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1.
Molecules ; 28(20)2023 Oct 13.
Artículo en Inglés | MEDLINE | ID: mdl-37894548

RESUMEN

BACKGROUND: Alstonia boonei, belonging to the family Apocynaceae, is one of the best-known medicinal plants in Africa and Asia. Stem back preparations are traditionally used as muscle relaxants. This study investigated the antispasmodic properties of Alstonia boonei Stem back and its constituents. METHOD: The freeze-dried aqueous Stem back extract of A. boonei, as well as dichloromethane (DCM), ethyl acetate, and aqueous fractions, were evaluated for their antispasmodic effect via the ex vivo method. Two compounds were isolated from the DCM fraction using chromatographic techniques, and their antispasmodic activity was evaluated. An in silico study was conducted by evaluating the interaction of isolated compounds with human PPARgamma-LBD and human carbonic anhydrase isozyme. RESULTS: The Stem back crude extract, DCM, ethyl acetate, and aqueous fractions showed antispasmodic activity on high-potassium-induced (K+ 80 mM) contractions on isolated rat ileum with IC50 values of 0.03 ± 0.20, 0.02 ± 0.05, 0.03 ± 0.14, and 0.90 ± 0.06 mg/mL, respectively. The isolated compounds from the DCM fraction were ß-amyrin and boonein, with only boonein exhibiting antispasmodic activity on both high-potassium-induced (IC50 = 0.09 ± 0.01 µg/mL) and spontaneous (0.29 ± 0.05 µg/mL) contractions. However, ß-amyrin had a stronger interaction with the two proteins during the simulation. CONCLUSION: The isolated compounds boonein and ß-amyrin could serve as starting materials for the development of antispasmodic drugs.


Asunto(s)
Alstonia , Ratas , Animales , Humanos , Alstonia/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Parasimpatolíticos/farmacología , Agua , Potasio
2.
J Ethnopharmacol ; 283: 114686, 2022 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-34571079

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The choice of extraction solvent is a significant consideration in ethnomedicine as optimal extraction could influence the bioactivity of the herbal medicinal product. AIM OF STUDY: This study investigated the possible influence of the choice of solvents (methanol and water) for extracting MAMA Powder (MP) against Plasmodium berghei-infected mice to optimize its antimalarial activity and for developing other pharmaceutical dosage forms. MATERIALS AND METHODS: Aqueous and methanol extracts of MP, obtained through the decoction and soxhlet methods, respectively, were subjected to liquid chromatography-mass spectroscopy (LC-MS) for their respective fingerprints. The antimalarial activities of the methanol and aqueous extracts (12.5-100 mg/kg) were evaluated orally using the chemosuppressive test model on chloroquine-sensitive Plasmodium berghei-infected mice. The methanol extract was subjected to the established infection and prophylactic antimalarial tests with chloroquine (10 mg/kg) and pyrimethamine (1.25 mg/kg) as positive controls, respectively. The aqueous extract was investigated in chloroquine-resistant P. berghei using the chemosuppressive (12.5-800 mg/kg) and established infection (25-400 mg/kg) antimalarial models. RESULTS: The LC-MS fingerprints of both aqueous and methanol extracts revealed similar indole alkaloid contents. Chemosuppressive activity of the aqueous extract (75.3%) was significantly (p < 0.05) higher than the methanol extract (67.6%). In the chloroquine-resistant P. berghei infection experiments, the aqueous extract (400 mg/kg) exhibited significant parasite clearance (72%). CONCLUSION: The study concluded that the water extract with higher antimalarial activity could be optimized for chloroquine-resistant malaria and can thus facilitate the production of liquid and solid dosage forms.


Asunto(s)
Antimaláricos/uso terapéutico , Malaria/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/uso terapéutico , Plasmodium berghei/efectos de los fármacos , Animales , Antimaláricos/química , Cloroquina/farmacología , Resistencia a Medicamentos , Ratones , Extractos Vegetales/química
4.
Front Pharmacol ; 12: 596855, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33981214

RESUMEN

The coronavirus disease 2019 (COVID-19) pandemic is caused by an infectious novel strain of coronavirus known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) which was earlier referred to as 2019-nCoV. The respiratory disease is the most consequential global public health crisis of the 21st century whose level of negative impact increasingly experienced globally has not been recorded since World War II. Up till now, there has been no specific globally authorized antiviral drug, vaccines, supplement or herbal remedy available for the treatment of this lethal disease except preventive measures, supportive care and non-specific treatment options adopted in different countries via divergent approaches to halt the pandemic. However, many of these interventions have been documented to show some level of success particularly the Traditional Chinese Medicine while there is paucity of well reported studies on the impact of the widely embraced Traditional African Medicines (TAM) adopted so far for the prevention, management and treatment of COVID-19. We carried out a detailed review of publicly available data, information and claims on the potentials of indigenous plants used in Sub-Saharan Africa as antiviral remedies with potentials for the prevention and management of COVID-19. In this review, we have provided a holistic report on evidence-based antiviral and promising anti-SARS-CoV-2 properties of African medicinal plants based on in silico evidence, in vitro assays and in vivo experiments alongside the available data on their mechanistic pharmacology. In addition, we have unveiled knowledge gaps, provided an update on the effort of African Scientific community toward demystifying the dreadful SARS-CoV-2 micro-enemy of man and have documented popular anti-COVID-19 herbal claims emanating from the continent for the management of COVID-19 while the risk potentials of herb-drug interaction of antiviral phytomedicines when used in combination with orthodox drugs have also been highlighted. This review exercise may lend enough credence to the potential value of African medicinal plants as possible leads in anti-COVID-19 drug discovery through research and development.

5.
Eur J Drug Metab Pharmacokinet ; 45(1): 81-88, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31642009

RESUMEN

BACKGROUND AND OBJECTIVE: MAMA decoction (MD) is an antimalarial product prepared from the leaves of Mangifera indica L. (Anacardiaceae), Alstonia boonei De Wild (Apocynaceae), Morinda lucida Benth (Rubiaceae) and Azadirachta indica A. Juss (Meliaceae). A previous report showed that MD enhanced the efficacy of amodiaquine (AQ) in malaria-infected mice, thus suggesting a herb-drug interaction. The present study hence evaluated the effect of MD on the disposition of AQ in mice with a view to investigating a possible pharmacokinetic interaction. METHODS: In a 3-period study design, three groups of mice (n = 72) were administered oral doses of AQ (10 mg/kg/day) alone, concurrently with MD (120 mg/kg/day), and in the 3rd period, mice were given AQ after a 3-day pre-treatment with MD. Blood samples were collected between 0 and 96 h for quantification of AQ and its major metabolite, desethylamodiaquine, by a validated high-performance liquid chromatography method. RESULTS: Maximum concentrations of AQ increased by 12% with the concurrent dosing of MD and by 85% in the group of mice pre-treated with MD. The exposure and half-life of desethylamodiaquine increased by approximately 11% and 21%, respectively, with concurrent administration. Corresponding increases of approximately 20% and 33% of desethylamodiaquine were also observed in mice pre-treated with MD. CONCLUSION: MD influenced the pharmacokinetics of AQ and desethylamodiaquine, its major metabolite. The increase in the half-life and systemic exposure of AQ following its co-administration with MD may provide a basis for the enhanced pharmacological effect of the combination in an earlier study in Plasmodium-infected mice.


Asunto(s)
Amodiaquina/farmacocinética , Antimaláricos/farmacocinética , Malaria/tratamiento farmacológico , Extractos Vegetales/farmacología , Amodiaquina/análogos & derivados , Amodiaquina/sangre , Amodiaquina/farmacología , Animales , Antimaláricos/sangre , Antimaláricos/farmacología , Combinación de Medicamentos , Interacciones Farmacológicas , Femenino , Interacciones de Hierba-Droga , Masculino , Ratones , Modelos Animales , Hojas de la Planta/química
6.
Pharm Biol ; 54(10): 2298-303, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-27057621

RESUMEN

CONTEXT: Co-administration of amodiaquine with MAMA decoction (MD), an herbal antimalarial drug comprising the leaves of Mangifera indica L. (Anacardiaceae), Alstonia boonei De Wild (Apocynaceae), Morinda lucida Benth (Rubiaceae) and Azadirachta indica A. Juss (Meliaceae) was investigated. The practice of concurrent administration of herbal medicines with orthodox drugs is currently on the increase globally. OBJECTIVE: The study was designed to investigate the possible enhancement of the antimalarial potency as well as possible herb-drug interaction resulting from concurrent administration of MAMA decoction with amodiaquine (AQ). MATERIALS AND METHODS: Combinations of MD with AQ were investigated in chloroquine (CQ)-sensitive Plasmodium berghei NK 65 in varying oral doses (mg/kg) at: sub-therapeutic [MD30 + AQ1.25], therapeutic [MD120 + AQ10] and median effective [MD40 + AQ3.8], using chemosuppressive and curative antimalarial test models. Secondly, P. berghei ANKA (CQ-resistant)-infected mice were orally treated with MD 120, 240, [MD120 + AQ10] and [MD240 + AQ10] mg/kg, using both models. The survival times of mice were monitored for 28 d. RESULTS: ED50 values of MD and AQ were 48.8 and 4.1 mg/kg, respectively. A total parasite clearance of CQ-sensitive P. berghei NK65 was obtained with the therapeutic combination dose in the curative test giving an enhanced survival time. In CQ-resistant P. berghei ANKA-infected mice, [MD120 + AQ10] and [MD240 + AQ10] mg/kg gave comparable activities with AQ (10 mg/kg) in both models. CONCLUSION: The therapeutic combination dose gave total parasite clearance of CQ-sensitive P. berghei NK65, whereas none of the doses tested showed notable activity against CQ-resistant P. berghei ANKA.


Asunto(s)
Amodiaquina/farmacología , Antimaláricos/farmacología , Medicamentos Herbarios Chinos/farmacología , Interacciones de Hierba-Droga , Malaria/tratamiento farmacológico , Extractos Vegetales/farmacología , Plasmodium berghei/efectos de los fármacos , Animales , Cloroquina/farmacología , Modelos Animales de Enfermedad , Resistencia a Medicamentos , Quimioterapia Combinada , Malaria/parasitología , Ratones , Pruebas de Sensibilidad Parasitaria , Factores de Tiempo
7.
Artículo en Inglés | MEDLINE | ID: mdl-25392579

RESUMEN

BACKGROUND: The root and stem bark of Cassia sieberiana DC. (Caesalpiniaceae) and the root of Senna obtusifolia (Linn) Irwin and Barneby (Caesalpiniaceae), used for constipation in Nigeria, were assayed for laxative properties in male albino rats using the official senna leaf (Senna alexandrina Mill. family Caesalpiniaceae) as the reference standard. This is with a view to finding alternative laxative drug to official senna which is presently being imported into Nigeria from the United Kingdom. MATERIALS AND METHODS: The mean percentage of wet faeces in rats, an indication of laxative activity, were obtained using established methods. The laxative activity was established at 500 mg/kg after the infusion of the drug was orally administered on male albino rats following established methods while a set of data was analyzed at 95 % confidence level. RESULTS: At 500 mg/kg, Senna obtusifolia root gave about 45 % wet faeces while Cassia sieberiana root gave about 40 % wet faeces while at the highest dose of 700 mg/kg, they produced 60 % and 38 % wet faeces, respectively. At these two doses, the official Senna gave 50.6 % and 66 % wet faeces, respectively. Thus, S. obtusifolia and C. sieberiana roots exhibited 89 % and 80 % of the potency of S. alexandrina (the official drug), respectively. The analysis of variance revealed a significant statistical difference in the levels of wet faeces produced by rats dosed with C. sieberiana root. CONCLUSION: The results have shown that the roots of the two species could be developed as mild laxative drugs for children and pregnant women for whom the official senna will be contraindicated.


Asunto(s)
Cassia , Estreñimiento/tratamiento farmacológico , Defecación/efectos de los fármacos , Laxativos/uso terapéutico , Extractos Vegetales/uso terapéutico , Senna , Animales , Heces , Laxativos/farmacología , Masculino , Nigeria , Corteza de la Planta , Extractos Vegetales/farmacología , Raíces de Plantas , Ratas Wistar
8.
Parasitol Res ; 113(5): 1977-84, 2014 May.
Artículo en Inglés | MEDLINE | ID: mdl-24658658

RESUMEN

Mangifera indica, Alstonia boonei, Morinda lucida and Azadirachta indica (MAMA) decoction, commonly prepared and used in Nigeria from 1:1:1:1 ratio of Mangifera indica L. (Anacardiaceae), Alstonia boonei De Wild (Apocynaceae), Morinda lucida Benth (Rubiaceae), and Azadirachta indica A. Juss (Meliaceae) leaves, plus four new variants of this combination were subjected to three in vivo antimalarial test models using chloroquine-sensitive Plasmodium berghei berghei to determine the most active under each of the test models. Using the original formulation, MAMA (1:1:1:1) which gave ED50 and ED90 of 101.54±2.95 and 227.18±2.95, respectively, as reference for comparison, MAMA-1 (1:2:2:2), with 79.58±1.30 and 170.98±1.30, gave significantly (p<0.05) higher survival at 85 and 340 mg/kg when 80 % of the mice survived for 15.6 and 17.8 days, respectively, while MAMA-2 (2:1:2:2), with 83.57±1.93 and 164.23±1.93, gave comparable survival except at 170 mg/kg with 60 % survivors for 12 days. MAMA-1 and MAMA-2 were the best curative formulations with MAMA-1 giving additional prophylactic activity. MAMA-3 (2:2:2:1) with 98.70±0.91 and 220.17±0.91, gave comparable (p>0.05) survival at 85 mg/kg with 60 % survival for 13.2 days and significantly higher survival at 42.5 mg/kg for 17 days with 40 % survival. Both MAMA and MAMA-3 were the best chemosuppressive formulations plus additional curative activities. MAMA-4 (1:1:2:2), the best prophylactic formulation with 94.87±2.43 and 201.20±2.43 gave significantly higher (p<0.05) survival at all doses except at 21.25 mg/kg which gave 60 % survival up to 10 days. Thus, the antimalarial therapy desired, following appropriate diagnosis, whether prophylactic, chemosuppressive or curative would determine which of the MAMA decoction formulations to be prescribed. This phenomenon of formulary optimization may also be applied to other pharmacological activities.


Asunto(s)
Antimaláricos/administración & dosificación , Malaria/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Plasmodium berghei/efectos de los fármacos , Animales , Antimaláricos/farmacología , Azadirachta/química , Cloroquina , Relación Dosis-Respuesta a Droga , Combinación de Medicamentos , Femenino , Masculino , Mangifera/química , Medicinas Tradicionales Africanas , Meliaceae/química , Ratones , Morinda/química , Nigeria , Pruebas de Sensibilidad Parasitaria , Extractos Vegetales/farmacología , Hojas de la Planta/química , Distribución Aleatoria
9.
Parasitol Res ; 113(2): 505-11, 2014 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-24271081

RESUMEN

The use of decoctions of different plant materials is common practice in antimalarial ethnomedicine in Africa. Scientific evaluation of such herbal combinations to verify the claims is important. The study has evaluated the antimalarial efficacy of MAMA decoction (MD), a multicomponent herbal preparation and its individual plant components, namely leaves of Morinda lucida Benth [Rubiaceae] (ML), Azadirachta indica A. Juss [Meliaceae] (AI), Alstonia boonei De Wild [Apocynaceae] (AB) and Mangifera indica L [Anacardiaceae] (MI) in Plasmodium berghei-infected mice. Each decoction was prepared by boiling the powdered leaf in water, concentrated in vacuo and freeze-dried. The acute toxicity of MD (LD50=3.8 g/kg) was determined using Lorke's method. The antimalarial activities of MD and its plant components were evaluated by oral administration of the freeze-dried extracts (15-240 mg/kg) using the early malaria infection test model. The established malaria infection test was used to evaluate MD (60-240 mg/kg) while amodiaquine [10 mg/kg] (AQ) and distilled water were employed as the positive and negative controls, respectively. From the early malaria infection test, the effective doses at 50 % (ED50) and 90 % (ED90) for MD, AB, AI, ML, MI and AQ were 43, 79, 140, 134, 208 and 3.9 mg/kg and 202, 276, 291, 408, 480 and 9.2 mg/kg, respectively. For the established infection test, MD (240 mg/kg) and AQ gave parasite clearance of 55 and 95 % on day 5 of treatment. MD possesses antimalarial activity and is relatively safe.


Asunto(s)
Antimaláricos/uso terapéutico , Malaria/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/uso terapéutico , Plasmodium berghei/efectos de los fármacos , África , Alstonia/química , Animales , Antimaláricos/toxicidad , Azadirachta/química , Femenino , Malaria/parasitología , Masculino , Mangifera/química , Medicina Tradicional , Ratones , Morinda/química , Extractos Vegetales/toxicidad , Hojas de la Planta/química , Distribución Aleatoria
10.
Fitoterapia ; 76(2): 250-3, 2005 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-15752643

RESUMEN

The aqueous extract of Calotropis procera was evaluated for its spasmolytic effect using in vitro trachea smooth muscle chain of Guinea-pig. The extract (50, 100 and 200 microg/ml) showed a dose-dependent relaxant activity probably exhibited through the direct relaxant action on the smooth muscle.


Asunto(s)
Calotropis , Parasimpatolíticos/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Tráquea/efectos de los fármacos , Animales , Relación Dosis-Respuesta a Droga , Cobayas , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Parasimpatolíticos/administración & dosificación , Parasimpatolíticos/uso terapéutico , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico
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