Pharmacology and Therapeutics

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(4-methoxy-benzo [1, 3] dioxol-5-yl)-phenylmethanone: An antibacterial benzophenone from Securidaca longepedunculata
(African Journal of Traditional, Complementary and Alternative Medicines, 2006-03-27) Moshi, Mainen J.
The dichloromethane extract of Securidaca longepedunculata Fresen yielded a benzophenone, (4-methoxy-benzo[1,3]dioxol-5-yl)-phenylmethanone (1), together with other three known compounds, 1,7-dihydroxy-4-methoxyxanthone (2), benzyl 2-hydroxy-6-methoxybenzoate (3), and methyl 2-hydroxy-6-methoxybenzoate (4). Compound (1) exhibited antibacterial activity against Pseudomonous aeruginosa, and antifungal activity against Aspergillus fumigatus. Compound 2 exhibited antibacterial activity against Staphylococus aureus, and antifungal activity against Aspergillus niger, Aspergillus fumigatus and a Penicillum species. Compounds 3 and 4 were inactive against all the tested bacteria and fungi. These results provide proof of efficacy of the extracts of S.longepedunculata in treating bacterial infections, but further studies should be carried out to ascertain these results with respect to the widely reported traditional use.
Analysis of Combined Effect of CYP2C19 Genetic Polymorphism and Proton Pump Inhibitors Coadministration on through concentration of Voriconazole
(Pharmacogenomics and Personalized Medicine, 2021) Mafuru, Magesa; Phillip, Amani; Mgone, Charles S.
Purpose: To analyze the combined effect of CYP2C19 genetic polymorphism and PPIs coadministration on voriconazole trough concentration (VCZ-Ctrough) in Chinese patients with hematological disorders. Patients and Methods: A prospective observational study involved 250 plasma samples from 114 adult patients receiving voriconazole with or without PPIs were analyzed. Demographics and clinical characteristics were obtained from patient’s records. A validated LC-MS/MS was used to quantify the plasma VCZ-Ctrough. Genotyping for CYP2C19*2 and CYP2C19*3 variant alleles was performed by PCR-RFLP followed by DNA sequencing. The combined total score (from 2 to 5) was calculated for each patient. The higher the score, the lesser the metabolism of the patient. Findings: Fifty percent of patients administered with voriconazole were coadministered with PPIs, predominantly omeprazole or esomeprazole. Patients exhibiting CYP2C19 poor metabolizer phenotype showed a significantly higher median VCZ-Ctrough, (4.31µg/mL [IQR, 1.64µg/mL–7.36µg/mL]) than patients with normal metabolizer (1.38µg/mL, [IQR, 0.79µg/mL–2.14µg/mL], p < 0.0001). Similarly, patients co-administration with PPIs had higher median VCZ-Ctrough (2.86µg/mL [IQR 1.33µg/mL–4.66µg/mL]), than PPIs non-users (1.71µg/mL, [IQR, 0.86µg/mL–3.48µg/mL], p = 0.001). However, we noted that the median VCZ-Ctrough for each factor was ranging within the normal recommended therapeutic range in the Chinese population (0.5µg/mL–5µg/mL). But when the two factors were combined, the median VCZ-Ctrough was steadily increasing as the metabolic capacity (reflected by combined total score) was increasing. Importantly, the median VCZ-Ctrough in PM/PPIs user (total score 5) was significantly elevated to supra-therapeutic levels compared to NM/PPI non-user group (total score 2) (5.83µg/mL [IQR, 2.19µg/mL–9.51µg/mL] versus 1.13µg/mL [IQR, 0.67µg/mL–1.82µg/mL]), respectively, P < 0.0001. Furthermore, we observed that the elevation of median VCZ-Ctrough to supra-therapeutic levels was largely contributed by omeprazole or esomeprazole compared to lansoprazole or pantoprazole. Conclusion: Coadministration with PPIs significantly increased voriconazole trough concentrations and there was an additive effect in CYP2C19 PMs, who were most likely to have supra-therapeutic levels.
Anthranoid Compounds with Antiprotozoal Activity from Vismia orientalis
(Planta Medica, 2004-08) Moshi, Mainen J.
A phytochemical investigation of the 80% ethanolic extract of stem bark of Vismia orientalis Engl. (Guttiferae or Clusiaceae), a plant used in traditional medicine in Tanzania, resulted in the isolation and spectroscopic characterisation of 3-geranyloxy-6-methyl-1,8-dihydroxyanthraquinone, emodin, vismione D and bianthrone A1. Vismione D exhibited a broad range of antiprotozoal activities against Trypanosoma brucei rhodesiense and T. cruzi (IC50 < 10 μg/mL), Leishmania donovani (IC50 0.37 μg/mL) and Plasmodium falciparum strain K1 (IC50 1.0 μg/mL). However, it was also slightly cytotoxic against human L6 cells (IC50 4.1 μg/mL). Emodin showed antileishmanial activity (IC50 2.0 μg/mL), while its IC50 against L6 cells was 20.3 μg/mL. Other antiprotozoal activities observed for emodin against both Trypanosoma species and P. falciparum, for bianthrone A1 against T. b. rhodesiense and P. falciparum, and for 3-geranyloxy-6-methyl-1,8-dihydroxyanthraquinone against T. b. rhodesiense, L. donovani and P. falciparum were in the range of 10 to 50 μg/mL. None of the compounds showed antibacterial or antiviral (including also HIV) activity. Key words Vismia orientalis - Guttiferae - Clusiaceae - 3-geranyloxy-6-methyl-1,8-dihydroxyanthraquinone - bianthrone A1 - emodin - vismione D - Plasmodium falciparum - Leishmania - Trypanosoma
Anti-plasmodial activity of Norcaesalpin D and extracts of four medicinal plants used traditionally for treatment of malaria
(BMC complementary and alternative medicine, 2017-03-24) Moshi, Mainen J.
Background: Malaria is an old life-threatening parasitic disease that is still affecting many people, mainly children living in sub-Saharan Africa. Availability of effective antimalarial drugs played a significant role in the treatment and control of malaria. However, recent information on the emergence of P. falciparum parasites resistant to one of the artemisinin-based combination therapies suggests the need for discovery of new drug molecules. Therefore, this study aimed to evaluate the antiplasmodial activity of extracts, fractions and isolated compound from medicinal plants traditionally used in the treatment of malaria in Tanzania. Methods: Dry powdered plant materials were extracted by cold macerations using different solvents. Norcaesalpin D was isolated by column chromatography from dichloromethane root extract of Caesalpinia bonducella and its structure was assigned based on the spectral data. Crude extracts, fractions and isolated compound were evaluated for antiplasmodial activity against chloroquine-sensitive P. falciparum (3D7), chloroquine-resistant P. falciparum (Dd2, K1) and artemisinin-resistant P. falciparum (IPC 5202 Battambang, IPC 4912 Mondolkiri) strains using the parasite lactate dehydrogenase assay. Results: The results indicated that extracts of Erythrina schliebenii, Holarrhena pubescens, Dissotis melleri and C. bonducella exhibited antiplasmodial activity against Dd2 parasites. Ethanolic root extract of E. schliebenii had an IC 50 of 1.87 μg/mL while methanolic and ethanolic root extracts of H. pubescens exhibited an IC 50 = 2.05 μg/mL and IC 50 = 2.43 μg/mL, respectively. Fractions from H. pubescens and C. bonducella roots were found to be highly active against K1, Dd2 and artemisinin-resistant parasites. Norcaesalpin D from C. bonducella root extract was active with IC 50 of 0.98, 1.85 and 2.13 μg/mL against 3D7, Dd2 and IPC 4912-Mondolkiri parasites, respectively. Conclusions: Antiplasmodial activity of norcaesalpin D and extracts of E. schliebenii, H. pubescens, D. melleri and C. bonducella reported in this study requires further attention for the discovery of antimalarial lead compounds for future drug development. Keywords: Antiplasmodial, norcaesalpin D, E. schliebenii, H. pubescens, D. melleri, C. bonducella
Antibacterial and cytotoxic triterpenoids from Lantana viburnoides ssp. viburnoides var. kisi
(Spatula DD-Peer Reviewed Journal on Complementary Medicine and Drug Discovery, 2011-12-07) Moshi, Mainen J.
Lantana viburnoides ssp. var. is used in traditional medicine as a mosquito repellent and sometimes chewed for treatment of gastrointestinal problems. Gastrointestinal problems are varied and may include microbial infections, parasitic infestation; inflammatory bowel disease, malignancies, peptic ulcers, or simply colic pains. This work seeks to establish proof of the concept on safety and efficacy for treatment of bacterial infections. METHODS Root and stem bark ethanol extracts, extract fractions and two isolated compounds were tested for antibacterial activity against five standard Gram positive and two Gram negative bacteria using the broth micro-dilution method. The extracts and isolated compounds were also tested for cytotoxic activity against brine shrimp larvae ( ). RESULTS The stem and root bark ethanol extracts exhibited strong antibacterial activity against (195.3 μg/ml) and (390.6 μg/ml). Camaric acid (1), isolated from the dichloromethane fraction of root bark extract, exhibited antimicrobial activity against (MIC = 19.5 μg/ml) (MIC = 19.5 μg/ml) (MIC = 9.76 μg/ml), (MIC = 4.88 μg/ml), and (MIC = 19.5 μg/ml), and was toxic to the shrimps (LC50 = 4.1 μg/ml). Betulinic acid (2) also from the same fraction exhibited poor anti-bacterial activity against all bacteria tested but showed high cytotoxic activity against brine shrimp larvae (LC50 = 2.4 μg/ml). Conclusion Detection of antibacterial activity and isolation of an antibacterial compound, camaric acid, from extracts of ssp. var. supports the traditional use of extracts of the plant for treatment of gastrointestinal problems. Betulinic acid and camaric acid are already established to have anticancer activity.
Anticonvulsant activity of diospyros fischeri root extracts
(African Journal of Traditional, Complementary and Alternative Medicines, 2007) Moshi, Mainen J.
Diospyros fischeri Gurke (Ebenaceae) is used in traditional medicine for the treatment of epilepsy. Dichloromethane, ethylacetate, and ethanol extracts of the roots, at doses between 100 and 1600 mg/kg BW, inhibited convulsions induced by the γ‐aminobutyric acid type A (GABAA) receptor antagonist, pentylenetetrazole (PTZ), in a dose dependent manner. The extracts also exhibited low toxicity against brine shrimps giving LC50 values between 45 .4 and 95.4 μg/ml. These results provide evidence for the potential of D. fischeri extracts to treat absence seizures, especially given their seemingly innocuous nature. Keywords: Diospyros fischeri; Pentylenetetrazole; Anticonvulsant activity; Brine shrimp toxicity
Anticonvulsant activity of extracts of diospyros fischeri stem bark
(African Journal of Traditional, Complementary, and Alternative Medicines, 2007-02-08) Moshi, Mainen J.
Evaluation of extracts of Diospyros fischeri Gurke (Ebenaceae), which is used traditionally for the treatment of epilepsy shows that the aqueous extract of the tem bark has no effect against picrotoxin induced convulsions in mice. However, an 80% ethanol extract of the bark caused dose‐dependent suppression of convulsions induced by 10 mg/kg body wt picrotoxin, , at doses between 100‐3200 mg/kg body wt. Petroleum ether, 1:1 dichloromethane:methanol, and methanol extracts also suppressed picrotoxin‐induced convulsions, but had a slightly lower inhibitory effect. The petroleum ether extract was the most active, but all were less active than the ethanol extract. Unlike phenobarbitone, which at 50 mg/kg body wt completely suppressed convulsions induced by 10 mg/kg body wt picrotoxin, none of the plant extracts completely suppressed convulsions in the mice. These results support the traditional uses of D.fischeri for the treatment of epilepsy. Given the seemingly innocuous nature of the extracts more work is suggested to ascertain their clinical application. Key words: Diospyros fischeri; Picrotoxin; Anti‐convulsant activity
Antifungal activity of some Tanzanian plants used traditionally for the treatment of fungal infections
(2006-11-03) Moshi, Mainen J.
Using the ethnobotanical approach, some Tanzanian plants reported to be used by traditional healers for the treatment of oral candidiasis and fungal infections of the skin were collected and screened for their antifungal activity against Candida albicans, Candida glabrata, Candida tropicalis, Candida parapsilosis, Candida krusei and Cryptococcus neoformans. A total of 65 crude methanol extracts belonging to 56 plant species and 38 families were screened using the broth microdilution method, according to the guidelines of the Clinical and Laboratory Standard Institute (CLSI) (formerly, National Committee for Clinical and Laboratory Standards) [National Committee for Clinical Laboratory Standards, 2002. Reference Method for Broth Dilution Antifungal Susceptibility Testing of Yeasts. Approved Standard-2nd Edition M27-A2, National Committee for Clinical Laboratory Standards, Wayne, PA, USA]. Among the tested plant species, 45% (25 species) showed antifungal activity against one or more of the test fungi. The most susceptible yeasts were Cryptococcus neoformans, followed by Candida krusei, Candida tropicalis, and Candida parapsilosis. The least susceptible were Candida albicans and Candida glabrata. Strong antifungal activity was exhibited by extracts of Clausena anisata Oliv., Sclerocariya birrea Sond, Turraea holstii Gurk, Sterculia africana (Lour) Fiori, Acacia robusta subsp. Usambarensis (Taub) Brenan, Cyphosterma hildebrandti (Gilg), Desc, Elaeodendron buchannanii (Lows), Acacia nilotica (L.) Wild ex Del, Jatropha multifida L., and Pteridium aquilinum (L.) Kuhn.
Antimalarial activity, Plasmodium berghei, traditional medicines.
(African Journal of Traditional, Complementary and Alternative Medicines, 2009) Moshi, Mainen J.
Aqueous ethanol (80%) extracts of six plants used traditionally for treatment of malaria, Vepris glomerata (F.Hoffm.) Engl (Rutaceae), Maranthus floribunda (Bak.) F.White (Chrysobalanaceae), Strophanthus eminii Asch. & Pax ex Pax (Apocynaceae), Cassia abbreviata Oliv. (Leguminosae) and Caesalpinia bonducella L. Fleming (Fabaceae) were screened for antimalarial activity to establish validity of their claims. The extracts exhibited antimalarial activity in the 4-day Peter’s suppressive antimalarial assay in mice inoculated with red blood cells parasitized with Plasmodium berghei. The extracts gave ID50 values of 42.8, 111.0, 639.3 and 1560 mg/kg body wt for C. bonducella, C. abbreviata, T. furialis and S. eminii, respectively. The ID50 values for V. glomerata and M. floribunda were above 2400 mg/kg body wt, above which point solubility was a problem. All the tested extracts were innocuous to the mice, up to 2400 mg/kg body wt, suggesting they may be safe for short-term use.
Antimicrobial activity and brine shrimp toxicity of extracts of Terminalia brownii roots and stem
(BMC complementary and Alternative Medicine, 2007-03-30) Moshi, Mainen J.
Background: Ternimalia brownii Fresen (Combretaceae) is widely used in traditional medicine to treat bacterial, fungal and viral infections. There is a need to evaluate extracts of this plant in order to provide scientific proof for it's wide application in traditional medicine system. Methods Extraction of stem bark, wood and whole roots of T. brownii using solvents of increasing polarity, namely, Pet ether, dichloromethane, dichloromethane: methanol (1:1), methanol and aqua, respectively, afforded dry extracts. The extracts were tested for antifungal and antibacterial activity and for brine shrimp toxicity test. Results Extracts of the stem bark, wood and whole roots of T. brownii exhibited antibacterial activity against standard strains of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, and Bacillus anthracis and the fungi, Candida albicans and Cryptococcus neoformans. Aqueous extracts exhibited the strongest activity against both bacteria and fungi. Extracts of the roots and stem bark exhibited relatively mild cytotoxic activity against brine shrimp larvae with LC50 values ranging from 113.75–4356.76 and 36.12–1458.81 μg/ml, respectively. The stem wood extracts exhibited the highest toxicity against the shrimps (LC50 values 2.58–14.88 μg/ml), while that of cyclophosphamide, a standard anticancer drug, was 16.33 (10.60–25.15) μg/ml. Conclusion These test results support traditional medicinal use of, especially, aqueous extracts for the treatment of conditions such as diarrhea, and gonorrhea. The brine shrimp results depict the general trend among plants of the genus Terminalia, which are known to contain cytotoxic compounds such as hydrolysable tannins. These results warrant follow-up through bioassay-directed isolation of the active principles.
Antimicrobial activity and phytochemical screening of Antidesma venosum root and stem bark ethanolic extracts
(International Journal of research in Phytochemistry and Pharmacology, 2012-06-26) Moshi, Mainen J.
Antidesma venosum E. Mey. ex Tull root and stem bark ethanol extracts and their dichloromethane, petroleum ether and methanol fractions exhibited strong antibacterial activity against 5 Gram positive bacteria including Staphylococcus aureus (ATCC25923), Bacillus anthracis (NCTC10073), Bacillus subtilis (clinical isolate), Streptococcus faecalis (clinical isolate) and Bacillus cerius (clinical isolate) with MICs ranging from 0.0195 to 0.7812 mg/ml. The crude ethanol extracts of both the stem bark and roots were inactive against Gram negative bacteria except for Pseudomonas aeruginosa (ATCC 29953) against which they both exhibited weak activity MIC 1.25 and 5.0 mg/ml, respectively, Escherichia coli (ATCC 25922) and Klebsiella pneumoniae (ATCC 700603) which gave MICs between 2.50-5.00 mg/ml. The Petroleum ether and dichloromethane fractions of the root ethanol extract showed weak activity against almost all the Gram negative bacteria with MICs between 2.5 and 5.0 mg/ml. Whereas the crude extracts did not show antifungal activity, the petroleum ether and dichloromethane fractions of both the root and stem bark ethanol extracts showed weak activity against Candida albicans (ATCC 90028) and Cryptococcus neo-formans (clinical isolate), MIC 2.5-5.0 mg/ml. The extracts of the stem bark and roots exhibited mild to moderate toxicity against brine shrimp larvae with LC50 ranging between 25.56-40.93 µg/ml for the stem bark and 62.97-80.26 µg/ml for the root ethanol extract. Phytochemical screening revealed the presence of terpenoids, tannins and steroids in both the root and stem bark extracts. These results show promising activity against Gram positive bacteria, especially by the petroleum ether and dichloromethane fractions of the roots and thus support the popular use of this plant for the treatment of conditions associated with bacterial infections such as cut wounds, chest infections and some types of diarrhoea. Further studies are ongoing to identify the active compounds.
Antimicrobial activity, acute toxicity and cytoprotective effect of Crassocephalum vitellinum (Benth.) S. Moore extract in a rat ethanol-HCl gastric ulcer model
(BMC research notes, 2014) Moshi, Mainen J.
A decoction of Crassocephallum vitellinum (Benth.) S. Moore (Asteraceae) is used in Kagera Region to treat peptic ulcers. This study seeks to evaluate an aqueous ethanol extract of aerial parts of the plant for safety and efficacy.
Antimicrobial and brine shrimp lethality of extracts of Terminalia mollis Laws
(African Journal of Traditional, Complementary and Alternative Medicines, 2006) Moshi, Mainen J.
Using the disc diffusion method it was demonstrated that extracts of the leaves, stem and roots of Terminalia mollis Laws (Combretaceae) have antibacterial activity against Staphylococcus aureus (NCTC 6571), Escherichia coli (NCTC 10418), Pseudomonas aeruginosa (NCTC 10662), Klebsiella pneumoniae (NCTC 9633), Salmonella typhi (NCTC 8385), and Bacillus anthracis (NCTC 10073) and antifungal activity against Candida albicans (Strain HG 392), and local strains of Aspergillus flavus and Cryptococcus neoformans. The root extracts were the most active followed by the stem, and leaf extracts. Extracts of the three parts also exhibited cytotoxicity to brine shrimp larvae with LC50 values ranging from 26.3 to 58.1, l0.4 to 69.5, and 42.9‐ 101.3μg/ml, for the root, stem, and leaf extracts, respectively. The results support the traditional uses of extracts of this plant for the management of bacterial and fungal infections. Key words: Terminalia mollis, Antimicrobial activity, Traditional medicine.
Antimicrobial and brine shrimp toxicity of some plants used in traditional medicine in Bukoba District, north-western Tanzania
(Tanzania Journal of Health Research, 2009-01) Moshi, Mainen J.
Herbal medicines constitute a potentially important resource for new and safe drugs for the management of microbial infections and other diseases. In this study, dichloromethane, ethylacetate and ethanol extracts of Canarium schweinfurthii Engl., Dissotis brazzae Cong., Iboza urticifolia (Bak) E.A.Bruce, Isoglosa lacteal Lindau, Strombosia Scheffleri Engl., and Whitfieldia elongate T. Anders were tested for antimicrobial activity and brine shrimp toxicity. The objective was to validate claims that they are used to treat bacterial infections, diarrhoea and heal wounds among the Haya tribe of north-western Tanzania. At least one extract of each plant showed antibacterial activity. Dichloromethane extracts were the most active while ethanol extracts were the least active. Extracts of Whitfieldia elongate and Isoglossa lacteal were the most and least active with MICs in the range 0.08-0.62 mg/ml and 15.6-62.5 mg/ml, respectively. The dichloromethane extract of Whitfieldia elongate exhibited strong antifungal activity against Cryptococcus neoformans. Against brine shrimp larvae, the extracts from the six plants exhibited a low to very low toxicity with LC50 values ranging from 15.35-374.0µg/ml. However, ethanol extracts of Dissotis brazzae and Strombosia scheffleri had LC50 values of >1000µg/ml. The seemingly innocuous nature and relatively good antibacterial activity against skin infections and gastrointestinal pathogenic bacteria support the traditional uses of the plants and deserve more detailed studies.
Antimicrobial and brine shrimp activity of Acanthus pubescens root extracts
(Tanzania Journal of Health Research, 2010-04) Moshi, Mainen J.
The root dichloromethane and ethyl acetate extracts of Acanthus puberscens (Oliv.) Engl (ACANTHACEAE) exhibited weak antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Bacillus anthracis, Salmonella typhi, Streptococcus faecalis, Streptococcus agalactiae and Pseudomonas aeruginosa, with MIC values ranging from 1.6-6.25 mg/ml. The two extracts also exhibited weak antifungal activity against Candida albicans (MIC 6.25 mg/ml). Using the brine shrimps lethality test ethanol, ethyl acetate and aqueous extracts were virtually non-toxic to brine shrimp larvae, but the dichloromethane extract (LC50 38.9 µg/ml) was mildly toxic. These results support the use of the plant in traditional medicine to treat gonorrhea, syphilis, gastroenteritis and pneumonia. Since the plant is used in combination with other plants it is difficult to make any final conclusions regarding safety and efficacy. Further work is needed to evaluate the activity of an extract made from a combination of the six plants.
Antimycobacterial activity and brine shrimp toxicity of wild mushrooms used by communities in southern Tanzania
(Research Journal of Pharmacognosy, 2024-03-12) Moshi, Mainen J.
Background and objectives: Several wild mushroom species occur in southern Tanzania and are used as food by the local tribes. Experience shows that some of them could contain phytochemical compounds with therapeutic potential for treating various diseases. This study aimed to evaluate wild mushrooms used by indigenous communities living near the Selous- Niassa corridor in Namtumbo district, in Southern Tanzania for safety and antimycobacterial activity. Methods: Wild mushroom samples were collected randomly during the wet season and extracted by cold maceration. Dried extracts were evaluated for safety using the brine shrimp lethality test and for antimycobacterial activity using a twofold microdilution method against non-pathogenic Mycobacterium madagascariense, Mycobacterium indicus pranii, and Mycobacterium aurum. Results: The mushroom extracts exhibited a good safety profile against brine shrimp larvae with LC50 values ranging from 20.28 µg/mL (moderately toxic) to 465.97 µg/mL (nontoxic). The extracts exhibited variable antimycobacterial activity against M. madagascariense, M. indicus pranii, and M. aurum with minimum inhibitory concentrations (MIC) between 0.78 and 12.5 mg/mL against M. madagascariense, 0.098 and 6.25 mg/mL against M. indicus pranii and 1.25 and 2.5 mg/mL against and M. aurum. Nineteen wild mushroom species (59.4%, n = 32) exhibited antimycobacterial activity against all three mycobacterial species used. Conclusion: Preliminary investigation has provided evidence that some of the mushrooms locally available are not toxic. Some of these mushrooms have the potential to yield antimicobacterial active compounds. Further studies to determine the therapeutic and nutritional value of these mushrooms are needed. Keywords: anti-mycobacterial; brine shrimp lethality test; therapeutic potential; wild mushrooms
Antimycobacterial activity of scopoletin from ethanolic extract of Hymenodictyon floribundum (Hochst. & Steud.) B.L.Rob. Stem bark
(Scientific African, 2023-06-21) Moshi, Mainen J.
The available tuberculosis (TB) therapies are taken for long time with complex regimens associated with adverse effects and drug-drug interactions. The emergence of multidrug resistant (MDR) and extensively drug resistant (XDR) strains of Mycobacterium tuberculosis and HIV co-infections necessitates the need for continued search for new effective anti-TB alternative leads with different mechanisms of action and safety profile. The aim of this study was to isolate and characterize antimycobacterial compounds from Hymenodictyon floribundum (Hochst. & Steud.) B.L.Rob. a plant used traditionally in the management of HIV/AIDS-related conditions. Antimycobacterial activity of the plant extracts and its constituents against Mycobacterium indicus pranii (MIP) and Mycobacterium madagascariense (MM) was tested using a twofold broth micro-dilution technique. Bioassay-guided isolation was used to isolate active compounds. Isolated compounds were also tested for activity against clinical isolates of Mycobacterium tuberculosis (Mtb). The crude plant extract had antimycobacterial activity and its ethyl acetate fraction was the most active with minimum inhibitory concentration (MIC) values of 97 µg/ml and 197 µg/ml against MIP and MM respectively. Three compounds were isolated from the ethyl acetate fraction; 7‑hydroxy-6-methoxycoumarin (1), 7,7′-dihydroxy-6,6′-dimethoxy-3,3′-biscoumarin (2) and 7,7′-dihydroxy-6,6′-dimethoxy-8,8′-biscoumarin (3). Compound 1 had growth inhibitory activity against MIP, MM and Mtb with MIC values of 0.2 M against MIP, 0.41 M against MM, 0.78 M against Mtb1 and 1.63 M against Mtb2. In conclusion, 7-Hydroxy-6- methoxycoumarin exhibited moderate antimycobaterial activity. The findings from this study support the use of H. floribundum by traditional health practitioners for treatment of HIV and AIDS-related conditions.
Antiparasitic Activity of Some xanthones and biflavonoids from the root bark of garcinia livingstonei
(Journal of natural products, 2006) Moshi, Mainen J.
A new biflavanoid, ent-naringeninyl-(I-3α,II-8)-4‘-O-methylnaringenin (6), along with five known xanthones and two known biflavonoids, was isolated from the root bark of Garcinia livingstonei collected in Tanzania. The absolute configuration of 6 was established by CD spectroscopy. This compound showed moderate activity against P. falciparum (IC50 6.7 μM). Antitrypanosomal activity (IC50 0.87 μM) was observed for 1,4,5-trihydroxy-3-(3-methylbut-2-enyl)-9H-xanthen-9-one (3). The dimeric xanthone garcilivin A (4) showed a higher and nonselective antiparasitic activity and cytotoxicity (IC50 2.0 μM against MRC-5 cells) than its diastereoisomer garcilivin C (5) (IC50 52.3 μM).
Antiplasmodial Biflavanones from the Stem Bark of Garcinia buchananii Engl.
(Pharmacogn. Commn, 2019) Moshi, Mainen J.
Introduction: Plants of the genus Garcinia are traditionally used treat a range of infectious and non-infectious diseases. Garcinia species are reported to have been shown to have a range of biological activities including cytotoxicity antimicrobial, antifungal, antioxidant, antimalarial and HIV-1 protease inhibitory activity among others. Methods: Solvent extraction was done using CH2Cl2: MeOH (1:1). Isolation was done using column chromatography with silica gel as the stationery phase and ethyl acetate and n-hexane used as mobile phase in increasing polarity. Thin layer chromatography was used to monitor the isolation. Structure elucida-tion was done using nuclear magnetic resonance and mass spectroscopic techniques. Chloroquine resistant (W2) and chloroquine sensitive (D6) P. falciparum strains were used for antiplasmodial assay. Results: Further bioassay guided fractionation of a CH2Cl2: MeOH (1:1) extract of Garcinia buchananii led to the isolation of two already reported biavanones, isogar-cinol (1) and guttiferone (2) with promising antiplasmodial activity against a chloroquine resistant (W2) Plasmodium falciparum strain with an IC50 of 2.8 ± 0.90 µg/mL for compound 1 and IC50 of 3.94 ± 0.38 µg/mL for compound 2. Compounds 1 and 2 also exhibited moderate activity against the chloro-quine sensitive (D6) Plasmodium falciparum strain with IC50 of 7.03±0.60 and 10.64±4.50 µg/mL, respectively. Conclusion: The results provide proof to support the use of G. buchananii by the indigenous community for anti-malarial therapy. Key words: Garcinia buchananii, Isogarcinol, Guttiferone F, Antiplasmodial activity
The association of 18 F-FDG PET/CT and biomarkers in confirming coronary microvascular dysfunction
(BMC research notes, 2018) Mafuru, Magesa
Objective: The purpose of this study is to evaluate the association between PET/CT CFR and biomarkers combined in confirming the diagnosis of coronary microvascular dysfunction. Results: A total of 28 patients (21 males and 7 females) were included in this descriptive observational study (both qualitative and quantitative). The mean patient age was 55.50 ± 10.21 years (range 27–70 years) and the median was 56.5 years (range 49–63 years). All patients underwent Echo, CAG and PET/CT scan. Chest tightness was the most common symptom in our study. Most patients had normal blood pressure (n = 18, 64.3%) while only (n = 10, 37.5%) had hypertension, and (n = 1, 3.6%) had diabetes mellitus. The mean HDL in CMVD (n = 25) and non-CMVD (n = 3) were 1.30 ± 0.39 and 1.08 ± 0.95, respectively, indicating that the difference between the groups was statistically significant (p = 0.04). Similarly, the mean HBA1c- (glycated haemoglobin) in CMVD (n = 25) and non-CMVD (n = 3) were 5.6 ± 0.53 and 5.0 ± 0.26, respectively, with (p = 0.03). Our findings managed to show the association between biomarkers and PET/CT CFR in confirming the diagnosis of coronary microvascular dysfunction. Keywords: Coronary microvascular dysfunction (CMVD), Brain natriuretic peptide (BNP), Red cell distribution (RDW), Coronary flow reserve (CFR)

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