In vitro fertilization using sperm activated by ML-2-3 isolated from Morinda lucida Bentham leaves.

Purpose: ML-2-3 is a novel tetracyclic iridoid derived from Morinda lucida Bentham leaves. This compound has anti-trypanosomal and anti-leishmanial effects. In this study, the authors investigated effects of ML-2-3 on in vitro fertilization (IVF) rates, motility, and acrosome reaction of the mouse sperm. Methods: IVF was performed using sperm from BALB/cByJJcl mice treated with ML-2-3. Computer-assisted sperm analysis (CASA) was performed on the sperm of C57BL/6J mice to investigate sperm motility. The effect of ML-2-3 on the acrosome reaction was examined by observing the fluorescence of sperm labeled with the acrosin-EGFP transgene. Results: ML-2-3 improved IVF in BALB/cByJJcl mice with low fertilization rates. The optimum concentration of ML-2-3 in sperm pre-culture medium was 20 µM, and no significant toxicity of ML-2-3 was observed in developing embryos at this concentration. ML-2-3 affected sperm motility but not the acrosome reaction. ML-2-3 increased the IVF rate of mouse sperm that had been refrigerated for 3 days. Conclusions: ML-2-3 can improve the outcome of IVF and motility without inducing the acrosome reaction in mice. These effects of ML-2-3 on sperm behaviors are different from those of the similar drugs.

In vitro antiprotozoan activity and mechanisms of action of selected Ghanaian medicinal plants against Trypanosoma, Leishmania, and Plasmodium parasites.

Trypanosomiasis, leishmaniasis, and malaria are protozoan infections of public health importance with thousands of new cases recorded annually. Control of these infection(s) with existing chemotherapy is limited by drug toxicity, lengthy parenteral treatment, affordability, and/or the emergence of resistant strains. Medicinal plants on the other hand are used in the treatment of various infectious diseases although their chemical properties are not fully evaluated. In this study, we screened 112 crude extracts from 72 selected Ghanaian medicinal plants for anti-Trypanosoma, anti-Leishmania, and anti-Plasmodium activities in vitro and investigated their mechanisms of action. Twenty-three extracts from 20 plants showed significant antiprotozoan activity against at least 1 of 3 protozoan parasites screened with IC50 values less than 20 µg/ml. Eleven extracts showed high anti-Trypanosoma activity with Bidens pilosa whole plant and Morinda lucida leaf extracts recording the highest activities. Their IC50 (selectivity index [SI]) values were 5.51 µg/ml (35.00) and 5.96 µg/ml (13.09), respectively. Nine extracts had high anti-Leishmania activity with Annona senegalensis and Cassia alata leaf extracts as the most active. Their IC50 (SI) values were 10.8 µg/ml (1.50) and 10.1 µg/ml (0.37), respectively. Six extracts had high anti-Plasmodium activity with the leaf and stem-bark extracts of Terminalia ivorensis recording the highest activity. Their IC50 (SI) values were 7.26 µg/ml (129.36) and 17.45 µg/ml (17.17), respectively. Only M. lucida at 25 µg/ml induced significant apoptosis-like cell death in Trypanosoma parasites. Anti-Leishmania active extracts induced varying morphological changes in Leishmania parasites such as multiple nuclei and/or kinetoplast, incomplete flagella division, or nuclear fragmentation. Active extracts may be potential sources for developing new chemotherapy against these infections.

Antitrypanosomal Activities and Mechanisms of Action of Novel Tetracyclic Iridoids from Morinda lucida Benth.

Trypanosoma brucei parasites are kinetoplastid protozoa that devastate the health and economic well-being of millions of people in Africa through the disease human African trypanosomiasis (HAT). New chemotherapy has been eagerly awaited due to severe side effects and the drug resistance issues plaguing current drugs. Recently, there has been an emphasis on the use of medicinal plants worldwide. Morinda lucida Benth. is a popular medicinal plant widely distributed in Africa, and several research groups have reported on the antiprotozoal activities of this plant. In this study, we identified three novel tetracyclic iridoids, molucidin, ML-2-3, and ML-F52, from the CHCl3 fraction of M. lucida leaves, which possess activity against the GUTat 3.1 strain of T. brucei brucei The 50% inhibitory concentrations (IC50) of molucidin, ML-2-3, and ML-F52 were 1.27 µM, 3.75 µM, and 0.43 µM, respectively. ML-2-3 and ML-F52 suppressed the expression of paraflagellum rod protein subunit 2, PFR-2, and caused cell cycle alteration, which preceded apoptosis induction in the bloodstream form of Trypanosoma parasites. Novel tetracyclic iridoids may be promising lead compounds for the development of new chemotherapies for African trypanosomal infections in humans and animals.

Procyanidin trimer C1 derived from Theobroma cacao reactivates latent human immunodeficiency virus type 1 provirus.

Despite remarkable advances in combination antiretroviral therapy (cART), human immunodeficiency virus type 1 (HIV-1) infection remains incurable due to the incomplete elimination of the replication-competent virus, which persists in latent reservoirs. Strategies for targeting HIV reservoirs for eradication that involves reactivation of latent proviruses while protecting uninfected cells by cART are urgently needed for cure of HIV infection. We screened medicinal plant extracts for compounds that could reactivate the latent HIV-1 provirus and identified a procyanidin trimer C1 derived from Theobroma cacao as a potent activator of the provirus in human T cells latently infected with HIV-1. This reactivation largely depends on the NF-κB and MAPK signaling pathways because either overexpression of a super-repressor form of IκBα or pretreatment with a MEK inhibitor U0126 diminished provirus reactivation by C1. A pan-PKC inhibitor significantly blocked the phorbol ester-induced but not the C1-induced HIV-1 reactivation. Although C1-induced viral gene expression persisted for as long as 48 h post-stimulation, NF-κB-dependent transcription peaked at 12 h post-stimulation and then quickly declined, suggesting Tat-mediated self-sustainment of HIV-1 expression. These results suggest that procyanidin C1 trimer is a potential compound for reactivation of latent HIV-1 reservoirs.

New anti-trypanosomal active tetracyclic iridoid isolated from Morinda lucida Benth.

Human African trypanosomiasis (HAT), commonly known as sleeping sickness has remained a serious health problem in many African countries with thousands of new infected cases annually. Chemotherapy, which is the main form of control against HAT has been characterized lately by the viewpoints of toxicity and drug resistance issues. Recently, there have been a lot of emphases on the use of medicinal plants world-wide. Morinda lucida Benth. is one of the most popular medicinal plants widely distributed in Africa and several groups have reported on its anti-protozoa activities. In this study, we have isolated one novel tetracyclic iridoid, named as molucidin, from the CHCl3 fraction of the M. lucida leaves by bioassay-guided fractionation and purification. Molucidin was structurally elucidated by (1)H and (13)C NMR including HMQC, HMBC, H-H COSY and NOESY resulting in tetracyclic iridoid skeleton, and its absolute configuration was determined. We have further demonstrated that molucidin presented a strong anti-trypanosomal activity, indicating an IC50 value of 1.27 µM. The cytotoxicity study using human normal and cancer cell lines indicated that molucidin exhibited selectivity index (SI) against two normal fibroblasts greater than 4.73. Furthermore, structure-activity relationship (SAR) study was undertaken with molucidin and oregonin, which is identical to anti-trypanosomal active components of Alnus japonica. Overlapping analysis of the lowest energy conformation of molucidin with oregonin suggested a certain similarities of aromatic rings of both oregonin and molucidin. These results contribute to the future drug design studies for HAT.

Assessment of the phytochemical composition and antimicrobial properties of Tapinanthus bangwensis leaves hosted by the branches of Persea americana.

BACKGROUND: Medicinal plants represent a valuable source for new effective and safe antimicrobial drugs making them an alternative therapy. Existing antimicrobial agents are costly and mostly associated with possible side effects. The aim of the present study therefore, was to assess the antimicrobial property and phytochemical composition of hydroethanolic extract of Tapinanthus bangwensis leaves and its fractions. METHOD: T. bangwensis leaves (harvested from its host plant, Persea americana) was extracted by cold maceration with 70% ethanol and further fractionated with different organic solvents using the solvent partitioning method to obtain the crude extract, petroleum ether, chloroform, ethyl acetate and the resulting aqueous fractions. The phytochemical constituents of the extracts were screened and quantified. Also, the TLC of the extracts were analyzed to serve as a fingerprint. Using the agar diffusion and broth dilution methods, the antimicrobial properties of the extracts were assessed. RESULTS: The study showed that the hydroethanolic (70%) crude extract of T. bangwensis leaves and its fractions contain phenolic compounds, flavonoids, saponins, phytosterols and reducing sugars. The phytoconstituents were well extracted into the ethyl acetate fraction than the other fractions evidenced in the high levels (p < 0.0001) of saponins (66.47 ± 1.72% w/w), phenolic compounds (77.75 ± 1.06 mg/100 mg GAE) and flavonoids (44.34 ± 0.06 mg/100 mg QE) contents. From the antimicrobial studies, all the microorganisms tested exhibited varying degrees of susceptibility to the extracts with MIC values between 0.78 to 12.5 mg/mL. The crude extract of T. bangwensis leaves, its ethyl acetate and chloroform fractions also exhibited lethal antimicrobial activity with MLC between 6.25 to 50 mg/mL. CONCLUSION: The crude extract of T. bangwensis leaves and its fractions demonstrated antimicrobial properties against Escherichia coli, Staphylococcus aureus, Staphylococcus saprophyticus and Candida albicans, thereby representing a potential source of natural antimicrobial agent. Further study is required to identify and isolate antimicrobial compounds from the plant for the development of the natural bioactive antimicrobial agents.

Anti-plasmodial, Cytotoxic and Antioxidant Activities of Selected Ghanaian Medicinal Plants.

Malaria affects about half of the world's population. The sub-Saharan African region is the most affected. Plant natural products have been a major source of antimalarial drugs; the first (quinine) and present (artemisinin) antimalarials are of natural product origin. Some secondary metabolites demonstrate adjuvant antioxidant effects and selective activity. The focus of this study was to investigate the anti-plasmodial activity, cytotoxicities and antioxidant properties of eight (8) Ghanaian medicinal plants. The anti-plasmodial activity was determined using the SYBR green assay and the tetrazolium-based colorimetric assay (MTT) was employed to assess cytotoxicity of extracts to human RBCs and HL-60 cells. Antioxidant potential of plant extracts was evaluated using Folin-Ciocalteu and superoxide dismutase assays. Phytochemical contstituents of the plant extracts were also assessed. All the extracts demonstrated anti-plasmodial activities at concentrations <50 µg/ml. Parkia clappertoniana and Terminalia ivorensis elicited the strongest anti-plasmodial activities with 50% inhibitory concentrations (IC50) of 1.13 µg/ml and 0.95 µg/ml, respectively. This is the first report on anti-plasmodial activities of Baphia nitida, Tabernaemontana crassa and Treculia Africana. T. Africana showed moderate anti-plasmodial activity with IC50 value of 6.62 µg/mL. Extracts of P. clappertoniana, T. Africana and T. ivorensis (0.4 mg/mL) showed >50% antioxidant effect (SOD). The extracts were not cytotoxicity towards RBCs at the concentration tested (200 µg/ml) but were weakly cytotoxic to HL-60 cell. Selectivity indices of most of the extracts were greater than 10. Our results suggest that most of the plant extracts have strong anti-plasmodial activity and antioxidant activity which warrants further investigations.

Approaches for the Elimination of Microbial Contaminants from Lippia multiflora Mold. Leaves Intended for Tea Bagging and Evaluation of Formulation.

Elimination of microorganisms from herbal products has been a major concern due to its implicated health risk to consumers. Drying of herbal materials has been employed for centuries to reduce the risk of contamination and spoilage. The present study adopted three drying approaches in an attempt to eliminate microorganisms from Lippia multiflora tea bag formulation. This study also evaluated the tea bags and optimized the extraction procedure. The L. multiflora leaves for tea bagging were air-dried and milled (A), oven-dried and milled (B), and microwaved (the milled air-dried leaves) (C). The moisture contents were determined at 105°C ± 2°C for 2 hours to constant weight. Phytochemical parameters such as phytochemical constituents, total water extractive, and pH were assessed. The microbial safety and quality of the L. multiflora tea bags were evaluated using the British Pharmacopoeia 2019 specifications. The uniformity of the mass of the formulated tea bags was also determined. Extraction from the Lippia tea bags was optimized. The results showed that using the approaches (A, B, and C) adopted for drying and processing, the moisture contents of the formulated tea bags were in the range of 9.75-10.71% w/w. All the formulated tea bags contained reducing sugars, phenolic compounds, polyuronides, flavonoids, anthracenosides, alkaloids, saponins, and phytosterols. The pH range of the formulations was 7.11-7.54, whereas the total water extractive values were in the range of 19.12-20.41% w/w. The one-way analysis of variance demonstrated no significant difference in the data obtained from the results from A, B, and C. The formulation from A was found to be unsafe for consumption due to unacceptable microbial contamination limits. Microbial load of the formulations from B and C were within the BP specifications. All the batches of the formulations passed the uniformity of mass test. An optimized extraction procedure was obtained when one tea bag was extracted in 250 mL of hot water within the specified time. L. multiflora leaves meant for tea bagging should be oven-dried or microwaved before tea bagging for safe consumption.

Bridelia ferruginea Benth.; An ethnomedicinal, phytochemical, pharmacological and toxicological review.

Ethnopharmacological relevance: Bridelia ferruginea belonging to the family Euphorbiaceae, identified as an important commonly growing shrub, is used in traditional medicine for managing arthritis, dysentery, constipation, chronic diabetes, skin diseases, bladder and intestinal disorders, oral infections, thrush, bites and as an arrow poison antidote. This review aims at providing information on the traditional medicinal uses, pharmacological activities, phytochemistry and toxicity studies of Bridelia ferruginea to bridge the gap between traditional medicinal uses and preclinical studies on B. ferruginea and subsequently lead to the development of valued added medicines from B. ferruginea. Materials and methods: Data in this review were compiled using databases such as Google Scholar, Science Direct, Scopus, PubMed, Springer link, Elsevier and Taylor and Francis, articles from peer reviewed journals and other grey literature (short notes, book chapters, short communications) to access all the relevant information available on B. ferruginea. Results: B. ferruginea contains different phytochemicals including flavonoids, phenolics, phytosterols, triterpenes, saponins, alkaloids and cardiac glycosides. Gallocatechin-(4'-O-7)-epigallocatechin, 3,5-dicaffeoylquinic acid, 1,3,4,5-tetracaffeoylquinic acid and some derivatives of 3-methoxyflavone, such as quercetin-3-methyl ether, quercetin 3-,7,3',4'-tetramethyl ether, myricetin 3',4',5'-trimethyl ether, myricetin 3,3',4',5'-tetramethyl ether, myricetin and quercetin 3-O-glucoside specific flavonoids and biflavonoids like apigenin, kaempferol and glycosides of both have been isolated and further characterized from B. ferruginea. B. ferruginea has several pharmacologically beneficial properties including anti-inflammatory, anti-diabetic, antioxidant, antimicrobial, anti-infective, antipyretic, analgesic, diuretic and natriuretic activities. Conclusion: The wide distribution, traditional medicinal uses and wealth of phytochemicals present in B. ferruginea suggests that the plant can be useful in lead compound discovery. Although B. ferruginea has been widely studied, further studies on the mechanism of action, bioavailability, pharmacokinetics, toxicity and side effects in humans need to be investigated.

Standardization and Quality Control of the Herbal Medicine Mist Nibima, Employed to Treat Malaria and COVID-19, Using Physicochemical and Organoleptic Parameters and Quantification of Chemical Markers via UHPLC-MS/MS.

Mist Nibima is an essential herbal medicine used to treat malaria, bacterial, yeast, and COVID-19 infections. However, the drug has not been standardized and its active chemical ingredients are also not known. This study employed physicochemical, organoleptic, qualitative, and quantitate phytochemical analysis to established standards for Mist Nibima. Additionally, UHPLC was used to quantify the alkaloid cryptolepine in the drug using calibration curve. The chemical ingredients in Mist Nibima were thereafter characterized using UHPLC-MS. Organoleptic evaluation shows that Mist Nibima is a very bitter, cloudy, broom yellow decoction with the following physicochemical parameters: pH = 6.10 ± 0.08 (at 28.3°C), total solid residue = 5.34 ± 0.27%w/v, and specific gravity = 1.0099 ± 0.0000. The total alkaloid (23.71 ± 1.311%) content of the drug is 3 times its total saponins (7.993 ± 0.067%) content. Methyl cryptolepinoate (37.10%), cryptolepine (33.56%), quindoline (20.78%), 11-isopropylcryptolepine (5.16%), and hydroxycryptolepine (3.14%) were the active chemical ingredients in the drug with the concentrations of 18.64 ± 0.255, 16.85 ± 0.231, 10.42 ± 0.143, 2.56 ± 0.034, and 1.70 ± 0.023 µg/mL, respectively. Administration of a single oral therapeutic dose (30 mL) of Mist Nibima corresponds to ingestion of 559.2 ± 7.662, 505.5 ± 6.930, 312.6 ± 4.285, 76.8 ± 1.028, and 51.0 ± 0.699 µg of methyl cryptolepinoate, cryptolepine, quindoline, 11-isopropylcryptolepine, and hydroxycryptolepine, respectively. This translates into a corresponding daily dose of 1677.6 ± 22.986, 1516.5 ± 20.790, 937.8 ± 12.855, 230.4 ± 3.084, and 153.0 ± 2.097 µg of methyl cryptolepinoate, cryptolepine, quindoline, 11-isopropylcryptolepine, and hydroxycryptolepine. These results could now serve as tools for authentication, standardization, and quality control of Mist Nibima to ensure its chemical and pharmacological consistency and safety.

Examining Vaccine Hesitancy in Sub-Saharan Africa: A Survey of the Knowledge and Attitudes among Adults to Receive COVID-19 Vaccines in Ghana.

The impact of COVID-19 vaccination programmes on disease transmission, morbidity and mortality relies heavily on the population's willingness to accept the vaccine. We explore Ghanaian adult citizens' vaccine hesitancy attitudes and identify the likelihood of participation or non-participation in the government's effort to get citizens vaccinated. A fully anonymised cross-sectional online survey of 2345 adult Ghanaians was conducted from 23 to 28 February 2021. Differences in intentions regarding COVID-19 vaccination were explored using Pearson Chi-square tests. Additionally, multinomial logistic regression was used to analyse the factors associated with willingness to receive vaccines. Responses were weighted using the iterative proportional fitting technique to generate a representative sample. About half (51%) of mostly urban adult Ghanaians over 15 years are likely to take the COVID-19 vaccine if made generally available. Almost a fifth (21%) of the respondents were unlikely to take the vaccine, while another 28% were undecided. Additionally, we find differences in vaccine hesitancy among some socio-demographic characteristics such as age, gender, and primary sources of information. Attaining the proverbial 63% to 70% herd immunity threshold in Ghana is only possible if the preventive vaccination programmes are combined with an enhanced and coordinated public education campaign. Such a campaign should focus on promoting the individual and population-level benefits of vaccination and pre-emptive efforts towards addressing misinformation about vaccines.

A review on anti-peptic ulcer activities of medicinal plants used in the formulation of Enterica, Dyspepsia and NPK 500 capsules.

Peptic ulcer disease affects many people globally. With the increasing resistance to some orthodox antibiotics such as Clarithromycin and Metronidazole, it is important that new acceptable, safer and effective therapies are developed to manage this disease. Various herbal medicines have been used traditionally for the remedy of peptic ulcer disease (PUD), however scientific information with regards to their anti-peptic ulcer both in-vivo and in-vitro as well as clinical studies supporting their use is still inadequate. The Centre for Plant Medicine Research, (CPMR) Mampong-Akuapem, Ghana manufactures three herbal Products namely Enterica, Dyspepsia and NPK 500 capsules which are currently used for the remedy of PUD as a triple therapy at its out-patient clinic with promising effects. The aim of this review is to gather information from literature on the anti-ulcer properties, pharmacological, phytochemical constituents and related activities of herbal plants used at the CPMR for formulation of the triple herbal therapy. This review may, provide some scientific bases for the use of Enterica, Dyspepsia and NPK 500 capsules in the management of Peptic ulcer at the CPMR out-patient clinic. METHODS: Organization for the review involved the on and/or offline search for information from available literature using electronic data and scientific research information resources such as PubMed, Science Direct and Google scholar. RESULTS: In this review, fifteen ethno-medicinal plants used for the formulation of Enterica, Dyspepsia and NPK capsules have been discussed, presenting the description of the plants, composition and pharmacological activity. INTERPRETATION: Tables with the summary of reviewed medicinal plants with their anti-ulcer models and inference on possible mechanisms of action were drawn up. The mechanism(s) of action of individual plants and products (Enterica, Dyspepsia and NPK 500 capsules) must be further investigated and established experimentally in-vitro in addition to in-vivo pharmacological and clinical activity studies to confirm their use in the remedy of PUD.

Anti-inflammatory activity and mechanism of action of ethanolic leaf extract of Morinda lucida Benth.

BACKGROUND AND AIM: Most developing countries resort to medicinal plants for treating diseases, but few of these have scientific backing for their use. The aim of the study was to validate traditional use of Morinda lucida leaves in treating inflammation and determine the mechanism of action. EXPERIMENTAL PROCEDURE: Effect of hydroethanolic leaf extract of M. lucida (HEML) on localized inflammation was evaluated using rat paw edema presented by sub-planter injections of λ-carrageenan, histamine or serotonin in separate experiments. Systemic inflammation was evaluated by lipopolysaccharide (LPS)-induced hyperthermia. Antioxidant activity of HEML was also evaluated using the free-radical scavenging assay. RESULTS AND CONCLUSION: No mortalities were recorded in acute toxicity assay after administering 5000 mg/kg HEML to rats. It showed very good activity against localized and systemic inflammation in inverse dose-dependent manner and caused reduction in nitric oxide and prostaglandin E-2 levels by affecting expression of inducible nitric oxide synthase, but not cyclooxygenases-2 in LPS-activated RAW 264.7 murine macrophages. HEML reduced pro-inflammatory cytokines interleukin (IL)-1ß and tumor necrotic factor, but elevated levels of anti-inflammatory cytokine IL-10 in vitro. HEML contains saponins, reducing sugars, polyphenols and flavonoids and showed antioxidant activity with EC50 = 0.6415 ± 0.0027 mg/ml. In conclusion, this study provides evidence that HEML possesses anti-inflammatory activity, possibly through modulation of production of early/late phase inflammation mediators.

Establishment of a quantitative and qualitative analysis and isolation method for tetracyclic iridoids from Morinda lucida Bentham leaves.

A new high performance liquid chromatography (HPLC) method has been established for quantitative and qualitative analysis of three tetracyclic iridoids: ML-2-3 (1), molucidin (2), and ML-F52 (3), which are responsible for anti-trypanosomal and anti-leishmanial activities of Morinda lucida Bentham leaves. Separation of 1-3 from dried 80% aqueous (aq.) ethanol extract was achieved on a reversed-phase cholester column packed with cholesteryl-bonded silica using an acetonitrile-0.1% aq. formic acid mobile phase system. Ultraviolet-visible (UV-VIS) spectroscopy was employed for detection of compounds, and their contents were determined by measuring absorbance at 254 nm. Depending on the above system, several factors potentially affecting the concentration of tetracyclic iridoids were evaluated resulting in several variation on plant organs, seasonality, variation between individual trees, and branch positions within the trees. Moreover, we developed a simple, quick, and effective method for tetracyclic iridoid isolation from M. lucida leaves that consisted of extraction by sonication into 80% aq. ethanol, basic hydrolysis, acid neutralization, liquid-liquid extraction into an organic solvent, and reverse phase open column chromatography. Employing this method, we have succeeded to obtain 1 as a colorless crystal yielding of 0.23%, which was 28 times higher than that of previous isolation method. Setting up methodology in this paper may be important for future in vitro and in vivo studies of tetracyclic iridoids and moreover for their applications in new drug design and development.

Antinflammatory and Analgesic Effects in Rodent Models of Ethanol Extract of Clausena anisata Roots and their Chemical Constituents.

The in vivo antiinflammatory and analgesic activities of the crude ethanol extract and chemical constituents of Clausena anisata roots were investigated. The crude extract, which was devoid of any visible acute toxicity, displayed significant antiinflammatory effect at the dose of 1000 mg/kg (p.o.) when assessed using the carrageenan-induced oedema model. In the acetic acid-induced writhing and hot plate tests, it produced a very significant (p < 0.001); dose- dependent analgesic effect, with maximum analgesic activity of 72.1% at 1000 mg/kg (p.o.). Phytochemical analysis of the crude extract resulted in the isolation of four coumarins (anisocoumarin B, osthol, imperatorin and xanthotoxol) and a carbazole alkaloid, heptaphylline. Among the isolated compounds, osthol and anisocournarin B produced the highest antiinflammatory activity at 9 mg/kg (p.o.): slightly better than the positive control, indomethacin. Except for xanthotoxol, all the isolated compounds administered at 6 mg/kg (p.o.) produced significant analgesic activity and higher than diclofenac; with- heptaphylline being the most potent (48.7%). The analgesic activity of anisocoumarin B (50.4%) was the highest among the isolates tested and the standard, tramadol, in the hot plate test. The nonselective opioid receptor antagonist, naloxone, abolished the analgesic effect of the crude extract and the tested isolates (anisocoumarin B and xanthotoxol) in the hot plate test suggesting an effect via the central opioidergic system. These findings provide the scientific basis for the use of C. anisata roots in traditional medicine as antiinflammatory and analgesic agents.

In Vitro Assessment of Anthelmintic Activities of Rauwolfia vomitoria (Apocynaceae) Stem Bark and Roots against Parasitic Stages of Schistosoma mansoni and Cytotoxic Study.

Schistosomiasis is a Neglected Tropical Diseases which can be prevented with mass deworming chemotherapy. The reliance on a single drug, praziquantel, is a motivation for the search of novel antischistosomal compounds. This study investigated the anthelmintic activity of the stem bark and roots of Rauwolfia vomitoria against two life stages of Schistosoma mansoni. Both plant parts were found to be active against cercariae and adult worms. Within 2 h of exposure all cercariae were killed at a concentration range of 62.5-1000 µg/mL and 250-1000 µg/mL of R. vomitoria stem bark and roots, respectively. The LC50 values determined for the stem bark after 1 and 2 h of exposure were 207.4 and 61.18 µg/mL, respectively. All adult worms exposed to the concentrations range of 250-1000 µg/mL for both plant parts died within 120 h of incubation. The cytotoxic effects against HepG2 and Chang liver cell assessed using MTT assay method indicated that both plant extracts which were inhibitory to the proliferation of cell lines with IC50 > 20 µg/mL appear to be safe. This report provides the first evidence of in vitro schistosomicidal potency of R. vomitoria with the stem bark being moderately, but relatively, more active and selective against schistosome parasites. This suggests the presence of promising medicinal constituent(s).

In vitro anti-Leishmania activity of tetracyclic iridoids from Morinda lucida, benth.

Leishmaniasis is an infectious disease transmitted by the sand fly. It is caused by over 20 different species of Leishmania and has affected over 14 million people worldwide. One of the main forms of control of leishmaniasis is chemotherapy, but this is limited by the high cost and/or toxicity of available drugs. We previously found three novel compounds with an iridoid tetracyclic skeleton to have activity against trypanosome parasites. In this study, we determined the activity of the three anti-trypanosome compounds against Leishmania using field strain, 010, and the lab strain Leishmania hertigi. The minimum inhibitory concentration (MIC) of the compounds against 010 was determined by microscopy while the IC50 of compounds against L. hertigi was determined by fluorescence-activated cell sorting with Guava viacount analysis. We found two of the three compounds, molucidin and ML-F52, to have anti-Leishmania activity against both strains. The fluor-microscope observation with DAPI stain revealed that both Molucidin and ML-F52 induced abnormal parasites with two sets of nucleus and kinetoplast in a cell, suggesting that compounds might inhibit cytokinesis in Leishmania parasites. Molucidin and ML-F52 might be good lead compounds for the development of new anti-Leishmania chemotherapy.

Shrinkage of Prostate and Improved Quality of Life: Management of BPH Patients with Croton membranaceus Ethanolic Root Extract.

Benign prostatic hyperplasia (BPH) is an enlargement of the prostate. The study aimed at validating the use of freeze-dried Croton membranaceus ethanolic root extract for BPH management. Thirty-three patients were observed before and after 3-month administration of 20 mg t.i.d orally. The International Prostate Symptom Score (IPSS), and the International Index of Erectile Function (IIEF) questionnaires were used. Total/free PSA (tPSA, fPSA), renal, liver function, lipid tests, and ultrasonographic imaging were performed. Thirty (30) patients (66 ± 11 years) completed the study. IPSS results showed 37% had severe, 40% moderate, and 23% mild symptoms before; 57% and 43% had moderate and mild symptoms, respectively, after treatment. IIED of patients' results showed 30% with severe, 40% moderate, 24% mild-moderate, 3% mild, and 3% no erectile dysfunction before treatment and 20% severe, 43% moderate, and 37% mild-moderate dysfunction, after treatment. Quality of life (QoL) improved (P = 0.001). Significant but non-pathological increases in total and indirect bilirubin as well as apolipoprotein A occurred. Mean tPSA reduced from 27.9 ± 19.0 to 16.2 ± 11.8 ng/mL (P = 0.002); fPSA from 6.1 ± 4.8 to 3.9 ± 2.9 ng/mL (P = 0.045); and prostate volume from 101.8 ± 41.3 to 54.5 ± 24.8 cm(3) (P = 0.023). C. membranaceus shrinks the prostate and improves QoL.

Natural radioactivity levels of some medicinal plants commonly used in Ghana.

Natural radioactivity levels in some selected medicinal plants commonly used in Ghana from the Centre for Scientific Research into Plant Medicine were investigated to determine the activity concentration and the annual committed effective dose due to naturally occurring radionuclides of (238)U, (232)Th and (40)K. The activity concentration was determined using gamma-ray spectrometry. The results of the analysis indicated an average activity concentration of (238)U, (232)Th and (40)K in the medicinal plants to be 31.8±2.8 Bq kg(-1), 56.2±2.3 Bq kg(-1) and 839.8±11.9 Bq kg(-1) respectively. Khaya ivorensis recorded the highest activity concentration of (238)U and (232)Th while Lippia multiflora recorded the highest activity concentrations of (40)K. The total annual committed effective doses ranged from 0.026±0.001 to 0.042±0.002 mSv a(-1) with an average value of 0.035±0.001 mSv a(-1). The average annual committed effective dose due to ingestion of the natural radionuclides in the medicinal plant samples were far below the world average annual committed effective dose of 0.3 mSv a(-1) for ingestion of natural radionuclides provided in UNSCEAR 2000 report. Therefore, the radiological hazard associated with intake of the natural radionuclides in the medicinal plants is insignificant. The results provide baseline values which may be useful in establishing rules and regulations relating to radiation protection as well as developing standards and guidelines for the use of medicinal or herbal plants to the appropriate authorities.