. The present study provides scientific evidence for the use of T. patula flower in cancer treatment by traditional healer.

Anti-inflammatory and antinociceptive activities of Homalium letestui

Abstract Context. Homalium letestui Pellegr (Flacourtiaceae) is used in various decoctions traditionally by the Ibibios of the Niger Delta of Nigeria to treat stomach ulcer, malaria and other inflammatory diseases, as well as an aphrodisiac. Objective: To investigate the anti-inflammatory and antinociceptive activities of the stem extract of the plant. Materials and methods: The ethanol stem extract (500, 750, 1000 mg/kg, i.p.) of H. letestui was investigated for anti-inflammatory activity using carrageenan, egg albumin-induced and xylene-induced ear edema models and analgesic activity using acetic acid-induced writhing, formalin-induced paw licking and thermal-induced pain models. The ethanol extract was administered to the animals orally, 30 min to 1 h depending on the model, before induction of inflammation/pain. The LD50 was also determined. GC–MS analysis of dichloromethane fraction was carried out. Results: The extract caused a significant (p < 0.05–0.001) reduction of inflammation induced by carrageenan (8.3–70.0%), egg albumin (10.0–71.42%) and xylene (39.39–84.84%). The extract also reduced significantly (p < 0.05–0.001) pain induced by acetic acid (44.22–73.65%), formalin (55.89–79.21%) and hot plate (93.0–214.5%). The LD50 was determined to be 4.38 ± 35.72 g/kg. Discussion and conclusion: The results of this study suggest that the ethanol stem extract of H. letestui possesses anti-inflammatory and analgesic properties which may in part be mediated through the chemical constituents of the plant as revealed by the GC–MS.

Fractionation of acacia honey affects its antioxidant potential in vitro

Abstract Objective To investigate the effects of fractionation of acacia honey on its antioxidant potential in contrast with the pure honey from whole blood, brain and liver in vitro. Methods Honey was partitioned into three fractions (dichloromethane, ethyl acetate and aqueous). Their immuno-modulatory effect on whole blood was assayed using Luminol-amplified chemiluminescence technique. Their antioxidant activities on rat brain and hepatic tissues which covers for catalase, SOD activities and lipid peroxidation. Results Fractions of the honey enhanced the production of radicals with no significant (P>0.05) antioxidant activity on whole blood where as pure honey does. Pure honey significantly (P 0.05) effects on lipid peroxidation. Conclusions Fractionation of acacia honey negatively affects its antioxidant potential thereby making it a radical generating agent in contrast with the unfractionated.

Antioxidant, mitogenic and immunomodulatory potentials of acacia honey

1Department of Biochemistry, University of Ibadan, Ibadan, Oyo State Nigeria 2 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi Pakistan 3 Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi Pakistan 4Department of Biochemistry, Ahmadu Bello University, Zaria, Kaduna State Nigeria Department of Biochemistry, University of Ibadan, Ibadan, Oyo State Nigeria and H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi Pakistan and Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi Pakistan and Department of Biochemistry, Ahmadu Bello University, Zaria, Kaduna State Nigeria

Cytotoxic Cardiac Glycoside from the Parasitic Plant Cuscuta reflexa

Bioassay guided fractionation of the cytotoxic extract of the plant Cuscuta reflexa, employing cytotoxic assay against a panel of 60 cell lines, led to the isolation of 13 compounds identified as odoroside H (1), 21-hydroxyodoroside H (2), neritaloside (3), strospeside (4), 16-β-hydroxydigitoxin (5), N-trans and cis feruloyl tyramines (6 and 7), ethyl caffeate (8), coumarins (9 and 10), ursolic acid (11), β-sitosterol glucoside (12), and 4-O-p-coumaroyl-β-D-glucoside (13). Compound 2 was found to be a new natural product while 1, 3, 4, 5, 6, 7, 10, and 11 are known compounds isolated from this source for the first time. Compounds 1, 3, and 4 possessed very good cytotoxic activity against renal and prostate cancer cell lines. Of these compounds, 1 showed a positive hollow fiber test and was selected for in vivo xenograft testing. The structures of compounds 1–5 have been established through chemical and spectral studies including UV, IR, mass, NMR (1H and 13C), and 2D NMR (COSY-45°, NOESY, HMQC, HMBC, and J-resolved) experiments.

Antiproliferative Activity and Characterization of Metabolites of Aspergillus nidulans: An Endophytic Fungus from Nyctanthes arbor-tristis Linn. against Three Human Cancer Cell Lines

BACKGROUND Endophytic fungi are receiving attention as sources of structurally novel bioactive secondary metabolites towards drug discovery from natural products. This study reports the isolation and characterization of secondary metabolites from an endophytic fungus Aspergillus nidulans, associated with Nyctanthes arbor-tristis Linn., a plant which has a traditional use to cure many ailments including cancer. OBJECTIVE The objective of this study was to evaluate the antiproliferative activity of the metabolites of A. nidulans from N. arbor-tristis on three human cancer cell lines, lung (NCI-H460), breast (MCF-7) and uterine cervix (HeLa), and carry out their characterization. METHODS The extracts of the endophytic fungus cultured on potato dextrose agar were subjected to various chromatographic techniques. Structures of pure compounds were determined using spectroscopic techniques. The non-polar constituents were analyzed by GC-MS. Antiproliferative activity was determined by sulforhodamine B (SRB) assay. RESULTS The extracts and fractions showed moderate to good growth inhibition of the aforementioned human cancer cell lines. The broth extract was most potent (IC50 = 10 ± 3.1 μg/mL and LC50= 95 ± 3.9) against HeLa whereas petroleum ether insoluble fraction of mycelium was most active against NCI-H460 and MCF-7 (IC50 = 10 ± 2.1 µg/mL and 18 ± 3.1 µg/mL respectively). GC-MS led to identify 12 compounds in mycelium and 19 compounds in broth. Four pure compounds were isolated and characterized one compound 5, 10-dihydrophenazine-1-carboxylic acid (1) from broth and three 1-hydroxy-3-methylxanthone (2), ergosterol (3) and sterigmatocystin (4) from mycelium. 1 has not been reported earlier as a plant/fungal metabolite while 2-4 are new from this source. Sterigmatocystin exhibited growth inhibitory effect (IC50 = 50 ± 2.5 µM/mL) against only MCF-7 cell line whereas other compounds had IC50 > 100. CONCLUSIONS In this paper, the cytotoxicity of mycelium and broth constituents of endophytic fungus Aspergillus nidulans from Nyctanthes arbor-tristis is reported for the first time. The study shows that fungus Aspergillus nidulans from Nyctanthes arbor-tristis is capable of producing biologically active natural compounds and provides a scientific rationale for further chemical investigations of endophyte-producing natural products.