• Microbiology and Biotechnology Letters
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• v.6 no.3
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• pp.121-127
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• 1978

This paper deals with investigation on the various effects of phosphodiesterase production of Streptomyces sp. and several properties of the enzyme. The results were as follows. 1) As a carbon source, sucrose was most effective PDase production when it was added. to the basal medium at 3％ concentration. 2) These enzymes were remarkably activated by $Ca^{2+}$, Co$^{2+}$ and Mn$^{2+}$ but inhibited by Cu$^{2+}$. It was observed that concentration of metal ions, 0.1％ of $Ca^{2+}$, 0.01％ of Co$^{2+}$ and 0.04％ of Mn$^{2+}$ were effective on the production of phosphodiesterase and phosphomonoesterase. 3) In case of the effect of aeration volume, 25 ml was very effective, that is, the more sufficient aeration, the better enzyme activity. Enzyme activity was to be found effective at 3％ of inoculation volume, and comparatively more effective at 2％, 4％ of inoculation volume. 4) Initial pH was 8. The enzyme activity reached to the maximum at 48 hours of cultivation time. 5) The optimum pH of phosphodiesterase was about 8 and that of phosphomonoesterase was about 9. The optimum temperature of phosphodiesterase and phosphomonoesterase was 6$0^{\circ}C$ and 5$0^{\circ}C$ respectively. respectively.

• The Journal of Pediatrics of Korean Medicine
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• v.23 no.3
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• pp.217-231
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• 2009

Objectives To evaluate that Okwada affected which factors for treatment of lung fibrosis. Methods Bleomycin induced lung fibrosis model made in mice. After Okwada lyophilized, power sample obtained and melt in distilled water. Okwada solution administered mice through oral route on 21 days after bleomycin instillation and this procedure performed once a day for 7 days. We divided by three groups; normal (control), bleomycin induced lung fibrosis without treatment (experimental), bleomycin induced lung fibrosis with treatment (treatment). On six weeks after bleomycin instillation, mice sacrificed and removed lung. We performed Western blot analysis for TGF-beta, phosphodiesterase 5A, interleukin (4,5,13) and compared therapeutic effects of Okwada. Results On western blot analysis, all normal and experimental mice detected TGF-beta, phosphodiesterase 5A, interleukin 4,5,13. The amount of band of TGF-beta, phosphodiesterase 5A, interleukin 5 in experimental and treatment group was similar. However, interleukin 4,13 of treatment group decreased compared with experimental group. Conclusions Okwada would be effected the lung fibrosis through suppression of interleukin 4,13.

• YAKHAK HOEJI
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• v.41 no.5
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• pp.547-553
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• 1997

The purpose of this investigation was to determine the inhibition on $Na^+,\;K^+$-ATPase, cyclic AMP phosphodiesterase and platelet activation by marine sterols isolated from octocorals. Three marine polyhydroxysterols, 7${\alpha},\;8{\alpha}-epoxy-3b{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholestane (1),\;24-methyl-7{\alpha},\;8{\alpha}-epoxy-3{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholest-22-ene (2),\;and\;7{\alpha},\;8{\alpha}-epoxy-3{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholest-22-ene (3)$, were isolated from the Gorgonian Acabaria undulata. Five marine sterols(compound 4, 5, 6, 7, 8) were isolated from the soft coral Alcyonium gracillimum. Three marine polyhydroxysterols (1, 2, 3) and pregna-1. 20-diene-3-one (8) exhibit a potent inhibitory effect on rabbit platelet aggregation induced by collagen and thrombin. Those polyhydroxysterols also exhibit a potent inhibitory effect on cyclic AMP phosphodiesterase. Compound 6 with an unusual cyclic enolether exhibit a inhibitory effect on $Na^+,\;K^+$-ATPase.

• Archives of Pharmacal Research
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• v.23 no.5
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• pp.471-476
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• 2000

DA-8159, a new phosphodiesterase 5 inhibitor, was assessed for its erectogenic potential by a penile erection test in rats, the relaxation of isolated rabbit corpus cavernosum (CC), and estimation of the intracavernous pressure (ICP) in the anesthetized dog. Oral administration of DA-8159 (0.3 to 1 ${\mu}g/kg$ ) increased the number of erections in rats with increasing dosage, with the highest penile erection index at 10 ${\mu}g/kg$ DA-8159 induced the relaxation of phenylephrine (PHE)-induced contractions in the rabbit CC and decreased the $IC_{50}$ of the nitric oxide donor sodium nitroprusside (SNP) in a dose-dependent fashion. In pentobarbital-anesthetized dogs, the intravenous administration of DA-8159 (1~300 ${\mu}g/kg$ ) potentiated the increase in ICP induced by the intracavernosal SNP in a dose-related manner. These findings suggest that DA-8159 has significant therapeutic potential in the treatment of erectile dysfunction.

• The Korean Journal of Zoology
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• v.29 no.2
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• pp.79-85
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• 1986

The purpose of the present experiment is to make certain the exsistence of cAMP phosphodiesterase (PDE) in mouse oocytes and confirm its possible role on meiotic resumption. The results showed two types of cAMP in the oocytes with different Michaelis constants (Km) with specific maximum (Vmax); The Km and Vmax of one of two types of PDE were estimated at $0.14 \\pm 0.01 \\muM$ and $0.42 \\pm 0.07$ fmol cAMP hydrolyzed/oocyte/minute, and the other at $14.5 \\pm 2.0 \\muM$ and $2.2 \\pm 0.5$ fmol cAMP hydrolyzed/oocyte/minute. cAMP hydrolysis by PDE was reversibly inhibited in vitro by presence of theophylline or isobutyl-methyl-xanthine (IBMX), which is well known as an inhibitor of oocyte maturation. Consequently, it can be assumed that maturation of oocyte is affected by the high level of intracellular cAMP, and its level is well maintained by presence of PDE inhibitor, such as theophylline and IBMX.

• Archives of Pharmacal Research
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• v.26 no.8
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• pp.612-619
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• 2003

In this study, we evaluated the effects of oral administration of DA-8159, a selective phosphodiesterase-5 inhibitor, on the development of pulmonary hypertension (PH) induced by monocrotaline (MCT). Rats were administered either MCT (60 mg/kg) or saline. MCT-treated rats were divided into three groups and received orally administered vehicle, or 1 mg/kg or 5 mg/kg of DA-8159, twice a day for twenty-one days. The MCT group demonstrated increased right ventricular weights, medial wall thickening in the pulmonary arteries, myocardial fibrosis and the level of plasma cyclic guanosine monophosphate (cGMP), along with decreased body weight gains. However, DA-8159 markedly and dose-dependently reduced the development of right ventricular hypertrophy and medial wall thickening. DA-8159 also amplified the increase in plasma cGMP level and significantly increased the level of lung cGMP, compared with the MCT group. Although the body weight gain was still lower from the saline-treated control group, DA-8159 demonstrated a significant increase in body weight gains, in both 1 mg/kg and 5 mg/kg groups, when compared with the MCT group. In myocardial morphology, MCT-induced myocardial fibrosis was markedly prevented by DA-8159. These results suggest that DA-8159 may be a useful oral treatment option for PH.

• Clinical and Experimental Reproductive Medicine
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• v.43 no.1
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• pp.26-30
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• 2016

Objective: We aimed to investigate the prevalence of erectile dysfunction (ED) and the usage of phosphodiesterase type 5 (PDE5) inhibitors for ED treatment in infertile couples. Methods: A total of 260 male partners in couples reporting infertility lasting at least 1 year were included in this study. In addition to an evaluation of infertility, all participants completed the International Index of Erectile Function (IIEF)-5 questionnaire to evaluate their sexual function. The participants were asked about their use of PDE5 inhibitors while trying to conceive during their partner's ovulatory period and about their concerns regarding the risks of PDE5 inhibitor use to any eventual pregnancy and/or the fetus. Results: Based on the IIEF-5 questionnaire, 41.5% of the participants (108/260) were classified as having mild ED (an IIEF-5 score of 17-21), while 10.4% of the participants (27/260) had greater than mild ED (an IIEF-5 score of 16 or less). The majority (74.2%, 193/260) of male partners of infertile couples had a negative perception of the safety of using a PDE5 inhibitor while trying to conceive. Only 11.1% of men (15/135) with ED in infertile couples had used a PDE5 inhibitor when attempting conception. Conclusion: ED was found to be common in the male partners of infertile couples, but the use of PDE5 inhibitors among these men was found to be very low. The majority of male partners were concerned about the risks of using PDE5 inhibitors when attempting to conceive. Appropriate counseling about this topic and treatment when necessary would likely be beneficial to infertile couples in which the male partner has ED.

• Applied Biological Chemistry
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• v.22 no.4
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• pp.210-216
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• 1979

RNA degrading bacteria were isolated from soil of Korea. One strain (no. JSC-114), having strong 5'-phosphodiesterase activity, was identified as belonging to the genus Streptomyces on the basis of taxonomic characteristics. The optimum conditions of 5'-phophosdiesterase production were found at $30^{\circ}C$ for 4 day in a medium containing 4.5% of soluble starch, 0.15% of peptone, 0.6% of yeast extract, 0.1% of $MgSO_4{\cdot}7H_2O$, 0.01% of $CaCl_2{\cdot}2H_2O$, 0.25% of $KNO_3$, and 0.5% of $KH_2PO_4$(pH 7.0). The maximum production rate of 5'-nucleotides from yeast RNA was 95% at $40-45^{\circ}C$ for 4hrs, and the products were identified as 5'-IMP, 5'-GMP, 5'-CMP and 5'-UMP(5.5 : 5.0 : 4.9 : 5.0).

• Korean Journal of Food Science and Technology
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• v.34 no.5
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• pp.867-872
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• 2002

This study was performed to investigate the optimum process conditions for manufacturing yeast extract from waste brewer's yeast using various enzymes. Contents of IMP, GMP, free amino acids, and crude protein of yeast extracts were measured by enzymes treatment. Crude protein contents of yeast extracts subjected to cell wall digestion enzyme treatment were 21.1, 33.6, and 28.0% for the control grouup, glucanase (0.5%, 12 h), and tunicase (1%, 18 h), respectively. Crude protein contents of yeast extracts subjected to protease treatment were 22.0, 30.8, and 29.8% for control group, bromelin (1%, 3 h), and protamex (1%, 3 h), respectively. Crude protein content of yeast extract subjected to glucanase and protamex mixed treatment was 34.4%. The total contents of IMP and GMP of yeast extracts subjected to G+P+A (glucanase+phosphodiesterase+adenyldeminase) and G+Pro+P+A (glucanase+protamex+phosphodiesterase+adenyldeaminase) treatments were 1,066 and 1,047 mg/100 g, respectively. The content of free amino acids of yeast extract was the highest (2,302 mg/100 g) in G+Pro+P+A treatment. Optimum concentration and process condition of enzyme treatment to obtain yeast extract with high IMP, GMP, and free amino acid content were in the order of glucanase (0.5%, 12 h), protamex (1%, 3h), phosphodiesterase (0.1%, 3 h) and adenyldeaminase (1%, 1.5 h) treatments.

• YAKHAK HOEJI
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• v.41 no.3
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• pp.345-351
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• 1997

The purpose of this investigation was to determine the inhibition of $Na^+,\;K^+$-ATPase, cyclicAMP phophodiesterase and platelet activation by secondary metabolites isolated from mar ine organisms. The secondary metabolites were isolated and identified as six diterpenoids(1 : astrogorgin, 2 : ophirin, 3 : calicophirin B, 4, 5 and 6 : cladiellin) from the dichloromethane extract of Muricellajsp., four ceramides(1,2,3, and 4) from Acabaria undulata and three antharaquinones(1,2 : crysophanol, and 3 : physcion) from Urechis unicintus. The results demonstrated that diterpenoids(2,3, and 4) showed the inhibition of cyclicAMP phosphodiesterase, and ceramides(1,3, and 4) showed the inhibition of cyclicAMP phosphodiesterase and thrombin(0.1 units/ml)-induced aggregation of washed rabbit platelet, and anthrapuinones((1,2, and 3) showed the inhibition of $Na^+,\;K^+$-ATPase. Among the anthraquionones, 1,2-dimethoxy-3-methyl-8-hydroxy-anthraquinone(1) showed the inhibition of collagen(1.0 ${\mu}g$/ml)-induced aggregation in a concenration-dependent manner with IC50 value of 42.8 ${\mu}g$M.