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Balanites aegyptiaca (L.) Delile (Zygophyllaceae), is used in traditional medicine for the treatment of intestinal worms, wounds, and inflammatory diseases. The purpose of this study is to assess the anti-proliferative effect and to analyse the pro-apoptotic and cell cycle arrest activities of B. aegyptiaca root bark extract and fractions against colorectal cancer cells HCT-116 and HT-29. The cytotoxicity of the crude extract and fractions were evaluated by MTS assay. The most active fractionwas subjected to crystal violet assay, Hoechst staining, cell cycle arrest, and annexin V/PI assays on cancer cells to highlight its mechanisms of action. The ethyl acetate fraction demonstrated the most cytotoxic effect on HCT-116 and HT-29 with IC50 values ranging between 3 and 4 µg/mL. At 10 µg/mL in the cell cycle arrest assay, the fraction increased G1 phase by 3.83% on HCT-116 and by 8.6% on HT-29 whilst G2/M phase was decreased by 5.63% on HCT-116 and by 6.62% on HT-29. Moreover, apoptotic cells were increased by 11.4% on HCT-116. The results suggest a potential source of anticancer molecules against colorectal cancer for isolation from the ethyl acetate fraction.

Lantana ukambensis (Vatke) Verdc. (Verbenaceae) and Balanites aegyptiaca (L.) Delile (Zygophyllaceae), are used in African traditional medicine for the treatment of wounds and inflammatory diseases. The purpose of this study is to assess the cytotoxicity, cell cycle arrest, and pro-apoptotic effects of the extracts and fractions of these plants against HCT-116 and HT-29 cells. MTS, crystal violet, Hoechst staining, annexin V/PI and cytometry methods were used in this study. The crude extracts of these plants showed significant cytotoxic effects against HCT-116 and HT-29 cells. The 1-butanol and ethyl acetate fractions of L. ukambensis decreased the G1 phase by 20.53% and 28.47% and increased the G2/M by 23.47% and 25.90%, respectively, on HCT-116. Moreover, the 1-butanol fraction increased the cumulative value of apoptotic cells by 49.77% on HCT-116 and the ethyl acetate fraction increased this value by 53.37% at 15 µg/mL after 48 hours of exposure. In the case of B. aegyptiaca, the ethyl acetate fraction increased G1 phase by 3.83% on HCT-116 and by 8.6% on HT-29, whilst G2/M phase was decreased by 5.63 % on HCT-116 and by 6.62% on HT-29. Moreover, apoptotic cells were increased by 11.4% on HCT-116. The outcome of this study suggests the potential of the ethyl acetate fraction of each plant for the isolation of natural anticancer molecules against colorectal cancer.

Oplopanax horridus, widely distributed in North America, is an herbal medicine traditionally used by Pacific indigenous peoples for various medical conditions. After oral ingestion, constituents in O. horridus extract (OhE) could be converted to their metabolites by the enteric microbiome before absorption. In this study, in order to mimic gut environment, the OhE was biotransformed using the enteric microbiome of healthy human subjects. For accurate and reliable data collection with optimized approaches in sample preparation and analytical conditions, ultra-performance liquid chromatography and quadrupole time-of-flight mass spectrometry were used to characterize parent constituents and their metabolites. In the extract, 20 parent compounds were identified including polyynes, sesquiterpenes, monoterpeondids, phenylpropanoids and phenolic acids. After the biotransformation, a total of 78 metabolites were identified, of which 37 belonged to polyynes metabolites. The common biotransformation pathways are hydroxylation, acetylization, methylation and demethylation. Based on the pathway distributions, the metabolism signature of OhE has been explored. The metabolism pathways of OhE compounds are dependent on their structural classifications and hydrophilic/hydrophobic properties. In summary, with comprehensive analysis, we systematically investigated human microbiome-derived OhE metabolites. The enteric microbial metabolism signature provides novel information for future effective use of O. horridus.

Chronic inflammation is recognized as a risk factor for colorectal cancer (CRC) development. Baicalin (BI), a major constituent in an anti-inflammatory herb Scutellaria baicalensis, can be biotransformed into baicalein (BE) by the intestinal microbiota. We evaluated the anti-inflammation and anti-CRC effects of the metabolite BE. The in vitro biotransformation by human intestinal microbiota from BI into BE has been determined with HPLC. Using a gut-specific ApcMin/+ mouse model, the effects of oral BE on the life span, organ index, and tumor multiplicity were evaluated. The expressions of inflammatory cytokines were determined using ELISA. To verify the in vivo data, the anti-inflammatory and antiproliferative effects of BE were determined with an in vitro cell model. HPLC analysis showed that BI was quickly transformed into BE by the intestinal microbiota. Oral BE (30 mg/kg/day) significantly increased the life span, from 125.2 to 218.4 days (P

Lantana ukambensis (Vatke) Verdc. is an African food and medicinal plant. Its red fruits are eaten and highly appreciated by the rural population. This plant was extensively used in African folk medicinal traditions to treat chronic wounds but also as anti-leishmanial or cytotoxic remedies, especially in Burkina Faso, Tanzania, Kenya, or Ethiopia. This study investigates the in vitro bioactivity of polymethoxyflavones extracted from a L. ukambensis as anti-proliferative and pro-apoptotic agents. We isolated two known polymethoxyflavones, 5,6,7,3′,4′,5′-hexamethoxyflavone (1) and 5-hydroxy-6,7,3′,4′,5′-pentamethoxyflavone (2) from the whole plant of L. ukambensis. Their chemical structures were determined by spectroscopic analysis and comparison with published data. These molecules were tested for the anti-proliferative, cytotoxic and pro-apoptotic effects on human cancer cells. Among them, 5-hydroxy-6,7,3′,4′,5′-pentamethoxyflavone (2) was selectively cytotoxic against monocytic lymphoma (U937), acute T cell leukemia (Jurkat), and chronic myelogenous leukemia (K562) cell lines, but not against peripheral blood mononuclear cells (PBMCs) from healthy donors, at all tested concentrations. Moreover, this compound exhibited significant anti-proliferative and pro-apoptotic effects against U937 acute myelogenous leukemia cells. This study highlights the anti-proliferative and pro-apoptotic effects of 5-hydroxy-6,7,3′,4′,5′-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis.

This investigation aims to provide a database of Dozo traditional knowledge of medicinal plants used for the treatment of common diseases.The study was conducted through individual interviews using a survey form. Data were recorded in a database allowing statistical analysis. Each plant was recorded and documented with a herbarium specimen. Settings/LocationSubjects: The term Dozo refers to great hunters from Burkina Faso, highly renowned for their knowledge of medicinal plants. Niamberla village was founded by Dozo hunters and is currently the residence of many traditional healers. Unfortunately, their indigenous knowledge is not well recorded and may be lost between two generations.A total of 16 traditional healers were interviewed, giving 89 recipes for the treatment of 37 diseases. The most common diseases are malaria (13%), psychological/spiritual issues (12%), gastric disorders (11%), sexually transmitted diseases (10%), and wounds (8%). A total of 56 medicinal plants have been identified, consisting mostly of trees (44%), shrubs (34%), and herbs (16%).The results of this research provide a basis for pharmacological and toxicological investigations and are necessary to preserve the indigenous knowledge of traditional medicine among Dozo hunters.

Although considerable effort and progress has been made in the search for new anticancer drugs and treatments in the last several decades, cancer remains a major public health problem and one of the major causes of death worldwide. Many sources, including plants, animals, and minerals, are of interest in cancer research because of the possibility of identifying novel molecular therapeutics. Moreover, structure-activity-relationship (SAR) investigations have become a common way to develop naturally derived or semi-synthetic molecular analogues with improved efficacy and decreased toxicity. In 2012, approximately 138 molecules from marine sources, including isolated compounds and their associated analogues, were shown to be promising anticancer drugs. Among these, 62% are novel compounds. In this report, we review the marine compounds identified in 2012 that may serve as novel anticancer drugs.

Cancer continues to be a major public health problem despite the efforts that have been made in the search for novel drugs and treatments. The current sources sought for the discovery of new molecules are plants, animals and minerals. During the past decade, the search for anticancer agents of marine origin to fight chemo-resistance has increased greatly. Each year, several novel anticancer molecules are isolated from marine organisms and represent a renewed hope for cancer therapy. The study of structure-function relationships has allowed synthesis of analogues with increased efficacy and less toxicity. In this report, we aim to review 42 compounds of marine origin and their derivatives that were published in 2011 as promising anticancer compounds.

Seven new ( 1 – 3 , 5 and 8 – 10 ) and three previously reported ( 4 , 6 and 7 ) 4α-methylated steroids were isolated from the organic extract of the gorgonian Litophyton mollis . The structures and the relative configurations of the isolated natural products were determined on the basis of extensive analyses of their NMR and MS data. Metabolites 1 and 5 – 8 exhibited cytotoxic activity against K562 human chronic myelogenous leukemia cells with IC 50 values below 10 μM, while at the same time displaying low toxicity against healthy PBMCs.

Traditional pharmacopeia is strongly involved in the continuous search for the well being of African populations. The World Health Organization (WHO) estimates that 80% of the population of developing countries relies on traditional medicine for their primary care needs. Medicinal plants are the major resource of this folk medicine where several species are used for the treatment of diseases with an inflammatory and/or infectious component as it is the case of old wounds, skin diseases and malfunctions affecting internal organs such as liver, lung, prostate and kidney. Many of these pathologies described by practitioners of traditional medicine have similarities with certain cancers, but the lack of training of many of these healers does not allow them to establish a link with cancer. However, ethnobotanical and ethnopharmacological surveys conducted by several researchers allowed to identify plants of interest for cancer treatment. Most scientific investigations on these plants demonstrated an anti-inflammatory or antioxidant effect, and sometimes, antiproliferative and cytotoxic activities against cancer cells were reported as well. The emergence of resistance to cancer chemotherapy has forced researchers to turn to natural products of plant and marine origin. In the West African sub-region, research on natural anti-cancer molecules is still in its infancy stage because of very limited financial resources and the scarcity of adequate technical facilities. However, several plants were investigated for their anticancer properties through north-south or south-south partnerships. In this review, we will review the role of West African traditional pharmacopeia in cancer treatment as well as medicinal plants with anti-cancer properties.

Ethnopharmacological relevance Olax mannii Oliv. (Olacaceae) is among the many medicinal plants used in Nigeria for the ethnomedicinal management of both cancer and inflammation. Such plants represent potential sources of innovative therapeutic agents for the treatment of cancer and other malignant disorders. While the majority of medicinal plants exert their anticancer effects by direct cytotoxicity on tumor cells, it is important that other mechanisms through which these plants can exhibit anticancer effects are investigated. Preliminary studies indicated that Olax mannii leaves are rich sources of novel flavonoid glycosides. The detailed chemistry as well the mechanisms through which these flavonoid constituents may exert their cancer chemo-preventive and therapeutic effects are, however, not yet investigated. Aim of the study The aim of this study is to carry out a detailed chemical investigation of Olax mannii leaves and the effects of the isolated constituents on the nuclear factor kappa B (NF-κB) pathway. Materials and methods A methanol leaf extract was subjected to various chromatographic separations to achieve isolation of flavonoid glycosides and the structures of the isolated compounds were elucidated by a combination of 1D and 2D NMR and high resolution mass spectrometry. Biological activities were assessed by measurement of cellular viability and proliferation using quantitative IncuCyte videomicroscopy, trypan blue staining and by quantification of the number of metabolically active K562 cells based on quantitation of ATP. The effect of the compounds on the inhibition of the NF-κB pathway as well as toxicity towards peripheral blood mononuclear cells to evaluate differential toxicity was also assayed. Results Chemical investigation of the methanol leaf extract of the plant material led to the isolation of three new flavonoid triglycosides, kaempferol 3-O-[α- d -apiofuranosyl-(1→2)-α- l -arabinofuranoside]-7-O-α- l -rhamnopyranoside (1), kaempferol 3-O-[β- d -glucopyranosyl-(1→2)-α- l -arabinofuranoside]-7-O-α- l -rhamnopyranoside (2), kaempferol 3-O-[β- d -arabinopyranosyl-(1→4)-α- l -rhamnopyranoside]-7-O-α- l -rhamnopyranoside (3), in addition to fourteen known flavonoid glycosides (4-17). Of all the tested compounds, only compound 9 (kaempferol 3-O-α- l -rhamnopyranoside) exhibited promising and specific antiproliferative activity on human K562 chronic myelogenous leukemia cells and dose-dependently inhibited NF-κB transactivation. Conclusion The presence of this flavonoid glycoside and derivatives may account for the reported efficacy of Olax mannii leaf extract in the ethnomedicinal management of cancer and inflammation.

After ethnobotanical surveys in central and western regions of Burkina Faso, five plants namely Lantana ukambensis (Verbenaceae), Xeoderris sthulmannii (Fabaceae), Parinari curatellifollia (Chrysobalanaceae), Ozoroa insignis (Anacardiaceae), and Ficus platyphylla (Moraceae) were selected for their traditional use in the treatment of parasitic diseases and cancer. Our previous studies have focused on the phytochemical, genotoxicity, antioxidant, and antiproliferative activities of these plants. In this study, the methanol extract of each plant was tested to reveal probable antileishmanial and antitrypanosomal activities. Colorimetric and spectrophotometric methods were used for the detection of antileishmanial and antitrypanosomal activities. Leishmania donovani (LV9 WT) and Trypanosoma brucei brucei GVR 35 were used to test the antileishmanial and antitrypanosomal activities, respectively. All extracts of tested plants showed a significant antitrypanosomal activity with minimum lethal concentrations between 1.5 and 25 μg/ml, the L. ukambensis extract being the most active. In the antileishmanial test, only the extract from L. ukambensis showed significant activity with an inhibitory concentration (IC(50)) of 6.9 μg/ml. The results of this study contribute to the promotion of traditional medicine products and are preliminary for the isolation of new natural molecules for the treatment of leishmaniasis and trypanosomiasis.

The antiproliferative activities of six medicinal plant extracts from Burkina Faso were evaluated in order to justify their traditional use for the treatment of cancer. The SOS chromotest method was used in vitro on Escherichia coli PQ37 to evaluate the mutagenic effect of the plant extracts. The DPPH method was used to evaluate the antioxidant activity of each plant. The antiproliferative activity was evaluated by MTS method on normal cells (Vero and MCR5) and cancer cells (KB) in contact with the extracts for 72 h. The results showed that the studied plants are not genotoxic. Lantana ukambensis and Acacia macrostachya induced a very significant antiproliferative effect against cancer cells with 94% and 95%, respectively. They also developed a strong antioxidant activity. The IC50 values were 5.96 ± 0.40 µg mL−1 for L. ukambensis and 4.30 ± 0.26 µg mL−1 for A. macrostachya. These two plants are therefore potential sources for isolating new antioxidant and anticancer molecules.

This study investigated the general acute, anti-inflammatory, analgesic and antipyretic effects of methanol extract of Lepidagathis anobrya Nees (Acanthaceae). Carrageenan-induced rat paw edema and croton oil-induced ear edema in rats were used for the evaluation of general acute anti-inflammatory effects. Acetic acid-induced writhing response and yeast-induced hyperpyrexia in mice were used to evaluate the analgesic and antipyretic activities respectively. The extract at doses of 10, 25, 50 and 100 mgkg-1 for carrageenan test and doses of 0.5 mg/ear for croton oil test induced a significant reduction (p < 0.001) of paw and ear edemas in rats. In the analgesic and antipyretic tests, the extract has shown a significant inhibition of writhes and hyperpyrexia with all the doses used when compared to the untreated control group. These results clearly show the anti-inflammatory, analgesic and antipyretic effects of the methanol extract of Lepidagathis anobrya and give the scientific basis for its traditional use. Further studies are needed to clarify the mechanism of action and the components responsible for these pharmacological effects.