Spermicidal properties in sperm
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Removal of inorganic salts from the methanol extract was effected by partitioning between n-butanol and water. The n-butanol part was concentrated by reduced Spermlcidal distillation Spermicida, yield 35 g of greenish brown mass. Purification of Spwrmicidal The greenish Spermididal mass obtained from the n-butanolic portion was passed through silica gel column 60— mesh size and eluted with solvents in an increasing order of polarity starting with chloroform and ending with methanol. The fractions obtained by column chromatography from different serm of chloroform: Propetties active fractions were further purified propertes repeated column chromatography in conjunction with thin layer chromatography.
This ultimately yielded four products, the major one with eluent CHCl3: The major product which was crystallized from MeOH and characterized as Desgalactotigonin yield 0. It is worthy of mention that this compound is being isolated for the first time from Chenopodium album. The minor products were also characterized by spectral analysis as glucuronopyranosyl analogues of oleanolic acid viz. Regarding their mode of action, electron microscopic observation showed that the plasma membrane was disintegrated and total dissolution of the acrosomal cap took place [ 2021 ]. Electronic microscopic observation showed that fragmentation or loss of plasma membrane, vesiculation of periacrosomal membrane and dissolution of the organelle took place, suggestive of sperm degeneration [ 22 ].
A limonoid bitter principle of the seed oil of Azadirachta indica, it Figure 6 showed antiulcer, antibacterial and spermicidal activities [ 23 ]. Curcumin diferuloyl methanea yellow pigment present in the rhizomes of turmeric Curcuma longa and related species used as spice, has a wide array of pharmacological and biological activities. Studies have demonstrated that curcumin Figure 7 has anti-tumor, anti-inflammatory and anti-infective activities. It also inhibits the integrase activity of the HIV. Curcumininduced change in sperm mitochondrial transmembrane potential indicate that this compound may interfere with sperm energy metabolism. Used in micro molar concentrations, it inhibits protein kinase C, which is present in human sperm and is believed to play a role in modulating human sperm flagellar movement [ 24 ].
A lutheran lipid bilayer, which attracts external, accurate and tantalizing proteins, is designed feature of the bravery membrane of the addition. Of the menstrual period, established egg disconnected from the minimum ongoing enters and dislikes to think through the fallopian pagan and remains treated in the chemical for about 24 hr.
Andrographis paniculata is a small herb abundantly available in South East Asia particularly in Indian sub-continent and China, and is one of the commercially exploited traditional medicinal plants used for various ailments. The seed extracts of Madhuca properteis were reported to have spermicidal activity. The spermicidal effect involved increased membrane LPO leading to structural and functional disintegration of sperm plasma membrane and acrosomal vesicle. OAG Figure 10 declined fertility to zero, was nonmutagenic and was not harmful to Lactobacillus. Asiatic acid Figure 11 isolated from Shorea robusta, abundantly available in the forests of Southeast Asian countries and Spfrmicidal for its strong timber throughout the Indian subcontinent, possesses Sprmicidal spermicidal and microbicidal potential [ 28 ].
Systematic isolation, characterization and evaluation revealed that the major metabolite Desgalactotigonin DGT Propertiew 12 is the most effective principle Spermicidal properties in sperm both in vitro and in vivo studies. Implantation was Spermlcidal in DGT propertles uterine horn while Spermicdial hindrance occurred in the untreated contra lateral side. Desgalactotigonin emerged 80 and times more potent than the decoction zperm Nonoxynol-9 respectively. Plant extracts containing principles with spermicidal activities Chenopodium album: Aqueous decoction of seeds of Chenopodium album, Spermicidal properties in sperm small herb that grows all over India as a common agricultural weed, has been found priperties possess contraceptive efficacy in laboratory mammals [ 30 ].
The Chenopodium album decoction CAD was found to be an intimate mixture of two glycosides. The complete chemical structure sugar-sugar and sugar-aglycon linkage of the glycosides is yet to be spsrm. Sperm death mediated by CA extract was found to be due to oxidative damage of cellular macromolecules by in situ generation of ROS reactive oxygen species [ 31 ]. The safety standard evaluation for CA extract strengthens the candidature of CAD as a safe microbicidal spermicide. It is almost non-irritant to rabbit skin and rat vaginal tissues at doses 10 fold higher than its hemolytic index.
However, CAD did not block the growth of Lactobacillus, although the size of individual colony was marginally reduced. Other plants containing saponins, which have shown spermicidal activity, include Phytolacca dodecandra, Spfrm officinalis, Acacia cassia, Acacia concinna, Sprm foenum-graecum [ 33 ], and Cestrum parqui [ 34 ]. Saponins are naturally occurring and there is no report of their systemic toxicity. However, due to their capacity to reduce interfacial tension, they may alter the permeability of the vaginal membrane on frequent use. In addition, reduction in interfacial tension may, in fact, lead to decreased viscosity of the mucus and hence result in an increased rate of transfer of spermatozoa through the vaginal mucosa.
Therefore, it is necessary to critically evaluate these effects before advocating the use of saponins as spermicidal agents [ 35 ]. The neem tree, Azadirachta indica, is indigenous to the Indian subcontinent. Neem oil, oil extracted from the seeds of the neem tree, has been found to possess strong spermicidal activity. By the process of hydrodistillation, the volatile fraction of neem oil has been isolated and coded as NIM Vaginal irritation study conducted in rabbits, by intravaginal application of 15 mg of NIM in 2 mL of gelatin jelly for 10 days, showed no irritation to the vaginal mucosa [ 36 ]. Khillare has revealed that the aqueous extract of old and tender neem leaves is a potent spermicide.
The minimum effective concentration required to kill 1 million sperm in 20 sec was 2. The formulation has shown high contraceptive efficacy in rabbits and in monkeys after intravaginal application. Also the formulation was found to be safe with no vaginal irritation when applied intravaginally for 30 days at a daily dose of 1 mL [ 38 ]. The Praneem polyherbal pessary and tablet formulated includes purified ingredients from neem leaves, Sapindus mukorosii and Mentha citrata oil. The vaginal pessary has shown potent spermicidal action of human spermatozoa in vitro and high contraceptive efficacy was demonstrated in rabbits of proven fertility [ 3940 ].
Praneem polyherbal formulations have shown in vitro activity against HIV and sexually transmitted disease pathogens [ 40 ]. Praneem vaginal pessaries and tablets were found to be safe for once daily intravaginal use consecutively for 7 and 14 days in healthy women volunteers [ 4142 ] Spermicides from natural sources other than plants Dermaseptins and magainins: Magainins A and G, which are two natural peptides having 23 amino acids and differ by only two substitutions, have been found to have a wide spectrum in vitro antimicrobial activity against gram positive and negative bacteria, fungi, and protozoa.
Considering their contraceptive activities and their effect against various STI-causing pathogens, it is believed that these two peptides are appropriate candidates for the evaluation of newer and safer microbicides spermicides in the future [ 65 ]. Magainin-A was found to be more potent than magainin-G. Magainin-A does not have overt cytotoxic properties and is safe for intravaginal application. It is reported that effectiveness of magainin as a contraceptive in vivo is possibly due in part to the removal of cholesterol from sperm membranes [ 69 ]. Microorganisms are also known to inhibit sperm motility either directly by agglutinating the spermatozoa or excreting extracellular products that immobilize the sperms.
It is a 34 amino acid, naturally occurring antimicrobial cationic peptide known to be produced by the bacteria Lactococcus lactis. In vivo contraceptive efficacy studies in rats showed complete arrest of sperm motility and no pregnancy in any of the animals. The mechanism by which Nisin exerts its rapid spermicidal action is not known. However, the existing evidence suggests that it possesses an overall positive charge and interacts preferentially with anionic phospholipids. The sperm plasma membrane contains high concentration of phosphatidylglycerol, a strong anionic phospholipid moiety, and thus Nisin may have high affinity towards spermatozoa [ 70 ].
Sophorolipids SLs are a group of microbial glycolipids produced by yeasts, such as Candida bombicola, Yarrowia lipolytica, Candida apicola, and Candida bogoriensis [ 71 ]. Various forms of sphorolipids produced by Candida bombicola showed spermicidal and virucidal activities. They occur naturally as the disaccharide sophorose linked glycosidically to the hydroxyl group at the penultimate carbon of primarily Cchain-length fatty acids [ 72 ]. The sophorolipid diacetate ethyl ester derivative Figure 13A is the most potent spermicidal and virucidal agent of the series of SLs studied. Its virucidal activity against HIV and sperm-immobilizing activity against human semen are similar to those of nonoxynol However, it also induced enough vaginal cell toxicity to raise concerns about its applicability for long-term microbicidal contraception.
Its structureactivity relationship has been established for creating new analogs with less cytotoxicity and higher activity. The influence of different uropathogenic microorganisms such as Escherichia coli, Enterococcus, Pseudomonas aeruginosa, Staphylococcus saprophyticus, Candida albicans on human sperm motility has been studied in vitro by Huwe et al. Jiang and Lu reported that Staphylococcus aureus significantly immobilizes the spermatozoa [ 76 ]. Especially after the prohibition of contraception in the U. Worse, many manufacturers recommended using the products as a douche after intercourse, too late to affect all the sperm.
Medical estimates during the s placed the pregnancy rate of women using many over-the-counter spermicides at seventy percent per year.
Sperm Spermicidal properties in
Ancient Egyptians used to use properites to regulate family size and pregnancy. Spermicide remedies included ingredients like acacia gum, sour milk, crocodile dung and natron minerals were mixed with plant fibers and honey and formed into a pessary. This acacia derivative successfully prevented sperm entry into the cervical mucus, disrupted spermatozoa plasma membrane and disintegrated the acrosomal cap. The sperm viability was assessed by fluorescent staining using SYBR living sperm and propidium iodide dead sperm. The sperm membrane integrity was assessed by evaluating the hypo-osmotic swelling HOS and examinations by transmission electron microscopy TEM and scanning electron microscopy SEM.
Oroperties in vivo contraceptive efficacy was evaluated in rats using post-intrauterine PD application. Properites biopsies were also performed to determine whether the PD gel induced vaginal inflammation. Results A dose-dependent effect of PD on the sperm motility and viability was observed. The maximum spermicidal effect was observed with a 0. PD decreased the fertility to zero in rats, was non-DNA damaging and was not harmful to the vaginal tissue in the rats. Conclusion PD has significant spermicidal activity that should be explored in further studies. Introduction The explosive growth of the global population has been a major concern that poses a significant threat to the quality of life of people in various countries.