Ethnomedicinal uses, phytochemistry, pharmacological activities and toxicological profile of Glycosmis pentaphylla (Retz.) DC.: A review.

ETHNOPHARMACOLOGICAL RELEVANCE: Glycosmis pentaphylla (Retz.) DC. is a perennial shrub indigenous to the tropical and subtropical regions of India, China, Sri Lanka, Myanmar, Bangladesh, Indonesia, Malaysia, Thailand, Vietnam, Philippine, Java, Sumatra, Borneo and Australia. The plant is used extensively within these regions as a traditional medicine for the treatment of a variety of ailments including cough, fever, chest pain, anemia, jaundice, liver disorders, inflammation, bronchitis, rheumatism, urinary tract infections, pain, bone fractures, toothache, gonorrhea, diabetes, cancer and other chronic diseases. AIM OF THE REVIEW: This review aims to present up-to-date information regarding the taxonomy, botany, distribution, ethnomedicinal uses, phytochemistry, pharmacology and toxicological profile of G. pentaphylla. The presented information was analyzed critically to understand current work undertaken on this species and explore possible future prospects for this plant in pharmaceutical research. MATERIALS & METHODS: Bibliographic databases, including Google Scholar, PubMed, Web of Science, ScienceDirect, SpringerLink, Wiley Online Library, Semantic Scholar, Europe PMC, Scopus, and MEDLINE, were explored thoroughly for the collection of relevant information. The structures of phytoconstituents were confirmed with PubChem and SciFinder databases. Taxonomical information on the plant was presented in accordance with The Plant List (version 1.1). RESULTS: Extensive phytochemical investigations into different parts of G. pentaphylla have revealed the presence of at least 354 secondary metabolites belonging to structurally diverse classes including alkaloids, amides, phenolic compounds, flavonoids, glycosides, aromatic compounds, steroids, terpenoids, and fatty derivatives. A large number of in vitro and in vivo experiments have demonstrated that G. pentaphylla had anticancer, antimutagenic, antibacterial, antifungal, anthelmintic, mosquitocidal, antidiabetic, antihyperlipidemic, anti-oxidant, anti-inflammatory, analgesic, antipyretic, anti-arsenicosis, and wound healing properties. Toxicological studies have established the absence of any significant adverse reactions and showed that the plant had a moderate safety profile. CONCLUSIONS: G. pentaphylla can be suggested as a source of inspiration for the development of novel drugs, especially anticancer, antimicrobial, anthelmintic, and mosquitocidal agents. Moreover, bioassay-guided investigations into its diverse classes of secondary metabolites, especially the large pool of nitrogen-containing alkaloids and amides, promises the development of novel drug candidates. Future pharmacological studies into this species are also warranted as many of its traditional uses are yet to be validated scientifically.

Ethnomedicinal uses, phytochemistry, and pharmacology of the genus Vepris (Rutaceae): A review.

ETHNOPHARMACOLOGICAL RELEVANCE: Species of the genus Vepris are used in traditional African pharmacopeia for the treatment of various conditions, including chronic diseases and other parasitic. Further uses are against whooping cough and colic in children and as an antidote against snakebite. Data presented will enable the interested scientists to work on this genus applying the so-called "ethnopharmacologic approach", which may lead towards the discovery of the effective, safe plant medicinal products. AIM OF THE REVIEW: This review article aims to collate and analyse the available information on the traditional uses, phytochemistry, pharmacology, and toxicological aspects of Vepris species in order to explore the trends and perspectives for further studies. METHODOLOGY: The present review paper collected the literature published prior to August 2020 on the ethnomedicinal uses, phytochemistry, and pharmacology of the genus Vepris. The available information about the genus Vepris was collected via Google Books, Google Scholar, PubMed, ScienceDirect, SciFinder, Web of Science, and other internet sources. The Global Biodiversity Information Facility (www.gbif.org), Plants of the world online (www.plantsoftheworldonline.org), and The Plant List (www.theplantlist.org) databases were used to verify the scientific names and provide distribution information of Vepris species. RESULTS: Comprehensive analysis of the literature provided information on ethnopharmacological uses of 30 species out of 83 members in the genus. A total of 213 compounds - predominantly alkaloids - were reported together with results from antioxidant, cytotoxic, antimicrobial, antiplasmodial, antitrypanosomal, antileishmanial, antidiabetic, antipyretic, analgesic, insect antifeedant, and toxicity assays. Arborinine (49) and skimmianine (4) isolated from the leaves of V. trichocarpa were tested toxic in rat skeletal myoblast cell line L6, a stable skeletal muscle progenitor cell line, while the leaves of V. heterophylla, the stem bark of V. louisii, and the roots of V. uguenensis were shown to be toxic against model organisms T. castaneum (Tenebrionidae), H. bakeri (Trychostrongylidae), and M. domestica (Muscidae), respectively. In addition, 6,7-methylenedioxy-5-hydroxy-8-methoxy-dictamnine (40) isolated from the leaves of a combined sample of V. renieri + V. suaveolens displayed an extremely low IC50 of 0.67 µM against the normal fibroblastic lung cell line MRC-5 indicating high toxicity. Thus, medical use of these plant parts, as well of the stem bark of V. verdoorniana used locally in poison fishing, should be avoided if alternative treatments exist. Furthermore, a good number of significantly in vitro bioactive compounds have been reported from the genus Vepris: against malaria and against microbial infections. CONCLUSIONS: Various Vepris species were found to be used in traditional African pharmacopeia. However, few of these species were studied for their bioactive chemical constituents with even fewer bioassay-guided isolation studies being reported. Moreover, detailed pharmacological studies in animal models to explore their mode of action were not reported. Therefore, future studies should focus on these aspects. In addition, we would like to recommend further research on some significantly bioactive crude extracts that were identified in this review: V. leandriana; V. lanceolata; V. nobilis; and V. trichocarpa, as well as those plants reported to be used against chronic diseases.

Pharmacological activities of the organic extracts and fatty acid composition of the petroleum ether extract from Haplophyllum tuberculatum leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: Haplophyllum tuberculatum is used in traditional medicine to treat many disorders including inflammation and pain. The aim of this study is to investigate the organic extracts from H. tuberculatum leaves against inflammation, gastric ulcer and pain. MATERIALS AND METHODS: Acute toxicity was studied in vivo to determine the toxic doses of the organic extracts. Anti-inflammatory activity was also evaluated in vivo using carrageenan-induced paw edema in Wistar rats. Gastroprotective activity was tested using the HCl/ethanol-induced gastric ulcer test in rats. Peripheral and central analgesic activities were assessed using the acetic acid-induced writhing test and the hot-plate method, respectively. The chemical composition of the fatty acids in the petroleum ether (PE) extract was determined with GC-MS. RESULTS: At 25, 50 and 100mg/kg PE extract was the most active against inflammation. Percentages inhibition 5h after carrageenan-injection were 51.12; 86.71% and 96.92%, respectively. The same extract at 100mg/kg showed good analgesic activities using the acetic acid-induced writhing test and the hot-plate method. The chloroform, ethyl acetate (EtOAc) and butanolic (n-BuOH) extracts exhibited strong anti-inflammatory, gastroprotective and analgesic activities at 100mg/kg. The GC-FID analysis revealed that the PE extract was rich in γ-linolenic acid (45.50%) followed by palmitic acid (18.48%), linoleic acid (10.73%), erucic acid (4.72), stearic acid (3.96%) and oleic acid (2.57%). CONCLUSION: The results of the present study support the traditional use of the leaves of H. tuberculatum and may possibly serve as prospective material for further development of safe new phytochemical anti-inflammatory, gastroprotective and/or analgesic agents.

Toxicity evaluation of some traditional African spices on breast cancer cells and isolated rat hepatic mitochondria.

BACKGROUND: Fagara leprieuri (FL), Fagara xanthoxyloïdes (FX), Mondia whitei (MW) and Xylopia aethiopica (XA) are used in many African countries as food spices or in traditional medicine to treat several maladies. In this work, we (a) investigate whether the crude spice extracts present selective cytotoxicity for breast cancer cell lines and (b) investigate whether the same extracts affect the bioenergetics and calcium susceptibility of isolated liver mitochondrial fractions. RESULTS: All extracts were cytotoxic to the cell lines studied, with the exception of MW, which was less toxic for a normal cell line. Interestingly, some of the extracts did not depolarize mitochondria in intact breast cancer MCF-7 cells, although this effect was observed in a normal breast cancer cell line (MCF-12A). All extracts increased hepatic mitochondrial state 2/4 respiration and decreased the respiratory control ratio and the transmembrane electric potential. Also, the extracts induced the mitochondrial permeability transition (MPT). CONCLUSIONS: Mitochondrial toxicity may be part of the mechanism by which the spices tested cause inhibition of proliferation and death in the cell lines tested. This study also warrants caution in the excessive use of these spices for human consumption.

The effect of the aqueous extract of Helietta parvifolia A. Gray (Rutaceae) stem bark on carrageenan-induced paw oedema and granuloma tissue formation in mice.

AIMS OF STUDY: Despite the ethnopharmacological relevance of Helietta parvifolia A. Gray (Rutaceae) in Mexico, we found no significant pharmacological studies of this plant in the scientific literature. The aim of the present study was to establish the anti-inflammatory effect of an aqueous extract of the stem bark of Helietta parvifolia in mice. MATERIALS AND METHODS: The anti-inflammatory activity of the aqueous extract of the stem bark of Helietta parvifolia was evaluated using carrageenan-induced paw oedema in mice, and the cotton pellet granuloma method. RESULTS: An extract dose ranging from 20 to 80 mg/kg p.o. showed a non-significant effect over the initial phase of carrageenan-induced oedema. However, it showed a significant inhibition of oedema after 3h, which can be related to the inhibition of the release of kinin-like substances. An ID(50) value of 47.4 mg/kg was obtained for the plant extract. The extract also suppressed granulomatous tissue formation during chronic inflammation. The inhibitory values were 19.2, and 22.2, corresponding to 40 and 80 mg/kg doses of extract respectively. CONCLUSIONS: Aqueous extract showed a statistically significant anti-inflammatory effect in mice during the late phase of acute inflammation and during chronic inflammation. However, the exact mechanism(s) of anti-inflammatory effects of Helietta parvifolia observed in this study remains unclear.

'Buchu' -Agathosma betulina and Agathosma crenulata (Rutaceae): a review.

South Africa has offered the world two indigenous aromatic plants from which commercially important natural products have been developed: Pelargonium graveolens (and its hybrids) the source of geranium oil and Agathosma betulina, from which 'Buchu' oil is produced. Despite the historical use of 'Buchu' and the commercial interest developed around this coveted indigenous resource the (limited) research has not been coherently assembled. This overview aims to unite aspects on the botany, traditional and modern day uses, chemistry and pharmacological data on 'Buchu' which is undeniably one of South Africa's most renowned botanical assets.