Momordica charantia L. extracts against Aedes aegypti larvae / Extratos de Momordica charantia L. sobre larvas de Aedes aegypti

Mormodica charantia (Curcubitaceae) is a plant with great medicinal potential, also used as an alternative of mosquitoes control as demonstrated by previous studies. We evaluated the larvicidal activity of crude extracts of ethyl acetate, methanol and hexane from flowers and fruits of M. charantia against Aedes aegypti (Culicidae). Flowers and fruits were macerated in methanol, ethyl acetate and hexane. Bioassays were performed with application of the extracts at final concentrations of 1 - 200 µg/mL in the middle of the third instar larvae of A. aegypti (L3). The results showed high toxicity to ethyl acetate extracts from flowers and fruits at concentrations of 200 µg/mL and 100 µg/mL, with 97% and 87% of larvae mortality (L3), respectively. Hexane extract demonstrated low toxicity, while methanol extract exhibited 78% larval mortality. The data suggested that the ethyl acetate extracts of flowers and fruits of M. charantia can effectively contribute to larvicidal activity. In addition, purification of M. charantia extracts may lead to a promising larvicidal activity to control the A. aegypti population.

Mormodica charantia (Curcubitaceae) é uma planta com grande potencial medicinal, sendo também uma alternativa no controle de mosquitos conforme demonstrado por estudos prévios. Avaliou-se a atividade larvicida dos extratos brutos de acetato de etila, metanólico e hexânico das folhas, flores e frutos de M. charantia no Aedes aegypti (Culicidae). Folhas, flores e frutos foram macerados em metanol, acetato de etila e hexano. Os bioensaios foram realizados com aplicação dos extratos nas concentrações finais de 1-200 µg/mL no meio de criação das larvas de terceiro estádio de A. aegypti (L3). Os resultados obtidos apontaram alta toxicidade para os extratos de acetato de etila das flores e frutos nas concentrações de 200 µg/mL e 100 µg/mL com mortalidade em L3 de 96,7% e 87%, respectivamente. Baixa toxicidade para o extrato hexânico e o extrato metanólico apresentou mortalidade de 78% larval. Os dados sugerem que os extratos de acetato de etila das flores e frutos de M. charantia podem contribuir efetivamente para atividade larvicida no controle da população de A. aegypti.

Bitter gourd (Momordica charantia) possess developmental toxicity as revealed by screening the seeds and fruit extracts in zebrafish embryos.

BACKGROUND: Bitter gourd (Momordica charantia) has attracted the focus of researchers owing to its excellent anti-diabetic action. The beneficial effect of Momordica charantia on heart has been reported by in vitro and in vivo studies. However the developmental toxicity or potential risk of M. charantia on fetus heart development is largely unknown. Hence this study was designed to find out the developmental toxicity of M. charantia using zebrafish (Danio rerio) embryos. METHODS: The crude extracts were prepared from fruit and seeds of M. charantia. The Zebrafish embryos were exposed to serial dilution of each of the crude extract. The biologically active fractions were fractionated by C18 column using high pressure liquid chromatography. Fourier-transform infrared spectroscopy and gas chromatography coupled with mass spectrophotometry was done to identify chemical constituents in fruit and seed extract of M. charantia. RESULTS: The seed extract of M. charantia was lethal with LD50 values of 50 µg/ml to zebrafish embryos and multiple anomalies were observed in zebrafish embryos at sub-lethal concentration. However, the fruit extract was much safe and exposing the zebrafish embryos even to 200 µg/ml did not result any lethality. The fruit extract induced severe cardiac hypertrophy in treated embryos. The time window treatment showed that M. charantia perturbed the cardiac myoblast specification process in treated zebrafish embryos. The Fourier-transform infrared spectroscopy analyses revealed diverse chemical group in the active fruit fraction and five new type of compounds were identified in the crude seeds extract of M. charantia by gas chromatography and mass spectrophotometry. CONCLUSION: The teratogenicity of seeds extract and cardiac toxicity by the fruit extract of M. charantia warned that the supplementation made from the fruit and seeds of M. charantia should be used with much care in pregnant diabetic patients to avoid possible damage to developing fetus.

Genotoxic and Antigenotoxic Potential of Momordica charantia Linn (Cucurbitaceae) in the Wing Spot Test of Drosophila melanogaster.

Momordica charantia, popularly known as bitter melon, is a plant widely used in ethnobotanical medicine. It has antibacterial, antifungal, anthelmintic, antidiabetic, antiviral, and antimalarial activities, among others. The goal of this study was to evaluate the genotoxic and/or antigenotoxic activity of the aqueous extracts obtained from the aerial parts and fruit of this plant by means of the Drosophila melanogaster wing spot test. Third-stage larvae that obtained standard (ST) cross and high bioactivation (HB) cross were treated with aqueous extracts of the aerial parts (IQA) and fruit (IQF) of M. charantia, following two protocols (genotoxicity and antigenotoxicity). The aqueous extracts are not genotoxic in lower concentrations. The frequencies of mutant spots observed in the descendants of the ST and HB crosses treated with doxorubicin (DXR) alone were 8.65 and 9.25, respectively, whereas in those cotreated with IQA and DXR, the frequencies ranged from 15.90 to 29 in the ST cross and from 15.05 to 24.78 in the HB cross. In cotreatment with IQF, the frequencies ranged from 30.10 to 30.65 in the ST cross and from 13.60 to 14.50 in the HB cross, whereas the frequencies obtained with DXR were 32.50 in the ST cross and 26.00 in the HB cross. In conclusion, the IQA has a synergistic effect, enhancing the genotoxicity of DXR in the ST cross and the HB cross, whereas the IQF has antigenotoxic effects in the HB cross.

Momordica charantia seed lectin: toxicity, bacterial agglutination and antitumor properties.

In last three decades, several studies were carried out on the D-galactose-specific lectin of Momordica charantia seeds (MCL). In the present study, in vitro growth inhibition (8-23 %) at different concentrations (6-24 µg/ml) of MCL was observed against Ehrlich ascites carcinoma (EAC) cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. MCL also showed 28, 45, and 75 % growth inhibitions against EAC cells when administered 1.2, 2.0, and 2.8 mg/kg/day (i.p.), respectively for five consequent days in vivo in mice. After lectin treatment, the level of red blood cell and hemoglobin was increased significantly with the decrease of white blood cell and maintained the normal level when compared with EAC-bearing control and normal mice without EAC cells. Although MCL caused cell cycle arrest at G0/G1 phase of EAC cells, any irregular shape or apoptotic morphological alterations in the lectin-treated EAC cells was not observed by an optical and fluorescence microscope. Lectin showed toxicity against brine shrimp nauplii with an LC50 value of 49.7 µg/ml. Four out of seven pathogenic bacteria were agglutinated by MCL in the absence of inhibitory sugar D-lactose/D-galactose. In conclusion, MCL showed strong cytotoxic effect and therefore can be used as a potent anticancer chemotherapeutic agent.

Toxicological studies of momordica charantia linn seed extracts in male mice / Estudios toxicológicos de los extractos de la semilla de Momordica charantia Linn en ratones macho

An attempt to find out the male contraceptive molecule of plant origin, the extracts of seeds of Momordica charantia were tested in male mice. Petroleum ether, chloroform and ethanolic extracts of Momordica charantia were administered at the dose level of 25mg/100gm body weight to the albino mice for 48 days intraperitoneally. All the extracts showed antispermatogenic effect as the number of spermatogonia, spermatocytes, spermatids and spermatozoa were decreased. The increase in the weight of epididymis, prostate gland, seminal vesicle and vas deferens indicates clearly the androgenic property of these extracts. After subjecting to preliminary phytochemical screening ethanol extract showed positive tests for alkaloids, flavonoids, glycosides, phenols, tannins, oils and fats. Out of the three extracts tested, the ethanol extract seems to be more potent in its contraceptive and androgenic activities.

En un intento por descubrir la molécula de anticoncepción masculina de origen vegetal, fueron probados los extractos de semillas de Momordica charantia en ratones machos. Extractos de éter de petróleo, cloroformo y etanol de Momordica charantia fueron administrados en dosis de 25mg/100g de peso corporal a ratones albinos de 48 días por vía intraperitoneal. Todos los extractos mostraron un efecto antiespermatogénicos, con reducción del número de espermatogonias, espermatocitos, espermátidas y espermatozoides. El aumento de peso del epidídimo, próstata, vesículas seminales y conductos deferentes indica claramente la propiedad androgénica de estos extractos. Después de someter el extracto de etanol a la detección preliminar fitoquímica se observaron resultados positivos para alcaloides, flavonoides, glucósidos, fenoles, taninos, aceites y grasas. De los tres extractos probados, el extracto de etanol parece ser más potente en sus actividades de anticonceptivas y androgénicas.

Atividade antifúngica de extratos de Momordica charantia L. sobre Colletotrichum musae / Antifungal activity of Momordica charantia L. extracts against Colletotrichum musae

Os objetivos do presente trabalho foram avaliar os efeitos de extratos de Momordica charantia sobre o crescimento micelial e a germinação de conídios de Colletotrichum musae, e a eficiência destes extratos no controle da antracnose, causada por C. musae, em bananas. Extratos aquoso e hidroetanólico, obtidos de folhas e ramos, na concentração de 50 por cento em relação ao volume adicionado, em meio sólido, proporcionaram 71 e 65 por cento de inibição do crescimento micelial, respectivamente, enquanto que em meio líquido, a inibição do crescimento micelial foi de 86 e 81 por cento, respectivamente. Somente o extrato aquoso e o tiofanato metílico, nas concentrações de 50 por cento e 1000 µg mL-1 respectivamente, proporcionaram 100 por cento de inibição da germinação de esporos de C. musae. Os extratos metanólico e aquoso inibiram em 80 e 70 por cento, respectivamente, o desenvolvimento das lesões em bananas, quando aplicados até dois dias antes da inoculação do fungo. Estes resultados foram semelhantes ao tratamento com tiofanato metílico, que inibiu 80 por cento do desenvolvimento das lesões. Confirma-se a presença de substância antifúngica nos extratos de M. charantia e outros estudos devem ser realizados para viabilizar seu uso no controle da antracnose da banana.

The aims of the present work were to evaluate the effects of Momordica charantia extracts on mycelial growth and conidial germination of Colletotrichum musae, as well as the efficiency of these extracts in controlling anthracnose caused by C. musae in bananas. Water and hydroethanol extracts were obtained from leaves and branches at 50 percent concentration relative to the added volume. In solid medium, extracts led to 71 and 65 percent mycelial growth inhibition, respectively, whereas in liquid medium the mycelial growth was inhibited at 86 and 81 percent, respectively. Only water extract and thiophanate-methyl, at 50 percent and 1000 µg mL-1, respectively, resulted in 100 percent inhibition of C. musae spore germination. Methanol and water extracts inhibited by 80 and 70 percent, respectively, the development of lesions in bananas when applied until two days before fungal inoculation. These results were similar to those of the treatment with thiophanate-methyl, which inhibited 80 percent development of lesions. The presence of antifungal substance was confirmed in M. charantia extracts. Future studies must be performed to make its use viable for the control of anthracnose in bananas.

Toxicidad aguda oral y ensayos de irritación de extractos acuoso e hidroalcohólico de Momordica charantia L / Acute oral toxicity and irritation tests in aqueous hydroalcoholic extracts from Momordica charantia L

Fundamentación: los extractos de Momordica charantia L. poseen potencial terapéutico avalado científicamente que posibilita el empleo de esta planta en diversas enfermedades, sobre todo en la diabetes, por lo que caracterizar su potencial tóxico es de gran importancia para avalar el empleo de esta planta como agente terapéutico. Objetivos: realizar los estudios de toxicidad aguda oral e irritación ocular y dérmica a extractos acuoso e hidroalcohólico de M. charantia, con la finalidad de caracterizar su potencial toxicológico agudo. Métodos: el ensayo de toxicidad aguda oral se llevó a cabo en ratas Wistar hembras mediante el método de las clases tóxicas agudas, con la dosis máxima de 2 000 mg/kg. Los ensayos de irritación dérmica y ocular se llevaron a cabo en conejos Nueva Zelanda siguiendo los métodos descritos en las normas OECD 404 y 405. Resultados: la evaluación del extracto hidroalcohólico de M. charantia en el ensayo de toxicidad aguda mostró signos tóxicos por causa de la presencia de etanol en el extracto y una ligera disminución del peso corporal que no fue significativa. La administración del extracto acuoso no provocó signos tóxicos ni mortalidad. Ambos extractos se clasificaron en categoría 5 para ubicarse en el rango de toxicidad de una DL50> 2 000 mg/kg. En el ensayo de irritación dérmica y ocular se clasificaron los extractos como no irritantes. Conclusiones: los extractos evaluados mostraron un bajo potencial tóxico agudo tanto por vía oral como tópica.

Rationale: Momordica charantia L. extracts have scientifically-endorsed therapeutical potentialities that make the use of this plant possible in several diseases, mainly for diabetes, so characterizing its toxic potential is of great significance to support this plant as a therapeutical agent. Objectives: to conduct acute oral toxicity and ocular and dermal irritation studies on aqueous hydroalcoholic extracts from M. charantia, with the aim of characterizing its acute toxicological potential. Methods: Acute oral toxicity test was applied to female Wistar rats through acute toxic class method, with maximum dose of 2000 mg/kg. Ocular/dermal irritation tests were made in New Zealand rabbits, following the described methods in OECD standards 404 and 405. Results: the evaluation of M. charantia hydroalcoholic extract in the acute toxicity test showed toxic signs due to ethanol in the extract and a minimum bodyweight reduction that was not significant. The administration of water extract elicited neither toxic signs nor mortality. Both extracts were classified into category 5 within the range of toxicity of DL50> 2 000 mg/kg. The dermal/ocular irritation test indicated that the studied extracts were not irritating. Conclusions: The evaluated extracts showed low acute toxic potential for both oral and topical administration.

Toxicidad aguda oral y ensayos de irritación de extractos acuoso e hidroalcohólico de Momordica charantia L / Acute oral toxicity and irritation tests in aqueous hydroalcoholic extracts from Momordica charantia L

Fundamentación: los extractos de Momordica charantia L. poseen potencial terapéutico avalado científicamente que posibilita el empleo de esta planta en diversas enfermedades, sobre todo en la diabetes, por lo que caracterizar su potencial tóxico es de gran importancia para avalar el empleo de esta planta como agente terapéutico. Objetivos: realizar los estudios de toxicidad aguda oral e irritación ocular y dérmica a extractos acuoso e hidroalcohólico de M. charantia, con la finalidad de caracterizar su potencial toxicológico agudo. Métodos: el ensayo de toxicidad aguda oral se llevó a cabo en ratas Wistar hembras mediante el método de las clases tóxicas agudas, con la dosis máxima de 2 000 mg/kg. Los ensayos de irritación dérmica y ocular se llevaron a cabo en conejos Nueva Zelanda siguiendo los métodos descritos en las normas OECD 404 y 405. Resultados: la evaluación del extracto hidroalcohólico de M. charantia en el ensayo de toxicidad aguda mostró signos tóxicos por causa de la presencia de etanol en el extracto y una ligera disminución del peso corporal que no fue significativa. La administración del extracto acuoso no provocó signos tóxicos ni mortalidad. Ambos extractos se clasificaron en categoría 5 para ubicarse en el rango de toxicidad de una DL50> 2 000 mg/kg. En el ensayo de irritación dérmica y ocular se clasificaron los extractos como no irritantes. Conclusiones: los extractos evaluados mostraron un bajo potencial tóxico agudo tanto por vía oral como tópica(AU)

Rationale: Momordica charantia L. extracts have scientifically-endorsed therapeutical potentialities that make the use of this plant possible in several diseases, mainly for diabetes, so characterizing its toxic potential is of great significance to support this plant as a therapeutical agent. Objectives: to conduct acute oral toxicity and ocular and dermal irritation studies on aqueous hydroalcoholic extracts from M. charantia, with the aim of characterizing its acute toxicological potential. Methods: Acute oral toxicity test was applied to female Wistar rats through acute toxic class method, with maximum dose of 2000 mg/kg. Ocular/dermal irritation tests were made in New Zealand rabbits, following the described methods in OECD standards 404 and 405. Results: the evaluation of M. charantia hydroalcoholic extract in the acute toxicity test showed toxic signs due to ethanol in the extract and a minimum bodyweight reduction that was not significant. The administration of water extract elicited neither toxic signs nor mortality. Both extracts were classified into category 5 within the range of toxicity of DL50> 2 000 mg/kg. The dermal/ocular irritation test indicated that the studied extracts were not irritating. Conclusions: The evaluated extracts showed low acute toxic potential for both oral and topical administration(AU)