Spermicidal Activity Research Articles

Investigation of the spermicidal action of quinine and emetine

Investigation of the spermicidal action of quinine and emetine

Spermicidal potential of saponins isolated from Indian medicinal plants

Saponins isolated from sixteen Indian plants showed spermicidal activity in human semen in both the Spot and IPPF tests. Spermicidal activity was found to be associated with the β-amyrin C-28 carboxylic acid type of sapogenins linked to a particular sequence of sugar moieties.

Investigations on spermicidal activity in the sheep vagina

This study was conducted to elucidate some of the effects of a synthetic progestagen and natural ovarian hormones on spermicidal activity in the sheep vagina. In the first experiment, parous ewes were treated for 17 days either intravaginally with medroxyprogesterone acetate (MAP) or subcutaneously with progesterone. They were inseminated artificially either on the last day of progestagen treatment or during estrus after progestagen withdrawal. Their vulvovaginal junctions were ligated to prevent the loss of sperm cells by drainage to the exterior. Untreated control ewes were inseminated during either estrus or the luteal phase of the estrous cycle. The ewes were killed 22 hr. after insemination, their vaginas flushed, and intact sperm cells and tailless sperm heads counted. In the second and third experiments, some of the ewes were bilaterally ovariectomized and inseminated several weeks later. Other ewes were ovariectomized and given subcutaneous injections of estradiol, progesterone, or both hormones. In the first experiment, most sperm cells were recovered intact from estrous or luteal phase control ewes. The intravaginal administration of MAP increased both the breakage of sperm cells into heads and tails and the disappearance of sperm cells. The spermicidal effects of MAP were just as great in ewes inseminated on the last day of treatment. as in those inseminated during the ensuing estrus; these results indicated that the peak estrogen secretion that occurs near the beginning of estrus was not necessary for the intensification of spermicidal activity. In the second experiment, ovariectomized ewes were compared to estrous and luteal phase ewes in regard to vaginal spermicidal activity. Sperm breakage and disappearance occurred least in estrous ewes, to a somewhat greater degree in luteal phase ewes, and to the greatest extent in ovariectomized ewes. The results suggested that endogenous ovarian hormones, particularly those in estrous ewes, suppress spermicidal mechanisms in the vagina. In the third experiment, the administration of estradiol and progesterone to ovariectomized ewes prevented the increase in sperm cell disappearance. Neither hormone alone prevented the increase.

The biological actions of endouterine copper

Biological activity of copper has been studied extensively over the last few years following Zipper's observations attributing an antifertility effect to copper when placed within the uterine cavity of rats and hamsters. The antifertility effect appears to be mediated at a local rather than a systemic level and present evidence points to changes in the endometrium resulting in disruption of implantation. The spermicidal action of copper cannot be discounted as contributing to the antifertility effect at the present time. However, it would appear that copper exerts no significant effects on ovulation, fertilisation, tubal motility or embryogenesis.

Spermicidal actions of extracts and compounds from [formula omitted

The crude saponins from three plants, four purified saponins, and two synthetic derivatives were tested for spermicidal activity by means of an in vitro incubation procedure. The crude saponins and two purified saponins derived from Phytolacca dodecandra were found to have potent spermicidal activity. The most active compound tested against human sperm was lemmatoxin, a trisaccharide of oleanolic acid. Based on ED 50 values obtained in our test system, the crude saponin preparation from P. dodecandra and lemmatoxin possessed nearly three times the spermicidal activities of a synthetic detergent currently used as a spermicidal agent. Biological activity could not be accounted for on the basis of surface activity.

Effects of a copper intrauterine contraceptive device on embryo survival, uterine spermicidal activity, and endometrial vascular porosity in the ewe

Pregnancy was maintained in 5 of 29 ewes into which a copper intrauterine contraceptive device (IUD) was inserted at 3, 7, or 22 days after mating. The results indicated that an embryo could survive in utero with its membranes in direct contact with copper. The presence of an IUD markedly increased spermicidal action in the uterine lumen, but a copper IUD did not stimulate spermicidal activity to a greater degree than did a stainless steel or plastic IUD. A plastic or stainless steel IUD intensified endometrial vascular porosity, but only in tissue in contact with the IUD. A copper IUD increased vascular porosity locally to a greater degree than did the others, and increased vascular porosity in the non-IUD uterine horn as well.

Route of progestagen administration to the ewe and spermicidal action in the vagina at the ensuing estrus.

Route of progestagen administration to the ewe and spermicidal action in the vagina at the ensuing estrus.

Some Effects of Intrauterine Devices on Reproductive Function in the Ewe

This presentation is limited to the antifertility effect of the IUD in ewes and to some of the changes in uterine function caused by its presence. Some of these changes may occur only in sheep. A custom-made plastic spiral, 5 cm long and 5-8 mm outside diameter, was inserted into the lumen of only 1 uterine horn. Ovum fertility occurred normally in control ewes but the fertility rate of IUD-wearing ewes was very low, as determined by ovum cleavage at 3 days after breeding. None of the 17 ova was cleaved when ovulation occurred on the spiral side and only 1 in 10 was cleaved when ovulation occurred opposite the spiral. Accessory sperm were not found in the zona pellucidae of any ovum in IUD-carrying ewes while in controls accessory sperm ranged from 10 to over 60. These findings indicate the IUD did more than interfere physically with the passage of sperm up the reproductive tract. The ova was found not defective nor was ovulation interfered with. Myometrial tissue removed and tested in vitro showed adequate contractility. However an altered motility pattern in test animals was shown by in vivo observations of exteriorized uteri. This might partly account for the absence of sperm from the oviducts. Sperm cells placed into the uterine horns were found to be broken into heads and tails or to have disappeared after 5 hours. This effect was markedly greater in horns containing the IUD. Some sperm cells were observed being phagocytized by leukocytes. Spermicidal activity in excised and washed uterine horns could be observed as early as 1 hour after semen injection. This activity was largely stopped when total uteri were excised. Phagocytosis of sperm cells was increased when an inflammatory reaction was producted by bacterial inoculation. Iv dye injections showed resulting dye concentrations directly beneath the turns of the spiral (p less than .01), which was considered to indicate the degree of leakage from the endometrial vascular system. Other experiments showed an IUD intensifies bacterial capabilities of the uterus by increasing the inflammatory response to the presence of foreign substances, whether semen or bacteria. It was concluded that as IUD in the sheep uterus inhibits sperm transport and ovum fertilization, perhaps by changing the nature of uterine motility.

On the mechanism of sperm immobilization induced by normal sera and anti-semen sera

Experimental evidence indicates that the primary cause of the immobilization of bull spermatozoa induced by normal rabbit sera (NS) and rabbit antisera against bull semen (ABS) is a membrane change effected by the action on the cells of antibodies and complement. Owing to this change, which initiates a transient swelling of the sperms, presumably of a colloid osmotic nature, the sperms become permeable to ATP, albumin and generally also to Ficoll. The functional integrity of the sperm motor apparatus is, however, not destroyed: the flagellation of serumimmobilized sperms is restored by the addition of ATP to the medium. This ATP-reactivated flagellation is not confined to a physiological milieu: for short periods of time it may continue, in spite of a greatly reduced ionic strength. The agglutination patterns of the sperms which developed in the sera were of the same type as those observed by earlier investigators. Thus, in NS there was a predominant head-to-head agglutination, whereas in ABS both head-to-head and tail-to-tail agglutination were observed with no real preference for either type. NS and ABS induced no haemolysis of bovine erythrocytes. This indicates that no overlapping serological reaction occurs between bull spermatozoa and bovine erythrocytes. On the other hand, both kinds of sera were haemolytic against sheep erythrocytes. This haemolytic activity was abolished by a previous absorption of the sera at 0 °C with a preparation of horse kidney, which specifically binds Forssman antibodies. However, the absorbed sera were spermicidal. This indicates that the haemolysins were of the Forssman-antibody type, but that they were not identical with the sperm lysins. The haemolytic activity was greatlv reduced after absorption of the sera with epididymal bull spermatozoa pretreated with bull seminal plasma. On the other hand, absorptions with epididymal spermatozoa per se had no significant influence on the haemolytic activity. The meaning of these findings is discussed. Rabbit erythrocytes, like bovine erythrocytes, were unaffected by NS and ABS. However, they were rendered susceptible to haemolysis in both NS and ABS by previous treatment with bull seminal plasma, but not by treatment with extract from epididymal bull spermatozoa or with hyaluronidase. This suggests that the seminal plasma factor, which, by coating, sensitized the cells to subsequent complement haemolysis in NS and ABS, was a true constituent of the seminal plasma, and not present in this liquid due to leakage from the sperms. The spermicidal and haemolytic activities were extended into higher serum dilutions in the presence of agglutinin- and lysin-free guinea-pig serum. This indicates that the limiting factor in the lytic strength of NS and ABS per se was the complement concentration rather than the lysin concentration. Dextran sulphate ( M ̄ w ~ 2 × 10 6 ) in concentrations of 10 −5 to 10 −7 M blocked the spermiolytic and haemolytic activities of the sera. This fact seems to reflect the binding of the actual antibodies by the negatively charged polysaccharide.

Toxicology and spermicidal activity of a new contraceptive cream containing chlorindanol and laureth 9

Lanettes® is a new contraceptive aerosol cream formulation containing two spermicidal ingredients: 7-chloro-4-indanol, and laureth 9, a polyoxyethylene lauryl ether. The aerosol cream was tested by three recognized spermicidal test procedures and was found to be a highly spermicidal preparation. Spermatozoa were immobilized in less than 20 seconds even after a 100-fold dilution. This preparation is a nongreasy, nonsoapy, nonstaining preparation and has moniliastatic and trichomonacidal properties. The individual dose units are so designed that the entire contents of the glass vial can be deposited in the vaginal vault. Expansion occurs in the vagina rather than in the dispenser, and the foam coats the vaginal walls and the streaming mucus and blocks a normally positioned cervical os. The aerosol cream was nonirritating to vaginal and cervical mucosae of beagle dogs when deposited 79 times in 183 days and it failed to adversely affect the animals in any way. Thirteen male volunteers repeatedly applied liberal amounts of the aerosol cream to penile surfaces for 8 hours or longer, four times a week for 2 weeks, and observed no ill effects. A challenge application 2 weeks later failed to elicit sensitization.

Spermicidal activity of bacterial endotoxin.

THE endotoxins of Gram-negative bacteria are a group of macromolecular lipopolysaccharide complexes which, on administration to experimental animals, produce a wide variety of physiological and pathological alterations1,2. Despite the similarity of some of the pathological findings in these varied reactions neither a common factor nor a basic mechanism responsible for the pathogenesis of these reactions has been established, and there is evidence that significant underlying physiological differences exist in some of these phenomena.

Spermicidal activity of surface-active agents.

Summary. The spermicidal activities against human spermatozoa of a range of non-ionic, anionic and cationic surface-active agents have been determined with the method of Baker, Ransom & Tynen (1937). Although it has been concluded that surface-tension-lowering properties do not directly influence spermicidal power, the surfacetension/concentration curves of a number of the compounds were studied. Solubilities in water, hexane, and ethyl oleate were also determined in an attempt to find out whether there was any relationship between spermicidal action and solubilities in these solvents. The results obtained on the compounds studied showed broadly that appreciable oil solubility and good surface-tension-lowering properties were desirable for spermicidal activity in non-ionic and anionic surface-active agents. The cationic compounds studied were active in spite of low fat solubility. The lack of precision of the spermicidal results made definite activity/ solubility or activity/surface-tension relationships difficult to formulate.

A NEW METHOD OF COMPARISON OF SPERMICIDAL ACTIVITIES

Summary. A new method of comparison of spermicidal activities of compounds is presented. The method depends on the fact that spermatozoa, when suspended in a sub-lethal concentration of a spermicidal compound, show a reduction in speed of movement. This speed when expressed as a percentage of the speed of the untreated spermatozoa varies with the concentration of spermicidal compound; comparisons of spermicidal activity are made by including a standard material in each test series. The spermicidal activities of a number of substances were compared and the protective effect of seminal plasma on spermatozoa was demonstrated quantitatively.

Evaluation of a New Contraceptive

A series of tests were performed to measure the spermicidal efficacy harmlessness and acceptability of Emko Vaginal Foam. The manufacturer describes the foam as an oil-in-water dispersion which is combined under pressure with a liquefied gas propellant so that the liquid dispersion can be expelled as a foam into a vaginal applicator. Laboratory tests were made first. Then clinical tests were made to assess the acceptability of the foam. These consisted of single-dose tests in 8 women and 21-day tests during which 12 women used a daily dose for 21 days. None showed any subjective or objective evidence of local discomfort or irritation. 32 postcoital test were performed after use of the foam in 22 selected couples of reproductive age all of whom had had previous excellent postcoital test results and good semen analyses. Except in 5 cases when the time interval was 8-11 hours the postcoital test were made within 4 1/2 hours after coitus. In 29 tests no motile spermatozoa were found in either vaginal or endocervical specimens. In 3 tests 1-3 sperm feebly motile and without forward motion were seen in the endocervical mucus after a search of more than 40 dry high-power fields. The foam appears to possess a high degree of spermicidal activity in vivo.(AUTHORS MODIFIED)

Screening of Organic Compounds for Spermicidal Activity

581 organic compounds were studied for their spermicidal activity by a modified Brown and Gamble method. Of 55 compounds that were considered highly effective in aqueous solutions of .5% or less 31 were surfactant substances. A new class of polyhydric phenols bismonohydroxy and bisdihydroxyphenyl derivatives of methane were discovered to have strong spermicidal activity. Low molecular weight sodium dialkyldithiocarbamates had the highest spermicidal activity of any material studied. Alkylxanthate salts were effective at .5% concentrations. 9 Class I spermicides were found in alkylphenoxypolyoxyethylene ethanols. Certain alykl derivatives of diphenyliodonium also showed strong spermicidal activity. Several of the materials notably the alkylthiopolyoxyethylene ethylene ethanols have not been previously reported as spermicides.

The spermicidal activity of hydrogen peroxide in vitro and in vivo.

SUMMARY The effect of hydrogen peroxide on the motility of bull, fowl, dog, ram, mouse, rabbit and human spermatozoa has been studied in vitro. Although 3 p.p.m. peroxide had a small but significant action on bull and fowl spermatozoa, those of the other species were more resistant, and 30–300 p.p.m. was usually required to produce substantial spermicidal effects, and even 3000 p.p.m. failed to immobilize rabbit spermatozoa completely. Ram, dog and rabbit spermatozoa were rendered more susceptible by washing, and the seminal plasma was found to decompose hydrogen peroxide. The agent, in rabbit seminal plasma at least, is probably catalase. Hydrogen peroxide given orally to mice and rabbits did not affect either the spermatozoa or fertility.

The Effect of Lactic Acid on the Functional Capacity of Turkey Semen in Vivo

The competitive ability of sperm from an initial turkey male in a mating with that of a replacing sire has been evaluated by Kosin and Wakely (1950) and Harper and Parker (1952). The results of these investigators indicate that the technique of shifting sires in single-male-matings is somewhat more limited with turkeys than with chickens. Spermicidal action on turkey semen in vivo should accommodate the possibility of obtaining more than one sire group of progeny from a given group of females.Iwanow (1924) found that female chickens laid fertile eggs after a spermicidal solution had been flushed through the oviduct. Baker (1931) reported that 06% lactic acid had definite spermicidal effects on guinea pig sperm in vitro.For the purpose of investigating the role of a spermicidal agent in inhibiting the persistency of fertility from the initial male or males of a mating in which the sire or sires have …

Ergothioneine in the equine ampullar secretion.

A STRIKING feature of semen and of the reproductive organs in mammals is the diversity in chemical composition and secretory function encountered among different species1. Recent studies on the occurrence of ergothioneine provide a good example of this behaviour. This sulphur-containing nitrogenous base, which has been isolated in a crystalline state from the boar vesicular secretion2 and which has been shown to be capable of protecting spermatozoa against the spermicidal action of sulphydryl-binding substances3, is present in large quantities in the semen of the boar but not in the semen of man, bull, ram or rabbit.

A critical study of methods of measuring spermicidal action.

A critical study of methods of measuring spermicidal action is prese nted. 4 of the methods were compared with several commercial preparatio ns. The preparations are all equal according to the 30-minute standard described in the New and Non-Official Remedies. Only 1 jelly has a rating time of 2nd best by the 5 minute criterion of the Brown and Gamble test (actual time 30 minutes). By the Sander-Cramer method only 2 are of equal potency while the others assume relative ranks. A further separation is seen with the zone and saturation tests which measure spermicidal and vehicle properties. Therefore it is possible to determine whether superior preparations are superior in all properties. In this laboratory the effect of pure spermicides are tested by the Sander-Cramer test while the finished preparations are examined not only by that test and the Brown-Gamble but also by saturation and zone tests.

The spermicidal activity of quinones and quinols

The spermicidal activity of quinones and quinols