A multicentric study with arteether in patients of uncomplicated falciparum malaria.

Two hundred and sixty seven patients of uncomplicated P. falciparum malaria completed study in a multicentric phase III clinical trial of Arteether. Arteether was given intramuscularly in a dose of 150 mg daily for three consecutive days. Each patient was followed upto 28 days of alpha, beta arteether therapy. The cure rate was 97% with fever clearance time between 1-7 days (24-168 hours) and parasite clearance time between 1-3 days (24-72 hours). Parasite reappearance rate was found to be 3% and reported at only three of the centres. Following the treatment no adverse effect was observed on haematological, biochemical and vital clinical parameters.

Bioactivity of marine organisms: Part VIII--Screening of some marine flora of western coast of India.

Methanolic extracts of 31 botanically identified species of marine flora, collected from Gujarat Coast, have been screened for a wide range of biological activities. Of these, 3 extracts showed anti-implantation, 2 had antiviral, 2 showed hypotensive, 1 had anti-inflammatory while 12 extracts showed diuretic activities. The antiviral activity; against EMCV, was confirmed in one alga. The active principles and results of these studies are reported.

Determination of proteins secreted by growing rat decidual cells in vitro.

Proteins secreted by rat decidual cells while growing in culture medium were monitored on gel electrophoresis. It was done by assuming that outgrowing cells in vitro mimic differentiated endometrial stromal tissue in vivo following attachment of embryo. The decidual cells were obtained from implantation swellings of day 10 pregnant rats, maintained in serum free medium and the cell dependent protein profile was analysed after 48 hr on single dimensional polyacrylamide gel electrophoresis (SDS-PAGE). The proteins identified were in molecular weight range of 29, 43 and 66 kDa respectively. The result indicated involvement of the differentiated stromal cells in secreting these low molecular weight proteins.

Post-coital contraceptive efficacy of the seeds of Nigella sativa in rats.

Hexane extract of the seeds of Nigella sativa L. prevented pregnancy in Sprague-Dawley rats treated orally at 2 g/kg daily dose on days 1-10 post-coitum. Significant antifertility activity was also observed in its column fractions and subfractions. At contraceptive dose, the active hexane extract exhibited only mild uterotrophic activity comparable almost to 0.002 mg/kg dose of 17 varies; is directly proportional to-Ethinylestradiol, but was devoid of any estrogenicity in the immature rat bioassay.

Diagnostic and prognostic significance of serum and tissue trace elements in breast malignancy.

50 cases of breast malignancy constituted the study group. 26 age and sex matched formed the control group. Serum and tissue trace element viz copper, zinc, selenium and molybdenum levels were estimated by atomic absorption photometry. The study group showed significant hypercupremia and molybdenemia, hypozincaemia and hyposeleniamia. The reversal of trend was documented after therapy. The tissue level of copper and molybdenum was high and zinc and selenium was low. An association between serum and tissue level of trace element, stage, histological differentiation was observed. It was postulated that levels of trace elements may help in diagnosis and prognosis of disease.

CDRI-85/287: studies on competition to estrogen binding sites in the immature rat uterus.

Ability of compound CDRI-85/287, a new nonsteroidal antiestrogen with negligible inherent estrogenicity, to inhibit uptake of 3H-estradiol (3H-E2) by the immature rat uterus in vivo was investigated. Different doses of 85/287 were administered either intraperitoneally 30 min before 3H-E2 or orally 1 and 6 hr before 3H-E2. A dose dependent inhibition in 3H-E2 uptake was observed after administration of the compound by either route and was 69% at 50 micrograms/rat ip dose and 80% at 2.5 mg/kg po dose. In in vitro competitive binding assay, however, the compound showed poor affinity (RBA 0.42% of estradiol-17 beta) for cytosolic estrogen receptors. Considering the potent anti-estrogenic as well as anti-implantation efficacy of the compound, its action in vivo appears to be mediated via its active metabolite(s).

Duration of antiestrogenecity of compound CDRI-85/287: a new orally active nonsteroidal antiimplantation agent.

Duration of antiestrogenic and antiimplantation action of CDRI-85/287, (2-(4-(2-N-piperidino)ethoxy phenyl)-3-phenyl(2H)benzo(2)pyran), was studied in rat. Pretreatment of ovariectomized immature rats with this compound caused translocation of cytoplasmic estrogen receptor (ER) to the nucleus and a marked depletion of cytoplasmic ER pool resulting in a nonresponsive state of the uterus to subsequent estrogen administration until day 4. While in rats pretreated with estradiol, increased cytoplasmic ER level made the uterus responsive to a second injection of estrogen. In the delayed implantation model, 85/287 pretreated rats were given estrone on days 4, 5 or 6 post-antiestrogen treatment. No implantations were observed after estrone administration on day 4, but were present when estrone was given on days 5 or 6. Summation of these results suggests the duration of action of 85/287 to be 3-4 days in rat.

Effect of centchroman and tamoxifen on protein patterns of fallopian tubes of rhesus monkeys, Macaca mulatta.

To study the effect of centchroman and tamoxifen on estrogen-dependent proteins of fallopian tubes of rhesus monkey, these antiestrogens were given with and without estradiol to ovariectomized monkeys. In absence of estradiol, both the compounds induced the synthesis of 130 and 95 K proteins. Concentration of 85 K protein was also increased markedly. These compounds, however, suppressed the estrogen stimulated synthesis of 130 K protein when administered with estradiol. The results show that both centchroman and tamoxifen possess estrogen agonistic as well as antagonistic properties and 130 K protein can be used as a marker protein to study estrogen action and for screening of antiestrogenic compounds in a primate model.

Effect of prolonged centchroman treatment on pituitary gonadotrophic activity in rhesus monkeys.

Daily oral administration of antiestrogen centchroman at 6.25, 12.5 and 25 mg/kg doses to adult female rhesus monkeys continuously for one year caused no significant effect on their total pituitary gonadotrophin content as evidenced by an almost similar extent of uterine weight gain, premature opening of vagina and cornification of vaginal epithelium in immature female mice treated with pituitary homogenates from control and centchroman treated monkeys.

Trace elements in the endometrium of infertile women.

Some essential trace elements were estimated in endometrium of regularly menstruating fertile women and in women with infertility due to cervical factors. The distribution of the trace elements zinc, copper, iron, selenium and manganese at any particular phase of cycle remains more or less semilier between control (i.e. fertile) and infertile (primary and secondary) subjects.