• Applied Biological Chemistry
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• v.4
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• pp.11-16
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• 1963

(1) The 30 strains of Penicillia and the 52 strains of Aspergilli have been screened for their producibility of 5'-Phosphodiesterase, and Penicillium sclerotiorum 7321, Penicillium sp M-11 and Penicillium citrinum UV-mutant 2032-72 were selected as having high 5‘-Phosphodiesterase activity. (2) Using the wheat bran medium the 5‘-Phosphodiesterase production was reached at maximum state by the plate culture for 10 days at $30^{\circ}C$ (3) The optimum conditions of the 5'-Phosphodiesterase activity of Penicillium sclerotiorum 7321 and Penicillium sp M-11 were pH 4.0 at $62.5^{\circ}C$, while the optimum condition of the 5'-Phosphodiesterase activity of Penicillium citrinum UV-mutant 2032-72 was pH 5.0 at $50^{\circ}C$.

• Applied Biological Chemistry
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• v.13 no.2
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• pp.111-129
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• 1970

As a series of studies on the nucleic acids and their related substances 210 samples were collected from 76 places such as farm soil, compost of heap, nuruk and meju to obtain microbial strains which produce 5'-phosphodiesterase. From these samples total of 758 strains were isolated by the use of dilution pour plate method. For all isolated strains primary screening of the productivity of RNA depolymerase was performed and useful strains with regard to 5'-phosphodiesterase productivities were identified. For these useful strains optimum condition, the effect of various compounds on the activity of 5'-phosphodiesterase, and the optimum condition for enzyme reaction were discussed. The quantitative of 5'-mononucleotides produced by the action of 5'-phosphodiesterase was performed using anion-exchange column chromatography and their identified was done by paper chromatography, thinlayer chromatography, ultra violet spectrophotometry, and characteristic color reaction using carbazole and schiff's reagent. (1) Penicillium citreo-viride PO 2-11 and Streptomyces aureus SOA 4-21 from soil were identified as a potent 5'-phosphodiesterase producing strains. (2) Optimum culture conditions for Penicillium citreo-viride PO 2-11 strain isolated were found to be pH 5.0 and $30^{\circ}C$, and the optimum conditions for enzyme action of 5'-phosphodiesterase were pH 4.2 and $60^{\circ}C$. Best carbon source for the production of 5'-phosphodiesterase was found to be sucrose and ammonium nitrate for nitrogen source. Addition of 0.01% corn steep liquor or yeast extract exhibited 20% increase in the amount of 5'-phosphodiesterase production compared to the control. 5'-phosphodiesterase produced by this strain was activated by $Mg^{++},\;Ca^{++},\;Zn^{++},\;Mn^{++}$ and was inhibited by EDTA, citrate, $Cu^{++},\;CO^{++}$. 5'-phosphodiesterase produced 5'-mononucleotide from RNA at a rate of 65.81%, and among the 5'-mononucleotides accumulated 5'-GMP only was found to have flavorous and the strain was also found lack of 5'-AMP deaminase. Productivity of flavorous 5'-GMP was found to be 186.7mg per gram of RNA. (3) Optimum culture canditions for the isolated Streptomyces aureus SOA 4-21 strain were pH 7.0 and $28^{\circ}C$, and the optimum conditions for the action of 5'-phosphodiesterase were pH 7.3 and $50^{\circ}C$. The best carbon source for 5'-phosphodiesterase production was found to be glucose and that of nitrogen was asparagine. Addition of 0.01% yeast extract exhibited increased productivity of 5'-phosphodiesterase by 40% compared to the non-added control. 5'-phosphodiesterase produced by this strain was activated by $Ca^{++},\;Zn^{++},\;Mn^{++}$ and was inhibited by citrate, EDTA, $Cu^{++}$. It was also found that the strain produce 5'-AMP deaminase in addition to 5'-phosphodiesterase. For this reason although decomposition rate was 63.58% the accumulation of 5'-AMP, 5'-CMP, 5'-GMP and 5'-UMP occurred by the breakdown of RNA. In the course of these reaction 5'-AMP deaminase converted 60% of 5'-AMP thus produced into 5'-IMP and flavorous 5'-mono nucleotide production was significantly increased by this strain over the above mentioned one. Production rates were found to be 171.8mg per grain of RNA for 5'-IMP and 148.2mg per gram of RNA for 5'-GMP, respectively.

• Journal of Plant Biology
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• v.27 no.1
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• pp.7-13
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• 1984

Activities of corn endosperm adenylate cyclase and phosphodiesterase were found right after germination, and phosphodiesterase activity was shown to increase steadily. Protease activity was also found. Corn peptide fraction purified by using Sephadex G-25 column was shown to enhance corn phosphodiesterase activity buy inhibit bovine phosphodiesterase activity. And the fraction inhibits corn adenylate cyclase activity. Trypsintreated peptide fraction was shown to enhance phosphodiesterase activity 80% compared to that of native peptide fraction. However, in case of DNase phosphodiesterase was shown to be innocuous. According to cumulative results, it is more likely that peptide fraction produced by protease inhibits adenylate cyclase activity and enhance phosphodiesterase, decreasing cAMP level.

• Korean Journal of Pharmacognosy
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• v.43 no.2
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• pp.184-191
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• 2012

The aim of this study was to explore the potent phosphodiesterase type 5 (PDE %) inhibitor from various herbal medicines for erectile dysfunctions. In this study, 61 herbal medicines, which were extracted with ethanol, have been investigated with PDE 5 assay using enzyme inhibitory activity on 22 species of herbal medicines. Of these, 5 species of herbal medicines, Cnidium monieri, Cuscuta chinensis, Epimedium koreanum, Morinda officinalis, and Tribulus terrestris were exhibited stronger inhibitory effect against phosphodiesterase 5 (PDE 5) among 61 species; Cnidium monieri ($IC_{50}=33.7{\mu}g/ml$), Cuscuta chinensis ($IC_{50}=65.7{\mu}g/ml$), Epimedium koreanum ($IC_{50}=90.3{\mu}g/ml$), Morinda officinalis ($IC_{50}=48.7{\mu}g/ml$) and Tribulus terrestris ($IC_{50}=32.5{\mu}g/ml$).

• Korean Journal of Pharmacognosy
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• v.45 no.3
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• pp.268-274
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• 2014

The aim of this study is to explore the potent phosphodiesterase 4 and 7 inhibitor from various herbal medicines for atopy treatment. In this study, 51 kinds of each herbal medicine, which were extracted with ethanol, was carried out the screening of PDE 4 and 7 inhibition using enzyme inhibitory assay. Of these, 8 species of herbal medicines, Rubus coreanus, Duchesnea chrysantha, Alisma orientale, Rehmannia glutinosa, Angelica dahurica, Thuja orientalis, Astragalus membranaceus and Perilla frutescens were screened as potential inhibitor against PDE 4 and 7. Among 8 species, Duchesnea chrysantha showed poteinial anti-atopic effect on DNCB-induced atopic model. Duchesnea chrysantha extract decreased serum IgE and histamine release significantly.

• Journal of the Korean Society of Food Science and Nutrition
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• v.29 no.2
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• pp.329-334
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• 2000

Two major oleananesaponins in Bupleuri radix, saikosaponin $\alpha$ and d, were extracted at various solvent compositions and leaching temperatures. Solvent composition was varied at 0 to 100%(v/v) of ethanol-water and methanol-water, whereas leaching temperature was adjusted to te range of 25~45$^{\circ}C$. The most effective extractant and leaching temperature were 70% ethanol and 45$^{\circ}C$, respectively. However, no major differences in saikosaponin content and cAMP phosphodiesterase inhibition were found at various leaching times. The cAMP phosphodiesterase inhibitions were alo the highest when 70% ethanol was used as the extractant.

• Journal of Korean Neurosurgical Society
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• v.50 no.2
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• pp.109-113
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• 2011

Objective : Peripheral neuropathy is characterized by hyperalgesia, spontaneous burning pain, and allodynia. The purpose of this study was to investigate the effect of rolipram, a phosphodiesterase-4-specific inhibitor, in a segmental spinal nerve ligation model in rats. Methods : Both the L5 and L6 spinal nerves of the left side of the rats were ligated. Phosphodiesterase-4 inhibitor (rolipram) and saline (vehicle) were administered intraperitoneally. We measured mechanical allodynia using von Frey filaments and a nerve conduction study. Results : The mechanical allodynia, which began to manifest on the first day, peaked within 2 days. Multiple intraperitoneal injections of rolipram ameliorated the mechanical allodynia. Furthermore, an intraperitoneal administration of rolipram improved the development of pain behavior and nerve conduction velocity. Conclusion : This study suggests that the phosphodiesterase-4 inhibitor, rolipram, alleviates mechanical allodynia induced by segmental spinal nerve ligation in rats. This finding may have clinical implications.

• Proceedings of the Korean Society for Applied Microbiology Conference
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• 1979.10a
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• pp.244.2-244
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• 1979

고분자 기질을 분해하는 효소의 고정화 후의 활성 yield을 높히고자 Polysaccharide의 표면에 acrylamide 및 N-hydroxysuccinimidyl acrylate을 graft 공중합 시킴으로써 긴 측쇄에 활성 ester을 가지는 새로운 carrier에 phosphiesterase을 고정화 시켰으며 이 고정화된 phosphodiesterase의 몇가지 성질을 조사하여 본래의 phosphiesterase의 성질과 비교하였다. 1) 이 Carrier에 phosphodiesterase을 직접 고정화시킨 결과 52%가 고정화되었으며 고정화된 효소는 38%의 비활성을 나타내 주었다. 2) phosphodiesterase는 이상과 같이 고정화됨으로써 최적작용 pH는 8.0부근에서 9.0부근으로 최적작용온도는 $50^{\circ}C부근에서$ $60^{\circ}C부근으로$ KM치는 1.11mg에서 2.1mg/ml로 변하였으며 열안정성은 훨씬 증가하여 본래의 phosphodiesterase의 열불활성속도상수가 0.4인데 고정화된 효소는 0.03 이었다. 또 $5^{\circ}C에서$ 수용액상태(pH 8.0 Tris buffer)로 6개월 보관후의 관존 활성은 본래의 효소가 0.2%인데 고정화된 효소는 42%로 높은 치를 나타내주었다.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1258-1262
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• 2004

Phosphodiesterase (PDE) 4 is an enzyme that degrades intracellular cAMP. In the present study, the effect of rolipram, a specific phosphodiesterase (PDE) 4 inhibitor, on osteoclast formation was investigated. Rolipram induced osteoclast formation in cocultures of mouse bone marrow cells and calvarial osteoblasts. This activity was not observed in the absence of calvarial osteoblasts, suggesting that calvarial osteoblasts are likely target cells of rolipram. Osteoclast formation by rolipram was completely blocked by the addition of osteoprotegerin (OPG), a soluble decoy receptor for the osteoclast differentiation factor, TNF-related activation-induced cytokine (TRANCE, identical to RANKL, ODF, and OPGL). Northern blot analysis revealed the effect of rolipram to be associated with the increased expression of TRANCE mRNA in mouse calvarial osteoblasts. Collectively, these data indicate that PDE4 inhibitor up-regulates the TRANCE mRNA expression in osteoblasts, which in turn controls osteoclast formation.

• The Korean Journal of Pharmacology
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• v.29 no.2
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• pp.253-261
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• 1993

Possible changes in the role of insulin-sensitive cyclic nucleotide phosphodiesterase(PDE) in mediating the antilipolytic action of insulin were investigated in adipocytes from streptozotocin-induced diabetic rats. Isolated adipocytes prepared from epididymal adipose tissue were incubated, with or without insulin, at $37^{\circ}C$ for 15 min following pretreatment with various drugs or toxins, and three (plasma membranes, microsomal membranes, and cytosol) fractions prepared by differential centrifugation were then assayed for cAMP phosphodiesterase activity. The PDE activities only in the crude microsomal (P2) fractions were activated by insulin both in diabetic and control rats. The basal PDE activities in P2 fractions of adipocytes from diabetic rats were higher than those from control rats, although the maximal effects observed at 2 nM of insulin, $100\;{\mu}M$ of isoproterenol or the combination of both were not significantly different from each other. The insulin-stimulated PDE activities in P2 fractions of adipocytes from diabetic rats were not changed by PIA, a $A_{1}$ adenosine receptor agonist, whereas they were decreased to the basal PDE activities in those from control rats. In addition, the adipocytes from diabetic rats showed an increased sensitivity to pertussis toxin compared to those from controls. There were no differences between diabetic and control rats in the sensitivity of adipocytes to cholera toxin. These data indicate that the impaired signalling through inhibitory receptors such as adenosine receptors in adipocytes from streptozotocin-induced diabetes relates to the loss or the decreased function of $G_i$ proteins, and leads to the increased activity of the insulin-dependent PDE at the basal states.