Oxytocic and oestrogenic effects of Monechma ciliatum methanol extract in vivo and in vitro in rodents

Various solvent extracts of the leaves of Monechma ciliatum (family Acanthecaea) were tested for oxytocic properties on uterine preparations in vivo and in vitro. The methanol extract (HME) contracted the nonpregnant uterus of the rat, guinea-pig and mouse as well as preparations obtained from guinea-pigs on days 6–7 and 11–12 of pregnancy. The rat pregnant uterus was not affected by the extract. Oral administration of HME to rats on days 15, 16 and 17 of pregnancy had no abortifacient effect compared with oxytocin. However, laparotomy on day 23 revealed fetal death in utero. The extract was also found to have oestrogenic activity based on parameters such as uterine weight ratio, premature vaginal opening and degree of vaginal cornification.     

Contractile response induced by a limonoid (humilinolide A) on spontaneous activity of isolated smooth muscle

The in vitro effect of the limonoid humilinolide A, isolated from Swietenia humilis (Meliaceae), on spontaneous contractions of guinea-pig ileum, and uterus from oestrus, dioestrus, ovariectomized and oestrogen-primed rats was studied. Humilinolide A caused a concentration dependent and non-reversible excitatory effect on intestinal and uterine smooth muscle, distinguished as spasmogenic and uterotonic action respectively. However, the potency of this compound to induce contraction was different in the distinct preparations assayed: in ileal musculature of male guinea-pigs, as well as in uterine muscle of dioestrus and ovariectomized rats, a slight excitatory effect was observed; in contrast to an intense excitatory effect displayed in rat uterus with high oestrogen levels (oestrus and oestrogenized). These data suggest that the contractile response induced by humilinolide A could be mediated by oestrogens, probably by occupancy of some receptors in myometrial plasma membranes to induce uterotonic response, which may be oestrogen-dependent. © 1997 John Wiley & Sons, Ltd.     

Effect of Water Extract of Cardiospermum grandiflorum Swartz on the Gravid Female Rat Uterus

The effect of a water extract of Cardiospermum grandiflorum Swartz (Sapindaceae) was investigated on a gravid female rat uterus. This extract showed a strong elevation in contractile activity, inhibited by atropine, of the female (pregnant) Wistar rat uterus. It was found to be dose dependent.     

The Anticonceptive and the Effect on Uterus of Ether Extract, 18312-J of Ricinus communis

The ether extract 18312-J of Ricinus communis seed (600 mg/kg and 1.2 g/kg) administered subcutaneously to rats possessed significant anticonceptive activity. The extract demonstrated an oestrogenic effect in immature ovariectomized rats and mice and was devoid of any antioestrogenic property. Furthermore, the extract did not induce a decidual response in oestrogen primed ovariectomized rats and did not inhibit deciduoma formation in rats treated with progesterone. Administration of 18312-J to rats significantly altered the activity profile of the uterine muscle with respect to the frequency and amplitude of contraction as well as decreased responsiveness to oxytocin, ergometrine, acetylcholine and transmural electrical stimulation (TNS, 1-20H_z). The anticonceptive effect of 18312-J may be due in part to a disturbance of the oestrogen/progesterone balance and as well as to a direct action on the uterus. © 1997 by John Wiley & Sons, Ltd.     

Antidiarrhoeal Activity of Hamelia patens Methanol Extract in Rats and Mice

The inhibitory action of Hamelia patens methanol extract was studied in vitro on uterus, ileum and duodenum, and the antidiarrhoeal activity was evaluated in vivo on mice and rats. It was found that for the uterus and intestine the inhibitory response was dose dependent and the major antidiarrhoeal effect was observed at a dose of 100 mg/kg.     

Evaluation of pharmacological activity of a crude hydroalcoholic extract from Jatropha elliptica

The pharmacological effect of the hydroalcoholic extract of Jatropha elliptica was analysed in in vivo and in vitro models. When given orally in mice, the extract showed a low acute toxicity (LD₅₀ 5 g/kg). In a dose of 0.5 or 1 g/kg p.o. the extract did not interfere with diuresis in the rat, but was found to be effective in blocking rat paw oedema induced by carrageenan and partially, serotonin-induced oedema. In the same dose, the extract failed to inhibit rat paw oedema induced by dextran and the increase of rat cutaneous vascular permeability caused by Bothrops Jararaca venom, dextran, histamine, PAF-acether and serotonin. Pre-incubation of the isolated rat uterus and guinea-pig ileum with the extract (0.2–0.8 mg/mL), produced a concentration-related and non-competitive inhibition of contractions induced by acetylcholine and bradykinin. However, the extract was about 2-fold more potent in inhibiting the contraction of both agonists in guinea-pig ileum than in rat uterine muscle. In rat aorta, the extract (50–100 μg/mL) caused a concentration-dependent inhibition of noradrenaline-evoked contractions, being about 5-fold more potent when compared to the IC₅₀ values obtained in rat uterus.     

Uterotonic properties of the methanol extract of Monechma ciliatum

The oxytocic activity of the hot methanol extract (HME) of the leaves of Monechma ciliatum was compared with other uterine stimulants like ergometrine, oxytocin, 5-hydroxytryptamine (5-HT), acetylcholine (ACh) and prostaglandins (PGs) E₂ and F₂α (PGE₂ and PGF₂α) in the presence of some antagonists in an attempt to explain the mechanism of action of the extract. The effects of the reference drugs on uteri isolated from rats pretreated with HME for 2 weeks were also observed. Atropine blocked the effect of ACh and partially blocked those of HME while L-366-948 blocked only the effect of oxytocin. Indomethacin inhibited the effects of HME as well as all the other drugs, except the PGs and ACh. D-600 blocked the effect of all the drugs including HME. Methysergide antagonised only the effect of 5-HT and partially blocked ergometrine. Prolonged treatment altered the uterine musculature and the activity profile of the reference drugs. These results suggest that the HME may be acting by more than one mechanism to contract the uterus and explains the mechanism of the anti-implantation activity of the plant.     

荫风轮总苷对动物子宫作用的研究

目的:研究荫风轮总苷对子宫功能的影响。方法:无菌植入异物造成大鼠子宫炎症模型,观察荫风轮总苷的治疗作用;于大鼠离体子宫和家兔在体子宫观察其对子宫活动力和子宫收缩幅度的影响;并测定了荫风轮总苷对大鼠子宫重量和血清中雌二醇、黄体酮含量的影响。结果:荫风轮总苷有增强子宫收缩能力,且对在体子宫的作用维持时间较长,能显著增加子宫重量,有减轻子宫炎症作用的趋势,对雌激素水平有升高趋势,对孕激素水平无显著影响。结论:荫风轮总苷对子宫的作用是用于治疗子宫出血的重要药理基础。     

Effect of Carica papaya seed extract on female rat ovaries and uteri

The effect of an aqueous extract of Carica papaya seed for 7 and 15 days on the physiology of rat ovaries and uterus was studied. The possible reversibility of the induced effects was also investigated. The results revealed that the effects were more pronounced in the ovary than in the uterus. The changes in biochemical profile of the ovary and uterus involved alterations in the levels of ascorbic acid, ascorbigen (ASG), ascorbic acid utilization (AUU), ascorbic acid macromolecular (AA-MM) complexing, ascorbic acid free radical (AA-FR) formation, total ascorbic acid and glutathione (GSH), cholesterol, protein and glycogen. The increase in ascorbate turnover is an adaptation to overcome the harmful effect of the extract. The fertility test was 100% negative and the oestrus cycle was irregular with a predominance of dioestrus. The uterine contractility was increased. The above mentioned changes indicate that the extract manifested antifertility, antiimplantation and abortifacient effects in the treated animals. The withdrawal of treatment overcame the adverse effects of the treatment in ovary and the uterus and restored fertility.     

Effects on rat uterine and aorta strip smooth muscle of Thymus leptophyllus extract

The diethylether extract from Thymus leptophyllus was found to be more active on uterine smooth muscle than on aorta strips. Rat uterus experiments with and without extracellular calcium, yielded similar IC₅₀ values. A non-specific mechanism for the relaxant activity can therefore be postulated. In rat aorta and in the presence of extracellular calcium the extract inhibited the contractile response induced by K⁺ depolarizing solution and had a less inhibitory effect on noradrenaline (NA) contraction. In a Ca²⁺-free solution the extract strongly reduced the Ca²⁺-release induced by NA, but it did not affect the transient contraction caused by caffeine (CAF).     

Pharmacological effects of Agapanthus africanus on the isolated rat uterus.

The Agapanthus africanus plant is used by South African traditional healers as a phytomedicine in herbal remedies to treat pregnancy-related ailments and to augment labour. It has already been shown that an aqueous extract of A. africanus causes smooth muscle contractions in the isolated uterus and ileum preparations. In the present study, the effects of an aqueous extract of A. africanus leaves was examined on receptor systems involved in contraction of the uterine smooth muscle in order to determine the mechanism of its pharmacological effect relevant to its ethnic use to augment labour. The extract was tested on the isolated rat uterus preparation. The aqueous extract of A. africanus leaves was found to exhibit agonist activity on uterine muscarinic receptors and to promote the synthesis of prostaglandins in the oestrogenized rat uterus. Some pharmacological justification for the ethnic use of A. africanus as a herbal oxytocic in prolonged labour has been provided.     

生化汤提取物对孕末期家兔子宫肌电活动的影响

目的 :观察生化汤提取物对孕末期家兔子宫体及子宫颈肌电活动的影响 ,探讨其效应及作用方式。方法 :用PowerLab/8s生命信号记录仪采集乌拉坦麻醉状态下的怀孕末期家兔子宫体及子宫颈平滑肌肌电活动。结果 :生化汤提取物 4 0mg·kg^-1能增加怀孕末期家兔子宫体的平滑肌动作电位脉冲的发放 (P<0.01) ,对其子宫颈平滑肌肌电活动则无显著的影响 (P>0.05)。结论 :提示生化汤提取物具有增加宫体肌电活动作用 ,可以发挥催产、止血的效应 ;对宫颈的电活动无明显影响 ,表明它不干预产道舒缩 ,有利于胎儿的娩出。     

Effect of Ipomoea intrapilosa Methanol Extract on the Serotonergic Response in Rat Uterus

A methanol extract (MEII) obtained from the seeds of Ipomoea intrapilosa and its isolated crude alkaloid fraction (ALKII) were tested as possible blockers of the serotonergic response in the rat uterus in vitro . The results obtained showed an unsurmountable non-selective inhibition of the contractile response induced by serotonin on isolated uterine smooth muscle.     

Oestrogenic rhythm induced by a single administration of the extract of Ferula jaeschkeana to immature rats

The hexane extract of Ferula jaeschkeana was studied for its effects on the oestrogenic rhythm following a single administration to immature rats. A 25 mg/kg single oral dose significantly increased the uterine wet weight and caused premature opening of the vagina and induced vaginal cornification. A uterotrophic peak was attained 2 days after administration and thereafter declined gradually. At 10 days, values became almost normal. A significant amount of glycogen was estimated in the uterus during the first 5 days after administration and thereafter decreased significantly. Histoarchitecture of the uterus showed a stimulated endometrium which continued for 6–8 days only. The oestrogenic rhythm induced by the hexane extract was compared with that following diethylstilbesterol administration.     

Ca++ channel blocking activity of Artemisia scoparia extract

Intravenous administration of a hydro-methanolic extract of Artemisia scoparia (3–30 mg/kg) produced hypotensive and bradycardiac effects. These effects remained unaltered in atropine treated animals and the presence of the extract did not modify the vasoconstrictor response of norepinephrine, indicating that cardiovascular effects of the plant extract are not mediated through activation of muscarinic receptors or adrenoceptor blockade. In the in vitro studies, it suppressed the spontaneous movements of rabbit jejunum in a concentration-dependent (0.1-1 mg/mL) manner. The plant extract inhibited K⁺-induced tonic contraction in a manner similar to that of verapamil. Exposure of tissue to Ca⁺⁺-free Kreb's solution abolished the spontaneous movements which were restored on addition of Ca⁺⁺. In tissue pretreated with plant extract or verapamil, addition of Ca⁺⁺ (50 μM) failed to restore spontaneous contractions. These data indicate that Artemisia scoparia cntains Ca⁺⁺ channel blocker-like constituent(s) which may explain the hypotensive effect observed in vivo and the traditional use of the plant as a spasmolytic.     

CNS depressant effects,anti-inflammatory activity and anti-cholinergic actions of Santolina chamaecyparissus extracts

The pharmacological activity of several extracts together with the lyophilized infusion of S. chamaecyparissus ssp. squarrosa were investigated. The lethal dose 50% (LD₅₀), effect on animal metabolism, mechanical and thermic analgesia and spontaneous, anti-inflammatory, and anti-ulcer activity have been determined. Studies on isolated organs (rat duodenum and rat uterus) were also carried out. The hexanic and chloroformic extracts were potent antagonists of the thermic analgesia test; the former extract was also active in the mechanical analgesia test. The chloroformic extract and, to a lesser extent, the ethyl acetate extract and lyophilized infusion demonstrated noteworthy activity as anti-inflammatory agents. No extract produced an ulcerogenic effect. The hexanic extract had the highest inhibitory effect on ACh induced contraction of rat duodenum and the ethyl acetate extract of oxytocin induced contraction of rat uterus.     

Antiinflammatory Effects of an Ethyl Acetate Extract of Euphorbia royleana

The antiinflammatory activity of the ethyl acetate extract (EA) from the residue of an 85% alcohol extract of the latex of plant Euphorbia royleana was tested in mice and rats. In acute tests EA displayed marked antiinflammatory activity. Significant antiarthritic activity was observed in subacute and chronic models of formaldehyde-induced arthritis, adjuvant-induced developing and established arthritis. It produced inhibition of the exudate volume and the leucocyte migration in rats and vascular permeability in mice. EA showed a poor inhibitory effect on the granuloma formation by cotton pellet and croton oil. In in vitro studies EA inhibited the spontaneous contractions of the isolated pregnant rat uterus and oxytocin-induced contractions of virgin rat uterus. It had a very low ulcerogenic potential. The oral LD₅₀ in both rats and mice was more than 2500 mg/kg.     

生化汤提取物对正常未孕、雌激素预处理及产后小鼠离体子宫平滑肌收缩功能的影响

目的:研究生化汤不同含量水提取物对正常未孕小鼠、雌激素预处理小鼠及产后小鼠子宫平滑肌收缩功能的影响。方法:采用正常未孕小鼠、雌激素预处理小鼠及产后小鼠离体子宫标本,以Medlab生物信号采集处理系统记录生化汤水提取物(3～12 mg.mL^-1)对子宫的收缩幅度及频率的影响。结果:生化汤水提取物对正常未孕小鼠及产后小鼠子宫的影响主要表现为活动力减弱;对雌激素预处理小鼠子宫收缩频率及子宫活动力均表现为明显增强,且未见明显量效关系。结论:雌激素预处理小鼠子宫对生化汤的反应不能代表正常未孕及产后小鼠子宫的药理作用。     

Spasmogenic effect of Datura metel root extract on rat uterus and rectum smooth muscles

The effect of Dautura metel leaf and root extracts, scopolamine and acetylcholine was studied on isolated smooth muscle preparations. Datura metel leaf extract and scopolamine showed antispasmodic effects, whereas Datura metel root extract and acetylcholine caused contracture in isolated rat uterus and rectum whole muscle. This suggests the presence of a spasmogenic factor in Datura metel root extract.     

Oestrogenic and pregnancy interceptory efficacy of a flavonoid mixture from Grangea maderaspatana poir (Artemisia maderaspatana) in the mouse

A mixture of flavonoids extracted from the plant Grangea maderaspatana possessed oestrogenicity and antiimplantational activities in the mouse. In the 3 day uterotrophic bioassay, administration of the drug at a dose of 20 mg/kg body weight per day, intramuscularly to ovariectomized females, resulted in a highly significant (p<0.001) increase in the wet uterine and vaginal weights. However, in comparison with conjugated oestrogen, the extract proved to be mildly oestrogenic. Flavonoids, if administered orally at the same dose level effectively interfere with all stages of pregnancy. Maximum interceptory efficacy was recorded when the drug was administered from days 4–6 post coitum. However, there was a reduction in antinidational activity only if the drug was administered from days 1–3 and 7–9 post coitum.