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Ethanol extract of whole plant of Trichosanthes cucumerina L. var. cucumerina was evaluated for antiovulatory activity in adult rats. The ethanol extract at the doses 200 and 400mg/kg body weight (orally) affected the normal estrous cycle showing a significant increase in estrus and metestrus phases and decrease in diestras and proestrus phases. The extract also significantly reduced the number of healthy follicles (Class I-Class VI) and corpora lutea and increased the number of regressing follicles (Stage IA, Stage IB, Stage IIA, and Stage IIB). The protein and glycogen content in the ovaries were significantly reduced in treated rats. The cholesterol level was significantly increased, whereas, the enzyme activities like 3b-HSD and 17b-HSD were significantly inhibited in the ovary of treated rats. Serum FSH and LH levels were significantly reduced in the treated groups were measured by RIA. In acute toxicity test, neither mortality nor change in the behavior or any other physiological activities in mice were observed in the treated groups. In chronic toxicity studies, no mortality was recorded and there were no significant differences in the body and organ weights were observed between controls and treated rats. Hematological analysis showed no significant differences in any of the parameters examined (RBC, WBC count and Hemoglobin estimation). These observations showed the antiovulatory activity of ethanol extract of whole plant of Trichosanthes cucumerina L. var. cucumerina in female albino rats.

El extracto de etanol de toda la planta de Trichosanthes cucumerina var. cucumerina (L.) se evaluó en cuanto a su actividad antiovulatoria en ratas adultas. El extracto de etanol en dosis de 200 y 400mg/kg de peso corporal (oral) afectó el ciclo normal estral, mostrando un aumentó significativo en las fases de estro y metaestro y la disminución de las fases de diestro y proestro. El extracto también redujo significativamente el número de folículos sanos (Clase I=Clase VI) y cuerpo lúteo y aumentó el número de folículos en regresión (etapa I, etapa IB, etapa II y etapa IIB). La proteína y el contenido de glucógeno en los ovarios se redujeron significativamente en las ratas tratadas. El nivel de colesterol aumentó significativamente, mientras que, actividad de las enzimas 3b-HSD y 17b-HSD se inhibió significativamente en el ovario de ratas tratadas. FSH sérico y los niveles de LH se redujeron significativamente en los grupos tratados y medidos por RÍA. En la prueba de toxicidad aguda, no hubo mortalidad ni cambio en el comportamiento fisiológico o de cualquier otra actividad en los grupos tratados de ratas. En estudios de toxicidad crónica, no se registró mortalidad y no hubo diferencias significativas en el peso corporal o el peso de los órganos entre los controles y las ratas tratadas. Los análisis hematológicos no mostraron diferencias significativas en ninguno de los parámetros examinados (eritrocitos, recuento de glóbulos blancos y estimación de hemoglobina). Estas observaciones mostraron la actividad antiovulatoria del extracto de etanol de toda la planta de Trichosanthes cucumerina var. cucumerina en ratas albinas hembras.

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To test the efficacy and clinical safety of a low and high dose of the GnRH antagonist, acyline, on estrous cycle interruption and anovulation in female dogs, 20 proestrous (<3d) bitches were randomly assigned to one of the following pharmacological protocols (given sc): acyline 110 microg/kg (ACY-L; n=6); acyline 330 microg/kg (ACY-H; n=8); or placebo (PLACE, n=6). The animals were monitored (clinical and vaginal cytology examinations) daily for 60d. Blood samples for serum progesterone serum concentrations were collected 14d after treatment to determine if ovulation had occurred. Appearance of side effects and days to the onset of the first spontaneous estrous cycle after treatment were also recorded. In both ACY groups, but not the PLACE group, estrous cycles were interrupted after treatment (P<0.05). The interval from treatment to estrus interruption in ACY-L and ACY-H groups was 3.0+/-0.6 and 3.2+/-0.2d, respectively (LSM+/-SEM; P>0.05). In the PLACE bitches, physical, behavioral and cytological proestrus slowly progressed to estrus and diestrus. Ovulation was absent in all ACY, but not in PLACE bitches (P<0.05). None of the females manifested side effects related to the treatments (P>0.05). Spontaneous return to a normal estrous cycle during the study period occurred in all ACY (ACY-L 19.5+/-2.7d vs ACY-H 24.8+/-2.0d; P>0.05), but in none of the PLACE bitches (P<0.05). In conclusion, acyline efficiently, safely and reversibly interrupted an early phase of the estrous cycle in bitches by preventing ovulation.

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BACKGROUND: Levonorgestrel (LNG) consistently prevents follicular rupture only when it is given before the onset of the ovulatory stimulus. As locally synthesized prostaglandin (PG) plays a crucial role in follicular rupture and cyclooxygenase-2 (cox-2) catalyses the final step of PG synthesis, we reasoned that adding a cox-2 inhibitor to LNG would prevent follicular rupture even after the ovulatory process had been triggered by the gonadotrophin surge. METHODS: Forty-one women were divided into two groups. One was treated when the size of the leading follicle was 15-17 mm (n=10) and the other when it was >or=18 mm (n=31). Each woman contributed with one cycle treated with LNG 1.5 mg single dose plus placebo and another treated with LNG + meloxicam (Melox) 15 mg, in a randomized order. Serial blood sampling for the assay of LH and follicular monitoring by transvaginal ultrasound were performed before and after treatment. RESULTS: Follicular rupture failed to occur within the 5-day period that followed treatment in 50 and 70% of cycles treated with LNG + Placebo and LNG + Melox, respectively, in the 15-17 mm group (P=0.15) and in 16 and 39% of cycles treated with LNG + Placebo and LNG + Melox, respectively, in the >or=18 mm group (P < 0.052). The overall proportion of cycles with no follicular rupture or ovulatory dysfunction increased significantly by the addition of Melox to LNG (66 versus 88%, P < 0.012; n=41-matched pairs). CONCLUSIONS: The trend towards increased incidence of no follicular rupture when Melox was combined with LNG suggests that the addition of a cox-2 inhibitor has the potential to improve the contraceptive efficacy of LNG by a pre-fertilization effect.

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La inhibición de la ovulación es el principal mecanismo o efecto buscado en los casos de utilización terapéutica o contraceptiva de los anticonceptivos orales (ACO). Los mecanismos de acción secundarios postfertilización tienen reparos éticos para aquellas pacientes que consideran la concepción como el comienzo del desarrollo de la persona humana. Quisimos saber en qué medida se inhibe la ovulación mediante la administración de ACO de bajas dosis, como primera aproximación al problema ético planteado por los efectos postfertilización y para analizar la eficacia terapéutica de los anticonceptivos orales. Se revisa la literatura entre los años 1985 y 2001 y se seleccionan 3 trabajos comparables entre si de los cuales se desprenden los resultados. En un período de seguimiento de 3 meses, las mujeres que ingieren en forma adecuada ACO monofásicos combinados de bajas dosis que contienen 20 µg de etinilestradiol, presentan ovulación demostrada hormonal y ecográficamente en 2.35 por ciento a 8.3 por ciento de las mujeres. Existe una tendencia al aumento de la actividad ovárica y de los diámetros foliculares a medida que transcurre el tiempo de observación. Si el objetivo terapéutico es la anovulación, estas cifras permiten considerar los ACO como terapias adecuadas. Frente a la utilización individual de los ACO en contracepción, las cifras expuestas permitirán abordar en qué medida actúan los mecanismos secundarios y así considerar parámetros más objetivos en el análisis de los aspectos éticos a evaluar por el médico y la paciente

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OBJECTIVE: To study the endocrinologic profile of regularly menstruating users of levonorgestrel subdermal implants. DESIGN: Observational, prospective, case-controlled comparative study. SETTING: The Family Planning Clinic of PROFAMILIA, in Santo Domingo, Dominican Republic. PATIENTS, PARTICIPANTS: Thirty one regularly cycling Norplant users and 12 nonhormonal contraceptors who volunteered to participate. INTERVENTIONS: Norplant contraceptive implants were inserted in 31 subjects between 13 and 77 months before this study. MAIN OUTCOME MEASURES: Follicle-stimulating hormone, luteinizing hormone, estradiol (E2), and progesterone (P) were serially assayed for one menstrual cycle. RESULTS: Almost half of the cycles among Norplant users were anovulatory; all the rest (55%) had some form of dysfunction: diminished gonadotropin surge, luteal phase insufficiency (low P levels and shortened luteal phase), and E2 profiles different from normal controls. CONCLUSIONS: Anovulation is clearly one of the main mechanisms of action of Norplant, but even in presumptive ovulatory cycles, the dysfunctions described possibly contribute to the high contraceptive effectiveness of Norplant.

PIP: The study sought to examine the endocrinologic profile of regularly menstruating users of levonorgestrel subdermal implants. This observational, prospective, case-controlled, comparative study occurred at the Family Planning Clinic of PROFAMILIA in Santo Domingo, Dominican Republic. 31 subjects agreed to receive Norplant contraceptive implants between 13-77 months prior to this study and there were 12 nonhormonal contraceptors who also volunteered to participate. Follicle stimulating hormone, luteinizing hormone, estradiol (E2), and progesterone (P) were serially assayed for 1 menstrual cycle, and almost 1/2 of the cycles of norplant acceptors were anovulatory: the remainder (55%) had some form of dysfunction such as diminished gonadotropin surge, luteal phase insufficiency (low P levels and shortened luteal phase), and E2 profiles different from controls. Anovulation is clearly 1 of the main mechanisms of Norplant action, but even in presumptive ovulatory cycles, the dysfunctions described could have contributed to the high contraceptive effectiveness of Norplant.

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