Abiodun Falodun

Proliferative effects of five traditional Nigerian medicinal plant extracts on human breast and bone cancer cell lines

ETHNOPHARMACOLOGICAL RELEVANCE The medicinal plants Hunteria umbellata (HUL), Cola lepidota (CCL), Persea americana leaf (PAL), Root bark of Persea americana (RPA) and Plukenetia conophora (PCL) are used in Nigerian traditional medicine for the treatment of cancer and cancer related diseases. AIM OF THE STUDY To scientifically evaluate the cell proliferative and apoptotic effects of the plants extracts using breast and osteocarcinoma cell lines, and also to identify the possible components via LC-MS to have a kind of chemical fingerprint. MATERIALS AND METHODS The antiproliferative and apoptotic effects of methanolic extracts (10 μg/ml) of the five medicinal plants were subjected to in vitro evaluation using four cancer cell lines (breast-MCF-7 and BT-20; Osteocarcinoma-MG-63 and Saos-2) measured by flow cytometry. Non-tumorigenic controls MCF-12A and primary isolated osteoblasts (POB) were chosen to eliminate negative influence on healthy tissue. RESULTS Of the five extracts RPA demonstrated a significant (P<0.05) anti-proliferative activity against estrogen receptor positive breast cancer cell lines (MCF-7). The proliferative phase was decreased by 18%, whereas, a significant increase in cell proliferation (about 27%) was observed for RPA at a concentration of 10 μg/ml. PCL, CCL, HUL and PAL did not show marked inhibition of the proliferation of cell line MCF-7. CONCLUSION These results give suggestive evidence that the plant extracts exhibit some correlation between the claimed ethnomedicinal uses and the cell proliferative activity. RPA extract includes chemical compounds with estrogen-like activity and validates its potential use as anticancer agent, particularly against breast carcinoma; provided important information potentially helpful in drug designing and discovery. Further studies will involve the isolation of anti tumour compounds in RPA by LC-MS and detailed mechanism of anticancer activities.

Anticancer activity of five forest crops used in African folklore: antiproliferative and pro-apoptotic effects

Acalypha wilkesiana, Caesalpinia bonduc, Jatropha multifida, Momordica charantia and Picralima nitida used in African folklore for treating cancer were investigated. All extracts except J. multifida resulted in no significant alteration in cell cycle distribution and apoptosis in MCF-7 and BT-20. The J. multifilda (JMR-Ch) caused cell cycle arrest at G1 checkpoint and apoptosis in MCF-7. Slight changes in the integrin expression of MCF-7 after treatment with 1 and 10 μg/mL of JMR-Ch were observed. Fluorescence-activated confocal microscopy shows changes in cell morphology and β1 integrin localisation within MCF-7 cells after exposure to 10 and 25 μg/mL of JMR-Ch. JMR-Ch (1 μg/mL) treatment resulted in time-dependent decrease in cell acidification and respiration in MCF-7 cells and a time-dependent decrease in BT-20 cell respiration, while in MCF-10A, there was an enhancement of acidification. These results revealed the probable application of JMR-Ch in cancer therapy.

Synthesis and Spectroscopic Characterization of Arylated Selenoureas

Abstract Selenoureas were prepared from isoselenocyanates and structurally characterized by spectroscopic methods and by X-ray crystal structure analyses. GRAPHICAL ABSTRACT

Synthesis of Functionalized Acetophenones by Formal [3+3] Cyclocondensations of 1,3-Bis(silyloxy)-1,3-butadienes with 3-Alkoxyand 3-Silyloxy-2-acetyl-2-en-1-ones

The TiCl4-mediated cyclization of 1,3-bis(silyloxy)-1,3-butadienes with 2-acetyl-1-silyloxybut-1- en-3-one and 3-acetyl-4-silyloxypent-3-en-2-one, readily available from 3-(formyl)acetylacetone and 3-(acetyl)acetylacetone (triacetylmethane), afforded a variety of functionalized acetophenones Graphical Abstract Synthesis of Functionalized Acetophenones by Formal [3+3] Cyclocondensations of 1,3-Bis(silyloxy)-1,3-butadienes with 3-Alkoxyand 3-Silyloxy-2-acetyl-2-en-1-ones

Anti-proliferative and Pro-apoptotic Effects of Caesalpinia bonduc Extract and its Fractions in Estrogen-Sensitive Human Breast Adenocarcinoma Cell Line

A study was conducted to determine proximate analysis, apoptotic, and anti-proliferative effect of Caesalpinia bonduc against human breast cancer cell line (MCF-7) in an in vitro model. The MCF-7 cells were treated with plant extract at 10 μg.mL−1 for 48 h and dimethylsulfoxide (DMSO) serving as control. The percentage of cells in the various phases was determined by flow cytometry. Results obtained from the flow cytometric analysis showed that chloroform fraction was the most active fraction against MCF-7 cells with 32.86 % decrease in proliferative phase. The apoptotic cells were calculated based on the appearance of the cells in sub-G1 phase. The result showed no significant pro-apoptotic effects in treated groups and control group. The finding suggested that the mechanism of cell death is probably through a mechanism other than the direct induction of apoptosis in tumor cell. The finding showed that C. bonduc extract at 10 μg.mL−1 induced anti-proliferative effect on MCF-7 cells by arresting the cell cycle at G2/M phase to prevent cell transition from G2 to M phase, thereby contributing less to cell division rather than DNA synthesis.

Berberis orthobotrys – A promising herbal anti-tumorigenic candidate for the treatment of pediatric alveolar rhabdomyosarcoma

ETHNOPHARMACOLOGICAL RELEVANCE Berberis orthobotrys (BORM) is a medical plant with a long history in traditional usage for the treatment of wounds, cancer, gastrointestinal malady and several other diseases. Our previous studies identified the endemic Pakistani plant Berberis orthobotrys Bien. ex Aitch. as promising source for the treatment of breast cancer and osteosarcoma. AIM OF THE STUDY The present study was aimed to evaluate the anti-cancer properties of 26 plant derived extracts and compounds including the methanolic root extract of Berberis orthobotrys (BORM) on pediatric alveolar rhabdomyosarcoma (RMA), which is known to develop drug resistance, metastatic invasion and potential tumor progression. MATERIALS AND METHODS The main anti-tumor activity of BORM was verified by focusing on morphological, cell structural and metabolic alterations via metabolic profiling, cell viability measurements, flow cytometry, western blotting and diverse microscopy-based methods using the human RMA cell line Rh30. RESULTS Exposure of 25 µg/ml BORM exerts an influence on the cell stability, the degradation of oncosomes as well as the shutdown of the metabolic activity of RMA cells, primarily by downregulation of the energy metabolism. Therefore glycyl-aspartic acid and N-acetyl serine decreased moderately, and uracil increased intracellularly. On healthy, non-transformed muscle cells BORM revealed very low metabolic alterations and nearly no cytotoxic impact. Furthermore, BORM is also capable to reduce Rh30 cell migration (~50%) and proliferation (induced G2/M cycle arrest) as well as to initiate apoptosis confirmed by reduced Bcl-2, Bax and PCNA expression and induced PARP-1 cleavage. CONCLUSIONS The study provides the first evidence, that BORM treatment is effective against RMA cells with low side effects on healthy cells.

Crystal structure and Hirshfeld surface analysis of the naturally occurring cassane-type diterpenoid, 6β-cinnamoyl-7β-hy­droxy­vouacapen-5α-ol

The title compound, a cassane-type diterpenoid, was isolated from a medicinally important plant, Caesalpinia pulcherrima (Fabaceae). In the molecule, the three cyclohexane rings are trans-fused and adopt chair, chair and half chair conformations.

Antiprotozoal and Cytotoxicity Studies of Fractions and Compounds from Enantia chlorantha

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, 300001, Nigeria. National Center for Natural Products Research, Institute of Pharmaceutical Sciences, University of Mississippi, 38677, USA. Pharmacognosy Department, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt. Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Campbell University, Buies Creek, NC 27506, USA. Department of Bio-Molecular Sciences, School of Pharmacy, University of Mississippi, 38677, USA. Office of Global engagement, University of Mississippi, 38677, USA.

Documentation of Ethnoveterinary Practices in the CKNP Region, Gilgit-Baltistan

Majority of the livestock holders in different areas of Central Karakoram National Park (CKNP) region in Gilgit-Baltistan lack the modern veterinary healthcare facilities. The local community mostly depends upon the traditional floral therapeutic veterinary practices for the cure of various livestock diseases. The lack of the ethnoveterinary surveys in the CKNP region results in loss in the scientific documentation of the traditional information and practices about the livestock healthcare. The present study deals with the documentation of the livestock diseases and the ethnoveterinary herbal and non-herbal therapeutic practices by the livestock holders in CKNP region. The study was conducted from March 2012 to March 2013 in the valleys of CKNP region. The ethnoveterinary data was collected through the semi-structured questionnaires and the techniques of interviews and field visits. And the productive interaction provided an enabling background for the successful Rapid Rural Appraisal and Participatory Rural Appraisal research. Total 156 local community members were interviewed in Thallay, Khaplu, Hushe and Shigar valleys. The survey showed the prevalence of the most common diseases e.g. FMD, intestinal problems etc. Among the 51 medicinal plants, the Asteraceae family exhibited the highest number of genera with the therapeutic species. The parts of the plants that were most frequently used for the therapeutic purposes were the leaves (55%), seed (15%) etc. The present study contributed to the documentation of the medicinal plants used in the ethnoveterinary practices in valleys in CKNP region, Gilgit-Baltistan.

Crystal structure and Hirshfeld surface analysis of pulcherrin J

The natural diterpene known as pulcherrin J was isolated from stem barks of medicinally important Caesalpinia pulcherrima (L.). The molecule is composed of a central core of three trans-fused cyclohexane rings and a near planar five-membered furan ring, along with an axially oriented cinnamate moiety and ahydroxyl substituent attached to the C-8 and C-9 positions of the steroid ring system, respectively. Hirshfeld surface analysis indicates that the most significant contacts in packing are H⋯H (67.5%), followed by C⋯H (19.6%) and H⋯O (12.9%).