Phosphodiesterase Inhibitors

Publication Title: 
Aging

The natural polyphenolic compound resveratrol was first discovered in the 1940s. In the recent years, this compound received renewed interest as several findings implicated resveratrol as a potent SIRT1 activator capable of mimicking the effects of calorie restriction, and regulating longevity in lower organisms. Given the worldwide increase in age-related metabolic diseases the beneficial effects of resveratrol on metabolism and healthy aging in humans are currently a topic of intense investigation.

Author(s): 
Timmers, Silvie
Auwerx, Johan
Schrauwen, Patrick
Publication Title: 
Paediatric Drugs

Eczema in childhood is almost always atopic eczema, a common disease with huge impact on the quality of life of the child and family. Although atopic eczema constitutes part of the atopic syndrome, avoidance of allergens is never enough for disease control. Treatment of eczema in childhood has the same components as in adults. Emollients constitute the preventive background therapy in all stages of eczema, and topical corticosteroids are still the mainstay of treatment. Infectious exacerbation may require the use of a short course of topical or systemic antimicrobials.

Author(s): 
Granlund, Håkan
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

The effect of pentoxifylline (PTX) was tested for its capacity to modulate cytokine responses during therapy of severe Plasmodium falciparum malaria in a placebo-controlled, randomized study in 45 adult patients in Bangkok, Thailand. The patients received standard antimalarial treatment with artesunate (120 mg intravenously given immediately, then 60 mg every 12 hr for a total dose of 600 mg). The patients received either low-dose PTX (20 mg/kg/day, n = 15), high-dose PTX (40 mg/kg/day, n = 15), or placebo (n = 15) as continuous infusion for the first three days of antimalarial treatment.

Author(s): 
Wenisch, C.
Looareesuwan, S.
Wilairatana, P.
Parschalk, B.
Vannapann, S.
Wanaratana, V.
Wernsdorfer, W.
Graninger, W.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

Pentoxifylline, an inhibitor of tumor necrosis factor, has been evaluated as an antimalarial agent in combination with artesunate in 45 patients with severe falciparum malaria. Patients were admitted to the intensive care unit at the Hospital for Tropical Diseases in Bangkok, Thailand, and randomly assigned to treatment for 72 hr with a combination of intravenously administered artesunate and 1) placebo, 2) low-dose pentoxifylline (0.83 mg/kg/hr), or 3) high-dose pentoxifylline (1.67 mg/kg/hr).

Author(s): 
Looareesuwan, S.
Wilairatana, P.
Vannaphan, S.
Wanaratana, V.
Wenisch, C.
Aikawa, M.
Brittenham, G.
Graninger, W.
Wernsdorfer, W. H.
Publication Title: 
Journal of Pharmaceutical and Biomedical Analysis

Ayurvedic/herbal healthcare products are considered safe under the impression that they are derived from natural products. But recently, there have been several reports worldwide on the adulteration of synthetic PDE-5 inhibitors in aphrodisiac herbal formulations. Therefore, the objective of the present study was to explore the presence of synthetic PDE-5 inhibitors (sildenafil, tadalafil and/or vardenafil) in ayurvedic/herbal healthcare products sold in Indian market for aphrodisiac/related uses. In total, 85 herbal formulations (HFs) were included in the study.

Author(s): 
Savaliya, Akash A.
Shah, Ravi P.
Prasad, Bhagwat
Singh, Saranjit
Publication Title: 
Journal of Immunology (Baltimore, Md.: 1950)

The genetic elimination of A2A adenosine receptors (A2AR) was shown to disengage the critical immunosuppressive mechanism and cause the dramatic exacerbation of acute inflammatory tissue damage by T cells and myeloid cells. This prompted the evaluation of the proinflammatory vs the anti-inflammatory effects of the widely consumed behavioral drug caffeine, as the psychoactive effects of caffeine are mediated largely by its antagonistic action on A2AR in the brain.

Author(s): 
Ohta, Akio
Lukashev, Dmitriy
Jackson, Edwin K.
Fredholm, Bertil B.
Sitkovsky, Michail
Publication Title: 
Paediatric Drugs

Eczema in childhood is almost always atopic eczema, a common disease with huge impact on the quality of life of the child and family. Although atopic eczema constitutes part of the atopic syndrome, avoidance of allergens is never enough for disease control. Treatment of eczema in childhood has the same components as in adults. Emollients constitute the preventive background therapy in all stages of eczema, and topical corticosteroids are still the mainstay of treatment. Infectious exacerbation may require the use of a short course of topical or systemic antimicrobials.

Author(s): 
Granlund, Håkan
Publication Title: 
Paediatric Drugs

Eczema in childhood is almost always atopic eczema, a common disease with huge impact on the quality of life of the child and family. Although atopic eczema constitutes part of the atopic syndrome, avoidance of allergens is never enough for disease control. Treatment of eczema in childhood has the same components as in adults. Emollients constitute the preventive background therapy in all stages of eczema, and topical corticosteroids are still the mainstay of treatment. Infectious exacerbation may require the use of a short course of topical or systemic antimicrobials.

Author(s): 
Granlund, Håkan
Publication Title: 
Chemical & Pharmaceutical Bulletin

A new sildenafil analogue, cyclopentynafil (1) and a new tadalafil analogue, N-octylnortadalafil (2) were isolated from a dietary supplement illegally marketed for erectile dysfunction. The structures of the sildenafil and tadalafil analogues were elucidated by using HPLC-photodiode array (PDA), LC-MS, high-resolution MS, NMR and circular dichroism (CD).

Author(s): 
Hasegawa, Takashi
Takahashi, Kazunaga
Saijo, Masaaki
Ishii, Toshiyasu
Nagata, Tomoko
Kurihara, Masaaki
Haishima, Yuji
Goda, Yukihiro
Kawahara, Nobuo
Publication Title: 
Diabetes

Phosphodiesterase 10A (PDE10A) is a novel therapeutic target for the treatment of schizophrenia. Here we report a novel role of PDE10A in the regulation of caloric intake and energy homeostasis. PDE10A-deficient mice are resistant to diet-induced obesity (DIO) and associated metabolic disturbances. Inhibition of weight gain is due to hypophagia after mice are fed a highly palatable diet rich in fats and sugar but not a standard diet. PDE10A deficiency produces a decrease in caloric intake without affecting meal frequency, daytime versus nighttime feeding behavior, or locomotor activity.

Author(s): 
Nawrocki, Andrea R.
Rodriguez, Carlos G.
Toolan, Dawn M.
Price, Olga
Henry, Melanie
Forrest, Gail
Szeto, Daphne
Keohane, Carol Ann
Pan, Yie
Smith, Karen M.
Raheem, Izzat T.
Cox, Christopher D.
Hwa, Joyce
Renger, John J.
Smith, Sean M.

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