Flavonoids of Chromolaena odorata (L.) R.M.King & H.Rob. as potential leads for treatment against tuberculosis.

Tuberculosis (TB) is currently rated as the 13th leading cause of mortality and the second leading cause of death after COVID-19, and above AIDS. Existing challenges relating to the development of multidrug-resistant strains and dangerous side effects of currently used drugs add impetus to the search for additional TB treatments. Hence, interest has grown in the use of medicinal plants as a source of bioactive preparations with efficacy against TB-causing organisms, and also with the ability to ameliorate the negative effects of TB drugs. This study aimed to evaluate the antimycobacterial and hepatoprotective potentials of extracts and isolated flavonoid compounds from invasive Chromolaena odorata. Test organisms used were pathogenic Mycobacterium bovis and M. tuberculosis H37RV, and the fast-growing M. aurum, M. fortuitum and M. smegmatis. The selectivity index (SI) values of the test substances were determined through cytotoxicity assays to promote these extracts and compounds as leads for the development of effective and safe anti-tubercular drugs. The antimycobacterial activity was evaluated using a serial microdilution method, and the SI was calculated from the 50% lethal concentrations calculated from cytotoxicity tests. Hepatoprotective activity was determined using HepG2 liver cells treated with rifampicin as a toxin. The extracts and compounds had a range of antimycobacterial activity with minimum inhibitory concentration (MIC) values ranging from 0.031 to 2.5 mg/mL. Two flavonoid compounds, 5,7,4'-trimethoxy flavanone and 5­hydroxy-3,7,4'-trimethoxyflavone showed promising antimycobacterial potential, and minimal toxicity was observed, as most SI values were higher than 1. The flavonoid compound 5,7,4'-trimethoxy flavanone had the highest SI (6.452), which was against M. tuberculosis H37RV. The HepG2 cells were reduced to 65% due to toxicity by rifampicin, however, the flavonoid compounds were able to improve cell viability to between 81 and 89% at different concentrations tested. Results obtained indicate that C. odorata may serve as a lead for the development of safe and effective antimycobacterial and hepatoprotective drugs.

Ethnopharmacology and biological activities of the Aizoaceae.

ETHNOPHARMACOLOGICAL RELEVANCE: The Aizoaceae is one of the largest succulent plant families. Most members of the family are ornamental and form part of specialist succulent collections. The exceptional diversity of the Aizoaceae is not only limited to its growth forms, habitat, and chemistry, but is also reflected in its many traditional uses. Selected species are well known for their use in traditional medicines, with recent scientific studies validating their biological activity. AIM OF THE STUDY: Herein, this review aimed to articulate foundational and current global research endeavors related to the traditional uses and pharmacological activities of the Aizoaceae. MATERIALS AND METHODS: Research articles and search terms related to the ethnopharmacology and bioactivities of the Aizoaceae between 1940 and 2022 were evaluated using electronic databases such as Google Scholar, PubMed, ScienceDirect, Scopus, JSTOR, and Web of Science. RESULTS: Popular Aizoaceae genera including Mesembryanthemum, Trianthema, and Tetragonia are noted for their cultural value and are key components in herbal medicines for the treatment of a myriad of disorders. Isolated bioactive compounds isolated from selected species demonstrated varied antimicrobial, antioxidant, and neuroprotective functions in basic pharmacological studies. However, most studies lacked reliable correlation to in vivo activity and did not adequately validate the safety and efficacy of potential therapeutic compounds. CONCLUSIONS: While the cultural and therapeutic value of popular Aizoaceae species have been highlighted in the literature, there remains glaring inconsistencies among other related species. Data deficiency may be ameliorated by further studies focused on taxonomic markers, chemical characterization and underlying molecular mechanisms of activity of a wider pool of species to enhance our knowledge of this hyperdiverse family.

Invasive alien plants and weeds in South Africa: A review of their applications in traditional medicine and potential pharmaceutical properties.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional pharmacopoeias are constantly evolving and adapting, hence the assimilation of alien plants and weeds into traditional systems of healing. Invasive plants are detrimental to the ecosystem, however they are also potential sources of secondary metabolites with useful biological activities. AIM OF THE REVIEW: The aim of this review was to investigate published reports of traditional use and biological activity of declared invasive alien plants and other weeds in South Africa. MATERIALS AND METHODS: Information was retrieved from scientific databases including Scopus, Web of Science, ScienceDirect, Google Scholar, PubMed, Chemical Abstracts Services and books, theses, dissertations and technical reports. Keywords used for the search engines were "South Africa" or "southern Africa" in conjunction with "(native weeds OR alien invasive)" AND "medicinal". Separate searches were conducted on the individual invasive plant species recorded as having been used in ethnobotanical surveys to determine their known biological activities and chemical components. RESULTS: A total of 89 plant species regarded as invasive species or weeds in South Africa were identified as being used in traditional medicine. The most commonly mentioned plant family was the Asteraceae with a total of 15 species followed by the Fabaceae and Solanaceae with 6 species each. Of the 89 species recorded, 68% were reported to have traditional usage with both phytochemical and biological data available. A history of traditional usage coupled with biological data was available for 12% of species. Records of traditional usage alone were linked to 11% of species. Invasive alien species comprised 61% of recorded species, while native and non-invasive alien weeds formed the remaining 39%. CONCLUSIONS: The exploration of alternative uses for weeds and particularly invasive plants, whether native or alien, as medicines for possible commercialisation may lead to innovative mechanisms for putting such species to good use.

Bioassay-guided purification, GC-MS characterization and quantification of phyto-components in an antibacterial extract of Searsia lancea leaves.

Phytocompounds in an aqueous methanol (70% MeOH) leaf extract of Searsia lancea were separated using liquid-liquid partitioning techniques and gravity-assisted column chromatography. The resultant fractions were screened for antibacterial properties (minimum inhibitory concentration, MIC) against four bacterial strains (Enterococcus faecalis, Klebsiella pneumoniae, Neisseria gonorrhoeae and Staphylococcus aureus). Bioactive fractions were purified using preparative thin layer chromatography (TLC) and subjected to further antibacterial screening. Phytocompounds in antibacterial sub-fractions were characterized and quantified using Gas Chromatography-Mass Spectrometry (GC-MS). An ethyl acetate sub-fraction purified from the aqueous methanol extracts of the leaves demonstrated potent antibacterial properties (MIC range: 31-61 µg/ml against E. faecalis and S. aureus). Based on GC-MS analysis, 81.5% of the sub-fraction consisted of broad-spectrum antibacterial compounds namely tetracosanol (43.98%) and nonadecanol (37.5%). Current research findings support the traditional use of S. lancea leaves to manage gastro-intestinal disorders and gonorrhoea.

New role for crinamine as a potent, safe and selective inhibitor of human monoamine oxidase B: In vitro and in silico pharmacology and modeling.

ETHNOPHARMACOLOGICAL RELEVANCE: The development of selective inhibitors of monoamine oxidase B (MAO-B) has been essential in treating Parkinson's disease. However, the apparent hepatotoxicity and drug-drug interactions of current inhibitors accentuate the need for the development of novel pharmacotherapies. Crossyne guttata (L.) D. & U. Müll-Doblies is used frequently by Rastafarian bush doctors to treat alcoholism, a disorder which is also accentuated by MAO. OBJECTIVE: The study sought to isolate, identify and characterise the biologically active constituents of C. guttata based on their ability to inhibit the MAO enzymes. MATERIALS AND METHODS: Column chromatography was used to isolate the biologically active alkaloids of C. guttata. The ability of the alkaloids to inhibit the biotransformation of 4-aminoantipyrine by the MAO enzymes was evaluated in vitro. In silico docking was conducted using AutoDock Vina server while the pharmacokinetic properties of the compounds were evaluated using SwissADME. RESULTS: Chromatographic separation of an ethanolic fraction of C. guttata yielded the alkaloids crinamine 1 and epibuphanisine 2. 1 and 2 along with structurally related alkaloids haemanthamine 3 and haemanthidine 4 were evaluated for their ability to inhibit the action of isozymes of MAO in vitro. Alkaloids effected submicromolar IC50 values against MAO-B, the most potent of which being crinamine 1 (0.014 µM) > haemanthidine 4 (0.017 µM) > epibuphanisine 2 (0.039 µM) > haemanthamine 3 (0.112 µM). Binding energies of the alkaloids correlated well with their inhibitory potential with crinamine displaying the best binding efficacy and binding energy score with MAO-B. DISCUSSION AND CONCLUSION: Crinamine and epibuphanisine exhibited potent and selective inhibitory activity towards MAO-B. After comprehensive in silico investigations encompassing robust molecular docking analysis, the drug-like attributes and safety of the alkaloids suggest the crinamine is a potentially safe drug for human application.

Ethnobotany, phytochemistry, toxicology and pharmacological properties of Terminalia sericea Burch. ex DC. (Combretaceae) - A review.

ETHNOPHARMACOLOGICAL REFERENCE: The use of medicinal plants in the treatment of infections is ancient. A wide variety of ethnotherapeutic properties and pharmacological actions has been attributed to Terminalia sericea. Studies by various groups of investigators reveal that it is a multipurpose medicinal plant used mostly in the treatment of diarrhoea, sexually transmitted infections, skin rashes, tuberculosis and other infections. The current paper is aimed at providing an overview of the ethnomedicinal uses, toxicology, pharmacology and the phytochemistry of Terminalia sericea. MATERIALS AND METHODS: Information was retrieved using various search engines, including Pubmed, Science Direct, Google Scholar, Scielo, SciFinder and Scopus. The key words used included Terminalia sericea, secondary metabolites, phytochemistry, biological activity, pharmacology, ethnobotanical survey, medicinal uses, safety, toxicology and other related words. RESULTS: Terminalia sericea is an important medicinal plant which possesses anti-HIV, anti-fungal, anti-bacterial, anticancer, lipolytic, wound healing, antiparasitic, anti-inflammatory and anti-oxidant activity, as the most valuable biological activities, thus lending pharmacological support to the plant's folkloric uses in indigenous medicine. Toxicologically, the extracts and isolated compounds from the plant species may have mild toxic effects. Phytochemically, the plant species possesses valuable compounds including triterpenes, alkaloids and flavonoids which may well contribute to its biological activity. CONCLUSIONS: Terminalia sericea contains secondary metabolites which are valuable in the treatment of a variety of human infections, including community acquired infections which may be prevalent in developing countries. The degree of toxicity reported in various extracts warrants further exploration of the cytotoxicity of the plant species, both against normal human cell lines and in vivo. Moreover, the acetylcholinesterase inhibitory and anti-inflammatory effects also need to be further investigated as there are only a few reports from the literature on these aspects. There is also a need to further understand the mode of action of the extracts against various enzymes relating to inflammation. Antioxidant activity of the plant extracts against various forms of free radicals needs to be investigated. Although T. sericea is reported to be used for ethnoveterinary infections, there are no scientific reports on the anti-parasitic activity of the plant species against common animal parasites.

Investigating the effect of cadmium and aluminium on growth and stress-induced responses in the micropropagated medicinal plant Hypoxis hemerocallidea.

Hypoxis hemerocallidea is a highly utilized medicinal plant in South Africa. Its cultivation has received considerable attention in order to meet the high demand. High levels of cadmium (Cd) and aluminum (Al) in H. hemerocallidea plants sold in traditional medicinal markets was previously reported. The present study used an in vitro propagation model to investigate the uptake of Cd and Al by H. hemerocallidea and their effect on plant growth, elemental uptake and some stress-induced responses such as pigment, malondialdehyde (MDA), proline content and ultrastructural changes. Shoot and root growth of plantlets exposed to Cd, Cd:Al and high concentrations of Al was significantly reduced. Highest concentrations of Cd accumulated in the corms of Cd-treated plantlets while highest Al concentrations occurred in the leaves and roots. There was higher accumulation of Cd and Al when applied singularly compared to the Cd:Al combination treatments. Cd and Al also reduced accumulation of trace elements in micropropagted H. hemerocallidea with lowest concentrations in the Cd:Al combination treatments. Exposure to Cd, Al and Cd:Al significantly reduced the level of chlorophyll but increased the levels of carotenoids, MDA and proline. Ultrastructural changes were also observed in H. hemerocallidea exposed to Cd and Al. All these factors contributed to the inhibition of plant growth and could potentially affect the ability of this important medicinal plant to synthesize bioactive compounds. It is thus necessary to understand heavy metal stress-induced responses in this highly valued medicinal plant to ensure a high quality product for the consumer.

Effect of smoke derivatives on in vitro pollen germination and pollen tube elongation of species from different plant families.

Plant-derived smoke stimulates seed germination in numerous plant species. Smoke also has a positive stimulatory effect on pollen germination and pollen tube growth. The range of plant families affected my smoke still needs to be established since the initial study was restricted to only three species from the Amaryllidaceae. The effects of smoke-water (SW) and the smoke-derived compounds, karrikinolide (KAR1 ) and trimethylbutenolide (TMB) on pollen growth characteristics were evaluated in seven different plant families. Smoke-water (1:1000 and 1:2000 v:v) combined with either Brewbaker and Kwack's (BWK) medium or sucrose and boric acid (SB) medium significantly improved pollen germination and pollen tube growth in Aloe maculata All., Kniphofia uvaria Oken, Lachenalia aloides (L.f.) Engl. var. aloides and Tulbaghia simmleri P. Beauv. Karrikinolide (10(-6) and 10(-7) m) treatment significantly improved pollen tube growth in A. maculata, K. uvaria, L. aloides and Nematanthus crassifolius (Schott) Wiehle compared to the controls. BWK or SB medium containing TMB (10(-3) m) produced significantly longer pollen tubes in A. maculata, K. uvaria and N. crassifolius. These results indicate that plant-derived smoke and the smoke-isolated compounds may stimulate pollen growth in a wide range of plant species.

Isolation and characterization of antimicrobial compounds from Terminalia phanerophlebia Engl. & Diels leaf extracts.

ETHNOPHARMACOLOGICAL RELEVANCE: The emergence of drug resistant-tuberculosis and other pathogenic diseases over the past decades, constitutes a serious threat to human health worldwide. According to a 2012 report by the World Health Organization (WHO), South Africa, China, India and Russia are the countries with the highest prevalence of Multi-Drug Resistant tuberculosis (MDR-tuberculosis) as they represented 60% of the total. Several reports have documented antimycobacterial properties of Terminalia species but only a few species from this genus have been explored for their antimycobacterial constituents. The crude extracts of Terminalia phanerophlebia showed good antimicrobial activities in our previous study against two Mycobacterium as well as two other bacterial strains responsible for opportunistic infections related to respiratory ailments. This paper studies the isolation of compounds responsible for such activities and to isolate compounds responsible for antimicrobial activities from the crude extracts of Terminalia phanerophlebia leaves. MATERIALS AND METHODS: Terminalia phanerophlebia crude extracts obtained from 80% methanol was successively extracted with hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and n-butanol. The fractions obtained and isolated compounds were tested for their antibacterial activities against Mycobacterium aurum, Mycobacterium tuberculosis, Staphylococcus aureus and Klebsiella pneumoniae. Bioguided fractionation of the EtOAc fraction afforded two bioactive compounds. Structure elucidation was carried out using NMR (1D and 2D) spectroscopic methods. RESULTS: EtOAc fraction exhibited highest antimicrobial activities and its fractionation afforded methyl gallate (methyl-3,4,5-trihydroxybenzoate) (1) and a phenylpropanoid glucoside, 1,6-di-O-coumaroyl glucopyranoside (2) These compounds are reported from Terminalia phanerophlebia for the first time. Both compounds showed good antimicrobial activity against all bacterial strains tested with minimum inhibitory concentration (MIC) values ranging from 63 to 250 µg/mL. Inhibition of Mycobacterium tuberculosis by 1,6-di-O-coumaroyl glucopyranoside (2) at a MIC value of 63 µg/mL was noteworthy, as this bacterial strain is reported to be the leading cause of tuberculosis worldwide. CONCLUSIONS: Good antimicrobial activities exhibited by the compounds isolated from Terminalia phanerophlebia authenticate the traditional use of this plant in treating tuberculosis and its related symptoms. Compound (2), 1,6-di-O-coumaroyl glucopyranoside could serve as a lead compound for tuberculosis drug discovery.

Antimycobacterial, anti-inflammatory and genotoxicity evaluation of plants used for the treatment of tuberculosis and related symptoms in South Africa.

ETHNOPHARMACOLOGICAL RELEVANCE: Emergence of drug-resistant tuberculosis strains and long duration of treatment has established an urgent need to search for new effective agents. The great floral diversity of South Africa has potential for producing new bioactive compounds, therefore pharmacological screening of plant extracts within this region offers much potential. To assess the in vitro antimycobacterial, anti-inflammatory and genotoxicity activity of selected plants that are used for the treatment of TB and related symptoms in South Africa. MATERIALS AND METHODS: Ground plant materials from 10 plants were extracted sequentially with four solvents (petroleum ether, dichloromethane, 80% ethanol and water) and a total of 68 extracts were produced. A broth microdilution method was used to screen extracts against Mycobacterium tuberculosis H37Ra. The cyclooxygenase-2 (COX-2) enzyme was used to evaluate the anti-inflammatory activity of the extracts and the Salmonella microsome assay using two Salmonella typhimurium strains (TA98 and TA100) to establish genotoxicity. RESULTS: Six out of 68 extracts showed good antimycobacterial activity. Three extracts showed good inhibition (>70%) of COX-2 enzyme. All the extracts tested were non-genotoxic against the tested Salmonella strains. CONCLUSION: The results observed in this study indicate that some of the plants such as Abrus precatorius subsp. africanus, Ficus sur, Pentanisia prunelloides and Terminalia phanerophlebia could be investigated further against drug-resistant TB strains.

Phytosynergy in some Hypoxis species and pharmacological properties of a Hypoxis-based phytopharmaceutical formula.

ETHNOPHARMACOLOGY RELEVANCE: Hypoxis species are used extensively in traditional medicine in southern Africa for several ailments including tuberculosis, chest infections, and nervous and urinary disorders. Several other claims have been made for extracts emanating from Hypoxis species and have led to the production of several commercial products used as immunostimulants mostly for people living with HIV/AIDS and cancer. This study was aimed at investigating the biological activity of four Hypoxis species and a commercial herbal product, 'African potato extract' (APE). MATERIALS AND METHODS: Antibacterial, antifungal, cyclooxygenase (COX) and acetylcholineasterase (AChE) inhibitory activities of four Hypoxis species (H. acuminata, H. colchicifolia, H. hemerocallidea and H. rigidula) and a popular Hypoxis-based herbal preparation, APE were tested. The phytoconstituents of the mixture were also profiled using TLC methods. Several combinations of the Hypoxis species were prepared and their synergism, additive, autonomic and antagonism effects investigated. As a quality control measure, batch to batch comparison in the phytoconstituents and biological activity of APE was carried out. RESULTS: The results confirmed H. colchicifolia and H. hemerocallidea as the phytoconstituents of APE. The extracts showed a broad spectrum of activities against the bacterial and fungal strains used. Of particular interest were the activities exhibited by the APE and combinations of H. colchicifolia and H. hemerocallidea. The APE mixture exhibited good antibacterial activity (MIC values of 0.78mg/ml each) in all the tested batches against the bacterial strains used. The water extracts of all four Hypoxis species, three batches of APE and the combination (water extracts) of H. colchicifolia and H. hemerocallidea exhibited high COX-1 and moderate COX-2 inhibitory activity except for H. acuminata which showed low activity against COX-2. All the extract, batches of APE and combinations showed low to moderate AChE inhibitory activity. These results provided some evidence of phytosynergy in some extracts of H. hemerocallidea and H. colchicifolia except for a few extracts which act as additive, autonomous and antagonistic when used to inhibit some bacterial and fungal strains. However, this was not the case for COX and AChE inhibition, as only acetone extracts acted in a synergistic way to reduce the activity of the enzyme. CONCLUSION: Even though the results give an indication of a positive interaction between some extracts of H. hemerocallidea and H. colchicifolia, the study was carried out on 1:1 v/v combinations only. It is therefore important to carry out isobologram studies, which considers more than one ratio of the combinations.

Antimicrobial, antioxidant, mutagenic and antimutagenic activities of Distephanus angulifolius and Ormocarpum trichocarpum.

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Distephanus angulifolius and Ormocarpum trichocarpum are used for treating stomach-related ailments in traditional medicine. AIMS OF THE STUDY: The present study evaluated the antibacterial, antioxidant, mutagenic and antimutagenic properties of extracts obtained from the leaves of Distephanus angulifolius and Ormocarpum trichocarpum. MATERIALS AND METHODS: The microtitre bioassay was used to determine the antibacterial activity against three Gram-positive and three Gram-negative bacteria. Antioxidant activity was determined using the free-radical scavenging and ß-carotene-linoleic acid model assays. The safety and possible protective properties of the extracts were investigated using Ames test. RESULTS: Dichloromethane fractions of both plants displayed a broad-spectrum antibacterial activity with minimum inhibitory concentrations ranging from 0.16 to 0.63 mg/ml. A dose-dependent antioxidant activity was recorded in both plant species. All the evaluated samples showed no mutagenic as well as weak or no antimutagenic properties in the absence of exogenous metabolic activation. CONCLUSION: The results demonstrated the antibacterial and antioxidant activities of the leaves obtained from the two plant species. Furthermore, the data provides a rationale for the use of the plant species in treating stomach-related ailments in traditional medicine.

Antimicrobial and acetylcholinesterase inhibitory activities of Buddleja salviifolia (L.) Lam. leaf extracts and isolated compounds.

ETHNOPHARMACOLOGICAL RELEVANCE: Buddleja salviifolia leaves are used for the treatment of eye infections and neurodegenerative conditions by various tribes in South Africa. AIM OF STUDY: This study was designed to isolate the phenolic constituents from the leaf extracts of Buddleja salviifolia and evaluate their antimicrobial and acetylcholinesterase (AChE) activities. MATERIAL AND METHODS: Three phenolic compounds were isolated from the ethyl acetate fraction of a 20% aqueous methanol leaf extract of Buddleja salviifolia using Sephadex LH-20 and silica gel columns. Structure elucidation of the isolated compounds was carried out using spectroscopic techniques: mass spectrometry (ESI-TOF-MS) and NMR (1D and 2D). The extracts and isolated compounds were evaluated for antimicrobial and acetylcholinesterase activities using the microdilution technique. The bacteria used for the antimicrobial assays were Gram-positive Bacillus subtilis and Staphylococcus aureus and Gram-negative Escherichia coli and Klebsiella pneumoniae. RESULTS: The isolated compounds were characterized as: 4'-hydroxyphenyl ethyl vanillate (1) a new natural product, acteoside (2) and quercetin (3). The crude extract, fractions and the isolated compounds from the leaves of the plant exhibited a broad spectrum of antibacterial activity. The EtOAc fraction exhibited good activity against Bacillus subtilis and Staphylococcus aureus with MIC values ranging from 780.0 to 390.0 µg/mL. Isolated compound 2 exhibited good activity against Staphylococcus aureus with an MIC value of 62.5 µg/mL. The hexane and DCM fractions of leaves showed the best activity against Candida albicans with MIC and MFC values of 390.0 µg/mL. In the AChE inhibitory test, among the tested extracts, the hexane fraction was the most potent with an IC50 value of 107.4 µg/mL, whereas for the isolated compounds, it was compound (3) (quercetin) with an IC50 value of 66.8 µg/mL. CONCLUSIONS: Activities demonstrated by the extracts and isolated compounds support the ethnopharmacological use of Buddleja salviifolia against eye infections and neurodegenerative diseases.

Anti-inflammatory and mutagenic evaluation of medicinal plants used by Venda people against venereal and related diseases.

ETHNOPHARMACOLOGY RELEVANCE: Inflammation is a major risk factor for various human diseases including venereal diseases, often resulting in treatment complications. Plants have been traditionally used for treatment of many different diseases and have been successfully proven to be an alternative source in treatment of infectious diseases. AIM OF THE STUDY: This study was aimed at evaluating the anti-inflammatory activities and the mutagenic properties of 12 medicinal plants used by the Venda people against venereal and related diseases. MATERIALS AND METHODS: The plants were evaluated for their anti-inflammatory activity against the cyclooxygenase (COX-1 and -2) enzymes and genotoxicity using the Ames test, with and without S9 (metabolic activation) against Salmonella typhimurium tester strain TA98. RESULTS: DCM and PE extracts of Adansonia digitata bark, Bolusanthus speciosus bark, Pterocarpus angolensis bark and Pappea capensis leaves and EtOH and water extracts of Bolusanthus speciosus stem and Ekebergia capensis bark showed the best anti-inflammatory activity in both COX-1 and -2 assays at 250 µg/ml. These were further evaluated at three other concentrations (31.25, 62.5, and 125 µg/ml) to determine IC50 values. Water extracts of Ekebergia capensis bark showed the best IC50 value towards COX-1. The Ames test revealed that all plant extracts were non-mutagenic towards Salmonella typhimurium strain TA98 except for Elephantorrhiza burkei and Ekebergia capensis that showed weak mutagenicity. CONCLUSION: The active plants may offer a new source of chemicals for the effective treatment of anti-inflammatory conditions related to venereal diseases.

Investigation into the genotoxicity of water extracts from Hypoxis species and a commercially available Hypoxis preparation.

We performed an in vitro evaluation of the genotoxic potential of water extracts from four Hypoxis species (Hypoxis hemerocallidea, H. colchicifolia, H. rigidula, H. acuminata) and a commercial preparation thereof using the neutral red uptake (NRU) assay, the alkaline comet assay and the cytome assay in human hepatoma HepG2 cells. The relative cytotoxicity of these samples was established by determining their NI50 values (50% inhibition of NRU), and these results were used for dose-finding in genotoxicity tests. None of the tested extracts were identified as genotoxic in both the alkaline comet assay and cytome assay.

South African plants and male reproductive healthcare: conception and contraception.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional remedies from plants have been use to treat male reproductive related disorders for ages in South Africa. AIM: This study reviewed the current status of medicinal plants used in male reproductive healthcare as well as their effectiveness as a mode of treatment. METHODOLOGY: A detailed literature search was done by consulting books, peer-reviewed papers, scientific databases such as Scopus, Science direct and PubMed, and Google scholars. Keywords such as aphrodisiacs, conception, erectile dysfunction, fertility, infertility and sterility in relation to medicinal plants were used during the search. Plant species were selected based on their traditional use in different aspects of male reproductive healthcare. RESULTS: A total of 61 plants species were found to be used in treating male impotency or as aphrodisiacs. However, only six species have been evaluated scientifically and these plants showed significant activities either in promoting conception by improving fertility and promoting erection or in contraception by decreasing sperm motility, virility and membrane integrity. CONCLUSION: The importance of herbal products in the treatment of male infertility and related sexual disorders is undeniable. Scientific evaluations of the six species have proved the empirical use of these plants in the improvement of male sexual disorders as well as validating their traditional uses.

Pharmacological properties and protein binding capacity of phenolic extracts of some Venda medicinal plants used against cough and fever.

ETHNOPHARMACOLOGY RELEVANCE: Several ailments are caused by infectious bacteria and in other diseases; they act as co-infection which complicate human life by causing health hazards. In Venda (South Africa), many plants are used in traditional medicine to treat cough and fever. AIM OF THE STUDY: This study was aimed at evaluating the antibacterial and antifungal properties, cyclooxygenases (COX), acetylcholinesterase (AChE) enzyme inhibitory effects and the phenolic composition as well as mutagenic properties of six medicinal plants used by the Venda people of Limpopo Province of South Africa against cough and fever. MATERIALS AND METHODS: The petroleum ether (PE), dichloromethane (DCM), 80% ethanol (EtOH) and water extracts of six plants were tested against four infectious bacteria (Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae and Staphylococcus aureus) and a fungus Candida albicans. The same extracts were evaluated for their ability to inhibit COX-1 and -2 enzymes. Methanolic and water extracts of the same plant were tested for acetylcholinesterase inhibitory effects. Total phenolics, flavonoids, gallotannins and condensed tannins were determined. The ability of the extracts to bind and precipitate proteins was also investigated. The extracts were investigated for genotoxicity with and without S9 (metabolic activation) against three Salmonella typhimurium tester strains TA98, TA100 and TA102. RESULTS: The organic extracts of Rhus lancea leaves exhibited the best antibacterial activity with minimum inhibitory concentration (MIC) values ranging from 0.0061 to 0.049mg/ml. The best antifungal activity was observed from a DCM extract of Syzygium cordatum leaves with a MIC value of 0.195mg/ml. The methanolic and water extracts of the same plant exhibited high inhibitory effects towards AChE with IC(50) values of 0.22 and 0.26mg/ml, respectively. The highest levels of flavonoids and gallotannins were detected in Spirostachys africana bark; 11.57 and 48.88µg/g, respectively. The highest percentages (1.2%) of condensed tannins were detected in Uvaria caffra leaves. The high levels of phenolic compounds may have been responsible for high antimicrobial activities for extracts of S. africana bark and U. caffra leaves. S. cordatum leaves represented the highest affinity for protein binding with 93%. All the extracts were non-mutagenic towards the three tested strains with and without S9 metabolic activation. CONCLUSION: The result obtained in this study goes a long way in validating the ethnobotanical usage of these medicinal plants in the treatment of cough and fever by the Venda people. However, more evidence obtainable from other assays not performed here are urgently required to confirm these results.

Ethnopharmacological study of plants from Pondoland used against diarrhoea.

ETHNOPHARMACOLOGICAL RELEVANCE: Waterborne diseases such as diarrhoea are common world wide, including in Bizana, South Africa where the majority of rural dwellers depend largely on water from unprotected sources. The people from Bizana use medicinal plants as their first line of health care to cure and prevent diarrhoea. AIM OF THE STUDY: To record and document plants used for the treatment of diarrhoea in Bizana, to evaluate antibacterial and anti-inflammatory activities of selected plant extracts as well as to perform genotoxicity testing of evaluated plants. MATERIALS AND METHODS: An ethnobotanical approach was used to select plants used for treating diarrhoea in Bizana for pharmacological assays using questionnaires. Nine plants were selected for bioassays based on their frequency index and the fact that they have never been evaluated against diarrhoea causing-microorganisms. The petroleum ether (PE), dichloromethane (DCM), 70% ethanol (EtOH), and water extracts were evaluated for antibacterial (Gram-positive Staphylococcus aureus, Gram-negative Escherichia coli and Shigella flexneri) activity using the microdilution technique, their ability to inhibit COX-1 and COX-2 enzymes. Genotoxicity was evaluated using the Salmonella microsome assay. RESULTS: This study revealed that 34 plant species belonging to 27 families are used for the treatment of diarrhoea in Bizana. The extracts showed good inhibitory activity with MIC values ranging from 0.39 to 12.5mg/ml. The best activity was exhibited by DCM extracts of Rapanea melanophloeos, and EtOH extracts of Ficus craterostoma and Maesa lanceolata with MIC values of 0.098mg/ml. The inhibitory activity against COX-1 enzyme was higher than COX-2, with 19 plant extracts for the former and 7 for the latter. All the tested plant extracts were not mutagenic at all concentrations tested against all tester strains of bacteria. CONCLUSION: In view of the fact that the plants were selected based on their ethnobotanical usage for treating diarrhoea, the activities reported here goes a long way in validating the plants for traditional use.

In vitro antimicrobial synergism within plant extract combinations from three South African medicinal bulbs.

ETHNOPHARMACOLOGICAL RELEVANCE: Tulbaghia violacea, Hypoxis hemerocallidea and Merwilla plumbea are used in South African traditional medicine for the treatment of some infectious diseases and other ailments. AIM OF THE STUDY: The study aimed at investigating the antimicrobial efficacies of independent and various within-plant extract combinations of three medicinal bulbs to understand the possible pharmacological interactions. MATERIALS AND METHODS: Bulb and leaf extracts of the three medicinal plants, independently and in combinations, were comparatively assessed for antimicrobial activity against two Gram-positive and two Gram-negative bacteria and Candida albicans using the microdilution method. The fractional inhibitory concentration indices (FIC) for two extract combinations were determined. RESULTS: At least one extract combination in each plant sample demonstrated good antimicrobial activity against all the test organisms. The efficacies of the various extract combinations in each plant sample varied, with the strongest synergistic effect exhibited by the proportional extract yield combination of PE and DCM extracts in Merwilla plumbea bulb sample against Staphylococcus aureus (FIC index of 0.1). Most extract combinations demonstrated either a synergistic, additive or indifferent interaction effect against the test bacteria with only a few exhibiting antagonistic effects. CONCLUSION: The observed antimicrobial efficacy and synergistic interactions indicate the beneficial aspects of combination chemotherapy of medicinal plant extracts in the treatment of infectious diseases.

Pharmacological, genotoxic and phytochemical properties of selected South African medicinal plants used in treating stomach-related ailments.

ETHNOPHARMACOLOGICAL RELEVANCE: The evaluated medicinal plants are used in South African traditional medicine in treating stomach-related ailments. AIMS OF THE STUDY: The study aimed at evaluating the pharmacological, genotoxic and phytochemical properties of the seven selected medicinal plants used for treating stomach-related ailments. MATERIALS AND METHODS: Ethyl acetate (EtOAc), ethanol (EtOH) 70% and water extracts of the selected plant parts were evaluated for their antimicrobial and anthelmintic activities using microdilution assays. Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus), Gram-negative bacterium (Escherichia coli) and Candida albicans were used for antimicrobial assays. Caenorhabditis elegans was used for the anthelmintic assay. Plant extracts were also assayed for their cyclooxygenase-inhibitory activity against cyclooxygenase-1 and -2 enzymes. The Ames test was used to evaluate the genotoxicity of the plant extracts. A spectrophotometric method was used to determine the total phenolics, gallotannins, flavonoids and saponins. RESULTS: Twelve extracts exhibited minimum inhibitory concentration (MIC) <1 mg/mL against the bacterial test strains, and five extracts exhibited MIC <1 mg/mL against Candida albicans. The EtOAc extract of Tetradenia riparia had the best minimum lethal concentration (MLC) value (0.004 mg/mL) against Caenorhabditis elegans. All the EtOAc extracts exhibited percentage inhibition in the range of 50.7-94.7% against COX-1 and -2 enzymes at 250 µg/mL. All the plant extracts were non-mutagenic towards Salmonella typhimurium tester strains TA98, TA100 and TA1537 without metabolic activation. Phytochemical analysis revealed relatively high amounts of total phenolics, gallotannins and flavonoids in the evaluated plant extracts. CONCLUSIONS: The general pharmacological activities exhibited by some of the plant extracts in this study support the traditional uses of the selected plants in treating stomach-related ailments. The Ames test showed that all the plant extracts were non-mutagenic but cytotoxicity tests are needed to ascertain the safety for long-term consumption.