In Vitro Studies on Antioxidant and Anti-Parasitic Activities of Compounds Isolated from Rauvolfia caffra Sond.

As part of an ongoing study of natural products from local medicinal plants, the methanol extract of stem bark of Rauvolfia caffra Sond was investigated for biological activity. Column chromatography and preparative thin-layer chromatography were used to isolate lupeol (1), raucaffricine (2), N-methylsarpagine (3), and spegatrine (4). The crude extract, fractions and isolated compounds were tested for anti-oxidant, antitrypanosomal and anti-proliferation activities. Two fractions displayed high DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity and reducing power with IC50 (The half maximal inhibitory concentration) and IC0.5 values of 0.022 ± 0.003 mg/mL and 0.036 ± 0.007 mg/mL, and 0.518 ± 0.044 mg/mL and 1.076 ± 0.136 mg/mL, respectively. Spegatrine (4) was identified as the main antioxidant compound in R. caffra with IC50 and IC0.5 values of 0.119 ± 0.067 mg/mL and 0.712 ± 0 mg/mL, respectively. One fraction displayed high antitrypanosomal activity with an IC50 value of 18.50 µg/mL. However, the major constituent of this fraction, raucaffricine (2), was not active. The crude extract, fractions and pure compounds did not display any cytotoxic effect at a concentration of 50 µg/mL against HeLa cells. This study shows directions for further in vitro studies on the antioxidant and antitrypanosomal activities of Rauvolfia caffra Sond.

Isolation, Chemical Profile and Antimalarial Activities of Bioactive Compounds from Rauvolfia caffra Sond.

In this study, the chemical profile of a crude methanol extract of Rauvolfia caffra Sond was determined by ultra-performance liquid chromatography-mass spectrometry (UPLC-MS). Column chromatography and preparative thin layer chromatography were used to isolate three indole alkaloids (raucaffricine, N-methylsarpagine and spegatrine) and one triterpenoid (lupeol). The antiplasmodial activity was determined using the parasite lactate dehydrogenase (pLDH) assay. The UPLC-MS profile of the crude extract reveals that the major constituents of R. caffra are raucaffricine (m/z 513.2) and spegatrine (m/z 352.2). Fraction 3 displayed the highest antiplasmodial activity with an IC50 of 6.533 µg/mL. However, raucaffricine, isolated from the active fraction did not display any activity. The study identifies the major constituents of R. caffra and also demonstrates that the major constituents do not contribute to the antiplasmodial activity of R. caffra.

The genus Pluchea: phytochemistry, traditional uses, and biological activities.

In this review, literature data on phytochemical and biological investigations on the genus Pluchea are compiled. Pluchea is a genus of flowering plants in the Asteraceae family and comprises ca. 80 species distributed mainly in Northern and Southern America, Africa, Asia, and Australia. Sesquiterpenoids and flavonoids are the main constituents of this genus. Compounds isolated from plants of the Pluchea genus display a variety of biological properties, viz., anticancer, antileishmanial, immunosuppressive, antioxidant, anti-acetylcholinesterase, antimicrobial, trypanocidal, hepatoprotective, cytotoxic, larvicidal, anti-ulcer, anti-inflammatory, and antinociceptive activities.

Isolation and relative stereochemistry of lippialactone, a new antimalarial compound from Lippia javanica.

The aerial parts of Lippia javanica were investigated for biologically active chemical compounds present in them. Chromatographic separation of the ethyl acetate extract of the aerial parts yielded a new antimalarial α-pyrone, lippialactone (2). Lippialactone is active against the chloroquine-sensitive D10 strain of Plasmodium falciparum with an IC50 value of 9.1 µg/mL, and is also mildly cytotoxic. The relative stereochemistry of lippialactone was determined by molecular modeling based on the determination of the relative configuration by quantum mechanical GIAO (13)C chemical shift calculations.

Chemistry and biology of genus Vismia.

CONTEXT: Many herbal remedies have been employed in the treatment and management of various human ailments since the beginning of human civilization. Vismia is an extensive genus of the family Hypericaceae and consists of small trees inhabiting the tropical and subtropical regions of South and Central America. Within the framework of an International Cooperative Biodiversity Groups project, three Vismia species were studied for their potential anticancer activity. OBJECTIVES: This review is an extensive study of the available scientific literature published and comprises of the ethnopharmacological, phytochemical and therapeutic potential of genus of plants under the umbrella Vismia. METHODS: The present review includes 134 natural products with 47 references compiled from the major databases, viz., Chemical Abstracts, Science Direct, SciFinder, PubMed, Dr. Dukes Phytochemical and Ethnobotany, CIMER, and InteliHealth. RESULTS: An exhaustive survey of the accessed literature revealed that flavonoids, flavanols, xanthones, anthraones, anthraquinones, benzophenones, lignans, steroids, monoterpenes and triterpenes constituted the major classes of phytoconstituents of this genus. Pharmacological reports revealed that it is used for skin diseases such as dermatitis, leprosy, syphilis, herpes, scabies and eczemas, and as an anticancer for human breast, CNS, and lung cancer cell lines. CONCLUSION: Genus Vismia plants seem to hold great potential for an in-depth investigation towards discovering biological activities, especially for the treatment of cancers affecting our society. Through this review, the authors hope to attract the attention of natural product researchers throughout the world to focus on the unexplored potential of Vismia plants, with the view of developing new formulations with an improved therapeutic value.

Phomosines H-J, novel highly substituted biaryl ethers, isolated from the endophytic fungus Phomopsis sp. from Ligustrum vulgare.

From the endophytic fungus Phomosis sp., four known phomosines A-D (1-4) and three new phomosines H-J (5-7) have been isolated. The structures of the new compounds were determined on the basis of their spectroscopic data analysis (1H, 13C, 1H-1H COSY, HMQC, and HMBC NMR, as well as mass spectrometry). The structures of phomosine H (5) and J (7) were also confirmed by semisynthesis from phomosine A (1). The remaining four known compounds [phomosines A-D (1-4)] were identified by comparing their spectroscopic data with those reported in the literature. The four known metabolites were biologically active. Of the novel metabolites, only 6 was antifungal and antibacterial.

Composition and antimicrobial activities of volatile components of Lippia javanica.

The volatile oil of Lippia javanica was prepared by hydrodistillation of leaves, flowers and stems, and characterized by GC-MS. The major component was 3-methyl-6-(1-methylethylidene)-cyclohex-2-en-1-one. The oil was tested for antimicrobial activity on cultures of Escherichia coli, Bacillus subtilis and Staphylococcus aureus, and found to inhibit E. coli and S. aureus at 1% dilution. The oil was also active against Plasmodium falciparum in micromolar concentrations.