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

Pharmacology
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Indication

No FDA-approved therapeutic indications.

Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Contraindications & Blackbox Warnings
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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.

TargetActionsOrganism
UToll-like receptor 4
activator
Humans
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
Medicalerrors
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Toxicity

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

Products
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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BEAUTIFUL CONTRACT - Deep V Breast contract -Hui Ju Sheng Enterprise Corporation Ltd.Capsule, gelatin coated35 mg/500mgOralPhytopia Co., Ltd.2016-04-012017-02-01US flag
Papaya Enzyme - Tablet 30 mgTabletOralHealth Wise Nutrition Inc.1997-08-152000-07-29Canada flag
Papaya Enzyme TabTabletOralCarmaran LtÉe1979-12-311996-09-09Canada flag
Papaya Enzyme Tab 200mgTabletOralBioforce Canada Inc.1994-12-311997-04-04Canada flag
Papaya Enzyme Tab 30mgTabletOralPharmetics (2011) Inc.1995-12-312006-07-27Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Bromelain and Papain TabPapain (35 mg) + Bromelains (75 mg)TabletOralVita Health Products Inc1978-12-312002-07-31Canada flag
Chewable Enzymes TabletsPapain (100 mg) + Bromelains (15 mg) + Pancrelipase amylase (5 mg)TabletOralGahler Enterprises Ltd.1988-12-312002-07-17Canada flag
DygestPapain (100 mg) + Betaine hydrochloride (90 mg) + Ox bile extract (75 mg) + Pancrelipase (200 mg) + Peppermint (50 mg) + Pepsin (125 mg)TabletOralCreative Nutrition Canada Corp.1987-12-312007-07-11Canada flag
Enzyme TabletsPapain (65 mg) + Betaine hydrochloride (65 mg) + Ox bile extract (8.125 mg) + Pancrelipase (100 mg) + Pancrelipase amylase (130 mg) + Pepsin (65 mg)TabletOralGeneral Nutrition Canada Inc.2001-10-202007-08-01Canada flag
Herbalax Forte No 70 TabPapain (129.6 mg) + Capsicum oleoresin (1.62 mg) + Frangula purshiana bark (97.2 mg) + Phenolphthalein (97.2 mg) + Sodium taurocholate (64.8 mg)TabletOralSantÉ Naturelle (Ag) LtÉe1981-12-311997-09-09Canada flag
Master Key Formula 3 TabPapain (50 mg) + Niacin (11.5 mg) + Silicon (50 mcg)TabletOralNutrition For Life International1997-01-272000-08-11Canada flag
Neo Life Beta Gest TabPapain (10 mg) + Betaine hydrochloride (275 mg) + Pepsin (130 mg)TabletOralGolden Neo Life International Ltd.1979-12-311997-08-01Canada flag
Neo Life Enzyme TabPapain (50 mg) + Pancrelipase (200 mg) + Pepsin (125 mg)TabletOralGolden Neo Life International Ltd.1979-12-311997-08-01Canada flag
Papaya Bromelain MycozymePapain (30 mg) + Bromelains (45 mg) + Pancrelipase amylase (30 mg)TabletOralAlive Vitamins1985-12-312002-07-12Canada flag
Pro Gest TabPapain (64.8 mg) + Betaine hydrochloride (105.3 mg) + Pancrelipase (11.4 mg) + Pepsin (32.4 mg) + Sodium taurocholate (64.8 mg)TabletOralPure Life International Prods Inc.1992-12-312000-07-27Canada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
BEAUTIFUL CONTRACT - Deep V Breast contract -Hui Ju Sheng Enterprise Corporation Ltd.Papain (35 mg/500mg)Capsule, gelatin coatedOralPhytopia Co., Ltd.2016-04-012017-02-01US flag
PuralorPapain (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, chewableOralCenturion Labs2014-01-012017-09-20US flag

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
  1. 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]
PubChem Substance
347911149
RxNav
7892
Wikipedia
Papain
AHFS Codes
  • 56:16.00 — Digestants
MSDS
Download (47.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
Not AvailableActive Not RecruitingBasic ScienceItching / Papain / Skin Prick Test (SPT)1
Not AvailableNot Yet RecruitingBasic ScienceItching1
Not AvailableUnknown StatusTreatmentMicrobial Colonization1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Capsule, gelatin coatedOral35 mg/500mg
TabletOral150000 USP UNITS
TabletOral4 mcg
Tablet, chewableOral15 mg
TabletOral2.5 mg
TabletOral10000 U
TabletOral150000 U
TabletOral
CapsuleOral5 mg
TabletOral
GelTopical0.5 g
CreamTopical0.5 g
TabletOral150,000 [USP'U]
Tablet, chewableOral
Tablet, delayed releaseOral270 FIP units
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySoluble in cold waterMSDS
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
  1. 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