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.     

Pharmacological studies on the antifertility effects of RICOM-1013-J from Ricinus communis var minor and preliminary clinical studies on women volunteers

The seed and petroleum ether fraction (PE; 5–20 mg/kg) of RICOM-1013-J demonstrated high antifertility efficacy in both animals and in women volunteers. Although PE demonstrated some oestrogenic activity in ovariectomized immature rats, there was no evidence of progestational activity. Administration of PE (5–20 mg/kg, s.c.) to rats and rabbits altered the activity profile of the uterus and fallopian tube from day 3 to day 90 of pretreatment. Moreover, the responsiveness of the uterine muscle and the fallopian tube to Ach, oxytoxin and ergometrine was significantly reduced from day 28 to day 90. Furthermore, PE induced histological changes in the ovary and altered the oestrous cyclicity. These results suggest that the high antifertility efficacy of RICOM-1013-J is unlikely to be due to any direct progestational activity and may be due partly to alteration in oestrogen/progesterone balance as well as to a direct effect on the uterus and fallopian tube. A survey of the contraceptive efficacy in women volunteers administered orally three seeds of RICOM-1013-J demonstrated the high efficacy of the seed in protecting against pregnancy for a period of 12 months with high compliance and minimal side effects. There was no evidence of side effects (nausea, vomiting, weight gain, morning sickness, increased blood pressure, etc) attributable to oestrogen in oral contraceptives; and these results may indicate a novel contraceptive effect due to both hormonal and direct effects on the reproductive system. © 1997 John Wiley & Sons, Ltd.     

Chemical, pathological and toxicological studies of the effects of RICOM-1013-J of Ricinus communis var minor on women volunteers and rodents

RICOM-1013-J (Ricinus communis var minor) administered orally once to each of 12 women volunteers at a dose of 2.5-2.7 g per 8 months, protected against pregnancy over a period of 7-8 months of study. A study of the effect of a contraceptive dose (20 mg/kg) on metabolic parameters in rat (food and water in-take, urine and faecal output and body weight) over a period of 4 months showed a slight decrease in all the parameters in the first 1-8 weeks. This effect was reversible attaining pretreatment levels from week 16. The LD(50) in an acute toxicity test in mice was 63.1 +/- 16.0 g/kg s.c. Determination of blood urea, sodium (Na(+)), potassium (K(+)), chloride (Cl(-)) and bicarbonate (HCORICOM-1013-J (Ricinus communis var minor) administered orally once to each of 12 women volunteers at a dose of 2.5-2.7 g per 8 months, protected against pregnancy over a period of 7-8 months of study. A study of the effect of a contraceptive dose (20 mg/kg) on metabolic parameters in rat (food and water in-take, urine and faecal output and body weight) over a period of 4 months showed a slight decrease in all the parameters in the first 1-8 weeks. This effect was reversible attaining pretreatment levels from week 16. The LD(50) in an acute toxicity test in mice was 63.1 +/- 16.0 g/kg s.c. Determination of blood urea, sodium (Na(+)), potassium (K(+)), chloride (Cl(-)) and bicarbonate (HCO$_?3? ?-?$)as a measure of renal function and alkaline phosphatase (ALP), transaminases (GPT and GOT) and transpeptidases (GGT) as a measure of liver function showed that liver function profiles in pretreated rats were not significantly different from control (p < 0.05) on day 21 to day 150. However, serum levels of ALP and GGT at day 120 to day 150 were moderately but significantly elevated (p > 0.05) compared with the control. There were no significant changes in renal function profiles in pretreated rats (p < 0.05) compared with the control. The results of the liver and renal function profiles in women volunteers showed that there were no significant (p < 0.05) changes in renal functions on day 206 following RICOM-1013-J administration. However, serum levels of ALP and GGT showed a slight rise in about 70% of volunteers, whereas bilirubin and transaminases levels were normal. The present results indicate a very high efficacy and margin of safety of RICOM-1013-J in women volunteers. The increase in ALP and GGT in both animal and women volunteers suggest mild intrahepatic cholestatic changes which may be attributed to an oestrogenic effect of RICOM-1013-J.     

Preliminary clinical investigation of the contraceptive efficacy and chemical pathological effects of RICOM-1013-J of Ricinus communis var minor on women volunteers

The seeds of Ricinus communis Linn, RICOM-1013-J, administered as a single oral dose of 2.3-2.5 g once per 12 months protected against pregnancy in 50 women volunteers for a period of one year. The antifertility and contraceptive efficacy of the seed was demonstrated in this study. Clinical observation revealed very minimal side effects. Some of the side effects investigated included headache, nausea, vomiting, weight gain, loss of appetite, raised blood pressure and dysmenorrhoea. Furthermore, both the renal and liver functions were not affected as revealed by urea, electrolyte and creatinine values as well as total bilirubin, conjugated bilirubin, serum albumin, total protein and transaminases values when compared with control values. In addition cholesterol and phospholipids were not significantly altered. When all these results are considered together, it seems unlikely that the antifertility and contraceptive efficacy of RICOM-1013-J is due to hormonal mechanisms alone since side effects, renal and liver function, and cholesterol effects attributable to oestrogen and/or progesterone were minimal in the volunteers.     

Anti-inflammatory and free radical scavenging activity of Ricinus communis root extract

Anti-inflammatory and free radical scavenging activities of the methanolic extract of Ricinus communis (RCM) (Euphorbiaceae) Linn. root was studied in Wistar albino rats. The methanolic extract at doses 250 and 500 mg/kg p.o. exhibited significant (P<0.001) anti-inflammatory activity in carrageenan-induced hind paw edema model. The extract at the dose of 500 mg/kg p.o. also exhibited significant (P<0.001) anti-inflammatory activity in cotton pellet granuloma model. The methanolic extract showed significant free radical scavenging activity by inhibiting lipid peroxidation initiated by carbon tetrachloride and ferrous sulphate in rat liver and kidney homogenates. The extract enhanced free radical scavenging activity of stable radical 2,2-diphenyl-1-picryl-hydrazyl (DPPH*), nitric oxide and hydroxyl radical in in vitro assay methods. The results of the study indicate that the methanolic extract of Ricinus communis root possess significant anti-inflammatory activity in acute and chronic inflammatory models in rats. The observed pharmacological activity may be due to the presence of phytochemicals like flavonoids, alkaloids and tannins present in the plant extract with various biological activities.     

Antifertility effects of Ricinus communis (Linn) on rats

The antifertility effects of 50% ethanol extracts of Ricinus communis have been studied in male rats. There was a drastic reduction in the epididymal sperm counts. Alteration in the motility, mode of movement and morphology of the sperms were observed. Reductions in the fructose and testosterone levels were suggestive of reduced reproductive performance. Reversibility tests showed that the antifertility effect of Ricinus communis was completely reversible on withdrawal of the drug. The ethanol extracts of Ricinus communis did not cause any hepatotoxicity since the hepatic GOT and GPT levels were unaltered.     

The water extract of adlay seed (Coix lachrymajobi var. mayuen) exhibits anti-obesity effects through neuroendocrine modulation

To find out whether the immunohistochemical expression of neuropeptid Y (NPY) and leptin receptor (LR) in the rat hypothalamus is influenced by adlay seed water extract (adlay), obesity in rats was induced by high fat diet (HFD) for 8 weeks; these rats were injected with 50 mg/100 g body weight adlay daily for 4 weeks. The results showed that the optical density of NPY immunoreactivity in paraventricular nucleus of rats increased approximately by 3.4 fold in HFD group compared to the normal diet group. Conversely, that of HFD + adlay group was about 2.6 fold lower than HFD group. The pattern of LR expression was similar to that of NPY. Both of NPY and LR mRNA levels, determined by real time PCR, in HFD + adlay group were decreased compared to those of HFD group, but there were no significant changes in the level of LR. These results suggest that adlay may regulate neuroendocrine activity in the brain. Accordingly, administration of adlay may be considered for therapies targeting obesity.     

Various uses of the castor oil plant (Ricinus communis L.) a review

The ancient and modern medicinal uses of the castor bean plant, Ricinus communis L. (Euphorbiaceae), in about fifty countries worldwide, has been surveyed. The different medicinal uses are grouped separately in relation to their pharmacological action, whether real or presumed, within the various medical specialities. The results show an extensive use of this plant throughout the world and the authors suggest that further research should be carried out to determine the active principles present in the various parts of the plant.     

The antiinflammatory and liver protective effects of Boussingaultia gracilis var. pseudobaselloides extract in rats

The pharmacological effects of Boussingaultia gracilis var. pseudobaselloides was studied against carrageenaninduced paw oedema, CCI₄ and D-galactosamine (D-GalN) induced hepatotoxicity in rats. The water extracts of B. gracilis var. pseudobaselloides (leaf, stem, brood bud) were found to maintain significant antiinflammatory activity against carrageenan-induced oedema. The administration of the brood bud extract (300 mg/kg) was more potent than indomethacin (10 mg/kg). Moreover, the water extracts of B. gracilis var. pseudobaselloides (leaf, stem, brood bud) significantly decreased the acute increase in serum GOT and GPT levels caused by CCI₄ and D-GalN. Histological changes such as necrosis, fatty change, ballooning degeneration, inflammatory infiltration of lymphocytes and Kupffer cells around the central vein (CCI₄-induced hepatotoxicity) and portal vein (D-GalN induced hepatotoxicity), were simultaneously improved by the treatment with B. gracilis var. pseudobaselloides (leaf, stem, brood bud).     

Post-testicular antifertility effects of Abrus precatorius seed extract in albino rats

Oral administration of a 50% ethanol extract of Abrus precatorius seeds (250 mg/kg) in albino rats for 30 and 60 days induced an absolute infertility in males which was reversible. Suppression of sperm motility in the cauda epididymis was the most pronounced effect of the treatment. Such treatment may affect the oxidative/energy metabolism of the cauda epididymis. Histological and histocytometric observations in testis and parareproductive tissues appeared normal while the protein, sialic acid, acid phosphatase and succinic dehydrogenase levels were significantly depleted.     

Protective effects of Garcinia kola seed extract against paracetamol-induced hepatotoxicity in rats

The hepatoprotective effect of Garcinia kola seed extract was investigated in rats treated with high doses of paracetamol. The extracts when administered at 100 mg/kg three times a day for five consecutive days reduced paracetamol- (800, 1000, 1200 mg/kg) induced lethality from 50, 90 and 100% to 0, 20 and 40%, respectively. There was a significant reduction in the liver enzymes SGOT and SGPT and histology scores. The hepatoprotective effect of the extract may be due to inhibition of cytochrome P-450 which normally converts paracetamol to the toxic intermediate metabolite N-acetyl-p-benzoquinoneimine (NAPQI).     

Preliminary investigation of contractile activity of Ricinus communis and Euclea divinorum extracts on isolated rabbit uterine strips

Ricinus communis and Euclea divinorum of the family Euphorbiaceae and Ebenaceae, respectively, are traditionally used by Traditional Birth Attendants (TBAs) in Machakos district of Kenya to induce or augment labor, manage protracted labor, post-partum hemorrhage and retained after birth. Ethno-pharmacological relevance of the study will be the provision of scientific evidence and justification for the ethnic use of both plants as oxytocic agents in the initiation of labor, treatment of prolonged labor, post-partum hemorrhage and retained placenta. MATERIALS AND METHODS: The plants were harvested in the wild, identified and voucher specimens preserved. The root bark was processed to powder form, from which aqueous and ethanol extracts were obtained. Each of the extracts was separately tested on isolated uterine muscle tissue from non-pregnant and pregnant rabbits. The effect on contraction frequency (number of contractions per second) in the absence or presence of oxytocin was evaluated statistically using ANOVA. P values <0.05 were considered significant. RESULTS AND CONCLUSIONS: All uteri exhibited a strong initial contraction following exposure to the aqueous and ethanol root bark extracts of both plants. After recovery, the resumed contraction frequencies varied with the plant extract and exogenous hormone. The results show that the extracts of both plants were able to stimulate uterine tissue contractility directly and to augment the tissue's response to oxytocin. The increase in uterine contractions as a percentage relative to negative controls was particularly significant in pregnant rabbit tissues in the presence of oxytocin, where increments of up to 245% were observed. Further pharmacological studies are however required to determine the active principles, possible mechanisms of action, efficacy and safety margins of the plant extracts.     

辣木种子提取物对小鼠实验性肝损伤的保护作用

目的考察辣木种子提取物对小鼠实验性肝损伤(急性酒精性肝损伤、四氯化碳致急性肝损伤)的保护作用。方法 RT-PCR、Western blotting分别检测小鼠肝组织ADH1和ALDH2 mRNA、蛋白表达。建立小鼠急性酒精性肝损伤模型,测定ALT、AST、ALP、LDH、GSH、MDA水平;建立小鼠四氯化碳致急性肝损伤模型,测定ALT、AST、GSH、MDA、T-SOD、GSH-Px、GR水平,RT-PCR检测C/EBPα、TNF-α、SREBP-1c、COX-2 mRNA表达,HE染色观察小鼠肝组织病理学变化。结果提取物(500 mg/kg)可提高ADH1 mRNA、蛋白表达,但对ALDH2无明显影响。对于急性酒精性肝损伤小鼠,各剂量提取物(125、250、500 mg/kg)降低ALT、AST、ALP、LDH、MDA水平,提高GSH水平;对于四氯化碳致急性肝损伤小鼠,各剂量提取物(32. 5、75、150 mg/kg)降低ALT、AST、MDA、GSHPx水平及COX-2、TNF-α、SREBP-1c mRNA表达,提高T-SOD、GSH、GR水平及C/EBPαmRNA表达,改善肝组织形态。结论辣木种子提取物对小鼠实验性肝损伤有明显保护作用,其机制可能与加快乙醇代谢、缓解炎症反应、抑制脂肪酸和胆固醇合成、改善脂质代谢紊乱有关。     

Sperm antimotility properties of a seed extract of Abrus precatorius

This study examined the inhibitory effects of a methanol extract of Abrus precatorius seeds on the motility of washed human spermatozoa. The extract caused a concentration-related impairment of percentage sperm motility; with the EC50 concentration being 2.29 mg/ml. This effect on motility was essentially irreversible. With the highest concentration tested (20.0 mg/ml), the onset of the antimotility action was almost immediate. In addition, this concentration impaired the functional integrity of the plasma membrane (hypoosmotic swelling test) and viability (nigrosin-eosin stain) of spermatozoa. In contrast, with a lower concentration (5.0 mg/ml), such effects were not evident. It is concluded that at the lower concentrations the antimotility action may result from a rise in intracellular calcium (not via influx) and/or a decline in cAMP content and/or enhanced generation of a reactive oxygen species.     

Phytochemical, Anti-oxidant, Larvicidal, and Antimicrobial Activities of Castor (Ricinus communis) Synthesized Silver Nanoparticles

Objective Castor possesses the medicinal properties. Hence, castor extract has the reducing power agent was used in nanoparticles synthesis. Extract of castor also produces secondary metabolites(phenolics, reducing agent) and exhibits anti-oxidant property, which was used as larvicide and antimicrobial agent. In the present study the silver nanoparticles(Ag NPs) were synthesized using aqueous leaf extract of castor. Methods The synthesized Ag NPs were characterized with UV-visible spectroscopy and transmission electron microscopy(TEM). The phenolics, reducing sugar and total sugar were evaluated performing Folin-Ciocalteu reagent method, DNS method and Phenol-sulphuric acid method. Anti-oxidant activity of synthesized nanoparticles was evaluated using DPPH assay. The larvicidal activity of synthesized Ag NPs was evaluated against the third instar of Anopheles stephensi and Aedes aegypti. The mortality was observed after 24 h by probit analysis. Further, the antimicrobial activity was reported against Staphylococcus aureus(Gram positive) and Pseudomonas aeruginosa(Gram negative). Results The UV spectra showed maximum absorbance at 445 nm and TEM analysis indicated spherical shape of nanoparticles with average size of 8.96 nm. The synthesized nanoparticles also possessed anti-oxidant potentials. Thus, it could be used as potential free radical scavenger. The larvae of A. stephensi were found more susceptible to Ag NPs than larvae of A. aegypti. Conclusion Due to the medicinal properties and reducing power activity, in the present study Ag NPs have been synthesized using the aqueous leaves extract of castor and access their phytochemical, anti-oxidant, larvicidal and antimicrobial properties.     

葡萄籽提取物的质量评价

概述了葡萄籽提取物常规品质的各项指标,着重阐述了国内外对葡萄籽提取物中各成分指标的概念及其相应的含量测定方法。     

Acute effects of Fraxinus excelsior L. seed extract on postprandial glycemia and insulin secretion on healthy volunteers

Aim of the study

Fraxinus excelsior L. (Family: Oleaceae) seeds are consumed as a food, condiment, and folk medicine. The seeds are traditionally used as a potent hypoglycemic agent, but no clinical evidence exists in as to this regard. We assessed the clinical efficacy and safety of the seed extract (FraxiPure™, Naturex), containing 6.8% of nuzhenide and 5.8% of GI3 (w/w), on plasma glucose and insulin levels against glucose (50 g) induced postprandial glycemia.

Materials and methods

Preselected dose (1.0 g) was used in a double blind, randomized, crossover, placebo (wheat bran) controlled study on 16 healthy volunteers. Each treatment was given immediately after a fasting blood glucose sample (0 min). Postprandial plasma glucose levels were estimated at 0, 15, 30, 45, 60, 90 and 120 min; and postprandial plasma insulin at 0, 30, 60, 90 and 120 min.

Results

The extract lowered the incremental postprandial plasma glucose concentration as compared to placebo at 45 min (P = 0.06) and 120 min (P = 0.07). It statistically (P = 0.02) reduced the glycemic area under the blood glucose curve. The seed, also, induced a significant (P = 0.002) secretion of insulin at 90 min after glucose administration. However, the insulinemic area under the blood insulin curve was not different than the placebo. No adverse events were reported.

Conclusions

Our findings confirm the hypoglycemic action of Fraxinus excelsior L. seed extract. These promising results, thus, encourage conducting long-term clinical studies to further evaluate the efficacy and safety of Fraxinus excelsior L. seed extract in healthy and diabetic volunteers and also to explore the possible mechanism(s) of action.     

Evaluation of estrogenic activity of alcoholic extract of rhizomes of Curculigo orchioides

The rhizomes of Curculigo orchioides Gaertn. (Amaryllidacea) is an important Ayurvedic as well as Unani drug. It is present in several drug formulations used in the treatment of menorrhagia and other gynecological problems. In this study, we conducted a comparative study of estrogenic activity of alcoholic extract of Curculigo orchioides with diethylstilbestrol in bilaterally ovariectomized young albino rats. Bilaterally ovariectomized albino rats were divided into five groups (n=9) receiving different treatments, consisting of vehicle (0.6% w/v sodium carboxy methyl cellulose), ethanolic extract of rhizomes of Curculigo orchioides at three different doses (viz., 300, 600, 1200 mg/kg body weight) and standard drug diethylstilbestrol (DES) at a dose of 2 mg/kg body weight. All these were administered orally daily for 7 days. Estrogenic activity was assessed by taking percentage vaginal cornification, uterine wet weight, uterine glycogen content and uterine histology as parameters of assessment. Alcoholic extract of Curculigo orchioides showed a significant increase in percentage vaginal cornification, uterine wet weight (P<0.001), uterine glycogen content (P<0.001) and a proliferative changes in uterine endometrium compared to the control.     

Antileukemic activity of Bidens pilosa L. var. minor (Blume) Sherff and Houttuynia cordata Thunb.

To evaluate the anti-leukemic activity of Bidens pilosa L. var. minor (Blume) Sherff and Houttuynia cordata Thunb., cytotoxicity tests with an XTT-based colorimetric assay were used. Five leukemic cell lines, namely L1210, U937, K562, Raji and P3HR1, were cultured with hot water extracts of B. pilosa var. minor or H. cordata. Hot water extracts of B. pilosa var. minor inhibited these five leukemic cells with IC50s between 145 microg/ml and 586 microg/ml. The effect was greatest on four cell lines, namely L1210, P3MR1, Raji and K562, with IC50s below 200 microg/ml and a selective index of more than 5. Hot water extract of H. cordata inhibited these five leukemic cells with IC50s between 478 microg/ml and 662 microg/ml. The selective index was between 1.5 and 2.1. B. pilosa var. minor was more effective than H. cordata in inhibiting most of the leukemic cells in our study. We suggest that B. pilosa L. var. minor (Blume) Sherff may prove to be a useful medicinal plant for treating leukemia.     

Antinociceptive,antiinflammatory and acute toxicity effects of Salvia leriifolia Benth seed extract in mice and rats

The antinociceptive and antiinflammatory effects as well as the acute toxicity of Salvia leriifolia aqueous seed extract were studied in mice and rats. Antinociceptive activity was assessed using the hot-plate and tail flick tests. The effect on acute inflammation was studied using vascular permeability increased by acetic acid and xylene-induced ear oedema in mice. The activity against chronic inflammation was assessed using the cotton pellet test in rats. The LD(50) of the extract was found to be 19.5 g/kg (i.p.) in mice. The aqueous seed extract showed significant and dose-dependent (1.25-10 g/kg) antinociceptive activity over 7 h, and was inhibited by naloxone pretreatment. Significant and dose-dependent (2.5-10 g/kg) activity was observed against acute inflammation induced by acetic acid and in the xylene ear oedema test. In the chronic inflammation test the extract (2.5-5 g/kg) showed significant and dose-dependent antiinflammatory activity. The aqueous seed extract of S. leriifolia may therefore have supraspinal antinociceptive effects which may be mediated by opioid receptors, and showed considerable effects against acute and chronic inflammation.