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Diarrhea continues to be one of the top causes of death in children under the age of five, particularly in developing nations. In Ethiopian traditional medicine, a variety of medicinal plants are used to treat diarrhea. One of these plants is Maytenus addat (Loes.) Sebsebe (fam. Celastraceae), which is endemic to the Afromontane forests, especially along forest margins, of Ethiopia. The air-dried powdered leaves of M. addat were macerated with 80% methanol to yield a crude extract. Additionally, the powdered plant material underwent sequential solvent extraction using chloroform, methanol, and water to obtain solvent fractions. The 80% methanol leaf extract, solvent fractions, and an isolated compound from M. addat were evaluated for their antidiarrheal activity using castor oil-induced diarrheal model, anti-enteropooling test, and charcoal meal test in mice. The results showed that the 80% methanolic leaf extract significantly reduced the onset of diarrhea, the weight of feces, and the frequency of defecation in all the tested doses. The methanol and water fractions of the hydroalcoholic extract also exhibited dose-dependent antidiarrheal activity, with the methanol fraction showing the highest activity at 400 mg/kg dose. Subsequently, the most active methanol fraction was subjected to C-18 solid phase extraction, resulting in the isolation of a 3-hydroxyflavone, identified as quercetin by ESI-qToF-MS, 1H, and 13C-NMR spectroscopic techniques. Quercetin demonstrated a strong antidiarrheal activity in a dose-dependent manner. Thus, the present study provided evidence that the leaves of M. addat possess genuine antidiarrheal activity upholding the traditional medicinal use of the plant for the treatment of diarrhea. The findings also suggest that quercetin is responsible, in full or in part, for the activity of the plant.
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Background: The emergence and rapid spread of antimicrobial drug-resistance microorganisms exacerbate the treatment of infectious diseases, underscoring the importance of finding new, safe, and effective drugs. In Ethiopia, the roots of Carduus leptacanthus have traditionally been employed to treat microbial infectious diseases The aim of this study was to evaluate the antibacterial activity of the root extract and its primary components against six bacterial strains (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumonia). Methods: The extraction involved maceration of air-dried and powdered roots of C. leptacanthus with 80% methanol. The compound was isolated from the root extract using silica gel column chromatography and recrystallization in CHCl3/MeOH (9 : 1) and was characterized using ESI-MS and 1D-NMR spectroscopy. Antibacterial activity of the extract was assessed using agar well diffusion and broth microdilution methods. Results: Syringin, a phenylpropanoid, was isolated and characterized from the extract of C. leptacanthus. The extract showed the most substantial efficacy against S. epidermidis (MIC = 5.33 mg/ml and inhibition zone diameter of 24 mm at 200 mg/m). Syringin also elicited antibacterial activity against S. aureus (MIC = 13.33 mg/ml), S. epidermidis (MIC = 16 mg/ml), and S. agalactiae (MIC = 16 mg/ml). Despite being tested up to a maximum concentration of 16 mg/ml, syringin did not exhibit antibacterial activity against the Gram-negative bacteria (P. aeruginosa, E. coli, and K. pneumonia). Conclusions: In conclusion, the findings suggest that syringin exhibits partial involvement in the root extract's antibacterial activity, thereby potentially supporting the traditional medicinal use of the plant.
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The honey bee (Apis mellifera) faces a significant threat from Varroa destructor, causing the losses of millions of colonies worldwide. While synthetic acaricides are widely used to control Varroa infestations, excessive application has led to resistant strains and poses side effects on the host. Consequently, there is an urgent need for a new acaricide that is both effective and affordable, yet safe to use on bees. One potential source of these acaricides is essential oils (EOs) and their constituents. This study evaluated the acaricidal properties of four essential oils (Eucalyptus globulus, Rosemary officinalis, Trachyspermum ammi (Ethiopian and Indian varieties), their constituents and mixture of constituents against V. destructor through the complete exposure method. Our finding showed that a 1:1 mixture of thymol and carvacrol (4 h-LC50 = 42 µg/mL), thymol (4 h-LC50 = 71 µg/mL), and T. ammi oil (4 h-LC50 = 81-98 µg/mL) were the most toxic test samples against V. destructor. Honey bee behavior and selectivity were also assessed with one additional EO Thymus schimperi, indicating that T. schimperi, T. ammi, and their components were selective and did not affect the learning and memory of bees. In conclusion, the thymol and carvacrol (1:1) mixture was shown to be a promising replacement for synthetic acaricides, being three times more toxic than a commercial acaricide, fluvalinate (4 h-LC50 = 143 µg/mL).
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Background: The leaves of Osyris quadripartita Salzm. ex Decne, endemic to Ethiopia, are traditionally used for the treatment of malaria. Previous phytochemical investigations of Osyris species showed the presence of flavonoids, anthracene derivatives, and sesquiterpene lactones as the main constituents. The aim of the present study was to investigate the antimalarial activity of the leaf extract of O. quadripartita and its isolated constituent against mice infected with Plasmodium berghei. Methods: Isolation of a compound was carried out on silica gel column chromatography of the extract eluting with gradient mixtures of CHCl3/MeOH. Structural elucidation of the isolated compound was achieved by ESI-MS and 1D-and 2D-NMR spectral data. Peter's 4-day suppressive test method was used to determine the antimalarial activity of the test substances. Level of parasitemia, survival time, and body weight change were used to determine the antimalarial activity of the test substances. Results: (-) Catechin was isolated and characterized from the hydroalcoholic extract of O. quadripartita. At a concentration of 400 mg/kg, both the extract and (-) catechin exhibited antimalarial activity with the highest chemosuppression values of 70.61% and 64.26%, respectively. Conclusion: These findings indicate that O. quadripartita is endowed with genuine antimalarial activity attributed in part, to its (-) catechin content. Hence, the present study may validate the traditional use of the plant for the treatment of malaria.
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Trypanosomiasis and leishmaniasis are among the major neglected diseases that affect poor people, mainly in developing countries. In Ethiopia, the latex of Aloe rugosifolia Gilbert & Sebsebe is traditionally used for the treatment of protozoal diseases, among others. In this study, the in vitro antitrypanosomal activity of the leaf latex of A. rugosifolia was evaluated against Trypanosoma congolense field isolate using in vitro motility and in vivo infectivity tests. The latex was also tested against the promastigotes of Leishmania aethiopica and L. donovani clinical isolates using alamar blue assay. Preparative thin-layer chromatography of the latex afforded a naphthalene derivative identified as plicataloside (2,8-O,O-di-(ß-D-glucopyranosyl)-1,2,8-trihydroxy-3-methyl-naphthalene) by means of spectroscopic techniques (HRESI-MS, 1H, 13C-NMR). Results of the study demonstrated that at 4.0 mg/mL concentration plicataloside arrested mobility of trypanosomes within 30 min of incubation period. Furthermore, plicataloside completely eliminated subsequent infectivity in mice for 30 days at concentrations of 4.0 and 2.0 mg/mL. Plicataloside also displayed antileishmanial activity against the promastigotes of L. aethopica and L. donovani with IC50 values 14.22 ± 0.41 µg/mL (27.66 ± 0.80 µM) and 18.86 ± 0.03 µg/mL (36.69 ± 0.06 µM), respectively. Thus, plicataloside may be used as a scaffold for the development of novel drugs effective against trypanosomiasis and leishmaniasis.
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Aloe/química , Antiprotozoários/farmacologia , Látex/química , Extratos Vegetais/farmacologia , Antiprotozoários/química , Relação Dose-Resposta a Droga , Leishmania/efeitos dos fármacos , Estrutura Molecular , Extratos Vegetais/química , Relação Estrutura-Atividade , Tripanossomicidas/química , Tripanossomicidas/farmacologiaRESUMO
BACKGROUND: Epilepsy is one of the most common serious neurological disorders, responsible for substantial morbidity and mortality due to limited efficacy and negative properties of antiepileptic drugs. Medicinal plants are believed to be an important source of new chemical substances with potential therapeutic effects. Pentas schimperiana (A. Rich.) Vatke is a medicinal plant used in Ethiopian traditional medicine for the treatment of epilepsy. However, it lacks scientific investigation on its anticonvulsant activity. Therefore, this study was conducted to evaluate the anticonvulsant activity of 80% methanol root bark extract and solvent fractions of Pentas schimperiana (A. Rich.) Vatke in mice. METHODS: Anticonvulsant activity was evaluated by using the pentylenetetrazole and maximal electroshock-induced seizure test. The 80% methanolic root bark extract was subjected to successive fractionation with solvents differing polarity, i.e., chloroform, butanol, and water. The test groups received 100, 200, and 400 mg/kg bodyweight of extract and its solvent fractions. RESULT: The ME400 and BF400 at the higher dose exhibited a significant (p < 0.001) anticonvulsant effect in both the pentylenetetrazole and maximal electroshock-induced seizure test compared with control. However, chloroform fraction only showed a significant (p < 0.001) anticonvulsant effect in the PTZ-induced seizure test, while aqueous fraction had least anticonvulsant activity in both seizure-induced tests. Phytochemical screening of Pentas schimperiana (A. Rich.) Vatke root bark extract revealed the presence of alkaloids, saponins, flavonoids, phenols, steroids, terpenoids, and tannins. CONCLUSION: This study indicated that the plant has anticonvulsant activity and is considered as a potential source to develop a new antiepileptic drug.
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BACKGROUND: Kniphofia foliosa is a flamboyant robust perennial herb which has dense clumps and tick upright rhizomes with leaves at the base. In Ethiopia, it has several vernacular names including Abelbila, Ashenda, Amelmela, Yeznjero Ageda, Shemetmetie and Yezinjero Ageda. The plant is endemic to Ethiopian highlands, where its rhizomes are traditionally used for the treatment of malaria, abdominal cramps and wound healing. In the present study, the 80% methanol extract of K. foliosa rhizomes and its constituents are tested against Plasmodium berghei in mice. METHODS: Isolation was carried out using column and preparative thin layer chromatography (PTLC). The chemical structures of the compounds were elucidated by spectroscopic methods (ESI-MS, 1D and 2D-NMR). Peters' 4-day suppressive test against P. berghei in mice was utilized for in vivo anti-malarial evaluation of the test substances. RESULTS: Two compounds, namely knipholone and dianellin were isolated from the 80% methanolic extract of K. foliosa rhizomes, and characterized. The hydroalcoholic extract (400 mg/kg) and knipholone (200 mg/kg) showed the highest activity with chemosuppression values of 61.52 and 60.16%, respectively. From the dose-response plot, the median effective (ED50) doses of knipholone and dianellin were determined to be 81.25 and 92.31 mg/kg, respectively. Molecular docking study revealed that knipholone had a strong binding affinity to Plasmodium falciparum l-lactate dehydrogenase (pfLDH) target. CONCLUSION: Results of the current study support the traditional use of the plant for the treatment of malaria.
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Antimaláricos/farmacologia , Asphodelaceae/química , Extratos Vegetais/farmacologia , Plasmodium berghei/efeitos dos fármacos , Plasmodium falciparum/efeitos dos fármacos , Animais , Antraquinonas/química , Antraquinonas/farmacologia , Antimaláricos/química , Feminino , Masculino , Camundongos , Extratos Vegetais/química , Rizoma/química , Testes de Toxicidade AgudaRESUMO
Aloesin (1) and 7-O-methyl-6'-O-coumaroylaloesin (2) were isolated from the leaf latex of Aloe monticola Reynolds, and their structures determined on the basis of NMR and mass spectroscopic analyses. The antimicrobial activities of the isolated chromones were evaluated against 21 bacterial and 4 fungal strains. Both compounds displayed antibacterial and antifungal effects against most bacterial and fungal strains tested, but their action was more prominent against Salmonella typhi, Shigella dysentery and Staphylococcus aureus (MIC = 10 µg/ml). Acute toxicity tests on mice revealed that neither the latex nor the isolated compounds possess toxicity up to a dose of 2000 mg/kg, signifying an oral LD50 greater than 2000 mg/kg. The results indicate that A. monticola possesses genuine in vitro antimicrobial effect attributed in full or in part to the presence of the isolated chromones in the latex.
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Aloe/química , Anti-Infecciosos/farmacologia , Cromonas/farmacologia , Látex/química , Folhas de Planta/química , Animais , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Cromonas/química , Cromonas/isolamento & purificação , Fungos/efeitos dos fármacos , Glucosídeos/química , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Dose Letal Mediana , Camundongos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Testes de Toxicidade AgudaRESUMO
Crinum abyscinicum Hochst. ExA. Rich bulb is traditionally used in Ethiopia for the treatment of various ailments including internal parasites, mastitis, rabies, colic diseases of animals, and cancer. Despite its importance in traditional cancer treatment, no research work has been reported on the antiproliferative activity of the bulb extract and its major constituents. Phytochemical investigation of the bulb extract of C. abyscinicum by PTLC over silica gel resulted in the isolation of two alkaloids, which were unequivocally identified as 6-hydroxycrinamine and lycorine on the basis of 1H- and 13C-NMR and MS analysis. The bulb extract, 6-hydroxycrinamine, and lycorine possessed significant antiproliferative activity, lycorine being the most active exhibiting GI50 values of 2.8 µg/ml and 3.4 µg/ml against A2780 and MV4-11 cells, respectively. Cell cycle analysis and annexin V/propidium iodide double staining in A2780 cells revealed that both compounds increased the percentage of cells in the S-phase at 30 µg/ml without inducing apoptosis. Our results suggest that the antiproliferative activities of the bulb extract of C. abyscinicum, 6-hydroxycrinamine, and lycorine could support the traditional claim of the plant against cancer.
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There are 46 Aloe species identified from Ethiopia out of which 67.3% are endemics but comprehensive data on their ethno-medicinal and bio-cultural values are lacking. Interview, focus group discussion (FGD), and guided field walks were conducted with 210 respondents (152 men and 58 women). Relative frequency of citation (RFCs), informants' consensus factor (Fic), use value (UVs), relative importance index (RIs), and cultural value index (CV) were analyzed. Non-parametric Kruskal Wallis and Wilcoxon tests were performed using R software. Twenty-three Aloe species were recorded in the study areas with 196 use-reports and 2158 citations, grouped into six major use categories (NUC = 6). Medicinal use categories accounted for 149 use-reports (76%) with 1607 citations. The species with the highest numbers of use-reports were Aloe megalacantha subsp. alticola, A. trichosantha subsp. longiflora and A. calidophila of which 87, 75 and 61.1% respectively were medicinal uses. Aloe calidophila has highest values in all indices UV (11.72), RFC (0.68), RI (0.89), and CV (6.2). Among Aloe parts, leaf exudate accounted for 111 use-reports (49.1%) of which 92.9% were used for medicinal purposes. Aloe retrospiciens and A. ruspoliana were reported poisonous to carnivores. Fic values of the six major use categories ranged from 0.86 to 0.22. Elderly people (>60) had more knowledge than 25-40 and 41-60 age groups (Kruskal-Wallis chi-squared = 12.17, df = 3, p = 0.006), which is significant difference in depth of ethno-medicinal knowledge. Men had more knowledge of medicinal uses than women (Wilcoxon test, p = 0.002) significantly different, while women were knowledgeable than men for cultural uses like, cosmetic (Wilcoxon test, p = 0.06), not significantly different. The ways in which aloes are used and valued have implications for their future medicinal utility, which instigate detailed phytochemical and pharmacological studies.
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Small hive beetle (Aethina tumida Murray), indigenous to Africa, has spread to other parts of the world where has become a threat to the honeybee industry. In the present study, insecticidal properties (contact, fumigant, and repellent toxicities) of three main constituents derived from Trachyspermum ammi (L.) Sprague ex Turrill fruits essential oil were evaluated against adult small hive beetles under laboratory conditions. The Hydrodistillation of T. ammi fruits, grown in Ethiopia, yielded a pale yellow essential oil (3.5% v/w) with a strong aromatic odor. Analyses by gas chromatography-mass spectrometry identified twenty-two compounds that accounted for 98.68% of the total essential oil. The essential oil was dominated by monoterpenoids, comprising -terpinene (32.72%), p-cymene (27.92%), and thymol (24.36%). The essential oil showed strong contact and fumigation toxicities against the small hive beetle adults, with a LD50 value of 66.64 µg/adult and a LC50 value of 89.03 mg/L air, respectively. Among the main constituents, thymol was the most toxic component found in both contact (LD50 = 41.79 µg/adult) and fumigation (LC50 = 52.66 mg/L air) toxicities. The other two components, -terpinene and p-cymene, were less effective in both contact and fumigant toxicities testing. The results showed that T. ammi essential oil and thymol could serve as potential alternatives to synthetic insecticides for the control of small hive beetle adults.
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Apiaceae/química , Besouros/crescimento & desenvolvimento , Frutas/química , Óleos Voláteis , Animais , Inseticidas/química , Inseticidas/isolamento & purificação , Inseticidas/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/farmacologiaRESUMO
The currently available antileishmanial drugs are either toxic or too expensive for routine use in developing countries where the disease is most common. Local people in the Somalia region of Ethiopia use the leaves of Aloe macrocarpa Todaro for the treatment of malaria, jaundice, and skin diseases. In our ongoing search for new, efficient, and safe antileishmanial drugs, we investigated the leaf latex of Aloe macrocarpa and its acid-hydrolyzed product aloin A/B (1), as well as the semisynthesized derivatives of aloin A/B, namely, aloe-emodin (2) and rhein (3) against promastigotes and axenically cultured amastigotes of Leishmania aethiopica and L. donovani clinical isolates. Activity study was carried out based on the fluorescence characteristic of resazurin added to drug-treated cultures. Oxidative hydrolysis of aloin A/B by ferric chloride and concentrated hydrochloric acid afforded aloe-emodin (2), which was further oxidized using sodium nitrite and concentrated sulfuric acid to furnish rhein (3). Cytotoxicity study of test substances was performed against human monocytic cell line THP-1 using Alamar Blue and cell viability was measured fluorometrically. The test compounds showed lower activity (IC50 = 6.7 to 12.1 µM for promastigotes and IC50 = 3.6 to 10.2 µM for axenic amastigotes) than the reference drug amphotericin B (IC50 = 1.3 to 2.7 µM). However, amphotericin B (LC50 = 11.1 µM) was much more toxic than the test compounds (LC50 = 369.2 - 611.6 µM) towards human monocytic cell line (THP-1) despite its efficiency. As demonstrated in the current study, high selectivity indices (SIs) of the test compounds represent a remarkable advantage over the reference drug and highlight their potential use as templates for further development of safe leishmanicidal drugs.
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The leaf latex of Aloe yavellana Reynolds is traditionally used for the treatment of various illnesses of humans and domestic animals in Ethiopia. In the present study, the latex and two major compounds isolated from it, namely, aloin A/B and microdontin A/B were assessed for their larvicidal activity against Amblyomma variegatum tick larvae using a larval packet test (LPT). The LC50 and LC99 of the latex were found to be 35.82 ± 2.27 and 83.48 ± 3.95 mg/ml, respectively. Although microdontin A/B showed better larvicidal activity (LC50 = 89.40 ± 4.45 mg/ml) than aloin A/B (LC50 = 257.69 ± 6.31 mg/ml), neither of the isolated compounds was as active as the latex suggesting that the compounds acted synergistically or minor compounds with potent larvicidal activity may exist in the latex. The results confirmed that the leaf latex of A. yavellana and its isolated compounds could have the potential to be used as larvicidal against A. variegatum ticks.
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Acaricidas/administração & dosagem , Aloe/química , Ixodidae/efeitos dos fármacos , Larva/efeitos dos fármacos , Látex/administração & dosagem , Folhas de Planta/química , Acaricidas/química , Acaricidas/isolamento & purificação , Animais , Bovinos/parasitologia , Doenças dos Bovinos/parasitologia , Emodina/análogos & derivados , Emodina/farmacologia , Humanos , Ixodidae/fisiologia , Látex/química , Látex/isolamento & purificaçãoRESUMO
Malaria is one of the three major global public health threats due to a wide spread resistance of the parasites to the standard antimalarial drugs. Considering this growing problem, the ethnomedicinal approach in the search for new antimalarial drugs from plant sources has proven to be more effective and inexpensive. The leaves of Aloe pulcherrima Gilbert and Sebsebe, an endemic Ethiopian plant, are locally used for the treatment of malaria and other infectious diseases. Application of the leaf latex of A. pulcherrima on preparative silica gel TLC led to the isolation of two C-glycosylated anthrones, identified as nataloin (1) and 7-hydroxyaloin (2) by spectroscopic techniques (UV, IR, ¹H- and 13C-NMR, HR-ESIMS). Both the latex and isolated compounds displayed antimalarial activity in a dose-independent manner using a four-day suppressive test, with the highest percent suppression of 56.2% achieved at 200 mg/kg/day for 2. The results indicate that both the leaf latex of A. pulcherrima and its two major constituents are endowed with antiplasmodial activities, which support the traditional use of the leaves of the plant for the treatment of malaria.
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Aloe/química , Antracenos/administração & dosagem , Antimaláricos/administração & dosagem , Malária/tratamento farmacológico , Parasitemia/tratamento farmacológico , Extratos Vegetais/química , Animais , Antracenos/química , Antracenos/isolamento & purificação , Antracenos/farmacologia , Antimaláricos/química , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Modelos Animais de Doenças , Etiópia , Látex/química , Medicina Tradicional , Camundongos , Estrutura Molecular , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plasmodium berghei/efeitos dos fármacosRESUMO
BACKGROUND: Health seeking behavior of people around the globe is affected by different socio-cultural and economic factors. In Ethiopia, people living in rural areas in particular, are noted for their use of medicinal plants as a major component of their health care option. This study was conducted to document ethnopharmacological information of the Hamer semi-pastoralists ethnic group in southwestern Ethiopia. METHODS: A cross-sectional study was carried out whereby information on demographic characteristics, prevalence of perceived illnesses, factors associated with preference of health care seeking options, medicinal plants used and hoarded as well as some healers' socio-economic characteristics were collected using two sets of semi-structured questionnaires - one for household (HH) heads and the other for traditional healers supplemented by focus group discussions (FGDs). Households were selected using a cluster sampling followed by systematic sampling techniques; whereas healers and FGD participants were purposively selected with the assistance of local leaders and elders from the community. RESULTS: The study revealed that the use of traditional medicine among the Hamer ethnic group is very high. Females preferred traditional medicine more than males. The main reasons for this preference include effectiveness, low cost and ease of availability. Malaria (gebeze) was the most frequently occurring illness in the area identified by all FGD participants. A total of 60 different medicinal plants were reported [34 by HH respondents, 14 by traditional healers and 12 by both]. Fifty-one medicinal plants were fully identified, 3 at generic level and 6 have not yet been identified. CONCLUSION: It can be concluded that traditional medical practices, particularly herbal aspect, is widely used by the Hamer ethnic group, although health seeking behavior of the community is affected by different socio-economic and cultural factors.
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Comportamentos Relacionados com a Saúde , Comportamento de Busca de Informação , Medicinas Tradicionais Africanas , Fitoterapia , Plantas Medicinais , Estudos Transversais , Etiópia , Etnofarmacologia , Feminino , Grupos Focais , Humanos , MasculinoRESUMO
BACKGROUND: The incidents of drug resistant microorganisms and the need of treatments for newly emerging pathogens are of great concern to the global community. Our ability to treat infectious diseases is dependent on the development of new pharmaceuticals, and one potential source being medicinal plants with traditional claims. The leaves of Aloe trigonantha L.C. Leach, an endemic Ethiopian plant, are locally used for the treatment of infectious and inflammatory diseases. This study explores the potential of the latex of this plant and compounds isolated thereof for their in vitro antibacterial and antifungal properties. METHODS: Analytical RP-HPLC and silica gel preparative TLC were used for identification and isolation of active constituents, respectively. Characterization of the compounds was based on UV, IR, HR-ESIMS, (1)H and (13)C NMR, and 2D-NMR spectral assignments. Antimicrobial activity studies were carried out against 21 pathogenic bacterial and 4 fungal strains using the disk diffusion method. Minimum inhibitory concentrations (MICs) were determined by the broth dilution method. RESULTS: A C-glycosylated chromone identified as aloesin, and three C-glycosylated anthrones characterized as 8-O-methy-7-hydroxyaloin A/B, aloin A/B and aloin-6'-O-acetate A/B were isolated. The latex and isolated compounds exhibited in vitro antibacterial activity against the tested pathogens. In some cases the activity of the isolated compounds (MIC = 10 µg/mL) was comparable with that of the standard drug ciprofloxacin, particularly against some of the Gram-negative bacterial strains tested. However, their activity towards the fungal pathogens tested was relatively weaker showing maximum activity against Candida albicans with MIC value of 400 µg/mL. CONCLUSION: The present findings can be used for further research aimed at the development of new antibacterial agents, and may also justify the ethnomedicinal claim of the plant for the treatment of infectious diseases.
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Aloe/química , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Látex/química , Látex/farmacologia , Candida albicans/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Folhas de Planta/químicaRESUMO
BACKGROUND: The traditional use of the oleo-gum-resin of Commiphora guidottii Chiov. ex. Guid., which is commonly called scented myrrh, for topical treatment of wound is well documented. The major objective of the present study was to investigate the essential oil and resin obtained from C. guidottii for their potential wound healing properties. Due to their influence on the wound healing process, the anti-inflammatory and antimicrobial activities of scented myrrh have also been investigated. METHODS: Powdered oleo-gum-resin of C. guidottii was steam-distilled to obtain essential oil, and the resin was extracted from the marc with MeOH and filtered. The TLC fingerprint profile of the resin has been recorded by using silica gel GF254 as stationary phase. The essential oil components were identified and quantified by GC-MS. Ointments prepared from the essential oil (4% v/w) and the resin (5% w/w) were used for wound healing activity tests. Toxicity of the formulated ointments was investigated according to Draize skin irritation test. Acute anti-inflammatory effect in mice was evaluated using carrageenan induced mouse hind paw oedema model. Antimicrobial activity tests were carried out using disk diffusion and broth dilution techniques against 21 pathogenic bacterial and 4 fungal strains. RESULTS: Ointment formulations of both the oil and resin were found to be non-irritant at the concentrations used and showed significant (p<0.05-0.001) increase in wound contraction rate, shorter epithelization time and higher skin breaking strength as compared to the negative control. Overall, the antibacterial and antifungal activities of the oil and resin were comparable with the standard antibiotics ciprofloxacin and griseofulvin, respectively. CONCLUSION: The results confirm that scented myrrh possesses genuine wound healing activity supporting the traditional use of the plant.
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Anti-Infecciosos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Commiphora/química , Fitoterapia , Pele/efeitos dos fármacos , Cicatrização/efeitos dos fármacos , Ferimentos Penetrantes/tratamento farmacológico , Animais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Masculino , Camundongos , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Pomadas , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Gomas Vegetais , Resinas Vegetais , Testes de Irritação da Pele , Resistência à Tração , Terpenos/farmacologia , Terpenos/uso terapêuticoRESUMO
BACKGROUND: Malaria is one of the major obstacles to the socioeconomic development of several developing countries. Adequate treatment of the disease is becoming increasingly difficult due to the worsening problems of drug resistance in many parts of the world. Therefore, increased efforts in antimalarial drug discovery are urgently needed. OBJECTIVES: This study was designed to evaluate the antimalarial activity of the leaf latex of Aloe citrina Carter and Brandham and its major constituent. MATERIALS AND METHODS: The leaf latex of A. citrina was dissolved in methanol and subjected to preparative thin layer chromatography. Structure of the isolated compound was determined on the basis of its electrospray-ionization tandem mass spectrometry, (1)H, (13)C NMR and DEPT spectral data. The latex and its isolated compound were tested for their in vivo antimalarial activity using a 4-day suppressive test against chloroquine sensitive ANKA strain of Plasmodium berghei in mice. RESULTS: Homonataloin A/B was isolated as a major component of the latex. Both the latex and isolated compound exhibited significant (P < 0.001) antimalarial activity at a dose of 400 mg/kg with parasite suppression of 60.59% and 67.52%, respectively. No significant adverse signs of toxicity were observed in mice treated with the leaf latex up to the highest dose (5000 mg/kg). CONCLUSION: The results of this study indicate that the antimalarial activity of the plant is attributed in part or in full to the presence of homonataloin A/B in the latex. It also validates the traditional use of the plant as an antimalarial agent.
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Phytochemical investigation of the leaf latex of Aloe trichosantha by preparative TLC gave two closely related anthrones, aloin A/B (1) and aloin-6'-O-acetate A/B (2). The identity of the compounds was established from HRESI-MS, 1H, 13C, DEPT, HMQC and HMBC spectral and chemical data. Whilst aloin A/B occurs in several Aloe species, aloin-6'-O-acetate A/B was isolated for the first time. The isolated compounds inhibited growth of several bacterial and fungal pathogens with minimum inhibitory concentration (MIC) from 10 to 400 microg/mL and 800 to 1000 microg/mL, respectively.
Assuntos
Aloe/química , Antracenos/farmacologia , Antibacterianos/farmacologia , Látex/química , Folhas de Planta/química , Antracenos/química , Antibacterianos/química , Antifúngicos/química , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Biologia MolecularRESUMO
Leishmaniasis is a major protozoal disease threatening the lives of 350 million people throughout the world. However, the therapeutic options for the disease are limited. In the present study, the antiprotozoal activity of the latex obtained from the Ethiopian plant Aloe calidophila Reynolds was evaluated by in vitro testing against Leishmania aethiopica and Leishmania major. It was found that the latex possesses moderate activity against both parasites with IC50 values of 64.05 and 82.29 µg/mL, respectively. Phytochemical investigation resulted in the isolation of three anthrones identified as aloinoside, aloin, and microdontin on the basis of IR, MS, (1) H NMR, and (13) C NMR spectral data. The isolated compounds showed strong antileishmanial activity with IC50 values ranging from 1.76 to 6.32 µg/mL against L. aethiopica and from 2.09 to 8.85 µg/mL against L. major. Although these values were higher than those of amphotericin B (IC50 = 0.109 and 0.067 µg/mL), the selectivity indices (813.35 and 694.90, respectively, against L. aethiopica and L. major) of aloinoside were much better than those of the standard drug (423.49 and 688.96). The results indicate that the isolated compounds have the potential to be used as a scaffold for the development of safe and cost-effective antileishmanial agents.