Characteristics of MR Neuroimaging Services Billed by Radiologists versus Nonradiologists.

BACKGROUND AND PURPOSE: Although most neuroimaging examinations are interpreted by radiologists, many nonradiologists provide interpretation services. We studied day of the week, site of service, and patient complexity differences for common Medicare MR neuroimaging examinations interpreted by radiologists versus nonradiologists. MATERIALS AND METHODS: Using carrier claims files for a 5% sample of Medicare beneficiaries from 2012 to 2014, we identified all claims for brain and lumbar spine MR imaging examinations. Services were categorized by physician specialty, day of the week, and the site of service. Patient complexity was calculated using Charlson Comorbidity Indices. The χ2 was performed to test statistical significance. RESULTS: A provider specialty could be identified for 568,423 brain and lumbar spine MR imaging examinations. Of weekday examinations, radiologists interpreted 475,288 (92.3%), and nonradiologists, 39,510 (7.7%). Of weekend examinations, radiologists interpreted 52,028 (97.0%) and nonradiologists 1597 (3.0%). Radiologists interpreted 145,904 (98.7%) examinations in the inpatient hospital and emergency department settings versus 1882 (1.3%) by nonradiologists. Of all examinations, 44,547 of those interpreted by radiologists (8.4%) were on the most clinically complex patients versus 2139 (5.2%) for nonradiologists. All interspecialty differences for day of the week, the site of service, and patient complexity were statistically significant (P < .001). CONCLUSIONS: Although radiologists interpret most common MR neuroimaging examinations for Medicare beneficiaries, in contrast to nonradiologists, they disproportionately render those services on weekends, in higher acuity sites, and on more complex patients. To optimize access and minimize disparities in necessary neuroimaging, quality metrics should consider such service characteristics.

Medicinal Mascarene Aloes: An audit of their phytotherapeutic potential.

A phytochemical and biological investigation of the endemic Mascarene Aloes (Aloe spp.), including A. tormentorii (Marais) L.E.Newton & G.D.Rowley, A. purpurea Lam, A. macra Haw., A. lomatophylloides Balf.f and A. vera (synonym A. barbadensis Mill.), which are used in the traditional folk medicine of the Mascarene Islands, was initiated. Methanolic extracts of the Aloes under study were analysed using high resolution LC-UV-MS/MS and compounds belonging to the class of anthraquinones, anthrones, chromones and flavone C-glycosides were detected. The Mascarene Aloes could be distinguished from A. vera by the absence of 2″-O-feruloylaloesin and 7-O-methylaloeresin. GC-MS analysis of monosaccharides revealed the presence of arabinose, fucose, xylose, mannose and galactose in all the Mascarene Aloes and in A. vera. The crude extracts of all Aloes analysed displayed antimicrobial activity against Bacillus cereus, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Only extracts of A. macra were active against P. aeruginosa and Klebsiella pneumoniae, while none of the Aloe extracts inhibited Propionibacterium acnes. A. macra displayed anti-tyrosinase activity, exhibiting 50% inhibition at 0.95mg/mL, and extracts of A. purpurea (Mauritius) and A. vera displayed activity in a wound healing-scratch assay. In vitro cytotoxicity screening of crude methanolic extracts of the Aloes, using the MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) showed that only A. purpurea (Réunion) elicited a modest toxic effect against HL60 cells, with a percentage toxicity of 8.2% (A. purpurea-Réunion) and none of the Aloe extracts elicited a toxic effect against MRC 5 fibroblast cells at a concentration of 0.1mg/mL. Mascarene Aloe species possess noteworthy pharmacological attributes associated with their rich phytochemical profiles.

Alkaloids from aerial parts of Annona senegalensis against Streptococcus mutans.

Antimicrobial potential of medicinal plants have been explored extensively these days. This study was carried out to evaluate the antibacterial potential from aerial parts of plant, called 'Annona senegalensis' and its constituents. Bioassay guided fractionation led to the isolation of four metabolites, (+)-catechin (1), (-)-anonaine (2), (-)-asimilobine (3) and (+)-nornantenine (4). This is the first report on the isolation of compounds 1, 3 and 4 from this plant. Compounds 2 and 4 showed good activity, whereas 1 and 3 displayed weak inhibition against Streptococcus mutans (ATCC 25175). The results showed that compound 2 and 3 showed significant activity with a minimum inhibition concentration (MIC) of 0.12 and 0.25 mg/mL, respectively. The present study reports for the first time the antibacterial activity of the extract of A. senegalensis and its constituents. As S. mutans is a rather resistant bacteria, the MIC obtained during the present study is significant.

Growth inhibition and induction of apoptosis in human cancerous HeLa cells by Maytenus procumbens.

The possible biochemical activities of the acetonic/ethanolic extract of the leaves of Maytenus procumbens (L.M.P), and its isolated compounds were investigated in the present study. In cytotoxicity assay, L.M.P showed IC(50) of 68.79, 51.22, 78.49, 76.59, and 76.64µg/ml on Caco-2, HeLa, HT29, NIH3T3, and T47D cells, respectively. Bioassay guided fractionation led to the isolation and identification of a new triterpene: '30-hydroxy-11α-methoxy-18ß-olean-12-en-3-one' (HMO) in addition to a known terpenoid: 'asiatic acid' (AA). HMO exhibited the most cytotoxicity against HeLa cells and was further investigated for its ability to induce apoptosis in HeLa cells. HMO induced apoptosis up to 20.41% in HeLa cells versus control group (0.40%). Antioxidant/oxidative properties of L.M.P and HMO were investigated using extracellular (DPPH), and intracellular (ROS) assays. Experimental samples represented a time and concentration-dependent formation of ROS in Hela cells. Generation of ROS seems one of the mechanisms by which HMO induces apoptosis in Hela cells. Conclusion is that the active components in L.M.P might serve as a mediator of the ROS scavenging system and have the potential to act as prooxidant or antioxidant depending on the biological environment of the cells.

Tyrosinase activity of Greyia flanaganii (Bolus) constituents.

Hyper-pigmentation of the skin is a common problem that is prevalent in middle aged and elderly people. It is caused by over production of melanin. Tyrosinase is known to be the key enzyme in melanin production. Ethanolic extract of Greyia flanaganii leaves showed significant (P<0.05) antityrosinase activity exhibiting the IC50 of 32.62 µg/ml. The total extract was further investigated for its toxicity and effect on melanin production by melanocytes cells, and showed significant inhibition (P<0.05) (20%) of melanin production at 6.25 µg/ml and low levels of cytotoxicity (IC50<400 µg/ml). The amount of antioxidants necessary to decrease the initial DPPH absorbance by 50% (EC50) by the total ethanolic extract was found to be 22.01 µg/ml. The effect of G. flanaganii against acne causing bacteria, Propionibacterium acnes, was investigated using microdilution assay. The MIC of the extract of G. flanaganii was found to be 250 µg/ml. Bioassay-guided fractionation led to the isolation of (3S)-4-hydroxyphenethyl 3-hydroxy-5-phenylpentanoate (1), 2',4',6'-trihydroxydihydrochalcone (2), 2',6',4-trihydroxy-4'-methoxydihydrochalcone (3), 2',6'-dihydroxy-4'-methoxydihydrochalcone (4), 5,7-dihydroxyflavanone [(2S)-pinocembrin] (5), 2',6'-dihydroxy-4',4-dimethoxy dihydrochalcone (6) and (2R,3R)-3,5,7-trihydroxy-3-O-acetylflavanone (7). The isolated compounds were tested for their antioxidant, cytotoxicity, tyrosinase inhibition and antibacterial activities. Compound 2 exhibited significant (P<0.05) antityrosinase activity exhibiting the IC50 of 69.15 µM. The isolated compounds showed low toxicity of the cells with reduction of melanin content of the cells. All compounds tested showed good radical scavenging activity. These data indicates that G. flanaganii extract and its isolated phenolic constituents could be possible skin lightening agents.

Hypoglycemic evaluation of a new triterpene and other compounds isolated from Euclea undulata Thunb. var. myrtina (Ebenaceae) root bark.

AIM OF THE STUDY: Investigate the hypoglycaemic activity of the four isolated compounds from a crude acetone extract of the root bark of Euclea undulata var. myrtina, which is used by traditional healers in the Venda area, Limpopo Province in the treatment of diabetes. MATERIAL AND METHODS: The hypoglycaemic activity of the four compounds isolated from Euclea undulata was determined by in vitro screening of glucose utilization by C2C12 myocytes at a concentration of 25 µg/ml or 50 µg/ml. The inhibition of α-glucosidase was also tested at concentrations ranging from 0.02 to 200.00 µg/ml. RESULTS: Assay-guided isolation of the crude acetone extract of the root bark of Euclea undulata var. myrtina afforded a new triterpene, α-amyrin-3O-ß-(5-hydroxy) ferulic acid (1), in addition to three known compounds; betulin (2), lupeol (3) and epicatechin (4). The in vitro results on C2C12 myocytes suggest that compound 4 may have some effect to lowers blood glucose levels, whereas compound 1 has the ability to inhibit α-glucosidase at a concentration of 200.0 µg/ml with an IC50 value of 4.79 that correlates with that of the positive control acarbose IC50 value 4.75. CONCLUSION: The results suggest that 4 may have some ability to lower blood glucose levels, whereas 1 has the ability to inhibit α-glucosidase. ETHNOPHARMACOLOGICAL RELEVANCE: These findings corroborate the ethnomedicinal use of Euclea undulata by traditional healers for the treatment of diabetes as two substances was isolated from the acetone plant extract that exhibit hypoglycaemic activity.

Evaluation of flavonoids from Dorstenia barteri for their antimycobacterial, antigonorrheal and anti-reverse transcriptase activities.

The aim of this study was to evaluate the antimycobacterial, antigonorrheal and reverse transcriptase activities of five flavonoids: isobachalcone (IBC); kanzanol C (KAN); 4-hydroxylonchocarpin (4-LCP); stipulin (SPL) and amentoflavone (AMF) from Dortenia barteri, together with the crude extract from this plant. The Agar disc diffusion, broth microdilution, microplate alamar blue assay (MABA), radiometric respiratory technique using BACTEC 460 system and the reverse transcriptase (RT) assay were used for the investigations. The results of the antimycobacterial assay showed that the crude extract and compounds were able to prevent the growth of Mycobacteria with MIC<10 microg/ml being recorded with IBC on M. tuberculosis. Results of the killing rate experiment revealed that total inhibition effect on M. tuberculosis H37Rv strain was noted with IBC and SPL at day 9 when tested at 4x MIC. The results of the antigonorrheal assay indicated that MIC values below 10 microg/ml were also recorded with IBC on all the tested N. gonorrhoeae strains, meanwhile good activities (MIC<10 microg/ml) were also noted with the extract, KAN, 4-LCP and SPL on some of these strains. The anti-reverse transcriptase activities of extract and compounds also demonstrated that all samples were able to inhibit at various extents the reverse transcriptase activity, with IBC and 4-LCP showing the best effects. The overall results of this work provided evidence that the crude extract as well as some flavonoids from D. barteri could be potential sources of new antimicrobial drug against tuberculosis (TB), gonorrhea and probably the acquired immunodeficiency syndrome.

Crude extracts of, and purified compounds from, Pterocarpus angolensis, and the essential oil of Lippia javanica: their in-vitro cytotoxicities and activities against selected bacteria and Entamoeba histolytica.

In a recent study, various extracts of Pterocarpus angolensis were prepared and tested against bacteria. The acetone extract was found to be the most active against all the bacteria investigated, with minimum inhibitory concentrations varying from 0.0156 mg/ml against Staphylococcus aureus to 2 mg/ml against Enterobacter cloacae. Seven pure compounds were subsequently isolated from the ethanol extract of P. angolensis. Using several chromatographic and spectroscopic methods, the structures of five of these compounds - phthalate and four derivatives of epicatechin [(-)-epicatechin, epicatechin-3-O-galate, epicatechin (4beta-8)-epicatechin (B2), and a hexamer of epicatechin] - were successfully determined. The seven purified compounds were then further tested, in vitro, against Staphylococcus aureus and Entamoeba histolytica, and for their in-vitro cytotoxic activity. Although all seven were active against S. aureus, just one of the purified compounds from P. angolensis and piperitenone, a pure compound isolated from Lippia javanica essential oil, were found to have marked activity against Entamoeba histolytica, with median inhibitory concentrations (IC(50)) of 25 and 100 microg/ml, respectively. The other P. angolensis compounds were either weakly active or showed no activity against the amoebae when tested at concentrations up to 400 microg/ml. All seven compounds isolated from P. angolensis showed less toxicity against cultures of human (HCT-8) cells than piperitenone, with IC(50) of 175-375 microg/ml. The presence of epichatechin and derivatives (with strong antibacterial activities but generally weak activities against Entamoeba histolytica) in the stem bark of P. angolensis has thus been demonstrated. Further investigation of the activities of these compounds and their potential use in the treatment of bacterial diseases appears justified.

Hypoglycaemic activity of four plant extracts traditionally used in South Africa for diabetes.

AIM: To validate plant species for hypoglycaemic activity. MATERIALS AND METHODS: Four plants were investigated for hypoglycaemic activity by evaluating inhibiting effects on carbohydrate-hydrolising enzymes: alpha-glucosidase and alpha-amylase. Acetone plant extracts were screened against C2C12 myocytes, 3T3-L1 preadipocytes and Chang liver cells by measuring glucose uptake. Cytotoxicity was done in preadipocytes and hepatocytes. RESULTS: Extract of Euclea undulata rootbark exhibited highest activity, displaying a glucose uptake of 162.2% by Chang liver cells at 50 microg/ml. An inhibition concentration of 50% for Euclea undulata was found to be 49.95 microg/ml for alpha-glucosidase and 2.8 microg/ml for alpha-amylase. No cytotoxicity was recorded for Euclea undulata, while Schkuhria pinnata and Elaeodendron transvaalense exhibited cytotoxicity at 12.5 microg/ml. Alpha-glucosidase and alpha-amylase assays showed inhibitory activity on enzymes for three plant extracts. CONCLUSION: Euclea undulata, Schkuhria pinnata and Elaeodendron transvaalense showed in vitro hypoglycaemic activity. Schkuhria pinnata and Elaeodendron transvaalense indicated cytotoxicity on 3T3-L1 preadipocytes and Chang liver cells. Euclea undulata, Pteronia divaricata and Elaeodendron transvaalense inhibited alpha-glucosidase and alpha-amylase enzymes. ETHNOPHARMACOLOGICAL RELEVANCE: Screening of plant extracts scientifically validated traditional use of Euclea undulata for treatment of diabetes. Cytotoxicity results revealed that acetone extracts of Schkuhria pinnata and Elaeodendron transvaalense are toxic and raise concern for chronic use.

In-vitro cytotoxicity and antimicrobial activities, against clinical isolates of Campylobacter species and Entamoeba histolytica, of local medicinal plants from the Venda region, in South Africa.

In the quest for alternative treatments against Campylobacter jejuni and Entamoeba histolytica, which are both aetiological agents of diarrhoea world-wide, the in-vitro activities against the two pathogens of extracts of 18 South African medicinal plants have recently been assessed. Forty extracts from the 18 plant species were prepared and tested against 110 clinical isolates of Campylobacter spp. In addition, extracts from eight of the plant species were tested against a standard strain (HM-1:IMSS) of E. histolytica, and the cytotoxicity of each of 19 extracts from 15 of the plant species was explored using Vero cell cultures and microdilution assays. At least one extract of each plant species investigated was found to be active against some of the Campylobacter isolates. Extracts of Lippia javanica and Pterocarpus angolensis had the highest antibacterial activity, each giving a minimum inhibitory concentration (MIC) of 90 microg/ml. Of the extracts tested against E. histolytica, however, only those of P. angolensis and Syzigium cordatum were found to have anti-amoebic activity, with MIC of 1.2 and 7.5 mg/ml, respectively. Although most of the extracts showed little toxicity against Vero cells, with most of the median inhibitory concentrations (IC(50)) recorded exceeding 400 microg/ml, an extract of Bauhinia galpini was quite toxic, with an IC(50) of just 2.7 microg/ml. Acetone and methanol extracts of several of the plants show promise as templates for the design of new anti-diarrhoeal therapies.

In vitro anti-HIV-1 properties of ethnobotanically selected South African plants used in the treatment of sexually transmitted diseases.

ETHNOPHARMACOLOGICAL RELEVANCE: [corrected The plants selected in this study are used traditionally in the treatment of sexually transmitted diseases and traditional healers interviewed claimed these plants can also help AIDS patients. AIM: To evaluating the in vitro anti-HIV properties of selected plants in various bioassays. MATERIALS AND METHODS: The extracts were evaluated for their inhibition against alpha-glycohydrolase, reverse transcriptase and viral proteins (NF-kappaB and Tat) which play a significant role in the HIV life cycle. RESULTS: Terminalia sericea extract (IC(50)=92mg/ml) exhibited a considerable alpha-glucosidase inhibitory activity which was better than acarbose (IC(50)=131mg/ml) under our assay conditions. In the reverse transcriptase assay, T. sericea also showed good inhibitory activity (IC(50)=43mg/ml), which was higher than that of the reference drug, Adriamycin (IC(50)=100mg/ml). The ethyl acetate extract of Elaeodendron transvaalense exhibited the most potent inhibitory activity in both the NF-kappaB and Tat assays with inhibitory activity of 76% and 75% respectively at a concentration of 15mg/ml. The acetone and chloroform extracts of E. transvaalense and Zanthoxylum davyi also showed good activity in the NF-kappaB and Tat assays.

The potential of South African plants against Mycobacterium infections.

ETHNOPHARMACOLOGICAL RELEVANCE: In South Africa, tuberculosis (TB) caused by Mycobacterium tuberculosis is the most commonly notified disease and the fifth largest cause of mortality, with one in ten cases of TB resistant to treatment in some areas. Many plants are used locally in traditional medicine to treat TB-related symptoms. AIM OF THE STUDY: The aim was to summarize currently available knowledge on South African plants used to treat TB symptoms, and antimycobacterial efficacy of plant-derived extracts and compounds. MATERIALS AND METHODS: The traditional uses of plants for respiratory ailments and TB were collated and tabulated. The antimycobacterial activity tests of extracts and chemical constituents of several of these plants and others using different methods and target organisms were summarized. RESULTS: Almost 180 plants used for TB-related symptoms in South African traditional medicine were documented. About 30% of these have been tested for antimycobacterial efficacy, mostly against fast-growing, non-pathogenic Mycobacterium species. CONCLUSIONS: Many plant species are used in traditional South African medicine to alleviate symptoms of TB, and several interesting leads have originated for further inquiry following in vitro antimycobacterial activity evaluation. However, much work remains to be done on the systematic assessment of anti-TB efficacy of local plants against pathogenic Mycobacterium species, both in vitro and in vivo.

Antimicrobial activity of medicinal plants against oral microorganisms.

Ethanol extracts of eight plant species used traditionally in South Africa for the treatment of oral diseases were investigated for in vitro antimicrobial activity against oral pathogens namely Actinobacillus actinomycetemcomitans, Actinomyces naeslundii, Actinomyces israelii, Candida albicans, Porphyromonus gingivalis, Privotella intermedia and Streptococcus mutans using the disk diffusion method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of ethanol extracts were determined against these microorganisms using micro dilution. The cytotoxicity and therapeutic index (TI) of selected active extracts were also determined. Out of eight plants, six (Annona senegalensis, Englerophytum magalismontanum, Dicerocarym senecioides, Euclea divinorum, Euclea natalensis, Solanum panduriforme and Parinari curatellifolia) exhibited MIC values ranging from 25.0 mg/ml to 0.8 mg/ml. Gram negative bacteria were found to be more resistant to the plant extracts than Gram positive bacteria, except for Euclea natalensis which inhibited all three Gram negative bacteria tested in this study. All plant extracts showed moderate cytotoxicity on the Vero cell line. The fifty percent inhibitory concentration (IC(50)) of all plants tested range from 92.3 to 285.1 microg/ml.

Antimicrobial activity of the crude extracts and compounds from Ficus chlamydocarpa and Ficus cordata (Moraceae).

The aim of this study was to evaluate the antimicrobial activity of the methanol extracts from Ficus chlamydocarpa (FCR), Ficus cordata (FCB), mixture of the two plants (FCM), as well as that of the isolated flavonoids Alpinumisoflavone (2), Genistein (3), Laburnetin (4), Luteolin (5) (isolated from FCR), Catechin (7) and Epiafzelechin (8) (isolated from FCB). Mycobacteria, fungi, Gram-positive and Gram-negative bacterial species were tested for their susceptibility to the above samples. The microplate dilution and radiometric respiratory methods were used to determine the susceptibility testing of the samples against Mycobacterium smegmatis and Mycobacterium tuberculosis, respectively. The disc diffusion assay was used to determine the sensitivity of the samples, whilst the micro-dilution method was used for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC) against fungi, Gram-positive and Gram-negative bacterial species. All the samples except compound 7 were found to be active to Mycobacterium smegmatis and the MIC ranged from 0.61 to 312.50microg/ml. Compound 4 showed the best activity against Mycobacterium tuberculosis exhibiting an MIC of 4.88microg/ml. The results of the diffusion test indicated that the crude extract from FCB, FCM as well as compounds 5 and 8 were able to prevent the growth of all tested (fungi, Gram-positive and Gram-negative bacteria) organisms. The inhibition effect of the crude extract from Ficus chlamydocarpa was observed on 10 (62.5%) of the 16 tested microorganisms (excluding mycobacteria) whereas that of compounds 4, 2 and 3 was respectively noted on 14 (87.5%), 8 (50.0%) and 7 (39.9%) of the tested microbial species. FCB was found to be more active than FCR on most of the tested organisms. The results provided evidence that the studied plants extract, as well as some of the isolated compounds might be potential sources of new antimicrobial drug.

Tyrosinase inhibition by extracts and constituents of Sideroxylon inerme L. stem bark, used in South Africa for skin lightening.

OBJECTIVE: To investigate the stem bark of Sideroxylon inerme L. and its compounds for tyrosinase-inhibition activity and to evaluate the mechanism involved of the most potent compounds in tyrosinase inhibition. MATERIALS AND METHODS: Three different extracts (acetone, methanol and dichloromethane) of Sideroxylon inerme L. were evaluated for their inhibitory effect in vitro on the monophenolase and diphenolase activated forms of tyrosinase, using a colorimetric procedure. This test was used for bioactivity-guided isolation of two active compounds using column chromatography and TLC. Active extracts were also investigated for their inhibitory effect on melanogenesis in cultured B16 melanoma cells. Antioxidant activities of the methanolic extract of Sideroxylon inerme and purified compounds were investigated using the 1,2-diphenyl-2-picrylhydrazyl (DPPH) antioxidant assay. The inhibition of tyrosinase activity relative to the inhibition of its activity at the transcriptional level was also studied by determination of the degree of expression of mRNAs for this gene by using extract of Sideroxylon inerme-treated cells (B16F10) and semi-quantitative RT-PCR. RESULTS: Methanolic and acetonic extracts of the stem bark of Sideroxylon inerme showed significant inhibition of monophenolase activity (IC50 values of 63 microg/ml and 82 microg/ml, respectively). The methanolic extract also exhibited 37% reduction of melanin content at 6.2 microg/ml in melanocytes without being significantly toxic to the cells. Examination for inhibition of monophenoloxidase in situ on TLC, followed by column chromatographic purification of the stem bark extract of Sideroxylon inerme, resulted in the isolation of two active compounds, epigallocatechin gallate and procyanidin B1, with IC50 values against monophenolase of 30 microg/ml and > 200 microg/ml, respectively. Epigallocatechin gallate exhibited a greater anti-tyrosinase activity than arbutin. Sideroxylon inerme bark extracts, epigallocatechin gallate and procyanidin B1 exhibited antioxidant DPPH radical scavenging activities with EC50 values of 1.54 microg/ml, 1.33 microg/ml and 1.68 microg/ml, respectively and were not particularly cytotoxic. During mechanism studies it was evident that at the transcription level, Sideroxylon inerme (25 microg/ml) was acting as a potent tyrosinase inhibitor compared to controls (untreated cells and kojic acid). CONCLUSION: The bark extract of Sideroxylon inerme and the two isolated compounds warrant further investigation in clinical studies to be considered as skin-depigmenting agents.

Activity of 7-methyljuglone in combination with antituberculous drugs against Mycobacterium tuberculosis.

The recent increase in the incidence of tuberculosis with the emergence of multidrug-resistant (MDR) cases has lead to the search for new drugs that are effective against MDR strains of Mycobacterium tuberculosis and can augment the potential of existing drugs against tuberculosis. In the present study, we investigated the activities of a naphthoquinone, 7-methyljuglone, isolated from the roots of Euclea natalensis alone and in combination with other antituberculous drugs against extracellular and intracellular M. tuberculosis. Combinations of 7-methyljuglone with isoniazid or rifampicin resulted in a four to six-fold reduction in the minimum inhibitory concentration of each compound. Fractional inhibitory concentration (FIC) indexes obtained were 0.2 and 0.5, respectively, for rifampicin and isoniazid, suggesting a synergistic interaction between 7-methyljuglone and these anti-TB drugs. The ability of 7-methyljuglone to enhance the activity of isoniazid and rifampicin against both extracellular and intracellular organisms suggests that 7-methyljuglone may serve as a promising compound for development as an anti-tuberculous agent.

Antibacterial activities of medicinal plants used for the treatment of diarrhoea in Limpopo Province, South Africa.

The ethnobotanical survey conducted in this study showed that 21 plant species belonging to 14 families are used in traditional medical practice in Limpopo Province, South Africa, for the treatment of diarrhoea. Methanol, ethanol, acetone and hot water extract from different plant parts (leaves, roots, bark and stem rhizome), of several of these plants (Indigofera daleoides, Punica granatum, Syzygium cordatum, Gymnosporia senegalensis, Ozoroa insignis, Elephantorrhiza elephantina, Elephantorrhiza burkei, Ximenia caffra, Schotia brachypetala and Spirostachys africana), were screened for antibacterial activity against Vibro cholera, Escherichia coli and Staphylococcus aureus, Shigella spp., Salmonella typhi. The antibacterial activity was determined by agar-well diffusion method and expressed as the average diameter of the zone of inhibition of bacterial growth around the wells. The minimum inhibitory concentration (MIC) of active extracts was determined by using the micro-plate dilution assay. Most of the extracts showed relatively high antibacterial activity against most of the tested microorganisms with the diameter of inhibition zones ranging between 10 and 31 mm. Of the plants studied, the most active extracts were those obtained from Punica granatum and Indigofera daleoides. All extracts from two plants, namely, Punica granatum and Ozoroa insignis, were active against all bacterial strains while only organic extracts of Indigofera daleoides inhibited the growth of all tested microorganisms. Water extract of Punica granatum were equally active as organic extracts against bacteria such as Staphylococcus aureus, Shigella sonnei and Shigella flexneri. All extracts of Elephantorrhiza elephantina, Elephantorrhiza burkei and Ximenia caffra and Schotia brachypetala were not active against Escherichia coli and Salmonella typhi. The MIC values for active extracts ranged between 0.039 and 0.6 mg/ml. The results obtained appeared to confirm the antibacterial potential of the plants investigated, and their usefulness in the treatment of diarrhoea.

Antiviral and antituberculous activity of Helichrysum melanacme constituents.

Bioassay guided fractionation of the acetonic extract of Helichrysum melanacme using human Influenza virus type A and a drug-sensitive strain of Mycobacterium tuberculosis in vitro resulted in the isolation of 2 4',6'-trihydroxy-3'-prenylchalcone (1) and 4',6',5''-trihydroxy-6'',6''-dimethyldihydropyrano[2'',3''-2',3'] chalcone (2) as active constituents. 3-O-methylquercetin and quercetin were also isolated but were inactive against the microorganisms tested in this study.

Characterization of Intracellular Activity of Antitubercular Constituents the Roots of Euclea natalensis.

Naphthoquinones and triterpenes isolated from the roots of Euclea natalensis. A.DC (Ebenaceae) were evaluated for their inhibitory activity against Mycobacterium tuberculosis.. Crude extract, diospyrin and 7-methyljuglone isolated from the plant, exhibited minimum inhibitory concentrations of 8.0, 8.0, and 0.5 µg ml-1, respectively, against M. tuberculosis. H37 Rv (ATCC 27294), a drug-sensitive strain. Minimum inhibitory concentrations (MICs) of 7- methyljuglone against a panel of clinical pan-sensitive and drug-resistant strains of M. tuberculosis. ranged from 0.32 to 1.25 µg/ml. The concentration of 7-methyljuglone that effected a 90% reduction of growth of M. tuberculosis. Erdman within J774.1 macrophages was 0.57 µg/ml. The superior intracellular and extracellular inhibition of M. tuberculosis. by 7-methyljuglone relative to that of the antituberculosis drugs streptomycin and ethambutol suggests that this compound be considered as a lead for further investigations.

Antimycobacterial activity of diospyrin derivatives and a structural analogue of diospyrin against Mycobacterium tuberculosis in vitro.

Three derivatives and one structural analogue of diospyrin were synthesized and investigated for their inhibitory activity against Mycobacterium tuberculosis employing the rapid radiometric method in vitro. A novel aminoacetate derivative was found to be more active than the parent compound, the MICs being 50 and 100 mg/L, respectively, for a drug-susceptible strain, H37Rv, of M. tuberculosis. This derivative also exhibited an MIC of 50 mg/L for a few multidrug-resistant strains of M. tuberculosis. The other two derivatives and the analogue did not show any significant antimycobacterial activity at the highest concentration (100 mg/L) tested.