Biological Activity and Isolation of Compounds from Stem Bark of Plumeria acutifolia.

BACKGROUND: Plumeria acutifolia (Apocynaceae) is an ornamental plant, used in the traditional medicine and known to have a variety of constituents as alkaloids, flavonoids, and iridoids. Extracts of this plant were proved to have antimicrobial and anticancer activities. OBJECTIVES: This research was conducted for the evaluation of the biological activities of P. acutifolia stem bark and isolation and structural elucidation of various chemical compounds from the biologically active fractions. MATERIALS AND METHODS: Methanol extract of stem bark of P. acutifolia was successively fractionated with petroleum ether, dichloromethane, ethyl acetate, and n-butanol. The fractions were evaluated for their antimicrobial, cytotoxic, and antioxidant activities. Fractions with promising biological activities were subjected to chromatographic techniques for the isolation of compounds, followed by structural elucidation using several spectroscopic techniques. RESULTS: P. acutifolia stem bark showed a significant antimicrobial activity, where the ethyl acetate fraction was active against Syncephalastrum racemosum (7.81 µg/ml) and Escherichia coli (3.9 µg/ml). The cytotoxic activity against HEPG-2, HCT-116, and MCF-7 cell lines was highest in the petroleum ether fraction, using concentrations of 1, 2.5, 5, and 10 µl/ml. The antioxidant activity was concentration dependent; ethyl acetate fraction showed the most predominant effect, with an IC50 of 197.1 µg/ml. Five compounds were identified as narcissin (1), quercitrin (2), sweroside (3), gaertneroside (4), and plumieride (5). CONCLUSION: P. acutifolia was proved to have significant antimicrobial, cytotoxic, and antioxidant activities; the isolated compounds were flavonoids, iridoids, and secoiridoid, some of which were reported for the first time in genus Plumeria and/or family Apocynaceae. SUMMARY: P. acutifolia stem bark showed a significant antimicrobial activity, where the ethyl acetate fraction was active against Syncephalastrum racemosum and Escherichia coli. The cytotoxic activity against HEPG-2, HCT-116, and MCF-7 cell lines was highest in the petroleum ether fraction. The antioxidant activity was concentration dependent; ethyl acetate fraction showed the most predominant effect. Five compounds were identified as narcissin (1), quercitrin (2), sweroside (3), gaertneroside (4), and plumieride (5). Abbreviations used: mp: Melting point, NMR: Nuclear magnetic resonance, s: Singlet, d: Double, t: Triplet, q: Quartet, dd: Double-double, m: Multiplet, br: Broad.

In vitro anti-proliferative activities of Aloe perryi flowers extract on human liver, colon, breast, lung, prostate and epithelial cancer cell lines.

Natural products, especially plant extracts have offered vast opportunities in the field of drug development due to its chemical diversity. The genus Aloe has for long been used for medicinal purposes in different parts of the world. The present study was designed to investigate the phytochemicals and anti-cancer potential of Aloe perryi flowers. The phytochemical analysis revealed the presence of carbohydrates, glycosides, phytosterols, phenols, flavonoids and proteins. While alkaloids and saponins were absent. The percentage inhibition of various extracts (viz. petroleum ether, chloroform, ethyl acetate, butanol and aqueous) of A. perryi flowers on seven human cancer cell lines (HepG2, HCT-116, MCF-7, A549, PC-3, HEp-2 and HeLa) has been evaluated using MTT assay. All the extracts significantly inhibit the proliferation of cancer cells in a concentration-dependent manner. The petroleum ether extract was most active, where the inhibition was recorded as 92.6%, 93.9%, 92%, 90.9%, 88.9%, 82% and 85.7% for HepG2, HCT-116, MCF-7, A-549, PC-3, HEp-2 and HeLa cells, respectively. The results also revealed that HCT-116 cells were more sensitive among all the cell lines studied.

Portulaca oleracea Seed Oil Exerts Cytotoxic Effects on Human Liver Cancer (HepG2) and Human Lung Cancer (A-549) Cell Lines.

Portulaca oleracea (Family: Portulacaceae), is well known for its anti-inflammatory, antioxidative, anti- bacterial, and anti-tumor activities. However, cytotoxic effects of seed oil of Portulaca oleracea against human liver cancer (HepG2) and human lung cancer (A-549) cell lines have not been studied previously. Therefore, the present study was designed to investigate the cytotoxic effects of Portulaca oleracea seed oil on HepG2 and A-549 cell lines. Both cell lines were exposed to various concentrations of Portulaca oleracea seed oil for 24h. After the exposure, percentage cell viability was studied by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT), neutral red uptake (NRU) assays, and cellular morphology by phase contrast inverted microscopy. The results showed a concentration-dependent significant reduction in the percentage cell viability and an alteration in the cellular morphology of HepG2 and A-549 cells. The percentage cell viability was recorded as 73%, 63%, and 54% by MTT assay and 76%, 61%, and 50% by NRU assay at 250, 500, and 1000 µg/ml, respectively in HepG2 cells. Percentage cell viability was recorded as 82%, 72%, and 64% by MTT assay and 83%, 68%, and 56% by NRU assay at 250, 500, and 1000 µg/ml, respectively in A-549 cells. The 100 µg/ml and lower concentrations were found to be non cytotoxic to A-549 cells, whereas decrease of 14% and 12% were recorded by MTT and NRU assay, respectively in HepG2 cells. Both HepG2 and A-549 cell lines exposed to 250, 500, and 1000 µg/ ml of Portulaca oleracea seed oil lost their normal morphology, cell adhesion capacity, become rounded, and appeared smaller in size. The data from this study showed that exposure to seed oil of Portulaca oleracea resulted in significant cytotoxicity and inhibition of growth of the human liver cancer (HepG2) and human lung cancer (A-549) cell lines.

Cytotoxicity assessments of Portulaca oleracea and Petroselinum sativum seed extracts on human hepatocellular carcinoma cells (HepG2).

The Pharmacological potential, such as antioxidant, anti-inflammatory, and antibacterial activities of Portulaca oleracea (PO) and Petroselinum sativum (PS) extracts are well known. However, the preventive properties against hepatocellular carcinoma cells have not been explored so far. Therefore, the present investigation was designed to study the anticancer activity of seed extracts of PO and PS on the human hepatocellular carcinoma cells (HepG2). The HepG2 cells were exposed with 5-500 µg/ml of PO and PS for 24 h. After the exposure, cell viability by 3-(4,5-dimethylthiazol-2yl)-2,5-biphenyl tetrazolium bromide (MTT) assay, neutral red uptake (NRU) assay, and cellular morphology by phase contrast inverted microscope were studied. The results showed that PO and PS extracts significantly reduced the cell viability of HepG2 in a concentration dependent manner. The cell viability was recorded to be 67%, 31%, 21%, and 17% at 50, 100, 250, and 500 µg/ml of PO, respectively by MTT assay and 91%, 62%, 27%, and 18% at 50, 100, 250, and 500 µg/ml of PO, respectively by NRU assay. PS exposed HepG2 cells with 100 µg/ml and higher concentrations were also found to be cytotoxic. The decrease in the cell viability at 100, 250, and 500 µg/ml of PS was recorded as 70%, 33%, and 15% by MTT assay and 63%, 29%, and 17%, respectively by NRU assay. Results also showed that PO and PS exposed cells reduced the normal morphology and adhesion capacity of HepG2 cells. HepG2 cells exposed with 50 µg/ml and higher concentrations of PO and PS lost their typical morphology, become smaller in size, and appeared in rounded bodies. Our results demonstrated preliminary screening of anticancer activity of Portulaca oleracea and Petroselinum sativum extracts against HepG2 cells, which can be further used for the development of a potential therapeutic anticancer agent.

Cytotoxicity of Nigella sativa seed oil and extract against human lung cancer cell line.

Nigella sativa (N sativa), commonly known as black seed, has been used in traditional medicine to treat many diseases. The antioxidant, anti-inflammatory, and antibacterial activities of N sativa extracts are well known. Therefore, the present study was designed to investigate the anticancer activity of seed extract (NSE) and seed oil (NSO) of N sativa against a human lung cancer cell line. Cells were exposed to 0.01 to 1 mg/ml of NSE and NSO for 24 h, then percent cell viability was assessed by 3-(4, 5-dimethylthiazol-2yl)-2, 5-biphenyl tetrazolium bromide (MTT) and neutral red uptake (NRU) assays, and cellular morphology by phase contrast inverted microscopy. The results showed NSE and NSO significantly reduce the cell viability and alter the cellular morphology of A-549 cells in a concentration dependent manner. The percent cell viability was recorded as 75%, 50%, and 26% at 0.25, 0.5, and 1 mg/ml of NSE by MTT assay and 73%, 48%, and 23% at 0.25, 0.5, and 1 mg/ml of NSE by NRU assay. Exposure to NSO concentrations of 0.1 mg/ml and above for 24 h was also found to be cytotoxic. The decrease in cell viability at 0.1, 0.25, 0.5, and 1 mg/ml of NSO was recorded to be 89%, 52%, 41%, and 13% by MTT assay and 85%, 52%, 38%, and 11% by NRU assay, respectively. A-549 cells exposed to 0.25, 0.5 and 1 mg/ml of NSE and NSO lost their typical morphology and appeared smaller in size. The data revealed that the treatment of seed extract (NSE) and seed oil (NSO) of Nigella sativa significantly reduce viability of human lung cancer cells.

Anticancer activity of Petroselinum sativum seed extracts on MCF-7 human breast cancer cells.

Pharmacological and preventive properties of Petroselinum sativum seed extracts are well known, but the anticancer activity of alcoholic extracts and oil of Petroselinum sativum seeds on human breast cancer cells have not been explored so far. Therefore, the present study was designed to investigate the cytotoxic activities of these extracts against MCF-7 cells. Cells were exposed to 10 to 1000 µg/ml of alcoholic seed extract (PSA) and seed oil (PSO) of Petroselinum sativum for 24 h. Post-treatment, percent cell viability was studied by 3-(4, 5-dimethylthiazol-2yl)-2, 5-biphenyl tetrazolium bromide (MTT) and neutral red uptake (NRU) assays, and cellular morphology by phase contrast inverted microscopy. The results showed that PSA and PSO significantly reduced cell viability, and altered the cellular morphology of MCF-7 cells in a concentration dependent manner. Concentrations of 50 µg/ml and above of PSA and 100 µg/ml and above of PSO were found to be cytotoxic in MCF-7 cells. Cell viability at 50, 100, 250, 500 and 1000 µg/ml of PSA was recorded as 81%, 57%, 33%, 8% and 5%, respectively, whereas at 100, 250, 500, and 1000 µg/ml of PSO values were 90%, 78%, 62%, and 8%, respectively by MTT assay. MCF-7 cells exposed to 250, 500 and 1000 µg/ml of PSA and PSO lost their typical morphology and appeared smaller in size. The data revealed that the treatment with PSA and PSO of Petroselinum sativum induced cell death in MCF-7 cells.

In vitro cytotoxic activity of seed oil of fenugreek against various cancer cell lines.

In the present study, investigations were carried out to screen the anticancer activities of fenugreek seed oil against cancer cell lines (HEp-2, MCF-7, WISH cells), and a normal cell line (Vero cells). Cytotoxicity was assessed with MTT and NRU assays, and cellular morphological alterations were studied using phase contrast light microscopy. All cells were exposed toi 10-1000 µg/ml of fenugreek seed oil for 24 h. The results show that fenugreek seed oil significantly reduced the cell viability, and altered the cellular morphology in a dose dependent manner. Among the cell lines, HEp-2 cells showed the highest decrease in cell viability, followed by MCF-7, WISH, and Vero cells by MTT and NRU assays. Cell viability at 1000 µg/ml was recorded as 55% in HEp-2 cells, 67% in MCF-7 cells, 75% in WISH cells, and 86% in Vero cells. The present study provides preliminary screening data for fenugreek seed oil pointing to potent cytotoxicity against cancer cells.