15 research outputs found
Synthesis and pharmacological studies of 1-<i>p</i>-nitrobenzoyl<b>-</b>3-(3-substituted-2-hydroxypropyloximino) indole-2,3-diones
258-261Sodium salt of 3-oximino indole-2,3-dione
on reaction with epichlorohydrin in N,N'-dimeth ylformamide gives 3-(2,3-epoxypropyloximino)
indole-2,3-dione 2. Compound 2 on reaction with diverse secondary
amines yields corresponding Mannich bases 3a-e, which on benzoylation
furnish 4a-e. The synthetic benzoyl derivatives of 4a-e have been
screened for their pharmacological activities
Germ cell death and their removal during initial stages of testicular ischemia and cryptorchidism: A comparative analysis
1080-1087Germ cell death and their removal from
the seminiferous epithelium are common in the affected testis in conditions of unilateral
ischemia or cryptorchidism; the similarities and differences, however, have not
been studied between these two conditions. The present study was designed to
examine the severity of the effect on testicular germ cells during the initial
stages of both ischemia and
cryptorchidism, which have significant implications on the restoration of
fertility following surgical repair. Complete absence of spermatids was observed
following 12 hr of ischemia as compared to 7 days of cryptorchidism. Germ cell
removal in either case was in the direction of lumen to basement membrane
leaving only a single layer of cells by 24 hr of unilateral ischemia as
compared to 15 days of cryptorchidism. Levels of intratesticular testosterone was
found lower in cryptorchidism (7 days) but not in ischemia till 24 hrs. Giant
cells frequently observed in cryptorchid testis were absent in the ischemic seminiferous
epithelium. There was a gradual increase in the number of apoptotic and non-viable
cells; the latter was more than 95% by 24 hr of ischemia. In contrast,
approximately 85% testicular cells were nonviable till IS days of
cryptorchidism. The 1c peak representing the population of haploid cells was
significantly reduced in cryptorchidism (7 days), while the peak was completely
abolished by 24 hr of ischemia. Rise in the levels of oxidative stress in the
affected testis was observed identically during the initial stages. These
findings indicate that coupled with the rise in tissue oxidative stress, the
number of apoptotic /nonviable germ cells was alarmingly high (>80%) by IS
days of cryptochidism or 24 hr of ischemia. Restoration of complete
spermatogenesis following surgical repair may not be possible in such cases
because of these acute adverse effects
Synthesis and biological evaluation of l-acetyl-3-(2-acetoxy-3-substituted propyloximino) indol-2(3<i>H</i>)-ones
971-9751-Acetyl 3-oximino-indol-2
(3H)-one 2 on reaction with epichlorohydrin in acetone gave l-acetyl-3-(2,
3-epoxy propyloximino) indol-2(3H)-one 3, which, on subsequent reaction
with piperidine, pyrolidine, dicyclohexyl amine, diphenyl amine gave corresponding
Mannich base 4, which on acetylation furnishes 5a-e. All these
synthetic compounds 2, 3 and 5a-e are
screened for their
anti-microbial action, gross behavioral, toxicity, antagonism of tetrabenazine induced
ptosis, inhibition of pentobarbitone-induced narcosis and effect on blood
presure and respiration rate in suitable experimental models. Test compouds
2, 3
and 5a-e reduce MIC against B. substilis, E. coli, and C. albicans.Further,
these compounds inhibit tetrabenazine induced ptosis in mice, of which except
compound 2, all shows a ptosis score of 2 at the end of 150 and 210
min. In the test of inhibition of pentobarbitone induced narcosis all compounds
except compound 2 possess a significant decrease in sleeping time. All test
compounds inhibit the histamine-induced fall in blood pressure except compound 2.
Test compounds 5a-e have a negligible skeletal muscle contraction effect
when tested on frog's rectus abdominus muscl
Differential response of testis and serum gonadotropins to testosterone in rats treated with a gonadotropin releasing hormone antagonist or estradiol 17 beta
Adult rats treated with a GnRH antagonist (Ac D2Nal1, D4Cl Phe2, DTrp3, DArg6, DAla10 GnRH; code: 103-289-10, National Institutes of Health, USA) for 5 weeks (250 micrograms/kg b.w) showed multiple degrees of impairment and atrophy of the genital organs concomitant with decreased serum levels of testosterone, LH and FSH. Inhibition of spermatogenesis was characterized by germ cell degeneration and overall decline in different cell numbers and in particular, spermatids of any kind were completely absent. Testosterone supplementation (60 micrograms/rat/day, sc) to GnRH antagonist treated rats, for the same period, significantly elevated the weights of the sex organs, and the serum levels of hormones. Spermatogenesis was improved both qualitatively and quantitatively; albeit failed to be restored back to control levels. Treatment with estradiol 17 beta (1 microgram/rat/day) for 5 weeks had insignificant effect on spermatogenesis but the weights of the genital organs (seminal vesicles by 19% and ventral prostate by 40%) and the levels of serum hormones (LH by 24%, FSH 22% and testosterone by 25%) were otherwise reduced. Administration of testosterone either alone or in combination with estradiol 17 beta had only a marginal effect on spermatogenesis or on other reproductive parameters. The results indicate a positive shift in the response of the testis and serum levels of gonadotropins to testosterone supplementation in rats treated with either GnRH antagonist or estradiol 17 beta
Effect of STS-557 (17α-cyanomethyl 17β-hydroxy-estra-4, 9(10)-dien-3-one) on blood hormone levels, the testis, accessory sex organs and fertility of rats
Treatment with STS-557 (17α-cyanomethyl 17β-hydroxy-estra-4,9(10)-dien-3-one; 10 mg kg-1 daily s.c.) for 4 weeks induced atrophy of the seminiferous tubules in adult rats with a reduction in tubule diameter and in the number of round sperma-tids at stage VII. Elongated spermatids were not detected. Leydig cells were atrophied from the second week of treatment with a concomitant decrease in blood levels of testosterone. The blood levels of FSH and LH were reduced from the third week of treatment. The weight of the reproductive organs was reduced after STS-557 treatment. The treatment induced sterility in 50% of rats after 2 weeks of treatment but after 4 weeks none of the treated males mated. Normal fertility and normal levels of testosterone and FSH were restored after 6 weeks and LH after 4 weeks of withdrawal of treatment. All other parameters studied recovered to pretreatment levels 6 weeks after withdrawal of treatment. STS-557 could act on the pituitary-gonadal axis (reducing gonadotrophin secretion) as well as directly affecting the Leydig cells. The consequent reduction in the blood levels of testosterone in combination with reduced gonadotrophins was presumably responsible for the suppression of spermatogenesis
Protective role of cyclosporine in experimental unilateral blunt testicular trauma: evaluation by <SUP>31</SUP>P MR spectroscopy
Magnetic resonance (MR) imaging is a useful tool to study the anatomy of the testis while <SUP>31</SUP>P magnetic resonance spectroscopy (MRS) provides a non-invasive alternative method to demonstrate the metabolic status of testes. This study was designed to test whether the protective role of cyclosporine in experimental unilateral blunt testicular trauma (UBTT) could be assessed by <SUP>31</SUP>P MRS. Male Wistar rats ( n=30) aged 20 days were randomised into group I (sham surgery), group II (UBTT) and group III (UBTT and cyclosporine for 7 days). Contralateral testicles of 5 rats from each group was evaluated by <SUP>31</SUP>P MRS at 30 and 60 days of age and phosphomonoesters (PM), phosphodiesters (PD), and adenosine triphosphate (ATP) levels were measured. At 60 days of age the PM/ATP ratio was 0.32±0.08 in group I whereas it was 0.68±0.31 in the group II ( p < 0.05). Group III rats showed PM, PD and PM/ATP ratios similar to the controls. In conclusion, it is observed that UBTT causes contralateral testicular damage which could be prevented by short-term cyclosporine treatment and <SUP>31</SUP>P MRS is an excellent modality for such an evaluation