Spermicidal Activity Research Articles

Antimicrobial Peptides with Spermicidal Activity as New Contraceptive Agents: Killing Two Birds with One Stone

Abstract: Antimicrobial peptides (AMPs) have emerged as promising candidates for dual-action contraceptive agents, offering both spermicidal and antimicrobial properties. This perspective explores the potential of AMPs in developing novel contraceptive technologies, focusing on their application in condom coatings and vaginal formulations. AMPs exert their effects through membrane disruption mechanisms, targeting both microbial pathogens and sperm cells. Their broad-spectrum activity against various microorganisms, coupled with spermicidal effects, makes them ideal for multipurpose prevention technologies. The incorporation of AMPs into condoms could enhance barrier protection, while vaginal applications offer non-hormonal, on-demand contraceptive options. However, challenges, such as potential vaginal irritation, microbiome disruption, and the need for long-term safety studies, must be addressed. Future research should focus on optimizing AMP selectivity, developing stable formulations, and conducting comprehensive efficacy and safety trials. The dual-action nature of AMPs aligns with the growing demand for integrated approaches to sexual and reproductive health, potentially revolutionizing contraception and STI prevention. By addressing current challenges and leveraging the unique properties of AMPs, researchers can develop a new generation of contraceptive products that offer improved efficacy, safety, and user acceptability.

Exploring the Pharmacological Potential of Acacia auriculiformis: A Comprehensive Review of Medicinal Properties and Therapeutic Applications

This review explores the pharmacological potential of Acacia auriculiformis, highlighting its diverse medicinal properties and therapeutic applications. Through a detailed analysis of experimental evidence, the study showcases the plant's efficacy in various health concerns. The plant exhibits significant wound healing, antifungal, antibacterial, antifilarial, antioxidant, antimalarial, hepatoprotective, chemoprotective, antimutagenic, CNS depressant, spermicidal, and cestocidal activities. The global interest in herbal medicine and the increasing utilization of A. auriculiformis underscore its importance in alternative healthcare approaches. The review emphasizes the need for further research to elucidate the mechanisms of action underlying the plant's pharmacological activities and to explore its potential clinical benefits. The findings suggest that A. auriculiformis holds promise as a source of therapeutic agents for a wide range of health conditions. Continued investigation into the bioactive compounds derived from the plant, along with clinical trials to assess efficacy and safety, could pave the way for the development of novel treatments. Overall, this review sheds light on the multifaceted medicinal properties of A. auriculiformis and its potential contribution to the field of herbal medicine and drug discovery.

PH-triggered polymeric nanoparticles in gel for preventing vaginal transmission of HIV and unintended pregnancy

Human Immunodeficiency Virus/Acquired Immunodeficiency Syndrome (HIV/ AIDS) and unplanned pregnancy affect female reproductive health globally. A single product providing a dual purpose of HIV prophylaxis and contraception may improve adherence to the therapy. Thus, we formulated a female-centric multipurpose prevention technology (MPT) comprising of nanoparticle loaded vaginal gel formulation acting as a contraceptive and microbicide. Eudragit® S100 nanoparticles of Atazanavir sulphate (ATZ; antiviral) and Fluoxetine hydrochloride (FLX; repurposed spermicide) were prepared for pH dependent drug release and loaded in carrageenan and HPMC K200M gel. The particle size of ATZ and FLX nanoparticles was 396.7 ± 20.64 nm and 226.5 ± 2.08 nm respectively. The in vitro release of the gel formulation in simulated seminal fluid (pH 7.6) showed 96.16% and 95.98% release of ATZ and FLX respectively at the end of 8 h. The in vitro anti-HIV and spermicidal activity of the formulation was above 80% for low drug concentrations. In vivo studies on murine model showed no signs of inflammation or vaginal epithelial injury. Curcumin based imaging confirmed the retention of the formulation in the reproductive tract of mice with minimal leakage. Nanoparticles in gel enabled non-invasive and localised delivery with minimal side effects and can be an effective prophylactic therapy.

Spermicide of Papaya Seed Oil and Compounds

This study aimed to determine the spermicidal activity of papaya seed oil (Carica papaya L) from local Bali varieties against Wistar rat spermatozoa by evaluating sperm quality and the correlation between the percentage of motility and viability spermatozoa to identify its active compounds. Papaya seed oil was obtained by extracting papaya seeds using n-hexane solvent. The study was designed as follows; group of spermatozoa Wistar rat were treated with NaCl 0.9% (control, P0), with Sodium carboxy methyl cellulose (NaCMC) 0.5% (P1), with n-hexane extract 0.1%(b/v) (P2), with n-hexane extract 0.3%(b/v) (P3), and with n-hexane extract 0.5%(b/v) (P4). Column chromatography was used to separate the n-hexane extract into two fractions, A and B. The spermicide test for fractions A and B followed the same design as the test for n-hexane extract but until the P7 group. The result showed that fraction B exhibited higher spermicidal activity, with 23.3% motility and 33.8% of viability sperm at 100 ppm. The identification of fraction B by LCMS showed at least 12 mixture compounds were venoterpine, vitamin K5, 5-phenyl-2-pyridinamine, harmalan, styrylquinoline, 1,2,3,4-tetrahydro-1-benzoyl-2-methyl-4-phenylamino-quinoline, calcitroic acid, siderol, N-benzyl-linoleamide, (3β)-3-(diisopropylamino)androst-5-en-17-one, pipereicosalidine, and 25-azacholesterol. Spermicidal activity may be a synergistic effect of several compounds that have a cytotoxic activity such as styrylquinoline, 1,2,3,4-tetrahydro-1-benzoyl-2-methyl-4-phenylamino-quinoline, siderol, and pipereicosalidine.

Safety of multiple administrations of spermicidal LL-37 antimicrobial peptide into the mouse female reproductive tract.

We have previously demonstrated spermicidal activity of LL-37 antimicrobial peptide on mouse/human sperm and its contraceptive effects in female mice. With its microbicidal action against Neisseria gonorrhoeae, LL-37 warrants development into a multipurpose prevention technology (MPT) agent for administering into the female reproductive tract (FRT). However, it is important to verify that multiple administrations of LL-37 do not lead to damage of FRT tissues and/or irreversible loss of fecundity. Herein, we transcervically injected LL-37 (36 µM-10× spermicidal dose) into female mice in estrus in three consecutive estrous cycles. A set of mice were sacrificed for histological assessment of the vagina/cervix/uterus 24 h after the last injection, while the second set were artificially inseminated with sperm from fertile males 1week afterwards, and then monitored for pregnancy. Mice injected with PBS in parallel were regarded as negative controls, whereas those injected with vaginal contraceptive foam (VCF, available over the counter), containing 12.5% nonoxynol-9, served as positive controls for vaginal epithelium disruption. We demonstrated that the vagina/cervix/uterus remained normal in both LL-37-injected and PBS-injected mice, which also showed 100% resumption of fecundity. In contrast, VCF-injected mice showed histological abnormalities in the vagina/cervix/uterus and only 50% of them resumed fecundity. Similarly, LL-37 multiply administered intravaginally caused no damage to FRT tissues. While our results indicate the safety of multiple treatments of LL-37 in the mouse model, similar studies have to be conducted in non-human primates and then humans. Regardless, our study provides an experimental model for studying in vivo safety of other vaginal MPT/spermicide candidates.

Microbial Surfactants to the Rescue

Microbial Surfactants to the Rescue

Family Araliaceae in Southern Africa: A Review of Ethnobotanical Uses, Phytochemistry, Pharmacology, and Toxicology

There is widespread use of species belonging to family Araliaceae in traditional medicine in southern Africa. The aim of this review was to assess medicinal uses, phytochemistry, pharmacology and toxicological properties of indigenous species belonging to family Araliaceae in southern Africa. Relevant articles, books, theses, dissertations, patents, and other English-only reports on the medicinal uses, phytochemistry, pharmacological and toxicological properties of species belonging to the family Araliaceae in southern Africa (Angola, Botswana, Eswatini, Lesotho, Malawi, Mozambique, Namibia, South Africa, Zambia and Zimbabwe) were reviewed. Databases such as PubMed, Web of Science, Elsevier, Google Scholar, Scopus, Springer, Science Direct, Taylor and Francis between January and July 2022. Eleven species, namely Cussonia. arborea, C. arenicola, C. natalensis, C. nicholsonii, C. paniculata, C. sphaerocephala, C. spicata, C. transvaalensis, C. thyrsiflora, C. zuluensis and Neocussonia umbellifera are used as traditional medicines against 48 human and animal diseases. This study showed that alkaloids, anthocyanins, anthracene glycosides, botulin, flavonoids, free gallic acid, iridoids, phenolics, saponins, steroids, tannins, triterpenoids and volatile oils have been identified from these species. Pharmacological research revealed that the crude extracts and compounds demonstrated isolated from these species are characterized by Aβ42 protein reduction, acetylcholinesterase, analgesic, antibacterial, antifungal, antiviral, anticancer, antihyperglycemic, anti-inflammatory, antileishmanial, antioxidant, antiplasmodial, antiprotozoal, anti-ulcer, immunomodulatory, larvicidal, molluscicidal, spermicidal, cytotoxicity and toxicity activities. Reports of medicinal uses, phytochemistry, pharmacology and toxicological properties of species belonging to the family Araliaceae in southern Africa could only be found for 11 species, suggesting that further investigation of largely unexplored family members is necessary.

Antifertility activity of Oroxylum indicum (L.) Kurz:In vitro and in vivo study on human sperm and male wistar rats

Oroxylum indicum (L.) Kurz, commonly called as Broken bones tree or Indian trumpet flower, belonging to Fam. Bignoniaceae, is traditionally used as a contraceptive by ethnic people of Tripura, North-East India. Here, we investigated the scientific basis for use of O. indicum as male antifertility agent by folklore healers. In vitro spermicidal activity of aqueous (AEOI) and methanolic (MEOI) extracts of O. indicum stem bark were studied on human sperm. The in vivo activity was experimented on male albino rats. The treated animals were allowed to mate and the pups delivered by female rat partners were counted. Phytochemical estimation of test samples was done using HPLC. The AEOI and MEOI treatments significantly decreased human sperm motility and viability. Test extracts have increased the hypo-osmotic swelling of sperm. Both the extracts were significantly declined the weight of reproductive organ. The MEOI treated rats have shown significant decrease in sperm motility and sperm counts. AEOI and MEOI treatment significantly reduced level of testosterone, but sharply raised dihydrotestosterone and prostaglandin in rats. Results testified the traditional claim for use of O. indicum as a male contraceptive agent, where MEOI have shown reversible action on male reproductive system leading to contraception without harming the libido.

Spermicidal, Antifertility and Contraceptive Effect of Azadirachta indica A. Juss. Seed Extract in Female and Male Wistar Rats

This study investigates the spermicidal and contraceptive effect of Azadirachta indica seed aqueous extract in male and female Wistar rats. The animals were divided into four groups (n=6), graded doses (2.5, 5, and 10 mg/kg) of the extract. They were exposed to female rats in a ratio of 2:1 after 24 hours, 7, and 14 days of administration. The spermicidal properties were evaluated. The female contraceptive study involved 14 days of pre-coital and post-coital administration of the neem seed extract, and contraceptive indexes were investigated. The results obtained from the spermicidal activity showed a significant decrease in male hormonal levels at 2.5, 5, and 10 mg/kg of A. indica (0.73, 0.50, and 1.08 ng/ml); and the sperm cells (102.5, 111.5, and 97 counts) after 24 hours. Administration and mating, compared to the control. Also, the histopathology of the testes showed normal testicles. The contraceptive study elicited a significant decrease in estrogen (1.46 ng/ml), luteinizing hormone (0.094 mg/dl) µand progesterone (1.82 ng/ml), at 5 mg/kg in day 14 post-coital study compared with the control. The histopathology of the treated uterus had no deteriorating effect compared with the control. The extract elicited spermicidal and contraceptive potential at a reduced dose, validating its folklore claim.

Novel Spirooxindole Derivatives as Potential Non‐Detergent Type Spermicides

AbstractThe aim of the present study is to explore the spermicidal potential of the synthetic spirooxindole derivatives and to examine the pathway behind the spermicidal action of the compounds. The in vitro spermicidal activities of the compounds were examined against human sperm by the modified Sander‐Cramer test. The pathway behind the spermicidal action of lead compounds was assessed by (a) hypo‐osmotic swelling test, (b) double fluoroprobe staining, (c) flowcytometric detection of apoptosis by FITC‐AnnexinV labelling, and (d) JC1 labelling. The haemolytic assay for topical toxicity of the compounds was carried out using rabbit erythrocytes. Two spirooxindole derivatives 4 a and 4 c were found to be most effective against human spermatozoa with MEC values of 500 μg/mL and 600 μg/mL lying in the range of standard spermicide Nonoxynol‐9 or N‐9 (MEC 550 μg/mL). The studies on the mechanism of action of the compounds unveiled that the compounds mediated sperm death were due to cellular apoptosis rather than general cell necrosis. The haemolysis assay assured the safeness of the lead molecules for topical usage. Thus, these spirooxindole derivatives may further be explored as new leads for the development of a non‐detergent type of topically applicable contraceptive formulation.

17BIPHE2, an engineered cathelicidin antimicrobial peptide with low susceptibility to proteases, is an effective spermicide and microbicide against Neisseria gonorrhoeae.

Is 17BIPHE2, an engineered cathelicidin antimicrobial peptide with low susceptibility to proteases, a better spermicide in cervicovaginal fluid (CVF) than its parental peptides, LL-37 and GF-17? At the same mass concentration, 17BIPHE2 exhibited the highest spermicidal activity on human sperm resuspended in CVF-containing medium. LL-37 and its truncated peptide GF-17 exert both spermicidal and microbicidal activities, although they are prone to proteolytic degradation in body fluids. Spermicidal activities of 17BIPHE2 were evaluated in vitro in mouse and human sperm, both resuspended in medium, and then on human sperm incubated in CVF-containing medium; in the latter condition, the spermicidal activity and peptide stability in CVF of 17BIPHE2 were compared with that of LL-37 and GF-17. The in vivo contraceptive effects of 17BIPHE2 and the reversibility thereof were then assessed in mice. Finally, in vitro microbicidal effects of 17BIPHE2 on Neisseria gonorrhoeae were determined. Sperm motility and plasma membrane integrity were assessed by videomicroscopy and exclusion of Sytox Green, a membrane-impermeable fluorescent dye, respectively. Successful in vitro fertilization (IVF) was determined by the presence of two pronuclei in oocytes following their coincubation with capacitated untreated or 17BIPHE2-treated sperm. Sperm alone or with 17BIPHE2 were transcervically injected into female mice and successful in vivo fertilization was indicated by the formation of two-cell embryos 42-h postinjection, and by pregnancy through pup delivery 21-25 days afterwards. Peptide intactness was assessed by immunoblotting and HPLC. Reversibility of the contraceptive effects of 17BIPHE2 was evaluated by resumption of pregnancy of the female mice, pretranscervically injected with 17BIPHE2, following natural mating with fertile males. Minimum inhibitory/bactericidal concentrations of 17BIPHE2 on N. gonorrhoeae were obtained through microdilution broth assay. At the same mass concentration, 17BIPHE2 was a more effective spermicide than LL-37 or GF-17 on human sperm resuspended in CVF-containing medium, with the spermicidal concentration of 32.4 µM. This was mainly due to lower susceptibility of 17BIPHE2 to CVF proteases. Importantly, the reproductive tract of mouse females treated three times with 32.4 µM 17BIPHE2 remained normal and their fecundity resumed after stopping 17BIPHE2 treatment. For ethical reasons, the inhibitory effects of 17BIPHE2 on fertilization and pregnancy cannot presently be performed in women. Also, while our study has proven the effectiveness of 17BIPHE2 as a spermicide for mouse and human sperm in vitro, dosage formulation (e.g. in hydrogel) of 17BIPHE2 still needs to be developed to allow 17BIPHE2 to remain in the vagina/uterine cavity with controlled release for its spermicidal action. Since 17BIPHE2 also exerted bactericidal activity against N. gonorrhoeae at its spermicidal concentration, it is a promising candidate to be developed into a vaginal multipurpose prevention technology agent, thus empowering women against unplanned pregnancies and sexually transmitted infections. This work was supported by the Canadian Institutes of Health Research (PJT 173268 to N.T.). There are no competing interests to declare. N/A.

Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

It was found that propranolol hydrochloride (PNL), which is a beta-blocker used for hypertension treatment, has a potent spermicidal activity through local anesthetic activity or beta-blocking effect on sperm cells subsequently it could be used as a contraceptive remedy. This study aimed to entrap PNL into invasomes (INVs) and then formulate it as a locally acting contraceptive gel. PNL-loaded mucoadhesive INVs were prepared via the thin-film hydration technique. The D-optimal design was utilized to fabricate INVs employing lipid concentration (X1), terpenes concentration (X2), terpenes type (X3), and chitosan concentration (X4) as independent variables, while their impact was observed for entrapment efficiency percent (Y1; EE%), particle size (Y2; PS), zeta potential (Y3; ZP), and amount of drug released after 6 h (Y4; Q6h). Design Expert® was bestowed to nominate the desired formula. The selected INV was subjected to further studies and formulated into a mucoadhesive gel for ex-vivo and in-vivo investigations. The optimum INV showed a spherical shape with EE% of 65.01 ± 1.24%, PS of 243.75 ± 8.13 nm, PDI of 0.203 ± 0.01, ZP of 49.80 ± 0.42 mV, and Q6h of 53.16 ± 0.73%. Differential scanning calorimetry study asserted the capability of INVs to entrap PNL. Permeation studies confirmed the desired sustained effect of PNL-loaded INVs-gel compared to PNL-gel, INVs, and PNL solution. Sperm motility assay proved the potency of INVs-gel to inhibit sperm motility. Besides, the histopathological investigation verified the tolerability of the prepared INVs-gel. Taken together, the gained data justified the efficacy of PNL-loaded INVs-gel as a potential locally acting contraceptive.

Novel Therapeutic Approach of Mollugo cerviana (L.) Ser Plant: A Review

These days, there has been a general inclination to use regular phytochemicals open in various characteristic-rich sources, for example, natural products, leaves, branches as well as underlying foundations of various plants on the grounds of the presence of substituents with bioactive possibilities, prosperity benefits, and useful fixings. In India, Mollugo cerviana (L.) ser is a medicinally valuable plant. Because of its high therapeutic properties, many rural people utilize this plant as food. The whole plant contains antioxidant, antipyretic, anti-inflammatory, and anti-microbial activity and also has spermicidal activity. It is used in different parts of India to increase vaginal discharge and uterine contraction after the baby is born. This review compiles a number of relevant studies on Mollugo cerviana and its bioactivities.

Size‐Dependent Inhibition of Sperm Motility by Copper Particles as a Path toward Male Contraception

Effective inhibition of sperm motility using a spermicide can be a promising approach in developing non‐invasive male contraceptive agents. Copper is known to have contraceptive properties and has been used clinically for decades as intrauterine contraceptive devices (IUDs) for contraception in females. Beyond that, the spermicidal use of copper is not explored much further, even though its use can also subdue the harmful effects caused by the hormonal female contraceptive agents on the environment. Herein, the size, concentration, and time‐dependent in vitro inhibition of bovine spermatozoa by copper microparticles are studied. The effectivity in inhibiting sperm motility is correlated with the amount of Cu2+ ions released by the particles during incubation. The copper particles cause direct suppression of sperm motility and viability upon incubation and thereby show potential as sperm‐inhibiting, hormone‐free candidate for male contraception. In addition, biocompatibility tests using a cervical cell line help optimizing the size and concentration of the copper particles for the best spermicidal action while avoiding toxicity to the surrounding tissue.

Comprehensive Review on Applications of Surfactants in Vaccine Formulation, Therapeutic and Cosmetic Pharmacy and Prevention of Pulmonary Failure due to COVID-19

Our world is under serious threat of environmental degradation, climate change and in association with this the out breaks of diseases as pandemics. The devastating impact of the very recent COVID-19, The sharp increase in cases of Cancer, Pulmonary failure, Heart health has triggered questions for the sustainable development of pharmaceutical and medical sciences. In the search of inclusive and effective strategies to meet today’s demand, improvised methodologies and alternative green chemical, bio-based precursors are being introduced by scientists around the globe. In this extensive review we have presented the potentiality and Realtime applications of both synthetic and bio-based surfactants in bio-medical and pharmaceutical fields. For their excellent unique amphoteric nature and ability to solubilise in both organic and inorganic drugs, surfactants are one of the most potential candidates for bio-medicinal fields such as dermatology, drug delivery, anticancer treatment, surfactant therapy, vaccine formulation, personal hygiene care and many more. The self-assembly property of surfactants is a very powerful function for drug delivery systems that increases the bio-availability of the poorly aqueous soluble pharmaceutical products by influencing their solubility. Over the decades many researchers have reported the antimicrobial, anti-adhesive, antibiofilm, anti-inflammatory, antioxidant activities of surfactants regarding its utility in medicinal purposes. In some reports surfactants are found to have spermicidal and laxative activity too. This comprehensive report is targeted to enlighten the versatile applications of Surfactants in drug delivery, vaccine formulation, Cancer Treatment, Therapeutic and cosmetic Pharmaceutical Sciences and prevention of pulmonary failure due to COVID-19.

IMPENDING CONTRACEPTIVES THAT MIGHT BE A POSITIVE METHODOLOGY TOWARDS THE MALE CONTRACEPTION

The total population has been developing dramatically; be that as it may, right now, the decisions for male contraception are restricted. This study investigates continuous explores of male contraceptives. This study article is primarily based on the thought of contraception that must be needed toward the increasing population and giving the ideal strategy to control the fertility of humans and animals. This review featured the recent oral male contraceptives that may be revolutionary products in our world as means of contraception. The audit article considers that these contraceptives are customarily utilized for their spermicidal activities and their fundamental hormones of the awkwardness for fertility and the mechanism of activity of the impact of the antifertility of contraceptives. The present study offers up-to-date data gathered on the contraceptives used for anti-fertility activity in males. The goal of this study is to spotlight the work on the anti-fertility effect of contraceptives. Therefore these products can provide options and lowering fertility would be higher than different contraceptives. This article can also assist investigators in developing the newer contraceptive preparation for anti-fertility activity in males. The innovations in this field are important to focus on current, more intense medication having a less detrimental effect on the body function and that can be administrable on its entity, less expensive, and quite reversible.

Effects of nonoxynol-9 (N-9) on sperm functions: systematic review and meta-analysis.

ObjectiveTo summarize the currently available phase I and II clinical trials of the effects of nonoxynol-9 (N-9) on human sperm structure and functions.MethodsA systematic review and meta-analysis aiming to evaluate the spermicidal activity of N-9 on motility, was conducted in PubMed, EMBASE, and Cochrane databases by 10 March 2021. The counted numbers of progressive motile (PR) sperm in cervical mucus and the vanguard sperm penetration distances were analyzed. Other effects on sperm structures and physiological activities were reviewed as well.ResultsIn the pooled results, percentages or counted numbers of PR sperm decreased after the treatment of N-9. Vanguard sperm penetration distance was shortened in treated groups. N-9 has been confirmed to damage the structures of sperm, as well as other organelles like acrosome and mitochondria. The physiological activities such as generation of reactive oxygen species, superoxide dismutase activity, acrosin activity, and hemizona binding were all inhibited in the reviewed studies.ConclusionsN-9 has several impacts on sperm owing to its potency in reducing sperm motility and cervical mucus penetration, as well as other functional competencies.Lay summaryNonoxynol-9 (N-9) has been used worldwide as a spermicide to kill sperm for more than 60 years but can cause side effects including vaginal irritation and can increase the rate of contraceptive failure. A detailed analysis of published literature aiming to evaluate the spermicidal activity of N-9 on sperm was carried out. In the pooled results, N-9 reduced the number of active sperm and the distance they traveled. It also caused damage to the structures of sperm and to the way the sperm acted and interacted with the egg. In conclusion, N-9 impacts on sperm in a number of ways that lead to sperm death and dysfunction.

Antibacterial, Sperm Immobilization and Spermicidal Activities of Bacteriocins Produced by Vaginal Lactobacilli

Abstract Lactobacillus bacteriocin is an interesting compound playing a dual spermicidal/bacteriocidal role so that this compound can be developed as an agent that can be able to replace the unsafety chemical, nonoxynol-9. The present study aimed to investigate the antibacterial, sperm immobilization, and spermicidal activities of bacteriocins that were produced from vaginal lactobacilli. Nine of 932 cell-free supernatants exhibited potent antibacterial activities against the standard bacterial strains and the pathogenic Niesseria gonorrhoeae. Ion exchange-purified bacteriocins B84/7 F2 demonstrated the lowest minimum inhibitory concentration and the highest bacteriocin activity against the tested pathogens. The isolate B84/7 was then identified as Lactobacillus crispatus. The rapid killing activity was exerted within 15 minutes after being exposed to the tested bacteria, and also significantly inhibited the exponential growth of the tested pathogen. Among 48 semen of volunteers, the median time of sperm immobilization of ion-exchange purified B84/7 F2 bacteriocin (18.70 mg/mL) was 30.42 seconds. Within 60 seconds, spermicidal activities of the partial fractionated and ion-exchange purified B84/7 F2 at the undiluted concentration were 83.67 and 80.75%, respectively. Its activity will significantly decline at pH > 8.0 or after being treated with alkaline and proteolytic enzymes. Two peptide bands of this bacteriocin were 7.08, and 8.81 kDa after being detected on a tricine SDS-PAGE gel. In-depth characteristics of this bacteriocin should be further investigated regarding the mode of action and purification. These findings can be applied to develop as the protecting agent of sexually transmitted infections especially gonorrhea, and unwanted pregnancy. Keywords: Antibacterial activity, Bacteriocins, Neisseria gonorrhoeae, Sperm immobilization, Spermicidal activity, Vaginal lactobacilli

Machine Learning Prediction of Antimicrobial Peptides.

Antibiotic resistance constitutes a global threat and could lead to a future pandemic. One strategy is to develop a new generation of antimicrobials. Naturally occurring antimicrobial peptides (AMPs) are recognized templates and some are already in clinical use. To accelerate the discovery of new antibiotics, it is useful to predict novel AMPs from the sequenced genomes of various organisms. The antimicrobial peptide database (APD) provided the first empirical peptide prediction program. It also facilitated the testing of the first machine-learning algorithms. This chapter provides an overview of machine-learning predictions of AMPs. Most of the predictors, such as AntiBP, CAMP, and iAMPpred, involve a single-label prediction of antimicrobial activity. This type of prediction has been expanded to antifungal, antiviral, antibiofilm, anti-TB, hemolytic, and anti-inflammatory peptides. The multiple functional roles of AMPs annotated in the APD also enabled multi-label predictions (iAMP-2L, MLAMP, and AMAP), which include antibacterial, antiviral, antifungal, antiparasitic, antibiofilm, anticancer, anti-HIV, antimalarial, insecticidal, antioxidant, chemotactic, spermicidal activities, and protease inhibiting activities. Also considered in predictions are peptide posttranslational modification, 3D structure, and microbial species-specific information. We compare important amino acids of AMPs implied from machine learning with the frequently occurring residues of the major classes of natural peptides. Finally, we discuss advances, limitations, and future directions of machine-learning predictions of antimicrobial peptides. Ultimately, we may assemble a pipeline of such predictions beyond antimicrobial activity to accelerate the discovery of novel AMP-based antimicrobials.

In vitro spermicidal effect of Thevetia Peruviana leaves on human spermatozoa.

An in vitro spermicidal effect of aqua-methanolic (2:3) extract of Thevetiaperuviana leaves on human spermatozoa was evaluated in a dose-dependent manner (20, 40, 80 and 160mg/ml) at a 1:1 ratio. Sperm motility, viability, hypo-osmotic swelling (HOS) and acrosomal status and function tests were performed immediately (20s), and after 5 and 10min of exposure of the spermatozoa to the extract of Thevetiaperuviana leaves at different dose concentrations. Nuclear chromatin decondensation (NCD) test, DNA fragmentation test and sperm revival test were also evaluated. The sperm motility was affected immediately at a dose of 20mg/ml and reduced gradually at doses of 40 and 80mg/ml of Thevetiaperuviana extract. Complete immobilisation of spermatozoa was observed at 160mg /ml dose of this extract treatment within 5min. 50% immobilisation of spermatozoa (EC50) was observed at 28mg/ml dose of Thevetiaperuviana extract within 20s. The sperm viability decreased significantly at a higher concentration of extract, and all spermatozoa were found to be non-viable after 10min when treated with 160mg/ml dose of Thevetiaperuviana extract. HOS and NCD of spermatozoa also reduced gradually at a higher concentration of extract administration. The percentage of DNA damage in spermatozoa was four times greater than in the control group. The findings indicate that the hydro-methanolic extract of Thevetiaperuviana leaves possesses appreciably potent spermicidal activity through an in vitro model, which may explore an effective vaginal contraceptive.