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An oxovanadium compound obtained from VO(OEt)Cl2 and AgOTf or MesSiOTf efficiently induced dehydrogenative aromatization of α,β-unsaturated cyclohexenones to give aryl ethyl ethers in good yields.

The influence of follicular maturation on progesterone production by isolated granulosa cells of the Japanese quail was examined. After determination of the concentrations of ovine LH (oLH) and dibutyryl cyclic AMP for the maximum response, the amount of progesterone produced during incubation at 40° for 3 hr with or without oLH or dibutyryl cyclic AMP was measured in granulosa cells isolated from follicles at 71 to 1 hr before ovulation. When cells were stimulated with oLH, we found a marked increase in responsiveness between 23 and 21 hr before ovulation. The degree of responsiveness of cells obtained prior to this period was far less than that of cells of the latter period. The amount of progesterone produced by oLH increased between 21 and 17 hr before ovulation, followed by a transient decrease. Maximum responsiveness to oLH was obtained at 5 hr before ovulation. The changes in responsiveness of cells to dibutyryl cyclic AMP were essentially the same as those to oLH.

During 3hr of incubation, the production of progesterone in the follicle wall from the largest preovulatory follicle (F1) of the Japanese quail was stimulated by ovine LH or dibutyryl cyclic AMP. The follicle walls from the second largest and the third largest follicles (F2 and F3) did not produce appreciable amounts of progesterone, while the granulosa cells isolated from these follicles produced significant amounts of progesterone. By incubating progesterone with the cell-free homogenates of the theca layer in the presence of NADPH, it was clarified that the metabolic rates of progesterone in the theca layer of F2 and F3 were higher than that of F1. These results suggested that in the quail follicles, progesterone is produced in the granulosa layer but the theca layers of the small follicles metabolize progesterone, so that only F1 secretes progesterone.

D. Ornstein and others proved important isomorphism theorems for a large class of automorphisms, i.e. measure preserving transformations. However, it is also interesting to explicitely determine an isomorphic mapping in each concrete case. R. Adler and B. Weiss [1] explicitely constructed an isomorphism between an ergodic group automorphism of a 2-dimensional torus and a Markov automorphism. Y. Takahashi [8] gave an isomorphism between a /9-automorphism and a Markov automorphism. The crucial point of their argument lies in the fact that the metrical entropy coincides with the topological entropy for these automorphisms. Using this fact and Parry's result [3], they showed that the representation mapping of the automorphism in consideration to a Markov subshift (of a symbolic dynamics) is actually an isomorphism in each case. In this paper, we will explicitely construct an isomorphism of a piecewise linear transformation (a generalization of /^-automorphism) to a Markov automorphism. Since the metrical entropy of such a transformation does not always attain its topological entropy, we cannot use the method mentioned above, so instead of topological entropy we use free energy as our main tool. In § 1 we define the free energy of a Markov subshift and show under certain conditions that a shift invariant measure with the minimal free energy is unique. This is a generalization of Parry's result about topological entropy [3]. In § 2 we define a piecewise linear transformation and investigate its properties. In § 3 we construct an isomorphic mapping from a piecewise linear transformation to a Markov automor

[14C] Progesterone was incubated in vitro with cell-free homogenates of GRS/A mouse mammary tumor and normal mammary gland in the present of NADPH. In the mammary tumor, 20α-hydroxy-4-pregnen-3-one, 5α-pregnane-3,20-dione, 20α-hydroxy-5α-pregnan-3-one, 3α-hydroxy-5α-pregnan-20-one, 5α-pregnane-3α,20α-diol and 4-pregnene-3α,20α-diol were identified as the metabolites. In the normal mammary gland, 20α-hydroxy-4-pregnen-3-one and 4-pregnene-3α,20α-diol were identified as the major metabolites, besides the 5α-reduced metabolites as minor ones. After establishment of the metabolic pathways of progesterone, 5α-reductase, and 3α- and 20α-hydroxysteroid dehydrogenases were suggested to be involved in the progesterone metabolism in these tissues. Activity of the 5α-reductase in the mammary tumor was higher than that in the normal mammary gland, but ovariectomy resulted in the reduction of this enzyme activity in the mammary tumor to the level of the normal mammary gland. By estradiol-17β-benzoate administration to ovariectomized tumor-bearing animals, 5α-reductase activity was restored to the level of the mammary tumor of intact animals.

1. 1. During 3 hr of in vitro incubation, the production of progesterone by granulosa cells from the largest preovulatory follicle (F1) of the Japanese quail was stimulated by 1 mM dibutyryl cyclic AMP. 2. 2. On the other hand, the progesterone production of the granulosa cells from the second largest and the third largest follicles (F2 and F3) were autonomous, since these cells produced significant amounts of progesterone in the incubation without dibutyryl cyclic AMP, and addition of dibutyryl cyclic AMP did not further stimulate the progesterone production. 3. 3. Cycloheximide or puromycin inhibited not only the progesterone production of the granulosa cells of F1, which was due to the action of dibutyryl cyclic AMP, but also the autonomous progesterone production of the granulosa cells of F2. 4. 4. These results suggest that in the quail ovary, the labile protein may play a role for the progesterone synthesis, but is not a mediator for the action of cyclic AMP.

ニワトリの人為的な性転換の方法を検討するために,発生初期胚への精巣の移植が雌胚の生殖器官に及ぼす影響を調べた。孵卵13日目の白色レグホーン種の雄胚から得た精巣を,孵卵3日目の名古屋種雄と横斑プリマスロック種雌とのF1の受精卵の胚体外体腔に移植した。移植した精巣に対する血管の新生は,移植後2日目に観察した。移植10日目または13日目に胚の生殖器官を観察したところ,血管の新生が認められた雌胚のうち約2/3ではミューラー管が左右ともに消失しており,また左右性腺の萎縮の程度はさまざまであった。強度の萎縮が認められた性腺には精巣様の管状組織が観察された。萎縮した性腺のテストステロンおよびエストラジオール-17β産生能をin vitroで測定した結果,萎縮が軽度の場合は正常な同時期の卵巣と比較して有意な差はなかった。しかし,萎縮が強度の場合には,卵巣の産生量より有意に少なくなっており,同時期の正常な精巣の産生量とほぼ同等であった。これらの結果から,13日齢の精巣はミューラー管の萎縮を促す物質を分泌することを示すとともに,未分化の性腺に作用してこれを精巣様に分化させるような物質を分泌することが示唆された。

プロゲステロンは,分娩に伴なう泌乳の開始を抑制しているホルモンと考えられている.本研究は,プロゲステロンおよびその生理的代謝産物である20α-ヒドロキシ-4-プレグネン-3-オンや5α-プレグナン-3,20-ジォンが,乳線の腺胞腔拡張にどのような効果をもっているかを調べるため,マウス乳線をこれらのステロイドや泌乳に必須と考えられている他のホルモンを含む合成培養液中で器官培養し,乳腺組織像の変化を観察した.乳腺をインスリンとコルチゾールを含む培養液中で培養すると腺胞腔の拡張がみられたが,その中に乳汁様分泌物が現われるためにはこれらのホルモンの他にプロラクチンが必要であった.これら3種類のホルモンにプロゲステロンを添加しても腺胞腔に乳汁様分泌物が認められる割合に変化はなかった.しかし,腺胞腔の大きさはプロゲステロンの添加量を増すにしたがって縮小した.このような効果はプロゲステロンばかりでなく,20α-ヒドロキシ-4-プレグネン-3-オンにも認められたが,5α-プレグナン-3,20-ジオンには認められなかった.これらの結果は,プロゲステロンおよび20α-ヒドロキシ-4-プレグネン-3-オンが,コルチゾールの腺胞腔拡張作用に対する拮抗作用をもつことを示しており,これがプロゲステロンによる乳汁分泌開始抑制機構の一部をなしているのかも知れない.

The purpose of this paper is to study a continuous spin system by introducing the relative free energy* which plays a role of the free energy in discrete spin systems. Although the usual free energy is a very important functional,it can be available to only identically distributed 2-spin lattice systems. About such systems, refer to Holley [1], [2]. On the other hand, our relative free energy enables us to deal with spin systems with state space not necessarily discrete nor identically distributed. In Section 3, we consider a 1-dimensional lattice spin system with continuous state space to show that the relative free energy does not increase with time and especiallyit strictly decreases if the initial state is not Gibbsian; this is one of the main results of this paper. From this fact, moreover we conclude that the time evolution of any shift invariant non-Gibbsian state converges to an equilibrium state. The precise definitions of the relative free eners-v et al are erivenin Section 2.

Collagenase activity was determined at various stages before and after ovulation in the stigma and non-stigma region of quail follicle. There were no appreciable changes in the activity in both regions until the time just before ovulation. On the other hand, the stigma region showed a remarkable increase in the activity just after ovulation. In addition, changes in collagenase activity were well coincident with those in the rate of collagen degradation in the follicles after ovulation, which indicated that an increased collagenase activity may be able to cause the degradation of collagen in vivo. These results suggest that collagenase involves in the rupture of follicles.

The activity of 17 alpha-hydroxylase, a key enzyme for progesterone metabolism in avian follicles, was measured in cell-free homogenates of isolated theca cells of Japanese quail. Kinetic studies revealed that differences in enzyme activity in the largest and the second largest follicles were mainly due to differences in Vmax values. In order to investigate the mechanism of regulation of 17 alpha-hydroxylase activity, quail were hypophysectomized at various time periods during the ovulatory cycle, and 17 alpha-hydroxylase activity in theca homogenates was measured 4 h after surgery. Hypophysectomy at 8 h before the predicted time of ovulation, which is the time when the preovulatory luteinizing hormone (LH) surge is initiated, resulted in a significant decrease in enzyme activity. In contrast, activity was increased when the pituitary was removed 20 h before ovulation. Hypophysectomy 24 h before ovulation had no effect on enzyme activity.

A high-power circulator at 915 MHz has been developed. This three-port waveguide circulator has a power-handling capability of 30 kW CW and an insertion loss of 0.1 dB. The high-power circulator is useful for protecting high-power microwave sources from reflected power. A high-power microwave system describing the design of the circulator, and giving the results of preliminary experiments in breaking concrete and rock are presented.

Two steroidal allyl alcohols, 4-pregnene-3α,20α-diol and 4-androstene-3α,17β-diol, were respectively identified as the metabolites of progesterone and testosterone produced in vitro by normal mammary tissue of rats (Sprague-Dawley strain) and mice (KA2 and GRS/A strains). In a 9,10-dimethyl-1,2-benzanthracene-induced tumour of the rat, however, no formation of these allyl alcohols was found. In a pregnancy-dependent tumour of the mouse (GRS/A strain), small amounts of 4-pregnene-3α,20α-diol were detected, though 5α-reduced steroids were obtained as the major metabolites. From these results, it was concluded that the predominant pathway of steroid metabolism in normal mammary tissue was different from those in the experimental tumours. In the pregnancy-dependent tumour of the GRS/A mouse, 5α-reductase activity was reduced by ovariectomy of the tumour-bearing animal, but remained unchanged by oestrogen treatment immediately after ovariectomy.

Cyclic ketones underwent ring-opening oxygenation on treatment with VO(OEt)Cl2 in alcohol under oxygen to give the corresponding keto ester or diesters depending on the substituent at 2-position. This system was applicable to a catalytic reaction.

After incubation of [4-14C]progesterone with cell-free homogenates of 9,10-dimethyl-1,2-benzanthracene (DMBA)-induced mammary tumor of rats, 20 alpha-hydroxy-4-pregnen-3-one, 5 alpha-pregnane-3,20-dione, 20 alpha-hydroxy-5 alpha-pregnan-3-one, 3 alpha-hydroxy-5 alpha-pregnan-20-one, and 5 alpha-pregnane-3 alpha, 20 alpha-diol were identified as the metabolites. In normal mammary tissue, however, 4-pregnene-3 alpha-diol was isolated in addition to 5 alpha-reduced, and 3 alpha- and 20 alpha-hydroxy metabolites. When radioactive testosterone was employed as a substrate, 5 alpha-dihydrotestosterone and 5 alpha-androstane-3 alpha, 17 beta-diol were obtained as the metabolites of the mammary tumor. In the normal mammary gland, only 4-andorstene 3 alpha, 17 beta-diol was formed as its metabolite. Although the enzyme activities relevant to the metabolism varied among the tumor examined, the activity of 20 alpha-hydroxysteroid dehydrogenase in the mammary tumor was significantly lower than that in the normal mammary gland, whereas the activity of 5 alpha-reductase was higher in some of the mammary tumors than in the normal gland. The 5 alpha-reductase activity in the normal mammary gland was mostly localized in the crude microsomal fraction, whereas the same enzyme activity in the tumor was detected in all the organelle fractions. The activities of 20 alpha-hydroxysteroid dehydrogenase and NADPH-linked 3 alpha-hydroxysteroid dehydrogenase were found mainly in the cytosol fractions of the tumor and the normal tissue. The NADH-linked 3 alpha-hydroxysteroid dehydrogenase activity was detected only in the cytosol fraction of the normal mammary gland, but in the tumor studied, the activity of this enzyme was detected in all the subcellular fractions examined.

A two-step procedure employing affinity chromatography has been used to purify rat ovary 20α-hydroxysteroid dehydrogenase. The initial step in the procedure involved ion exchange chromatography of ovarian cytosol on agarose-multichain (poly- dl -alanine-poly- l -lysine). In the second step, the effluent from the first column was adsorbed on agarose-multichain (poly- dl -alanine-poly- l -lysine) to which 11α-hydroxyprogesterone hemisuccinate had been coupled. Adsorbed enzyme was eluted with alkaline buffer at room temperature. The two-step procedure achieved a 250-fold purification of enzyme with a recovery of 34%.

When [4–14C]pregnenolone was aerobically incubated in vitro in the presence of NAD+ and NADPH with cell-free homogenates of testicular tissue of adult domestic goats (Capra hircus), progesterone, 17α-hydroxypregnenolone, 17α-hydroxyprogesterone, 17α,20α-dihydroxy-4-pregnen-3-one, dehydroepiandrosterone, androstenedione and testosterone were identified as its known metabolites. Time-course studies on this metabolism showed that the production of 17α,20α-dihydroxy-4-pregnen-3-one and testosterone constantly increased up to the end of incubation, suggesting that these are both end-products of pregnenolone metabolism in this system. The other metabolites behaved as intermediates and were ultimately converted, in part, to testosterone by the testicular homogenates, indicating that testosterone was synthesized through both 4-ene and 5-ene-pathways. Furthermore, besides these metabolites, 5-pregnene-3β,17α,20α-triol was also identified as an intermediary metabolite, formed from pregnenolone through 17α-hydroxypregnenolone in the presence of NADPH, and further convertible into 17α,20α-dihydroxy-4-pregnen-3-one by the microsomal fraction and into 17α-hydroxypregnenolone by the cytosol fraction in the presence of NAD+ and NADP It was not, however, significantly transformed into C19-steroids. Furthermore, 17α,20α-dihydroxy-4-pregnen-3-one, which was formed either from 5-pregnene-3β,17α,20α-triol or from 17α-hydroxyprogesterone, remained almost unchanged without conversion to C19-steroids when incubated with the caprine testicular homogenates.

The cell-free homogenates of the theca layers and granulosa layers of quail follicles were incubated at 39 degrees C with 14C-labeled steroids in the presence of NADPH. At the end of incubation, radioactive steroids were extracted and analyzed by thin-layer chromatography. When radioactive progesterone was employed as the substrate, 17 alpha-hydroxyprogesterone and androstenedione were obtained as the metabolites. 17 alpha-Hydroxylase activity, estimated from the amounts of these two metabolites, was high in the theca layers of the second largest (F2) and the third largest (F3) follicles. The theca layer of the largest follicle (F1) and the granulosa layers of all three follicles were essentially devoid of this enzyme activity. The activity of C17-20 lyase was estimated from the amount of androstenedione that was obtained as a sole metabolite in the incubation of radioactive 17 alpha-hydroxyprogesterone. This enzyme showed a tissue distribution similar to 17 alpha-hydroxylase. When radioactive androstenedione was used as the substrate, testosterone, 5 beta-androstane-3,17-dione, and 3 beta-hydroxy-5 beta-androstan-17-one were identified as the metabolites. 17 beta-Hydroxysteroid dehydrogenase activity, estimated from the amount of testosterone, was higher in the granulosa layers than in the theca layers. On the other hand, 5 beta-reductase activity, estimated from the sum of 5 beta-androstane-3,17-dione and 3 beta-hydroxy-5 beta-androstan-17-one, was almost equally distributed in the two layers. In order to investigate the changes in the enzyme activities during the ovulatory cycle, birds were killed at various times before the predicted ovulation of F1. When the 17 alpha-hydroxylase activity was estimated in the cell-free homogenates of the theca layers, peaks in the activity were observed 32, 42, 54, and 66 h before ovulation of F1. There was a small peak 18 h before ovulation, and activity then started to decrease. The change of C17-20 lyase activity during the cycle was completely parallel with that of 17 alpha-hydroxylase activity.

Cyclic ketones underwent ring-opening oxygenation on treatment with VO(OEt)Cl2 in alcohol under oxygen to give the corresponding keto ester or diesters depending on the substituent at 2-position. This system was applicable to a catalytic reaction.