Screening of ethyl acetate extract of Bridelia micrantha for hepatoprotective and anti-oxidant activities on Wistar rats

Objective:To explore the hepatoprotective and anti-oxidant activities of the methanolic leaf extract of Bridelia micrantha(B.micrantha) on paracetamol induced liver damage in Wistar rats. Methods:Parameters were measured including alanine aminotransaminase(ALT),aspartate aminotransferase(AST),alkaline phosphatase(ALP),bilirubin and total protein.The anti-oxidant effects were studied using the 1,l-Diphenynl-2-Picrylhydrazyl(DPPH) and Ferric Reducing Antioxidant Power(FRAP) assay methods.Results:B.micrantha extract decreased the level of AST in the rats given PCM from(129.47±0.921) IU/L to(57.78±1.71) IU/L(P【0.05).This was lower than the value for Silymarin which was(59.92±1.41) IU/L.ALT concentration was reduced from (150.18±2.23) IU/L to(79.10±2.01) IU/L(P【0.05).ALP was reduced from(49.86±0.85) IU/L to(29.64±1.53) IU/L(P【0.05).Total bilirubin was reduced from(2.14±0.10 mg/dL) to(0.18±0.07) mg/dL (P【0.05) while total protein was increased from(4.26±0.30) mg/dL to(6.20±0.19) mg/dL(P【0.05). Concentrations ranging from 10 - 400μg/mL of B.micrantha were assayed for antioxidant activities.The DPPH assay showed 98%antioxidant activity at concentration of 400μg/mL. The FRAP values were 0.016,0.39,0.455,0.601 and 1.382μM at 10.50,100,200 and 400μg/ mL respectively.Conclusions:Results suggest that B.micrantha has hepatoprotective and anti oxidant potentials.However,further work involving fractionation needs to done to isolate the active compound responsible for the hepatoprotective activity.

Antihyperglycemic effects of the methanol leaf extract of Diaphananthe bidens in normoglycemic and streptozotocin—induced hyperglycemic rats

Objective:To evaluate the methanol leaf extract of Diaphonathe bidem(D.bidenx)(AFZEL EX SW) SCHLTR for antihyperglycemic activity in order to confirm it antidiabetic potential.Methods: D.bidenx was extracted by cold maceration for 48 h and concentrated in vacuo to yield D.bidenx extract(DBE).Hyperglycemia was induced by intraperitoneal administration of slreplozotocin (75 mg/kg).Oral glucose tolerance test was done with 2 g/kg glucose load in normal rats.DBE (150.300 and 600 mg/kg) was administered orally,while tolbutamide(100 mg/kg.p.o.) was used as the standard reference drug.Blood glucose levels determined using ACCUCHEK glucose autoanalyzer. The acute toxicity and phytochemical studies were also carried out.Results:DBF. (600 mg/kg) and tolbutamide(100 mg/kg) significantly(P【0.05,0.005) reduced blood glucose levels of rats between 120 and 480 nun post administration in normal rats.In the streptozotoeininduced hyperglycemic rats,DBE(150.300.600 mg/kg) caused significant(P【0.001)dose- and time- dependent reduction in the blood glucose levels by 1.7%.22.8%and 43.4%,respectively at 480 min compared to the negative control group.DBE(600 mg/kg) reduced the blood glucose level of rats by 1.2%in the oral glucose tolerance test when compared with the normal saline treated group.The acute toxicity test showed that DBE was safe at the doses used and the phytochemical screening revealed the presence of saponins,steroids,tannins and terpernoids.Conclusions:D. bidens extract possess antihyperglycemic activity which may be mediated through pancreatic and extra-pancreatic pathways,thereby justifying it folkloric use.

Synergy in antibacterial activities of Ampicillin trihydrate, stabilized with a synthetic aluminum-magnesium silicate and immune-stimulants, on resistant <i>Escherichia coli</i>infection

To treat resistant Escherichia coli infection in chicks, Ampicillin was stabilized with a synthetic aluminum-magnesium silicate (AMS) to prolong its bioavailability. Its dose was also reduced to minimize adverse side effects. Vitamins A, C, E and Selenium levels in the chicks’ feeds were increased to enhance immune response of the chicks. E. coli coloning forming units, per ml of bile of the chicks, treated with Ampicillin and with Ampicillin in AMS, were: 228800.00 ± 90103.50 and 134500.00 ± 44937.97 at 10 mg/kg, 104400.00 ± 36024.44 and 34800.00 ± 8014.97 at 7.5 mg/kg, 198400.00 ± 129301.80 and 156800.00 ± 109392.70 at 5 mg/kg. Mean bacterial loads of the untreated groups, fed normal feed and those fed the fortified feed were 824400.00 ± 322424.80 and 534800.00 ± 277832.80. At 7.5 mg/kg. Ampicillin in the AMS, effectively (P E. coli infection in chicks, fed immune-stimulants, with the infection rate reduced by 95.8%.

Histological changes and antidiabetic activities of Icacina trichantha tuber extract in beta-cells of alloxan induced diabetic rats

Objective:To investigate the antidiabetic,hypolipidaemic activities and histopathological changes ofIcacina trichantha(I.trichantha)tuber extract in alloxan induced diabetic rats.Methods:In the present study,80%methanol extract of I.trichanthatuber was tested on alloxan induced diabetic rats.They were randomly grouped into control(distilled water and glibenclamide)and experimental(200,400 and 600 mg/kg body weight).Diabetes was induced by a single intraperitoneal injection of 160 mg/kg body weight of alloxan.Blood glucose levels weremeasured using blood glucose test strips with AccuCheck Advantage II glucometer at 1,3,6,and 24 h on the first day and 1 h after treatment on Day 7,14 and 21.Blood samples were collected and centrifuged to separate serum for estimation of lipid profile and other biochemical parameters.Histopathological changes in diabetic rats pancreas were also studied after extract treatment.Results:Daily oral administration ofI.trichanthatuber extract(200,400,and 600 mg/kg bodyweight)and glibenclamide(2 mg/kg)showed beneficial effects on blood glucose level(P<0.01)as well as improving liver,kidney functions and hyperlipidaemia due to diabetes.The extract had a favourable effect on the histopathological changes of the pancreas in alloxan induced diabetes.Conclusions:I.trichanthatuber extracts posses antidiabetic activities as well as improve liver and renal profile and total lipids levels.I.trichanthatuber extracts also have favourable effects to inhibit the histopathological changes of the pancreas in alloxan induced diabetes.

Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells

Non-small cell lung cancer(NSCLC)is often characterized by an underlying mutation in the epidermal growth factor receptor(EGFR),contributing to aggressive metastatic disease.Methyl 2-cyano-3,11-dioxo-18 beta-olean-1,12-dien-30-oate(CDODA-Me),a glycyrrhetinic acid derivative,reportedly improves the therapeutic response to erlotinib(ERL),an EGFR tyrosine kinase inhibitor.In the present study,we performed a series of studies to demonstrate the efficacy of CDODA-Me(2μM)in sensitizing HCC827 R(ERL-resistant)cells to ERL.Herein,we first established the selectivity of ERL-induced drug resistance in the HCC827 R cells,which was sensitized when ERL was combined with CDODA-Me(2μM),shifting the IC50 from 23.48μM to 5.46μM.Subsequently,whole transcriptomic microarray expression data demonstrated that the combination of ERL+CDODA-Me elicited 210 downregulated genes(0.44%of the whole transcriptome(WT))and 174 upregulated genes(0.36%of the WT),of which approximately 80%were unique to the ERL+CDODA-Me group.Synergistic effects centered on losses to cell cycle progression transcripts,a reduction of minichromosome maintenance complex components(MCM2-7),all key components of the Cdc45·MCM2-7 GINS(CMG)complex,and replicative helicases;these effects were tantamount to the upregulation of processes associated with the nuclear factor erythroid 2 like 2 translational response to oxidative stress,including sulfiredoxin 1,heme oxygenase 1,and stress-induced growth inhibitor 1.Collectively,these findings indicate that the synergistic therapeutic effects of ERL+CDODA-Me on resistant NSCLC cells are mediated via the inhibition of mitosis and induction of oxidative stress.

The effects of combination of methanolic leaf extract of Azadirachta indica and diminazene diaceturate in the treatment of experimental Trypanosoma brucei brucei infection in rats

Objective:To investigate the effects of combination therapy of methanolic leaf extract of Azadirachta indica(A.indica) and diminazene diaceturate(DDA) in the treatment of experimental Trypanosoma brucei brucei(T.brucei brucei) infection in rats.Methods:Acute toxicity study of the drug and extract combinations were done.Selection of the best drug and extract combinations was carried out using fifty four rats of both sexes separated into 9 groups.Three dose combinations were derived from selection of the best drug and extract combinations used for the final study viz:7 mg/kg bw DDA plus 125 mg/kg bw extract(group B),3.5 mg/kg bw DDA plus 250 mg/kg bw extract(group C),and 1.8 mg/kg bw DDA plus 500 mg/kg bw extract(group D).The final study had in addition to the three groups derived from the dose response study,four other groups viz:uninfected untreated negative control(group F),infected and treated with 3 000 mg/kg bw extract alone(group E),infected and treated with 7 mg/kg bw DDA alone(group A),and infected untreated positive control(group G).The parameters assessed were onset of parasitaemia(OP), level of parasitaemia(LOP),clearance of parasites post treatment(COPPT),relapse infection period(RIP),post infection survival period(PIST).Results:There was no significant difference in OP between the groups(P【0.05).One day post treatment,the mean LOP of groups A,B,and C were found to be significantly lower than that of group D which in turn was lower than that of group E and G respectively.The mean LOP of group E was significantly lower than group G two days post treatment and this trend continued throughout the experimental period.Mean COPPT of group D was significantly longer than that of groups A,C and B.There was no significant difference in the mean COPPT among groups B,C and A.The mean RIP of group D was significantly shorter than group C,and that of group C was significantly shorter than that of group A.There was no relapse of infection in group B.The PIST of group E did not differ significantly from group G.Conclusions:This experiment stands to conclude that combination of 125 mg/kg bw extract and 7 mg/kg bw DDA is very effective in the treatment of trypanosomosis,caused by T. brucei.This combination therapy proved to be better than single therapy of DDA.

Dietary substitution of soybean oil with coconut oil in the absence of dietary antibiotics supports growth performance and immune function in nursery and grower pigs

Background:We hypothesized that supplementation of nursery and grower pig diets with coconut oil in the absence of antibiotics would yield maintenance of glucose homeostasis,growth performance,and immune function similar to what is achieved with nursery and grower pig diets containing antibiotics.Pigs received the same base treatment diets from d24(weaning)to d71 of age and had blood and fecal samples collected on d24,d31,d45 and d71 for measurement of whole blood glucose,serum insulin,cortisol and cytokines,and fecal microbiome.Pigs had weekly weights and daily feed consumption measured throughout the study.Animals were euthanized at d71 and subcutaneous fat and ileal contents were collected for assessment for fatty acids and microbiome,respectively.Diet treatments consisted of 2%soybean oil plus antibiotics(ABX;n=22),2%soybean oil without antibiotics(NABX;n=22),and 2%coconut oil without antibiotics(COC;n=22).Statistical analysis examined the effect of diet within each timepoint using a repeated measures ANOVA.Results:Pigs fed COC diet had decreased serum insulin levels,maintained feed intake,feed conversion and weight gain,and,based on serum cytokines and fecal microbiome,were immunologically similar to ABX-fed pigs.However,NABX-fed pigs performed similarly to the ABX-fed pigs in all parameters except for serum cytokines.Additionally,there was no difference in the incidence of diarrhea between any of the diet treatments.Conclusions:This study demonstrates that dietary antibiotics are not necessary to maintain growth performance in nursery and grower pigs.However,dietary antibiotics appear to modulate circulating cytokine levels.Dietary coconut oil is neither harmful nor helpful to growth performance or immune function in nursery and grower pigs but does modulate serum insulin levels.Therefore,while coconut oil fed at 2%by weight is a suitable substitute for dietary antibiotics,this study suggests that no substitute for dietary antibiotics is needed at all.

Effect of L-carnitine supplementation during in vitro maturation and in vitro culture on oocyte quality and embryonic development rate of bovines

Objective:To assess the effect of L-carnitine supplementation during in vitro oocyte maturation and in vitro culture process of bovine oocytes.Methods:L-carnitine(3.8 mM)was added to maturation medium and the effect was assessed in the quality(Experiment 1)and in the cleavage and 4-cells stage(Experiment 2).Besides,the effect of L-carnitine addition on maturation medium(3.8 mM)and culture medium(1.5 mM)on embryo rate production was assessed.In Experiment 1,bovine oocytes from abattoir were randomly separated into two groups(the control group and L-carnitine group)forin vitro maturation.Matured oocytes were examined for cumulus cells expansion as an indicator of maturation,and the content of the mitochondrial activity,the presence of lipid droplets,the reduced glutathione,and the reactive oxygen species were measured by using specific fluorochromes.In Experiment 2,oocytes were matured as performed in Experiment 1,afterward fertilized and cultured until day 3,and cleavage rate and 4-cells stage rate were determinated.In Experiment 3,in vitro maturation and fertilization were done as performed in Experiment 2,but at day 3 of culture,each group of embryos was separated into two new groups,and L-carnitine(1.5 mM)was added in culture media until day 8.The cleavage and embryo development rate were determined on the basis with the oocytes put on maturation.Hatching rate was calculated from cleaved embryos.Results:The cumulus expansion rate at gradeⅢand mitochondrial activity were significantly higher in the L-carnitine group in comparison with the control group(P0.05).In addition,cleavage and the proportion of embryo development and hatching rate were similar for all groups(P>0.05).Conclusions:L-carnitine as a supplement in culture media improves the cumulus expansion and increases the mitochondrial activity during in vitro maturation process but has no apparent effect on the cleavage and development of bovine embryos.Further investigations of L-carnitine addition on in vitroculture are needed to test their effect on embryo quality.

Acute and chronic toxicity studies of hydromethanol leaf extract of Helianthus annuus Linn.in rats

Objective:To investigate the safety levels of hydromethanol leaf extract of Helianthus annuus Linn.(H.annuus) in rat.Methods:Acute oral toxicity test of hydromethanol leaf extract of H.annuus was conducted through up and down method at 2.00 g/kg dose limit in rats.The chronic toxicity study was conducted by administering different concentrations(0.25,0.50 and 1.00 g/kg) of hydromethanol extract of H.annuus in feed,for 90 consecutive days.On days 30,60 and 90,blood samples were collected from the retro-orbital plexus of the rats for determination of serum biochemical parameters.Histopathological examination of the pancreas,livers,kidneys and testis were also conducted.Results:The LD_(50) of the hydromethanol extract of H.annuuswas greater than 2.00 g/kg and it significantly(P < 0.05) reduced serum cholesterol.On days 60 and 90,the serum urea and creatinine levels of hydromethanol extract of H.annuustreated groups were elevated when compared with the control group.There were fibrosis in the kidneys and livers;degeneration and necrosis in the testis and significant dose-dependent increases in number and size of pancreatic islet of langerhans.Conclusions:The findings suggest that hydromethanol extract of H.annuus is tolerated in short term administration,but long term(up to 90 days) administration at high doses,may elicit hepatic,testicular and nephrotic disorder.

Anthelmintic activity of Securidaca longepedunculata(Family:Polygalaceae)root extract in mice,in vitro and in vivo

Objective:To elucidate the pharmacological bases of oral administration of Securidaca longepedunculata(S.longepedunculata) root extract as an anthelmintic in folkloric medicine. Methods:Albino mice were infected with infective third(L3) larval stage of Heligmosomoides polygyrus(H.polygyrus) by esophageal intubation.Following establishment of the adult worms in the intestine,the mice were treated with 0-2 000 mg/kg body weight(bw) of methanolic root extract of S.longepedunculata and 100 mg/kg bw of pyrantel embonate,the reference drug in vivo. Bioactivity and larvicidal effects of the extract were tested by exposing brine shrimps(Artemia salina) to 0.00-1.00 mg/mL and the L3 stage of Heligmosomoides contortus(H.contortus) and H.polygyrus to 0.00-2.50 mg/mL of the extract in vitro.Results:The percentage yield of the extract was 7.13%w/w dry matter.The brine shrimps toxicity bioassay resulted in an LC_(50) of 74.18 μ g/mL.The extract had a significant,dose-dependent larvicidal effect on the L3 stage of H.contortus and H.polygyrus with the terminal effect of 75%and 70%at the highest exposure concentrations,respectively.The extract however,did not affect the number of worm eggs per gram(epg) of fecal materials(P<0.05) and total worm burden(twb) of adult H.polygyrus in infected mice.Treatment with pyrantel embonate significant reduced both the fecal egg count and twb to 0 compared to the untreated control(P<0.05).Conclusions:These results indicate that S.longepedunculata root extract contains potent bioactive compounds and has larvicidal effect on L3 stage of H.contortus and H.polygyrus,substantiating its use as anthelmintic in alternative medicine.

Experimental Trypanosoma brucei infection at immediate post partum period:effects on dam and the offspring

Objective:To investigate the effects of immediate post-partum infection with Trypanosoma brucei（T.brucei） on dam and offspring.Methods:Sixty female Albino rats（Rattus norvegicus） weighing between 130-170 g were used as animal model.The animals were divided as follows: 25 infected between 1-5 days post partum;10 infected unbred as positive controls;and 25 uninfected as negative controls.The following parameters were evaluated:packed cell volume （PCV）,level of parasitaemia,survival time,litter size and litter weight at birth and on days 7, 14 and 21 post delivery,using conventional methods.Possible trans-mammary transmission of infection to litter through milk was also assessed.Results:The results showed a comparatively （P【0.05） higher mean PCV value for the uninfected negative control on the 8 day post infection compared with the infected groups which corresponded with the increasing level of parasitaemia in the two infected groups.Mean litter size and litter weights were higher（P【0.05） in the uninfected controls on the 21st day.Survival time in the infected groups were similar.No evidence of trans-mammary transfer of infection was recorded.Conclusion:T.brucei infection during immediate post partum period is detrimental to the dam and impairs growth of the offspring.

Seasonal changes in sperm parameters, testicular histology and circulating levels of reproductive hormones in the male African straw-colored fruit bat (Eidolon helvum)

Objective: To investigate seasonal changes in some reproductive characteristics of the male African straw-colored fruit bat [Eidolon (E.) helvum] in a tropical rain forest area of South-East Nigeria.Methods: Spermatozoal characteristics in the testes and cauda epididymides, testicular histology, and the circulating levels of the reproductive hormones, testosterone, follicle stimulating hormone and luteinizing hormone were evaluated in male bats captured in late January (peak dry season), late May (early rainy season) and late September (late rainy season) of 2019. The bats were captured in Obiagu community in Enugu State, South-East Nigeria. Data were analyzed with analysis of variance. Results: There were high serum concentrations of testosterone in early and late rainy season and of luteinizing hormone in early rainy season, but the concentrations of both hormones were low during peak dry season. These hormonal changes corresponded with the testicular seminiferous and spermatogenic activities and testicular and epididymal sperm concentrations, which were also maximal during early and late rainy season but minimal during peak dry season. Epididymal sperm motility and vitality were also high in early and late rainy season but low in peak dry season, while sperm morphological abnormalities were low in early and late rainy season but elevated in peak dry season. There was histological evidence that spermatogenesis did not cease completely during testis regression, but continued at a reduced rate during the dry season. Conclusions: The findings do not support concurrent epididymal sperm storage with testis regression in E. helvum. Altogether, these indicate that seasonal changes significantly alter sperm characteristics, testicular histology and circulating levels of reproductive hormones in E. helvum within the study area.

Chemical Composition of the Marc of a Wild Tropical Plant <i>Tacca involucrata</i>(Schumach and Thonn, 1827)

Tacca involucrata (Batflower or Polynesian arrowroot) tubers are a stable food in tropics where it occurs. In central Nigeria, it is processed locally after digging it from the ground by peeling with sharp sand, grating and soaking in fresh water after which it is filtered and the filtrate is dried and is cooked with other ingredients. The marc, said to be bitter, is usually discarded by deep burial as it is considered poisonous to livestock and humans. All parts of the plant are used in folk medicine to treat various diseases. The aim of this work was to analyze quantitatively the phytochemical, elemental, vitamin and proximate composition of the marc of the tubers with a view of assessing its pharmacological and nutritional potentials. The marc was obtained from Jandeikyura Village in Wukari LGA of Taraba State, Nigeria, and was extracted with 80% methanol for 72 hr to give a yield of 10.1% w/w and was whitish in colour. Phytochemical analysis showed the presence of reducing sugars, tannins, flavonoids, steroids, glycosides and hydrogen cyanide at 195.65 ± 0.5, 3.44 ± 0.2, 1.29 ± 0.5, 0.83 ± 0.4, 1.36 ± 1.0 and 0.00985 ± 0.3 (mg/100g), respectively. The elemental analysis showed the presence of potassium, sodium, magnesium, selenium, manganese, vanadium and some heavy metals like lead, aluminium, arsenic and mercury at 36.45 ± 0.1, 44.04 ± 0.1, 1.52 ± 0.2, 0.80 ± 0.9, 0.52 ± 0.7, 0.27 ± 0.7, 0.07 ± 0.6, 0.008 ± 0.05, 0.085 ± 0.6 and 0.026 ± 0.6 (mg/100g), respectively. Vitamin analysis showed the presence of vitamins A, B1, B2, B3, C and E in various amount as 2.26 ± 0.8 μg, 0.83 ± 0.8 mg/100g, 0.58 ± 0.4 mg/100g, 0.33 ± 0.6 mg/100g, 9.80 ± 0.4 mg/100g and 6.86 ± 0.9 mg/100g, respectively. The proximate analysis showed the marc to contain moisture, ash, fats, fibre, crude protein and carbohydrate in the range of 10.83% ± 0.3%, 1.93% ± 0.6%, 1.06% ± 0.5%, 4.42% ± 0.4%, 6.12% ± 0.6% and 86.07% ± 0.3%, respectively. This shows that despite the presence of hydrogen cyanide and some heavy metals in traces amount which are considered poisonous to livestock and humans, the marc contains some elements, vitamins, phytochemical and nutrients which are pharmacologically and nutritionally important.

Silencing Fas-associated phosphatase 1 expression enhances efficiency of chemotherapy for colon carcinoma with oxaliplatin

AIM:To investigate whether silencing Fas-associated phosphatase 1(FAP-1)expression enhances the efficiency of chemotherapy for colon carcinoma with oxaliplatin.METHODS:Expression of FAP-1 in mRNA and protein was detected by reverse transcription polymerase chain reaction(RT-PCR)and flow cytometry.Small interfering RNA(siRNA)was designed according to the FAP-1 mRNA sequence.Cell proliferation was evaluated by methyl thiazolyl tetrazolium(MTT)assay.Anenxin V-and propidine iodine(PI)were assayed by flow cytometry for the detection of apoptosis. RESULTS:The expression of FAP-1 was increased in SW480 cells after chemotherapy with oxaliplatin. Transfection of FAP-1 siRNA into SW480 cells silenced the expression of FAP-1 and consequently abolished the inhibitory function of Fas/FasL-mediated apoptosis pathway,thus increasing the efficacy of chemotherapy for colon carcinoma with oxaliplatin. CONCLUSION:RNA interference combined with conventional chemotherapy is more effective against colon cancer.

Transcription factors specificity protein and nuclear receptor 4A1 in pancreatic cancer

Specificity protein(Sp)transcription factors(TFs)Sp1,Sp3 and Sp4,and the orphan nuclear receptor 4A1(NR4A1)are highly expressed in pancreatic tumors and Sp1 is a negative prognostic factor for pancreatic cancer patient survival.Results of knockdown and overexpression of Sp1,Sp3 and Sp4 in pancreatic and other cancer lines show that these TFs are individually pro-oncogenic factors and loss of one Sp TF is not compensated by other members.NR4A1 is also a prooncogenic factor and both NR4A1 and Sp TFs exhibit similar functions in pancreatic cancer cells and regulate cell growth,survival,migration and invasion.There is also evidence that Sp TFs and NR4A1 regulate some of the same genes including survivin,epidermal growth factor receptor,PAX3-FOXO1,α5-andα6-integrins,β1-,β3-andβ4-integrins;this is due to NR4A1 acting as a cofactor and mediating NR4A1/Sp1/4-regulated gene expression through GC-rich gene promoter sites.Several studies show that drugs targeting Sp downregulation or NR4A1 antagonists are highly effective inhibitors of Sp/NR4A1-regulated pathways and genes in pancreatic and other cancer cells,and the triterpenoid celastrol is a novel dual-acting agent that targets both Sp TFs and NR4A1.

Antifertility effects of Azadirachta indica methanol seed extract on canine spermatozoa in vitro

Objective:To investigate the effects of Azadirachta(A.)indica methanol seed extract on canine male fertility in vitro.Methods:The effect of the A.indica methanol seed extract(2.5,5.0,10.0 and 20.0 mg/mL,respectively)on canine spermatozoa was evaluated in vitro at 1.0,2.5,5.0 and 10.0 min post-treatment.The two controls were comprised of sperm sample in phosphate-buffered saline,and sperm sample in phosphate-buffered saline and 1%dimethyl sulfoxide,respectively.The experiment was repeated(n=3)in duplicates with semen collected from 3 adult Basenjis.The effect of A.indica methanol seed extract treatments on canine spermatozoal total and progressive motility(phase-contrast microscopy),sperm vitality(eosin-nigrosin vital staining method)and total abnormalities(phase contrast microscopy,eosin-nigrosin staining and Papanicolaou staining methods)were determined.Results:A.indica methanol seed extract treatment caused a concentration and time-dependent decrease in sperm percentage total motility,progressive motility and vitality.The absence of sperm revival post-treatment provided evidence of a permanent or irreversible incapacitation of sperm by A.indica methanol seed extract.Conclusions:The inhibition of sperm motility and significant spermicidal effect observed post-treatment suggest that A.indica methanol seed extract may produce a potent antifertility or contraceptive effect in dogs if applied as an intra-vaginal cream pre-coitus.

Endocrine disruptors and falling sperm counts： lessons learned or not!

In summary, it has become evident that multiple factors can affect sperm counts and quality. Most reports indicate that there has not been a worldwide decrease in sperm counts over the past 20 or 50 years, and the validity of the endocrine disruptor hypothesis or testicular dysgenesis syndrome with respect to sperm counts is highly questionable.

Effect of Gongronema latifolium on gastric emptying in healthy dogs

AIM:To investigate sonographically the effect of Gonogronema latifolium (G.latifolium) on gastric emptying of semi-solid meals in healthy dogs.METHODS:In a randomized,placebo-controlled experiment,twenty-five clinically healthy dogs were randomly allotted into five groups of five dogs in each group.The placebo group served as the control,and the low,moderate and high dose groups ingested the methanolic leaf extract of G.latifolium in capsules at 100 mg/kg,250 mg/kg and 500 mg/kg,respectively,while the prokinetic group ingested 0.5 mg/kg capsules of metoclopramide.After a 12-h fast,each group ingested its treatment capsules 30 min before the administration of a test meal.Measurements of gastric emptying and blood glucoselevels were obtained 30 min before and immediately after the ingestion of the test meal and thereafter every 15 min for 4 h.This was followed by further measurements every 30 min for another 2 h.RESULTS:The gastric emptying times of the placebo,low dose,moderate dose,high dose and prokinetic dose groups were 127.0 ± 8.2 min,135.5 ± 3.7 min,155.5 ± 3.9 min,198.0 ± 5.3 min and 59.0 ± 2.5 min,respectively.Gastric emptying times of the moderate and high dose groups were significantly slower than in the placebo control group (155.5 ± 3.9 min,198.0 ± 5.3 min vs 127.0 ± 8.2 min,P=0.000).No significant difference in gastric emptying between the low dose and placebo control groups was noted (135.5 ± 3.7 min vs 127.0 ± 8.2 min,P=0.072).Gastric emptying of the prokinetic group was significantly faster than that of the control group (59.0 ± 2.5 min vs 127.0 ± 8.2 min,P=0.000).The hypoglycaemic effect of G.latifolium and gastric emptying were inversely related (r=-0.95,P=0.000).CONCLUSION:G.latifolium delays gastric emptying and lowers postprandial blood glucose in healthy dogs.It reduces the postprandial blood glucose by delaying gastric emptying.

V_2加压素受体拮抗剂SK&F105494对猪子宫肌催产素受体的阻断作用(英文)

目的:确定V_2加压素受体拮抗剂SK&F105494(SK&F)对催产素受体的阻断作用。方法:采用猪离体子宫收缩试验和受体结合试验。结果:SK&F对赖氨酸加压素(Lyp)和催产素(Oxy)引起的子宫收缩均有阻断作用,并随SK&F浓度增加而加强。K_i值小于Lyp,近似于Oxy受体特异性阻断剂L-366948,分别为1.73±0.32,14.36±1.73和1.79±0.35nmol·L^(-1)。结论:SK&F对Oxy受体有强烈的阻断作用。