The aim of hormonal male contraception is to prevent unintended pregnancies by suppressing spermatogenesis. Hormonal male contraception is based on the principle that exogenous administration of androgens and other hormones such as progestins suppress circulating gonadotropin concentrations, decreasing testicular Leydig cell and Sertoli cell activity and spermatogenesis. In order to achieve more complete suppression of circulating gonadotropins and spermatogenesis, a progestin has been added testosterone to the most recent efficacy trials of hormonal male contraceptives. This review focusses on the potential effects of male hormonal contraceptives on cardiovascular risk factors, lipids and body composition, mainly in the target group of younger to middle-aged men. Present data suggest that hormonal male contraception can be reasonably regarded as safe in terms of cardiovascular risk. However, as all trials have been relatively short (< 3 years), a final statement regarding the cardiovascular safety of hormonal male contraception, especially in long-term use, cannot be made. Older men with at high risk of cardiovascular event might not be good candidates for hormonal male contraception. The potential adverse effects of hormonal contraceptives on cardiovascular risk appear to depend greatly on the choice of the progestin in regimens for hormonal male contraceptives. In the development of prospective hormonal male contraception, data on longer-term cardiovascular safety will be essential.
Age Factors ; Androgens/therapeutic use* ; Antispermatogenic Agents ; Cardiovascular Diseases/epidemiology* ; Contraceptive Agents, Male/therapeutic use* ; Gonadotropins/metabolism* ; Humans ; Male ; Progestins/therapeutic use* ; Testosterone/therapeutic use*

Rhynchosia volubilis Lour has been a major drug in a folk prescription for contraception in China, whereas its mechanism remains unknown. Its antifertility effects on male mice and antimicrobial activities on sexually transmitted infection (STI) pathogens were previously reported. This study was undertaken to develop the n-Butanol extract of Rhynchosia volubilis Lour (BERVL) as a spermicidal agent with STI prevention. The spermicidal activities of BERVL with different doses were assessed using selected high-motile sperms of normal human semen samples, and their inhibitory effects on Lactobacillus acidophilus were determined. The mechanism of the spermicidal activity was explored by aqueous Eosin Y and Hoechst 33342/PI staining. The results showed spermicidal activities and inhibitory effects of BERVL on Lactobacillus acidophilus were dose-dependent. Dose of 90 mg/mL BERVL terminated all progressive sperm motility within 2 min, and had slight inhibitory effect on Lactobacillus acidophilus, suggesting it was an effective and safe dose for contraception use. About 80% sperms exposed to BERVL displayed changes consistent with high permeability of head membrane. It is concluded that BERVL as spermicide has advantages over N-9 with strong ability to instantaneously kill human sperm and possesses light inhibitory effect on Lactobacillus acidophilus.
1-Butanol ; chemistry ; Adult ; Dose-Response Relationship, Drug ; Fabaceae ; chemistry ; Humans ; Lactobacillus acidophilus ; drug effects ; growth & development ; Male ; Plant Extracts ; chemistry ; pharmacology ; Sperm Motility ; drug effects ; Spermatocidal Agents ; chemistry ; pharmacology ; Spermatozoa ; drug effects ; physiology ; Young Adult

OBJECTIVETo explore the antispermatogenic and testicular antisteroidogenic activities of Feronia limonia fruit pulp southern India.

METHODSFourty Wistar male albino rats (Rattus norvegicus) were equally divided into four groups. Experimental groups were administered with the ethanolic extract of Feronia limonia (F. limoni) fruit pulp at doses of 250 and 500 mg/kg body weight once daily for 55 days. All treated rats had corresponding recovery groups. At the end of each treatment periods, various spermatological indices, tissue biochemicals and testicular enzymes levels were analysed. Blood profiles were also estimated.

RESULTSCompared with the control, the F. limonia fruit pulp at both dose levels did not decrease body weight, which were associated with decline in epididymal sperm count, motility, viability and increased percent of abnormal sperm. Further, F. limonia fruit pulp at 500 mg/kg body weight markedly reduced the epididymal and testicular protein content by 24.58% and 29.86%, respectively, as well as the glucose-6-phosphate dehydrogenase and Δ(5)-3β-hydroxy steroid dehydrogenase) levels by 42.82% and 38.08%, respectively, while a significant elevation was observed in testicular cholesterol and ascorbic acid content. A gradual recovery of all parameters was observed after 55 days of treatment withdrawal. No significant alterations in haematological indices were observed.

CONCLUSIONSThe present findings indicate that F. limonia fruit pulp may have reversible antispermatogenic and antisteroidogenic properties, and could partially support the traditional use as male contraceptive.

Administration, Oral ; Animals ; Antispermatogenic Agents ; administration & dosage ; chemistry ; pharmacology ; Ascorbic Acid ; chemistry ; Cell Survival ; drug effects ; Cholesterol ; chemistry ; Female ; Fruit ; chemistry ; Lethal Dose 50 ; Male ; Plant Extracts ; administration & dosage ; chemistry ; pharmacology ; Rats ; Sperm Count ; Sperm Motility ; drug effects ; Spermatozoa ; drug effects ; Testis ; drug effects ; metabolism ; Toxicity Tests, Acute ; Tracheophyta ; chemistry

OBJECTIVETo observe the spermicidal effect of alcohol extracts from different ratios of Sophora flavescens Ait/Chinese Bulbul in vitro.

METHODSSemen samples aseptically obtained by masturbation and prepared by density gradient centrifugation from 15 healthy men were incubated in the alcohol extracts from 9 different ratios of Sophora flavescens Ait/Chinese Bulbul for 20 seconds, 2 minutes and 4 minutes. Then the motility and movement parameters of the sperm were detected by computer-assisted semen analysis, and the minimal effective concentrations of the instant spermicidal effect of the extracts were determined.

RESULTSAt the ratio of 3:1, the extract at 0.5 mg/ml significantly inhibited the sperm motility and other sperm movement parameters VCL, VSL, VAP, ALH, WOB and MAD, as compared with the control group. The minimal effective concentration of the instant spermicidal effect of the extracts was 3.5 mg/ml at 3:1.

CONCLUSIONThe alcohol extracts from Sophora flavescens Ait and Chinese Bulbul at the ratio of 3:1 have the best spermicidal effect in vitro.

Adult ; Humans ; Male ; Plant Extracts ; pharmacology ; Pulsatilla ; Semen Analysis ; Sophora ; Sperm Motility ; drug effects ; Spermatocidal Agents ; pharmacology ; Spermatozoa ; drug effects ; Young Adult

OBJECTIVETo study the anti-fertility effect of maximum-dose Tongbi Composition and its reversibility in male rats.

METHODSThirty-six male SD rats were equally randomized into a control group and a medication group, the former given normal saline at 10 ml/(kg x d), while the latter treated with Tongbi Composition at 10 g/(kg x d), both for 60 days. Half the rats of each group were sacrificed randomly at the cessation of treatment, and the rest killed at 72 days after it. The relative testis weight, testis volume, sperm concentration and sperm motility were measured, and the pathological changes in the testicular tissue observed under the optical microscope.

RESULTSAfter 60 days of treatment, no statistically significant differences were found between the two groups in the relative testis weight, testis volume and sperm concentration (P > 0.05) , and the sperm motility of the medication group dropped to zero, but it was restored to normal at 72 days after drug withdrawal. Almost no lesions were observed in the testis tissue of the medication group.

CONCLUSIONThe short-term use of Tongbi Composition at the maximum clinical dose has an obvious anti-fertility effect, but it is reversible.

Animals ; Antispermatogenic Agents ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Male ; Rats ; Rats, Sprague-Dawley ; Sperm Motility ; Sterilization Reversal ; Testis ; drug effects

AIMTo investigate the effect of Morinda lucida Benth (Rubiaceae) on the reproductive activity of male albino rats.

METHODSTwo groups of rats were treated with 400 mg/(kg .d) of Morinda lucida leaf extract for 4 and 13 weeks, respectively. The control rats received the vehicle. All the treated rats had corresponding recovery groups. At the end of each experimental period, animals were killed and organ weights, sperm characteristics, serum testosterone levels, histology of the testes and fertility were assessed.

RESULTSMorinda lucida leaf extract did not cause any changes in body and somatic organ weights, but significantly increased the testis weight (P 0.05). The sperm motility and viability, and the epididymal sperm counts of rats treated for 13 weeks were significantly reduced (P 0.05). Sperm morphological abnormalities and serum testosterone levels were significantly increased (P 0.05). There were various degrees of damage to the seminiferous tubules. The extract reduced the fertility of the treated rats by reducing the litter size. Reversal of these changes, however, occurred after a period of time.

CONCLUSIONThe extract of Morinda lucida has reversible antispermatogenic properties.

Animals ; Antispermatogenic Agents ; pharmacology ; Body Weight ; drug effects ; Epididymis ; cytology ; drug effects ; Fertility ; drug effects ; Litter Size ; drug effects ; Male ; Morinda ; Organ Size ; drug effects ; Plant Extracts ; pharmacology ; Plant Leaves ; chemistry ; Rats ; Rats, Wistar ; Sperm Count ; Sperm Motility ; drug effects ; Testosterone ; blood

To further understand triptolide, this paper has introduced the pharmacology, pharmacokinetics, toxicity, the clinic application and semi-synthesis of triptolide on basis of importance and significant contents of reference which have been consulted in the past twenty years. Presently triptolide and Tripterygium wilfordii have been a hot spot of modernization of Chinese traditional medicine. It is very important to develop a new dosage form of high effect and low toxicity by making use of advanced technology according to its characteristics.
Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Antineoplastic Agents, Alkylating ; pharmacology ; Antispermatogenic Agents ; pharmacology ; Diterpenes ; chemical synthesis ; isolation & purification ; pharmacology ; toxicity ; Epoxy Compounds ; Humans ; Immunosuppressive Agents ; pharmacology ; Phenanthrenes ; isolation & purification ; pharmacology ; toxicity ; Tripterygium ; chemistry

Spermicidal effect of Jieze No. 1 (JZ1) in combination with nonoxynol-9 (N-9) was examined in vitro. The minimum spermicidal concentration of JZ1 decoction, N-9 and their mixture solution in 20 s and 3 min were examined by improved spermicidal test of Sander-cramer in vitro. The percentages of progressively moving spermatozoa, moving spermatozoa and viable spermatozoa were also observed 20 s, 3 min and 30 min after the addition of the liquid medicine. Our results showed that sperms did not recover their activities in a revival test when the minimum spermicidal concentration of either JZ1 decoction, or N-9, or the mixed solution of the two agents, was used. N-9 (JZ1 in the mixed group) showed significant differences in the percentages of progressively moving spermatozoa, moving spermatozoa, and visible spermatozoa in 20 s, 3 min, and 30 min, when compared with N-9 alone (P < 0.01). We are led to conclude that JZ1 decoction can improve N-9 spermicidal action in vitro, and when used in combination with N-9, it has synergic effect.
Drugs, Chinese Herbal/*pharmacology ; Nonoxynol/*pharmacology ; Semen/drug effects ; Spermatocidal Agents/*pharmacology ; Spermatozoa/*drug effects

OBJECTIVETo study the effect of tea saponin in ameliorating nonoxynol(N-9) spermicidal action in vitro.

METHODSAccording to the improved spermicidal test method in vitro recommended by International Planned Parenthood Foundation (IPPF), we evaluated the minimum spermicidal concentration of N-9, tea saponin and their mixed solution in 20 s and 3 min.

RESULTSThe minimum spermicidal concentration of N-9 in the mixed solution was (0.13 +/- 0.05) g/L in 20 s and (0.05 +/- 0.004) g/L in 3 min, and that of the tea saponin in the mixed solution was (2.40 +/- 1.07) g/L in 20 s and (1.27 +/- 0.38) g/L in 3 min, compared with the single ingredient N-9 [(0.48 +/- 0.15) g/L in 20 s, (0.34 +/- 0.079 g/L in 3 min], and tea saponin [(5.78 +/- 1.40) g/L in 20 s, (1.71 +/- 0.176) g/L in 3 min], P < 0.01.

CONCLUSIONTea saponin can improve N-9 spermicidal action in vitro, and tea saponin and nonoxynol have proved of synergic effect.

Animals ; Drug Synergism ; Male ; Nonoxynol ; pharmacology ; Rabbits ; Saponins ; pharmacology ; Spermatocidal Agents ; pharmacology ; Tea

OBJECTIVESTo test in vitro the spermatozocidine drug which can also prevent sex transmitting diseases (STD) pathogens.

METHODSChlorheridine diacetate and other three chemical compounds were applied in vitro spermatozocidine and sperm inhibitting tests.

RESULTSThe lowest concentrations of chlorheridine diacetate and p-nitrophenol which can inhibit human sperm in 20 seconds were 1.25 mg/ml. The minimal inhibitory concentration and minimal bactericidal concentration of chlorheridine diacetate and p-nitrophenol on Streptococcus albus Stemberg were 0.125 to 0.50 mg/ml and 0.25 to 1.00 mg/ml.

CONCLUSIONSChlorheridine diacetate and p-uitrophenol have strong spermatozocidine and antibacteria effects.

Acetates ; pharmacology ; therapeutic use ; Anti-Bacterial Agents ; pharmacology ; therapeutic use ; Humans ; Male ; Microbial Sensitivity Tests ; Neisseria gonorrhoeae ; drug effects ; Nitrophenols ; pharmacology ; therapeutic use ; Sexually Transmitted Diseases ; prevention & control ; Spermatocidal Agents ; pharmacology ; therapeutic use ; Spermatozoa ; drug effects ; Streptococcus ; drug effects