Immunosuppressive and hepatoprotective potential of Sarcococca saligna and its biomarker components.

Sarcococca saligna methanolic extract, fractions and isolated pure compounds saracocine (1), saracodine (2), pachyximine-A (3) and terminaline (4) were found to possess potent immunosuppressive activities. The fractions and compounds were tested in-vitro for their effects on human T-cell proliferation, and cytokine (IL-2) production. All the fractions, sub-fractions and purified compounds showed significant suppressive effect on IL-2 production in a dose-dependent manner. They also exhibited a suppressive effect on the phytohemagglutinin-stimulated T-cell proliferation. None of the extracts and purified compounds showed any cytotoxicity effects on the 3T3 mice fibroblast cell line. The crude extract, DCM fraction (pH9), DCM fractions (pH7) and one of the steroidal alkaloids (terminaline) were checked in-vivo for their hepato-protective potential against CCl4-induced liver injury. In in-vivo experiments, the basic and neutral DCM fractions and terminaline (4) significantly reduced inflammation in the liver. DCM fraction (pH9), DCM fractions (pH7) and compound 4 reduced the serum enzyme levels (ALT, AST, and ALP) down to control levels despite CCl4 treatment. They also reduced the CCl4-induced damaged area to almost zero as assessed by histopathology. The pale necrotic areas and mixed inflammatory infiltrate which are seen after CCl4 treatment were absent in the cases of basic, neutral fractions and terminaline treatment. These hepato-protective effects were better than the positive control silymarin. Our results suggest the therapeutic effect of S. saligna extract, fractions and bioactive steroidal alkaloids against CCl4-induced liver injury in vivo and their immunosuppressive function in vitro.

Cytotoxic and antioxidant properties of phenolic compounds from Tagetes patula flower.

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 [Formula: see text] (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.

Antimycobacterial activity of selected medicinal plants traditionally used in Sudan to treat infectious diseases.

ETHNOPHARMACOLOGICAL RELEVANCE: The emergence of multidrug-resistant strains of Mycobacterium tuberculosis underscores the need for continuous development of new and efficient methods to determine the susceptibility of isolates of Mycobacterium tuberculosis in the search for novel antimycobacterial agents. Natural products constitute an important source of new drugs, and design and implementation of antimycobacterial susceptibility testing methods are necessary to evaluate the different extracts and compounds. In this study we have explored the antimycobacterial properties of 50 ethanolic extracts from different parts of 46 selected medicinal plants traditionally used in Sudan to treat infectious diseases. MATERIALS AND METHODS: Plants were harvested and ethanolic extracts were prepared. For selected extracts, fractionation with hydrophilic and hydrophobic solvents was undertaken. A luminometry-based assay was used for determination of mycobacterial growth in broth cultures and inside primary human macrophages in the presence or absence of plant extracts and fractions of extracts. Cytotoxicity was also assessed for active fractions of plant extracts. RESULTS: Of the tested extracts, three exhibited a significant inhibitory effect on an avirulent strain of Mycobacterium tubercluosis (H37Ra) at the initial screening doses (125 and 6.25µg/ml). These were bark and leaf extracts of Khaya senegalensis and the leaf extract of Rosmarinus officinalis L. Further fractions of these plant extracts were prepared with n-hexane, chloroform, ethyl acetate, n-butanol, ethanol and water, and the activity of these extracts was retained in hydrophobic fractions. Cytotoxicity assays revealed that the chloroform fraction of Khaya senegalensis bark was non-toxic to human monocyte-derived macrophages and other cell types at the concentrations used and hence, further analysis, including assessment of IC50 and intracellular activity was done with this fraction. CONCLUSION: These results encourage further investigations to identify the active compound(s) within the chloroform fraction of Khaya senegalensis bark.

Cellular reactive oxygen species inhibitory constituents of Hypericum thasium Griseb.

The phytochemical investigation of the ethyl acetate extract of Hypericum thasium has led to the characterization of four benzophenone derivatives 1-4, a known benzophenone 5 and four known flavonoids, quercetin (6), quercitrin (7), isoquercetin (8), and 3, 8''-biapigenin (9). Lucigenin- and luminal-based chemiluminescence assays were employed to monitor the inhibitory activity of these compounds towards the production of reactive oxygen species (ROS) by human polymorphoneutrophils (PMNs). The assay results showed that benzophenones 1 and 3 are extracellular inhibitors of ROS production, while flavonoids 6, 8, and 9 can modulate intracellular ROS production.