Papain
Identification
- Name
- Papain
- Accession Number
- DB11193
- Description
Papain, also known as papaya proteinase I, is a cysteine protease (EC 3.4.22.2) enzyme that is found in species of papaya, Carica papaya and Vasconcellea cundinamarcensis. The enzyme is found to be localized in the skin of papaya, and is collected from slashed unripe papayas as a crude latex. Papain is used in food, pharmaceutical, textile, and cosmetic industries. While it has been used for the treatment of inflammation and pain via topical administration, papain has also shown to have anthelmintic and tooth-whitening properties. Present in over-the-counter mixture products consisting of different digestive enzymes, its active site contains a catalytic diad that plays a role in breaking peptide bonds. Papain is also used as an ingredient in various enzymatic debriding preparations.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Papain
- Papaína
Pharmacology
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No FDA-approved therapeutic indications.
- Associated Conditions
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- Pharmacodynamics
Papain is a digestive enzyme and often acts as a skin allergen.
- Mechanism of action
When topically applied, papain induces an allergen-like inflammatory response via recruiting neutrophils, mast cells, and CD3-positive cells and by induction of a TH2-biased antibody response 1. In vitro, treatment of papain resulted in the breakdown of tight junctions of primary human keratinocytes that maintain the epithelial barrier integrity. These tight junction proteins include zonula occludens-1, claudin-4, and occludin 1. It is proposed that papain induces allergic responses via activation of TLR4, leading to an increase in neutrophils, CD3+ cells, mast cells, and CCL8-positive cells 1.
Target Actions Organism UToll-like receptor 4 activatorHumans - Absorption
No pharmacokinetic data available.
- Volume of distribution
No pharmacokinetic data available.
- Protein binding
No pharmacokinetic data available.
- Metabolism
No pharmacokinetic data available.
- Route of elimination
No pharmacokinetic data available.
- Half-life
No pharmacokinetic data available.
- Clearance
No pharmacokinetic data available.
- Adverse Effects
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Acute oral LD50 of 200 mcu papain is 4000 mg/kg in rat and 12500 mg/kg in mouse MSDS. It acts as an irritant in case of inhalation or contact with eyes.
- Affected organisms
- Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image BEAUTIFUL CONTRACT - Deep V Breast contract -Hui Ju Sheng Enterprise Corporation Ltd. Capsule, gelatin coated 35 mg/500mg Oral Phytopia Co., Ltd. 2016-04-01 2017-02-01 US 
Papaya Enzyme - Tablet 30 mg Tablet Oral Health Wise Nutrition Inc. 1997-08-15 2000-07-29 Canada 
Papaya Enzyme Tab Tablet Oral Carmaran LtÉe 1979-12-31 1996-09-09 Canada Papaya Enzyme Tab 200mg Tablet Oral Bioforce Canada Inc. 1994-12-31 1997-04-04 Canada Papaya Enzyme Tab 30mg Tablet Oral Pharmetics (2011) Inc. 1995-12-31 2006-07-27 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Bromelain and Papain Tab Papain (35 mg) + Bromelains (75 mg) Tablet Oral Vita Health Products Inc 1978-12-31 2002-07-31 Canada Chewable Enzymes Tablets Papain (100 mg) + Bromelains (15 mg) + Pancrelipase amylase (5 mg) Tablet Oral Gahler Enterprises Ltd. 1988-12-31 2002-07-17 Canada Dygest Papain (100 mg) + Betaine hydrochloride (90 mg) + Ox bile extract (75 mg) + Pancrelipase (200 mg) + Peppermint (50 mg) + Pepsin (125 mg) Tablet Oral Creative Nutrition Canada Corp. 1987-12-31 2007-07-11 Canada Enzyme Tablets Papain (65 mg) + Betaine hydrochloride (65 mg) + Ox bile extract (8.125 mg) + Pancrelipase (100 mg) + Pancrelipase amylase (130 mg) + Pepsin (65 mg) Tablet Oral General Nutrition Canada Inc. 2001-10-20 2007-08-01 Canada Herbalax Forte No 70 Tab Papain (129.6 mg) + Capsicum oleoresin (1.62 mg) + Frangula purshiana bark (97.2 mg) + Phenolphthalein (97.2 mg) + Sodium taurocholate (64.8 mg) Tablet Oral SantÉ Naturelle (Ag) LtÉe 1981-12-31 1997-09-09 Canada Master Key Formula 3 Tab Papain (50 mg) + Niacin (11.5 mg) + Silicon (50 mcg) Tablet Oral Nutrition For Life International 1997-01-27 2000-08-11 Canada Neo Life Beta Gest Tab Papain (10 mg) + Betaine hydrochloride (275 mg) + Pepsin (130 mg) Tablet Oral Golden Neo Life International Ltd. 1979-12-31 1997-08-01 Canada Neo Life Enzyme Tab Papain (50 mg) + Pancrelipase (200 mg) + Pepsin (125 mg) Tablet Oral Golden Neo Life International Ltd. 1979-12-31 1997-08-01 Canada Papaya Bromelain Mycozyme Papain (30 mg) + Bromelains (45 mg) + Pancrelipase amylase (30 mg) Tablet Oral Alive Vitamins 1985-12-31 2002-07-12 Canada Pro Gest Tab Papain (64.8 mg) + Betaine hydrochloride (105.3 mg) + Pancrelipase (11.4 mg) + Pepsin (32.4 mg) + Sodium taurocholate (64.8 mg) Tablet Oral Pure Life International Prods Inc. 1992-12-31 2000-07-27 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BEAUTIFUL CONTRACT - Deep V Breast contract -Hui Ju Sheng Enterprise Corporation Ltd. Papain (35 mg/500mg) Capsule, gelatin coated Oral Phytopia Co., Ltd. 2016-04-01 2017-02-01 US Puralor Papain (20 mg/1) + 1-(c14-c18 esteroyl)-2-docosahexanoyl-sn-glycero-3-phosphocholine (5 mg/1) + 1-(c14-c18 esteroyl)-2-docosahexanoyl-sn-glycero-3-phosphoethanolamine (2.5 mg/1) + Acetylcysteine amide (5 mg/1) + Ascorbic acid (25 mg/1) + Cholecalciferol (100 [iU]/1) + Citric acid (1.6 mg/1) + Cobamamide (2 mg/1) + Egg phospholipids (42.5 mg/1) + Folic acid (42.5 mg/1) + Gastric intrinsic factor (2.5 mg/1) + Magnesium L-threonate (2.5 mg/1) + Leucovorin (3 mg/1) + Levomefolic acid (0.4 mg/1) + Magnesium glycinate (1 mg/1) + Niacin (0.5 mg/1) + Pantethine (2.5 mg/1) + Riboflavin (0.5 mg/1) + Sodium citrate (0.8 mg/1) + Thiamine chloride (0.5 mg/1) Tablet, chewable Oral Centurion Labs 2014-01-01 2017-09-20 US
Categories
- Drug Categories
- Classification
- Not classified
Chemical Identifiers
- UNII
- A236A06Y32
- CAS number
- 9001-73-4
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Stremnitzer C, Manzano-Szalai K, Willensdorfer A, Starkl P, Pieper M, Konig P, Mildner M, Tschachler E, Reichart U, Jensen-Jarolim E: Papain Degrades Tight Junction Proteins of Human Keratinocytes In Vitro and Sensitizes C57BL/6 Mice via the Skin Independent of its Enzymatic Activity or TLR4 Activation. J Invest Dermatol. 2015 Jul;135(7):1790-1800. doi: 10.1038/jid.2015.58. Epub 2015 Feb 23. [PubMed:25705851]
- External Links
- AHFS Codes
- 56:16.00 — Digestants
- MSDS
- Download (47.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count Not Available Active Not Recruiting Basic Science Itching / Papain / Skin Prick Test (SPT) 1 Not Available Not Yet Recruiting Basic Science Itching 1 Not Available Unknown Status Treatment Microbial Colonization 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule, gelatin coated Oral 35 mg/500mg Tablet Oral 150000 USP UNITS Tablet Oral 4 mcg Tablet, chewable Oral 15 mg Tablet Oral 2.5 mg Tablet Oral 10000 U Tablet Oral 150000 U Tablet Oral Capsule Oral 5 mg Tablet Oral Gel Topical 0.5 g Cream Topical 0.5 g Tablet Oral 150,000 [USP'U] Tablet, chewable Oral Tablet, delayed release Oral 270 FIP units - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Soluble in cold water MSDS - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- Curator comments
- Activation is indicated in vitro.
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- Cooperates with LY96 and CD14 to mediate the innate immune response to bacterial lipopolysaccharide (LPS). Acts via MYD88, TIRAP and TRAF6, leading to NF-kappa-B activation, cytokine secretion and ...
- Gene Name
- TLR4
- Uniprot ID
- O00206
- Uniprot Name
- Toll-like receptor 4
- Molecular Weight
- 95679.19 Da
References
- Stremnitzer C, Manzano-Szalai K, Willensdorfer A, Starkl P, Pieper M, Konig P, Mildner M, Tschachler E, Reichart U, Jensen-Jarolim E: Papain Degrades Tight Junction Proteins of Human Keratinocytes In Vitro and Sensitizes C57BL/6 Mice via the Skin Independent of its Enzymatic Activity or TLR4 Activation. J Invest Dermatol. 2015 Jul;135(7):1790-1800. doi: 10.1038/jid.2015.58. Epub 2015 Feb 23. [PubMed:25705851]
Drug created on December 03, 2015 16:51 / Updated on February 24, 2021 19:34