Synthetic High Molecular Weight Enzyme Inhibitors. I. Polymeric Phosphates of Phloretin and Related Compounds.

Diczfalusy, E.; Fernö, O.; Fex, H.; Högberg, B.; Linderot, T.; Rosenberg, Th.

doi:10.3891/acta.chem.scand.07-0913

Cited by 97 publications

(10 citation statements)

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“…It is of interest to note that non-steroidal anti-inflammatory drugs such as meclofenamate have been found to antagonize the contractions produced by PGF2a on human isolated bronchial muscle (Collier & Sweatman, 1968). Whether or not the prostaglandin-blocking activity of PPP is related to its ability to inhibit a wide variety of enzymes (Diczfalusy et al, 1953) must await further investigation.…”

Section: Discussionmentioning

confidence: 99%

Antagonism of some smooth muscle actions of prostaglandins by polyphloretin phosphate

Eakins

Karim

Miller

1970

British J Pharmacology

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Summary1. The antagonism of the smooth muscle stimulating actions of PGF2a and PGE2 by polyphloretin phosphate (PPP) was studied on several isolated smooth muscle preparations and on the blood pressure of the anaesthetized rabbit. 2. PPP (2'5-20 ,ug/ml) reversibly inhibited contractions of the jird colon produced by PGE2 or PGF2a; PGF2a was more readily antagonized than PGE2. 3. PPP (2S5-30 jug/ml) reversibly antagonized contractions produced by PGE2 and PGF2a on the isolated rabbit jejunum and uterus. In these preparations PPP antagonized PGE2 as readily as PGF2a. 4. It is concluded that PPP is a selective antagonist to the prostaglandins on these tissues, for contractions produced by other agonists, such as acetylcholine, angiotensin, 5-hydroxytryptamine and bradykinin were not reduced by concentrations of PPP which markedly antagonized responses to the prostaglandins. 5. Intravenous injections of PPP (25-200 mg/ kg) resulted in a variable antagonism to the fall in blood pressure produced by intravenous injections of PGF2a in the anaesthetized rabbit; vasodepressor responses produced by PGE2 and acetylcholine were not antagonized. 6. The mechanism of this antagonism by PPP is not clear and must await further investigation.

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Section: Discussionmentioning

confidence: 99%

Antagonism of some smooth muscle actions of prostaglandins by polyphloretin phosphate

Eakins

Karim

Miller

1970

British J Pharmacology

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“…The organic phosphates tested had a pronounced inhibitory effect. These com pounds are reported to be potent inhibitors of enzymes [8,22], but both produce fibrinolytic activity in guinea pig serum [16]. Our results indicate that the activating effects referred to in the introduction as the 'peptone effect' must be caused by an indirect mechanism of activation.…”

Section: Discussionmentioning

confidence: 67%

Effects of Some Polysaccharide Sulfates and Some Phosphates on Neutral Proteases and Plasminogen Activators

Ray¹,

Astrup²

1973

Pathophysiol Haemos Thromb

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Several polysaccharide sulfates (heparin, dextran sulfate, chitin disulfate, cellulose sulfate) and some phosphates (α-tocopherol phosphate, polyphloretin phosphate, hexametaphosphate) were investigated for their direct effects on fibrinolytic agents (neutral proteases and plasminogen activators). α-Tocopherol phosphate and polyphloretin phosphate were strong inhibitors. The remainder of the compounds had mostly weak inhibitory or enhancing effects varying from compound to compound and with the type of fibrinolytic agent. Some (heparin, chitin disulfate, hexametaphosphate) had little or no influence at the concentrations used.

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“…The phloretin derivatives used are negatively charged and highly hy drophilic [6], Their antianaphylactic effect might be exerted at the mast cell membrane, possibly by inhibiting enzymatic reactions triggered by the allergen-antibody complex. Negatively charged high molecular weight po lymers including derivatives of phloretin have been shown to exhibit en zyme inhibitory properties against, e.g., alkaline phosphatase and hyaluronidase [6].…”

Section: Discussionmentioning

confidence: 99%

“…A polymer of phloretin and phosphoric acid, polyphloretin phosphate [6], has been shown to antagonize the bronchoconstrictor action of PGF2a on isolated human bronchi at concentrations which had no influ ence on the responses to histamine, acetylcholine or prostaglandin E, [17]. In addition, this polymer inhibits the release of histamine and the formation of SRS in guinea pig lung tissue [2], These properties make PPP a substance of potential clinical interest with regard to the therapy of bronchial asthma.…”

Section: Introductionmentioning

confidence: 99%

Inhibition by Derivatives of Phloretin of Anaphylactic Histamine Release from Human Lung Tissue and of Prostaglandin F<sub>2α</sub>-Induced Bronchoconstriction

Foucard¹,

Strandberg²

1975

Int Arch Allergy Immunol

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Derivatives of phloretin (25–1,000 μg/ml) among them polyphloretin phosphate (PPP), inhibited in a dose-dependent manner anaphylactic (birch pollen or horse dander) histamine release from human lung tissue passively sensitized with reaginic serum. Pretreatment with PPP of lung tissue sensitized both to birch pollen and horse dander counteracted to a similar extent the release of histamine induced by either allergen administered in sequence. The phloretin derivatives also antagonized the constrictor action of prostaglandin F_2α on isolated human bronchi at concentrations which did not impair the responses to histamine. The low and high molecular weight derivatives of phloretin were comparably active on a weight basis in both experimental systems.

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Synthetic High Molecular Weight Enzyme Inhibitors. I. Polymeric Phosphates of Phloretin and Related Compounds.

Cited by 97 publications

References 0 publications

Antagonism of some smooth muscle actions of prostaglandins by polyphloretin phosphate

Antagonism of some smooth muscle actions of prostaglandins by polyphloretin phosphate

Effects of Some Polysaccharide Sulfates and Some Phosphates on Neutral Proteases and Plasminogen Activators

Inhibition by Derivatives of Phloretin of Anaphylactic Histamine Release from Human Lung Tissue and of Prostaglandin F<sub>2α</sub>-Induced Bronchoconstriction

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