[Computed image analysis of neutrophils: alkaline phosphatase]. / Komp'iuternyi analiz izobrazheniia neitrofil'nykh leikotsitov: shchelochnaia fosfataza.

Alkaline phosphatase (AP) activity was detected under optic microscope in neutrophilic leukocyte granules and intergranular cytoplasm. Computer analysis of the image showed that activation of neutrophils in the blood of patients with purulent peritonitis was paralleled by a drastic increase in the activity of AP and its intracellular redistribution. AP granules increased in size and their capacity to conglomeration increased. The enzyme activity increased both in the granules and diffuse zone of the cytoplasm. Total area of AP granules directly correlated with the size of the zone of the enzyme diffuse-granular location.

[Computed imaging analysis of neutrophils: myeloperoxidase]lysis of. / Komp'iuternyi analiz izobrazheniia neitrofil'nykh leikotsitov: mieloperoksidaza.

Computer analysis of the cell image showed granular and diffuse activities of myeloperoxidase (MP) in the neutrophil cytoplasm. MP in the intergranular cytoplasm can be regarded as a product of secretory activity of azurophilic granules. The patterns of MP distribution in the neutrophils of normal subjects and patients with peritonitis are different. Parameters characterizing the number of MP granules in a cell, total area of granules and the zone of diffuse granular distribution of MP in combination with their optic density reflect the functional activity of neutrophils and can be used as diagnostic signs.

[Cytochemical detection of cationic proteins in blood granulocytes using amido black 10B for visual assessment and computer imaging analysis]. / Tsitokhimicheskoe vyiavlenie kationnykh belkov v granulotsitakh krovi amido chernym 10B dlia vizual'noi otsenki i komp'iuternogo analiza izobrazheniia,

Cytochemical method for selective detection of the leukocyte lysosomal and cationic proteins by Amido Black 10B at pH 8.1-8.2 is described. A much better color contrast of the cytological picture in comparison with Stable Green FCF staining facilitates visual assessment of the results and creation of TV image for computer processing of the results.

[Experimental research on the safety of the new gestagen preparation acetomepregenol]. / Eksperimental'noe issledovanie bezvrednosti novogo gestagennogo preparata atsetomepregenola.

In the experiments on mature females of 50 rats, 10 rabbits, 8 dogs it was established that a new gestagenic drug acetomepregenol was not toxic both for pregnant and nonpregnant animals. The two-month administration of the drug in the therapeutic and maximal doses did not exert the irreversible effects on the reproductive function and did not influence the embryonal and postnatal development of the offspring. A single administration of acetomepregenol in the critical periods of pregnancy was found to exert the embryotoxic effect which did not manifest itself during daily administration of the drug from the 6th through the 16th days of pregnancy.

[Pharmacology of new gestagens: derivatives of 17-alpha-hydroxyprogesterone]. / Farmakologiia novykh gestagenov--proizvodnykh 17-alpha-oksiprogesterona.

The experimental data on the pharmacological activity of the modified analogs++ of 17 alpha-hydroxyprogesterone are presented. A high gestagenic activity was shown to be related to the presence of the methyl group in position 6, the double bond in position C6-C7, the hydroxyl and acetoxy groups in position 3. Such modification of the molecule provides a high degree of the secretory degeneration of the female rabbit endometrium at any method of administration as compared with progesterone but not always provides a high level of pregnancy preservation. Among the studied compounds, mepregenol diacetate with the acetoxy++ groups in positions 3 and 17 alpha is the most active in the ability of the secretory degeneration of the endometrium. The compound served as the basis for the development of the drug acetomepregenol possessing contraceptive and therapeutic effects.

[Comparative study of the progestagenic action of 16 alpha, 17 alpha-cyclohexanoprogesterones (pregna-D'6-pentarans) when administered by different routes]. / Sravnitel'noe izuchenie progestagennogo deistviia 16 al'fa, 17 al'fa-tsiklogeksanoprogesteronov (pregna-D'6-pentaranov) pri razlichnykh putiakh vvedeniia.

A comparative study of the progestational activity of modified pentarans depending on the dose and the route of administration was carried out. It was shown that modification of the molecule of 16 alpha, 17 alpha-cyclohexanoprogesterones by introducing and additional double bond in positions 6, 7 and methyl group in position 6 provided a high gestational effect, being particularly pronounced at intramuscular administration.

[Relation of the progestagenic activity and conformation of the 17beta-acetyl side chain in the D'6-pentarane series]. / Zavisimost' progestagennogo deistviia v riadu pregna-D'6-pentaranov ot konformatsii 17beta-atsetil'noi bokovoi tsepi.

The synthesis of 2' beta-methyl-16 alpha,17 alpha-cyclohexanoprogesterone and its MM2 conformational analysis have been performed. The acetyl side chain was shown to have an unusual conformation with the torsion angle C13-C17-C20-O20 being -32.1 degrees. This conformation is by 5.4 kJ.mol-1 more stable than the usual one with the torsion angle 130.3 degrees. 2' beta-Methyl-16 alpha,17 alpha-cyclohexanoprogesterone proved to be inactive as a progestogen (pregnancy maintenance and McPhail tests). The lack of the activity may be due to the additional methyl group in D'-ring causing a change of the conformation of the 17 beta-acetyl side chain, thus hindering the formation of the conformation necessary for binding to the progesterone receptor.

[Hormonal properties of new 17 alpha-hydroxyprogesterone derivatives]. / Gormonal'nye svoistva novykh proizvodnykh 17 al'fa-oksiprogesterona.

The paper is devoted to an experimental study of the hormonal properties of two new derivatives of 17 alpha-oxyprogesterone--mepregenol monoacetate and mepregenol diacetate--for their possible use as minipills. Both compounds showed a high progestational activity which was much higher than that of progesterone and the activity of alpha-norgestrel in peroral administration. The above compounds made no inhibitory effect on hypophyseal gonadotropic function; on the contrary, they stimulated follitropine secretion. Besides, different dose-related influence of the steroids on a progesterone level was revealed: the use of small doses resulted in enhanced secretion and larger doses brought about the suppression of secretion. Thus, the new compounds of the progesterone series--mepregenol monoacetate and mepregenol diacetate--appear promising compounds for monohormonal contraception and for the management of conditions with lowered function of the corpus luteum.

[Progestagenic activity and the mechanism of the contraceptive action of mecygeprone]. / Progestagennaia aktivnost' i mekhanizm kontratseptivnogo deistviia metsigeprona.

Progestagenic activity of a modified analog of progesteron-6 alpha-methyl-cyclogexan-[1', 2', 16 alpha, 17 alpha]-pregn-4-en-3,20-dion including into mecygepron composition has been studied; its activity is proved to be 5 times as great as that of progesteron at any way of administration. Mecygepron affects processes of ovogenesis and early embryogenetic development in rats. A decreased number of washed out embryos is observed, while the number of lutein bodies specific for intact rats remains the same, decelerated rate of cleavage and increased number of unfertilized ova. In the mechanism of the changes observed an essential role plays a decreased secretion of lutropin resulting in a prolonged estrol cycle and, evidently, in intrafollicular overmaturation of the ova, which loose their ability to be fertilized. Besides, the disturbed hormonal balance under mecygepron influence can affect the character of the oviduct and uterine contents and, thus, prevent the normal development of the fertilized gametes.

[Pharmacological activity of modified analogs of steroid estrogens. Racemic 8-isoestradiol]. / Izuchenie farmakologicheskoi aktivnosti modifitsirovannykh analogov steroidnykh éstrogenov. Ratsemicheskii 8-izoéstradiol.

The authors have studied pharmacological activity of an estradiol isoanalog-8-isoestradiol. The drug has been shown to possess dissociated hormonal properties. Having a relatively high vaginotropic and antifertile activity, the drug exerts a negligible antigonadotropic effect on the pituitary and a fairly weak uterotropic action.

Pregna-D'-pentaranes - a new class of active gestagenes.

A new class of modified progesterones with an additional ring in the 16 alpha , 17 alpha-position (pregna-D'-pentaranes) are described. Compounds containing 4- and 6-membered D'-ring (D'4- and D'6-pentaranes) were synthesized by the cycloaddition of acetylene or 1,3-butadiene, respectively, to the conjugated 16-double bond of 16-dehydro-20-keto steroids. The D'3-pentarane was prepared by the addition of diazomethane to the steroidal olefin followed by decomposition of the intermediate 16 alpha , 17 alpha-pyrazoline. The D'5-pentarane was obtained by conventional contraction of cyclohexane D'-ring of the corresponding D'6-pentarane. Progestational and contraceptive activity has been investigated for these compounds. They were found to exhibit a high progestational activity in the McPhail assay and also to be active in the pregnancy maintenance test in ovariectomized rabbits. Some of the D'-pentaranes displayed a remarkable contraceptive effect in combination with mestranol.

[Contraceptive activity and mechanism of action of combinations of 6-methyl-substituted D'6-pentaranes and mestranol]. / Kontratseptivnaia aktivnost' i mekhanizm deistviia kompozitsii 6-metilzameshchennykh D'6-pentaranov i mestranola.

It has been shown in experiments on rats, mice and rabbits that 6 alpha-methyl-16 alpha, 17 alpha-cyclohexano-pregna-4-en-3, 20-dion and 6-methyl-16 alpha, 17 alpha-cyclohexano-pregna-4,6-dien-3,20-dion belonging to the series of D'6-pentaranes exhibit high contraceptive activity when combined with mestranol. The contraceptive activity of D'6-pentaranes combined with mestranol arises primarily from their inhibitory effect on luteinizing function of the hypophysis.

[Contraceptive activity and mechanism of action of combinations of a new 17 alpha-acetoxyprogesterone derivative and ethinyl estradiol]. / Kontratseptivnaia aktivnost' i mekhanizm deistviia sochetanii novogo proizvodnogo 17 al'fa-atsetoksiprogesterona i étiniléstradiola.

It was shown in experiments on rats and rabbits that a new derivative of 17 alpha-acetoxyprogesterone--mepregnol diacetate--combined with ethinyl estradiol in varied doses and ratios elicits a pronounced contraceptive effect. This steroid combination exerts neither antigonadotropic nor antiovulatory action. The changes detected in the RNA content are apparently of importance in the mechanism of the drug effect on reproduction. A role has been demonstrated of the central cholino- and adrenoreactive systems in providing the contraceptive effect of decreased doses of ethinyl estradiol and mepregnole diacetate.

[Progestagen and contraceptive activity of a 16alpha-methylene derivative of progesterone]. / Progestagennaia i kontratseptivnaia aktivnost' 16alpha-metilenproizvodnogo progesterona.

Data of experimental character reflecting the pharmacological activity of 16alpha-methylene derivative of progesterone--melengesterol acetate--are presented. A high progestagenic activity of the preparation was revealed in a series of tests, namely, the appearance of secretory changes in the uterine endometrium of infantile female rabbits and persistence of pregnancy in ovariectomized rabbits. A high contraceptive activity not accompanied by suppression of ovulation was found in administration of the preparation in low doses combined with mestranol.

[Nature of the ovulation and the state of the preimplantation fetuses in the experimental administration of hormonal and neurotropic agents]. / Kharakter ovuliatsii i sostoianie predimplantatsionnykh zarodyshei pri vvedenii nekotorykh gormonal'nykh i neirotropnykh sredstv v éksperimente.

PIP: The authors have studied the effects of hormonal and neurotopic agents on ovulation and on the fetus in the preimplantation period. The experiments were done on 100 female rats divided in 5 groups. The 1st group received megestranol in a contraceptive dosage; the 2nd group was administered half of the contraceptive dosage of megestranol; the 3d group received spasmolitin, the 4th a combination of megestranol and spasmolitin, and the 5th group served as a control. Male rats were placed with the females after 2 weeks of treatment. The time of conception was determined by the presence of spermatozoa in vaginal smears. Megestranol was found to increase the quantity of corpus luteum, while the combination of twice as much megestranol with spasmolitin did not have any effect on the corpus luteum. Within 60 hours following the fecundation the fetuses were found in all rats to be in the 2nd-4th stage. The number of normal and degenerated fetuses did not significantly differ from 1 group to the next. In the control group, 5% of the blastocysts showed signs of degeneration; this rate was 23.5% in the rats who were given the combination of spasmolitin and megestranol, and 70% in the rats who received contraceptive dosages of megestranol. These reulsts show that megestranol and combinations of megestranol and spasmolitin affect the ovulation and the development of impregnated ovules.^ieng

[Pharmacological activity of progesterone derivatives]. / Farmakologicheskaia aktivnost' nekotorykh proizvodnykh progesterona.

Tests conducted on rabbits demonstrated that the progesterone derivatives--megestol-acetate, mepregnol-diacetate, melengestrol-acetate, megestro-capronate--display a higher progestagenic action than do progesterone and pregnene. Tests with rats revealed the contraceptive action to be highest with a long-term administration of low doses of mestranol and melengestrol-acetate (ratio of 1:50), or with introduction of mestranol and megpregno-diacetate (ratio of 1:20). When used together with mestranol megestrol-capronate manifests a greater ability of prolonged action and a higher effectiveness in the pre-implantation period as compared to a combination of megestrol-acetate and mestranol.

[Change in the RNA content in the rat endometrium under the action of estrogen-megestrol and neurotropic substances]. / Izmenenie soderzhaniia RNK v éndometrii krys pri deistvii éstrogen-megestrolovykh i neirotropnykh veshchestv

The effect of the hormone-like estrogen-progestagen preparation megestranol and of megestranol-spasmolytin combination on the activity of metabolic processes in the uterine mucous membrane was studied in experiments on rats. Results of cytochemical studies showed megestranol and megestranol-spasmolytin combination to change the metabolic activity of the uterine mucous membrane resulting in a decrease in the RNA content in the epithelial cells of the endometrial glands, thereby creating conditions preventing normal implantation and development of the fertilized ovum.

PIP: The effect of the estrogen-progestagen preparation megestranol and of a megestranol-spasolytin combination on the activity of metabolic processes in the uterine mucous membranes of rats was studied. Results of cytochemical studies showed these preparations cause a change in the metabolic activity of the uterine mucous membrane resulting in a decrease in the RNA content in the epithelial cells of the endometrial glands, thereby creating conditions preventing normal implantation and development of the fertilized ovum.