I was looking into vegetable enzymes when i saw Risa mention something about them, and i ran into this very interesting substance called seaprose. Apparently there are numerous studies on it's mucolytic and antiinflammatory properties.
There is a company called enzymedica that makes this product called mucostop. Their main active ingredient ingredient is seaprose, and as far as i can tell, this is the only thing available that has seaprose in it at the moment (although i haven't looked THAT hard)...
Anyways, if you search pubmed, there are a few really good articles about it. :
Effects of seaprose on the rheology of bronchial mucus in patients with chronic bronchitis. A double-blind study vs placebo.
Braga PC, Moretti M, Piacenza A, Montoli CC, Guffanti EE. Int J Clin Pharmacol Res. 1993;13(3):179-85. PMID: 8225701 [PubMed - indexed for MEDLINE]
Centre for Respiratory Pharmacology, School of Medicine, University of Milan, Italy.
There are changes in the rheological characteristics of mucus (viscoelasticity) in several pulmonary pathologies, and especially in chronic bronchitis. Seaprose, a proteolytic enzyme, is one of the pharmacological possibilities for affecting the rheology of bronchial mucus to correct mucostasis and improve its clearance. The action of this drug on the viscoelasticity of bronchial mucus was assessed in a double-blind vs placebo study with 20 randomly balanced chronic bronchitis patients using a new kind of portable rheometer with special features designed for routine bronchial mucus analysis in clinical practice at the patient's bedside. <b>It was found that in the group of patients who were given the placebo, there were no particular changes in the rheological behaviour of mucus, while in those patients who were given seaprose there were significant changes in both viscosity and elasticity at the end of treatment</b>. Eight days after the end of treatment with seaprose, there was still a significant beneficial effect on the viscoelasticity of mucus and a sort of "post-mucolytic effect" can be postulated. <b>Seaprose also had antiinflammatory action, and since in chronic bronchitis there are variable degrees of inflammations, its beneficial long-lasting effect could also be ascribed to this concomitant action.</b>
Effects of seaprose on sputum biochemical components in chronic bronchitic patients: a double-blind study vs placebo.
Moretti M, Bertoli E, Bulgarelli S, Testoni C, Guffanti EE, Marchioni CF, Braga PC. Int J Clin Pharmacol Res. 1993;13(5):275-80. PMID: 8200722 [PubMed - indexed for MEDLINE]
Istituto di Tisiologia e Malattie dell' Apparato Respiratorio, Universita di Modena, Italy.
Seaprose is a semialkaline proteinase endowed with proteolytic effect and antiinflammatory activity tested in different clinical trials. <b>There is clinical evidence that seaprose reduces sputum viscoelastic properties in chronic hypersecretory bronchitis</b>. The present study evaluated (in a double-blind design vs. placebo) the activity of seaprose on bronchial inflammation, mucus glycoprotein secretion and bronchial humoral defence mechanism in chronic bronchitic patients clinically stable (10 per group). Markers of bronchial inflammation (albumin, albumin/total protein ratio) and bronchial infection (DNA), of mucus glycoproteins (fucose and N-acetylneuraminic acid) and of humoral defence mechanism (secretory-IgA) were tested in sputum. <b>We found that ten-day treatment with seaprose (90 mg/day) reduced sputum albumin during the observation period, the difference being statistically significant at the 18th day. The sputum albumin/total protein ratio also decreased by 50% at the end of the study</b>. In the same group, sputum DNA, secretory-IgA, fucose and N-acetylneuraminic acid remained unchanged after treatment. The placebo group did not show any significant changes in the sputum marker substances. <b>This study provides experimental evidence for the antiinflammatory activity of seaprose on bronchial mucosa in chronic bronchitic patients studied in a stable phase of their disease</b>. Furthermore the drug does not seem to affect mucus glycoprotein secretion or secretory-IgA production.
And finally....
he influence of seaprose on erythromycin penetration into bronchial mucus in bronchopulmonary infections.
Braga PC, Piatti G , Grasselli G, Casali W, Beghi G, Allegra L. Drugs Exp Clin Res. 1992;18(3):105-11. PMID: 1425205 [PubMed - indexed for MEDLINE]
Centre of Respiratory Pharmacology, University of Milan, Italy.
<b>In bronchopulmonary infections antibiotics can be combined with other drugs, called mucoactive drugs, that act to reduce the abnormal viscoelasticity of the mucus enabling a deeper penetration of more antibiotic into the mucu</b>s. <b>Seaprose is a protease that interacts with the polymeric fibrillar structure of the bronchial mucus to shorten the long chains of mucoproteins, DNA and other macromolecules, thus reducing the viscosity of the mucus</b>. In order to assess whether the combination of seaprose (60 mg/8 h) plus erythromycin (500 mg/8 h) allows higher antibiotic levels in sputum than erythromycin (500 mg/8 h) plus placebo, the pharmacokinetic behaviour in sputum and in blood of these two treatments was investigated in a double-blind study in two groups of twenty patients each with bronchopulmonary infections. Serum and sputum levels were determined for each patient at the first and seventh day of the two drug regimens. <b>Statistically significant differences for peak, AUC and MRT, were observed for erythromycin between the first and last dose in the group of patients treated with seaprose plus erythromycin; moreover significant differences for these parameters were observed between the two groups</b>. <b>These findings indicate the presence of a pharmacokinetic synergism between seaprose and erythromycin which allows erythromycin to penetrate bronchial secretion more easily and in higher amounts, performing a sterilizing action with therapeutic advantages</b>
That last abstract I find very interesting, because erythromycin is in the same family I believe as zithromax....and it seems to make it a lot more effective. Any thoughts on this?
I think this is my next investigational drug...
Kiel
There is a company called enzymedica that makes this product called mucostop. Their main active ingredient ingredient is seaprose, and as far as i can tell, this is the only thing available that has seaprose in it at the moment (although i haven't looked THAT hard)...
Anyways, if you search pubmed, there are a few really good articles about it. :
Effects of seaprose on the rheology of bronchial mucus in patients with chronic bronchitis. A double-blind study vs placebo.
Braga PC, Moretti M, Piacenza A, Montoli CC, Guffanti EE. Int J Clin Pharmacol Res. 1993;13(3):179-85. PMID: 8225701 [PubMed - indexed for MEDLINE]
Centre for Respiratory Pharmacology, School of Medicine, University of Milan, Italy.
There are changes in the rheological characteristics of mucus (viscoelasticity) in several pulmonary pathologies, and especially in chronic bronchitis. Seaprose, a proteolytic enzyme, is one of the pharmacological possibilities for affecting the rheology of bronchial mucus to correct mucostasis and improve its clearance. The action of this drug on the viscoelasticity of bronchial mucus was assessed in a double-blind vs placebo study with 20 randomly balanced chronic bronchitis patients using a new kind of portable rheometer with special features designed for routine bronchial mucus analysis in clinical practice at the patient's bedside. <b>It was found that in the group of patients who were given the placebo, there were no particular changes in the rheological behaviour of mucus, while in those patients who were given seaprose there were significant changes in both viscosity and elasticity at the end of treatment</b>. Eight days after the end of treatment with seaprose, there was still a significant beneficial effect on the viscoelasticity of mucus and a sort of "post-mucolytic effect" can be postulated. <b>Seaprose also had antiinflammatory action, and since in chronic bronchitis there are variable degrees of inflammations, its beneficial long-lasting effect could also be ascribed to this concomitant action.</b>
Effects of seaprose on sputum biochemical components in chronic bronchitic patients: a double-blind study vs placebo.
Moretti M, Bertoli E, Bulgarelli S, Testoni C, Guffanti EE, Marchioni CF, Braga PC. Int J Clin Pharmacol Res. 1993;13(5):275-80. PMID: 8200722 [PubMed - indexed for MEDLINE]
Istituto di Tisiologia e Malattie dell' Apparato Respiratorio, Universita di Modena, Italy.
Seaprose is a semialkaline proteinase endowed with proteolytic effect and antiinflammatory activity tested in different clinical trials. <b>There is clinical evidence that seaprose reduces sputum viscoelastic properties in chronic hypersecretory bronchitis</b>. The present study evaluated (in a double-blind design vs. placebo) the activity of seaprose on bronchial inflammation, mucus glycoprotein secretion and bronchial humoral defence mechanism in chronic bronchitic patients clinically stable (10 per group). Markers of bronchial inflammation (albumin, albumin/total protein ratio) and bronchial infection (DNA), of mucus glycoproteins (fucose and N-acetylneuraminic acid) and of humoral defence mechanism (secretory-IgA) were tested in sputum. <b>We found that ten-day treatment with seaprose (90 mg/day) reduced sputum albumin during the observation period, the difference being statistically significant at the 18th day. The sputum albumin/total protein ratio also decreased by 50% at the end of the study</b>. In the same group, sputum DNA, secretory-IgA, fucose and N-acetylneuraminic acid remained unchanged after treatment. The placebo group did not show any significant changes in the sputum marker substances. <b>This study provides experimental evidence for the antiinflammatory activity of seaprose on bronchial mucosa in chronic bronchitic patients studied in a stable phase of their disease</b>. Furthermore the drug does not seem to affect mucus glycoprotein secretion or secretory-IgA production.
And finally....
he influence of seaprose on erythromycin penetration into bronchial mucus in bronchopulmonary infections.
Braga PC, Piatti G , Grasselli G, Casali W, Beghi G, Allegra L. Drugs Exp Clin Res. 1992;18(3):105-11. PMID: 1425205 [PubMed - indexed for MEDLINE]
Centre of Respiratory Pharmacology, University of Milan, Italy.
<b>In bronchopulmonary infections antibiotics can be combined with other drugs, called mucoactive drugs, that act to reduce the abnormal viscoelasticity of the mucus enabling a deeper penetration of more antibiotic into the mucu</b>s. <b>Seaprose is a protease that interacts with the polymeric fibrillar structure of the bronchial mucus to shorten the long chains of mucoproteins, DNA and other macromolecules, thus reducing the viscosity of the mucus</b>. In order to assess whether the combination of seaprose (60 mg/8 h) plus erythromycin (500 mg/8 h) allows higher antibiotic levels in sputum than erythromycin (500 mg/8 h) plus placebo, the pharmacokinetic behaviour in sputum and in blood of these two treatments was investigated in a double-blind study in two groups of twenty patients each with bronchopulmonary infections. Serum and sputum levels were determined for each patient at the first and seventh day of the two drug regimens. <b>Statistically significant differences for peak, AUC and MRT, were observed for erythromycin between the first and last dose in the group of patients treated with seaprose plus erythromycin; moreover significant differences for these parameters were observed between the two groups</b>. <b>These findings indicate the presence of a pharmacokinetic synergism between seaprose and erythromycin which allows erythromycin to penetrate bronchial secretion more easily and in higher amounts, performing a sterilizing action with therapeutic advantages</b>
That last abstract I find very interesting, because erythromycin is in the same family I believe as zithromax....and it seems to make it a lot more effective. Any thoughts on this?
I think this is my next investigational drug...
Kiel