Barbaloin

Barbaloin at a Glance

Barbaloin — almost always called aloin — is the bitter, yellow anthrone C-glucoside that gives the leaf latex of aloe its purgative reputation, and one of the aloins present in aged cascara sagrada bark. Chemically it is the 10-C-glucosyl anthrone of aloe-emodin: a sugar bolted onto an anthrone core through a carbon–carbon bond rather than the usual oxygen link. That single structural detail governs almost everything about the molecule — it survives the stomach and upper gut, reaches the colon largely intact, and is only there converted by resident bacteria into the compound that actually works.

Its one genuine, long-established human effect is as a stimulant laxative, and even that is indirect: barbaloin is a prodrug. Gut anaerobes cleave the C-glucosyl bond to release aloe-emodin-9-anthrone, the real purgative, which stimulates colonic motility and secretion ^{1,2Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 2Hattori M et al. · 1988Metabolism of barbaloin by intestinal bacteriaView study →}. Beyond laxation, the isolated molecule shows a scatter of preclinical activities — antimicrobial, antiviral, anti-inflammatory, antioxidant, anticancer — but these are cell and animal findings, not demonstrated human uses ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}.

The headline that now dominates this molecule is regulatory and toxicological. Barbaloin sits inside the hydroxyanthracene derivative class flagged for genotoxicity: its downstream metabolite aloe-emodin is genotoxic in vivo, aloe whole-leaf extract is a clear rodent carcinogen, and on that basis the FDA removed aloe and cascara OTC laxatives in 2002 and the EU restricted these substances in food ^{4,5,6,7Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →Reference 7Commission Regulation (EU) 2021/468 · 2021Amending Annex III to Regulation (EC) No 1925/2006 as regards botanical species containing hydroxyanthracene derivatives (aloin A/B, aloe-emodin, emodin, danthron)View study →}. This page treats that history as the honest spine of the safety story.

Barbaloin Is Aloin

The most important thing to state plainly: barbaloin and aloin are the same molecule. “Aloin” is the older pharmacognosy name for the bitter principle of aloe; “barbaloin” is the same anthrone C-glucoside, the name deriving from Aloe barbadensis (a synonym of Aloe vera).

Aloin is a pair of diastereomers. What is sold and studied as “aloin” is a roughly equal mixture of two stereoisomers that differ only in configuration at the C-10 anthrone carbon: aloin A and aloin B. They share the molecular formula C₂₁H₂₂O₉ (MW ~418) and are readily interconvertible/co-eluting, which is why the literature usually reports them together as “aloin” or “barbaloin” ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}. Strictly, aloin A is barbaloin and aloin B is isobarbaloin, but in practice the names are used interchangeably for the diastereomeric pair, and that convention is followed here.

The C-glucosyl anthrone structure is the point. Barbaloin is 10-C-β-D-glucopyranosyl-aloe-emodin-9-anthrone — the anthrone form of aloe-emodin (barbaloin’s aglycone-relative in the anthraquinone family, alongside emodin and rhein) carrying a glucose unit attached by a carbon–carbon (C-glycosidic) bond at position 10, rather than the oxygen-linked (O-glycosidic) bond of an ordinary glucoside ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}. That distinction is not academic. Human digestive enzymes and stomach acid hydrolyse O-glycosides comparatively easily; a C-glucosyl bond is far more resistant, so barbaloin passes through the upper gut largely unabsorbed and undigested and is only cleaved deep in the colon by specialised bacteria ^{1,2Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 2Hattori M et al. · 1988Metabolism of barbaloin by intestinal bacteriaView study →}. The same chemistry links it to its plant relatives: the pharmacopoeial cascara markers cascaroside A and B are barbaloin-derived C-glucosyl anthrones, and cascarosides C/D are the corresponding derivatives of chrysophanol ^{4Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →}.

What It's Used For

Barbaloin’s evidence base is lopsided. There is one real, mechanistically well-understood human effect — stimulant laxation — and a diffuse cloud of isolated-molecule preclinical activities that have never translated to human use. The laxative action, moreover, is not barbaloin’s own: it is the action of a bacterial metabolite.

Evidence by IndicationStrength of support · Beta

Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. Only the laxative row has real human standing (and it is now a restricted use); the rest is isolate preclinical work.

01Stimulant laxativePromising52%Long-established purgative + defined prodrug→anthrone mechanism, but now regulatorily restricted ^{1,2,4Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 2Hattori M et al. · 1988Metabolism of barbaloin by intestinal bacteriaView study →Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →}

02Antimicrobial / antiviralShaky26%In-vitro isolate activity; no human data ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}

03Anti-inflammatory & other preclinicalShaky24%Cell/animal isolate signals (NF-κB/MAPK/Nrf2, antioxidant, anticancer) ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}

Mechanisms

The load-bearing rows are the top two: barbaloin does nothing until a bacterium turns it into aloe-emodin anthrone. The same colon-targeted delivery of a reactive anthrone that produces the effect also underlies the harm.

Pharmacokinetics

Barbaloin’s kinetics are the direct consequence of its C-glycosidic bond. It is poorly absorbed from the upper gastrointestinal tract and resistant to gastric/enzymatic hydrolysis, so most of an oral dose reaches the colon intact, where bacterial C-glucosidases (notably from Eubacterium sp. BAR) split off glucose to give aloe-emodin-9-anthrone, which is then oxidised to aloe-emodin ^{1,2Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 2Hattori M et al. · 1988Metabolism of barbaloin by intestinal bacteriaView study →}. This is a colon-targeted prodrug by accident of chemistry: little parent barbaloin circulates, and the pharmacology happens locally in the large bowel. Reported plasma barbaloin peaks around ~3 hours after oral intake in the pharmacological literature ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}. The practical reads for a compound page: (1) activity is flora-dependent — no suitable anaerobes, no active metabolite, no effect ^{1Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →}; and (2) the poor systemic bioavailability that concentrates the molecule (and its reactive anthrone metabolite) in the colon is exactly why the large intestine is the target organ for both the laxative effect and the toxicological concern ^{5,6Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →}.

Clinical Trials

There are no modern controlled efficacy trials of isolated barbaloin/aloin. Its human “evidence” is the long historical record of aloe- and aloin-containing stimulant laxatives, which regulators judged to lack adequate safety substantiation rather than efficacy — the FDA moved aloe/cascara from Category I to III and then off the OTC market for want of the requested genotoxicity/carcinogenicity data ^{4Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →}. The active contemporary literature is toxicological, not therapeutic (rodent carcinogenicity and microbiota studies) ^{5,6,8Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →Reference 8Pandiri AR et al. · 2011AnimalAloe vera non-decolorized whole leaf extract-induced large intestinal tumors in F344 rats share similar molecular pathways with human sporadic colorectal tumorsView study →}.

Last checked: July 2026.

The Regulatory History (FDA & EMA)

Barbaloin is unusual among plant molecules in that its defining modern story is regulatory. The efficacy and the hazard share the same chemistry — the hydroxyanthracene structure that makes it a laxative is the structure that carries the genotoxicity signal — so the compound could not be cleanly separated into “useful” and “unsafe,” and regulators acted on the whole class.

United States — FDA, 2002. After reopening the OTC laxative record in 1998 and reclassifying aloe and cascara sagrada from Category I (monograph) to Category III (more data needed), the FDA requested mutagenicity, genotoxicity and carcinogenicity data on these stimulant-laxative ingredients. The data were not supplied. In a final rule effective November 5, 2002, the agency ruled that the stimulant-laxative ingredients aloe (including aloe extract) and cascara sagrada (including casanthranol and the cascara extracts) in OTC products are “not generally recognized as safe and effective” — removing them from the US OTC market ^{4Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →}.

European Union — EFSA/EMA and Regulation (EU) 2021/468. In a 2018 scientific opinion, EFSA concluded that hydroxyanthracene derivatives should be regarded as genotoxic and carcinogenic unless specific data show otherwise, that aloe-emodin and emodin are genotoxic, that aloe whole-leaf extract is carcinogenic, and that no safe daily intake could be established ^{5Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →}. On that basis Commission Regulation (EU) 2021/468 prohibited aloin A/B (barbaloin), aloe-emodin, emodin and danthron as such, and preparations in which they are present, from use in food — tolerating only trace levels ^{7Reference 7Commission Regulation (EU) 2021/468 · 2021Amending Annex III to Regulation (EC) No 1925/2006 as regards botanical species containing hydroxyanthracene derivatives (aloin A/B, aloe-emodin, emodin, danthron)View study →}.

The genotoxicity/carcinogenicity evidence behind the bans. The toxicology is specific and colon-directed. The US National Toxicology Program found clear evidence of carcinogenic activity for a non-decolourised aloe vera whole-leaf extract in F344/N rats given it in drinking water for two years — dose-related adenomas and carcinomas of the large intestine at the 1% and 1.5% concentrations, with none at 0.5% ^{6Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →} — and these rat tumours were shown to share molecular pathways (Kras, Ctnnb1/WNT, MAPK) with human sporadic colorectal cancer ^{8Reference 8Pandiri AR et al. · 2011AnimalAloe vera non-decolorized whole leaf extract-induced large intestinal tumors in F344 rats share similar molecular pathways with human sporadic colorectal tumorsView study →}. A 13-week study of aloin itself reproduced dose-related mucosal (goblet-cell) hyperplasia and pathological changes with microbiota shifts in the rat large intestine — the pre-neoplastic changes seen with the whole extract ^{9Reference 9Boudreau MD et al. · 2017AnimalAloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male ratsView study →}. And barbaloin’s own metabolite, aloe-emodin, causes DNA fragmentation in the mouse in vivo comet assay ^{10Reference 10Nesslany F et al. · 2009AnimalAloe-emodin-induced DNA fragmentation in the mouse in vivo comet assayView study →}, the genotoxic signal that anchors the EFSA classification ^{5Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →}.

The honest caveat. The direct carcinogenicity evidence is strongest for aloe whole-leaf extract and for the metabolite aloe-emodin; pure barbaloin has not itself been run through a two-year cancer bioassay. But it is a hydroxyanthracene-derivative prodrug that delivers a genotoxic anthrone to the colon and produces pre-neoplastic rat pathology in its own right ^{9Reference 9Boudreau MD et al. · 2017AnimalAloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male ratsView study →}, which is why regulators treat it within the class rather than exempting it.

Isolate vs. Plant Studies

The two evidence bases here point the same direction, which is unusual. The laxative mechanism is isolate-and-plant-consistent: purified barbaloin and crude aloe/cascara latex both work through the same colonic metabolite (aloe-emodin anthrone), so the isolate faithfully reproduces the whole-plant action ^{1,2Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 2Hattori M et al. · 1988Metabolism of barbaloin by intestinal bacteriaView study →}. The safety signal, likewise, spans both: the marquee carcinogenicity data are for the whole-leaf aloe extract ^{6,8Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →Reference 8Pandiri AR et al. · 2011AnimalAloe vera non-decolorized whole leaf extract-induced large intestinal tumors in F344 rats share similar molecular pathways with human sporadic colorectal tumorsView study →}, while the isolated aloin study confirms the pre-neoplastic mucosal changes on its own ^{9Reference 9Boudreau MD et al. · 2017AnimalAloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male ratsView study →} and the isolated metabolite carries the genotoxicity ^{10Reference 10Nesslany F et al. · 2009AnimalAloe-emodin-induced DNA fragmentation in the mouse in vivo comet assayView study →}. The remaining “activities” (antimicrobial, anti-inflammatory, anticancer) are almost entirely isolated-molecule in-vitro work with no whole-plant human corroboration ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}. Net: for barbaloin the isolate-vs-plant distinction does not rescue a safety story — both forms carry the same class hazard.

Prevalence in Nature

Barbaloin is a defining constituent of aloe leaf latex — the bitter yellow exudate (distinct from the inner clear gel) that drains from cut leaves of aloe (Aloe vera), Cape aloes (Aloe ferox) and related species. The historical drug “aloes” (dried aloe latex) is largely aloin, so in that material the molecule is a major, not trace, component; its concentration varies strongly with species, leaf age, leaf part and position, with younger leaf tissue generally richer ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}. Because aloin sits in the latex rind and not the gel, decolourised/purified inner-leaf aloe products are formulated specifically to exclude it.

It also occurs in the anthraquinone-laxative barks, most relevantly aged cascara sagrada bark, where the aloins (barbaloin plus chrysaloin) make up roughly 10–30% of the anthracene glycosides but are overshadowed by the diastereomeric cascarosides (~60–70% of the glycoside fraction), which are themselves barbaloin- and chrysophanol-derived C-glucosyl anthrones ^{4Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →}. In cascara it therefore reads as a minor aloin among the cascarosides, whereas in aloe latex it is the star. Quantitative barbaloin figures on a comparable dry-weight basis across sources are not well tabulated (see the compound’s gaps tracker).

Discovery & Synthesis

Aloe latex has been used as a purgative since antiquity, and its bitter active principle was named “aloin” by nineteenth-century pharmacognosists — the name “barbaloin” attaching the aloin of Aloe barbadensis (A. vera). What took much longer was the stereochemistry: that “aloin” is in fact a pair of diastereomers, aloin A and aloin B, differing at the C-10 anthrone centre, and the assignment of their conformation and absolute configuration as 10-C-glucosyl-9-anthrones, was resolved in twentieth-century aloe chemistry ^{3Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}. Commercially, barbaloin/aloin is obtained by extraction from aloe latex (it is available as a purified reference standard and reagent), not by total synthesis — the C-glucosyl anthrone is more practically isolated from the abundant natural source than built.

Patents: not yet researched.

Toxicity & Safety

Barbaloin carries a moderate flag — heavier than an ordinary plant phenolic and on par with its relative emodin — because it is a hydroxyanthracene-derivative prodrug that delivers a genotoxic anthrone to the colon. The flag stops short of a carcinogen badge only because the direct two-year cancer data are for aloe whole-leaf extract and for the metabolite aloe-emodin rather than for pure barbaloin; the class membership, the rat pre-neoplastic pathology of aloin itself, and the metabolite’s genotoxicity are the reasons it is treated as a genuine concern rather than a benign bitter ^{5,6,9,10Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →Reference 9Boudreau MD et al. · 2017AnimalAloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male ratsView study →Reference 10Nesslany F et al. · 2009AnimalAloe-emodin-induced DNA fragmentation in the mouse in vivo comet assayView study →}.

Genotoxicity & carcinogenicity (the class hazard). EFSA classifies hydroxyanthracene derivatives — barbaloin among them — as genotoxic and carcinogenic unless shown otherwise, with aloe-emodin genotoxic in vivo and no safe intake establishable ^{5Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →}. Aloe whole-leaf extract is a clear NTP rodent large-intestine carcinogen ^{6,8Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →Reference 8Pandiri AR et al. · 2011AnimalAloe vera non-decolorized whole leaf extract-induced large intestinal tumors in F344 rats share similar molecular pathways with human sporadic colorectal tumorsView study →}, and isolated aloin produces the corresponding pre-neoplastic mucosal changes in rats ^{9Reference 9Boudreau MD et al. · 2017AnimalAloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male ratsView study →}.

GI and functional harms. As a stimulant laxative it can cause cramping, fluid and electrolyte loss (notably potassium), and dependence/atony with chronic use; at higher exposure aloin increases intestinal epithelial permeability and disturbs the colonic microbiota, lowering butyrate ^{11Reference 11Gokulan K et al. · 2019Dose-dependent effects of aloin on the intestinal bacterial community structure, short chain fatty acids metabolism and intestinal epithelial cell permeabilityView study →}. These are the everyday harms behind the “don’t use stimulant laxatives long-term” rule, layered on top of the genotoxic-class concern.

Pregnancy (prose only). Stimulant anthranoid laxatives are conventionally cautioned in pregnancy (theoretical uterine-stimulant and fluid/electrolyte concerns), and the class genotoxicity signal is an added reason for avoidance; a molecule delivering a genotoxic anthrone to the gut is not a compound to take electively while pregnant. Pregnancy/lactation decisions belong to the herb or product page where intake is actually decided, not to this molecule page — no isolate-specific verdict is issued here.

Safety at a Glance

⚠️ Moderate toxicity

• Its own systemic absorption is low. The C-glucosyl bond keeps barbaloin in the gut lumen; little intact parent circulates ^{1,3Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 3Patel DK et al. · 2012Barbaloin: a concise report of its pharmacological and analytical aspectsView study →}.
• Hydroxyanthracene-derivative genotoxicity concern. The class is treated as genotoxic/carcinogenic-until-proven-otherwise; aloe whole-leaf extract is a clear rodent large-intestine carcinogen, and isolated aloin causes pre-neoplastic rat mucosal changes ^{5,6,9Reference 5EFSA ANS Panel · 2018Safety of hydroxyanthracene derivatives for use in foodView study →Reference 6Boudreau MD et al. · 2013AnimalClear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N ratsView study →Reference 9Boudreau MD et al. · 2017AnimalAloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male ratsView study →}.
• Removed / restricted by regulators. FDA took aloe & cascara stimulant laxatives off the US OTC market (2002); the EU restricts aloin A/B, aloe-emodin, emodin and danthron in food to trace levels ^{4,7Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →Reference 7Commission Regulation (EU) 2021/468 · 2021Amending Annex III to Regulation (EC) No 1925/2006 as regards botanical species containing hydroxyanthracene derivatives (aloin A/B, aloe-emodin, emodin, danthron)View study →}.
• Stimulant-laxative harms. Cramping, electrolyte (potassium) loss, dependence/atony with chronic use, and microbiota/barrier disruption at higher exposure ^{11Reference 11Gokulan K et al. · 2019Dose-dependent effects of aloin on the intestinal bacterial community structure, short chain fatty acids metabolism and intestinal epithelial cell permeabilityView study →}.
• Flora-dependent and unpredictable. The active metabolite forms only if the right colonic anaerobes are present, so effect and exposure vary between people ^{1,2Reference 1Akao T et al. · 1996A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthroneView study →Reference 2Hattori M et al. · 1988Metabolism of barbaloin by intestinal bacteriaView study →}.

Dosage

There is no recommended dose for barbaloin/aloin. Historically, aloe latex and aloin were dosed as a stimulant (purgative) laxative, but that use has been withdrawn or restricted: the FDA removed aloe and cascara stimulant-laxative ingredients from the US OTC market in 2002 ^{4Reference 4Food et al. · 2002Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives)View study →}, and the EU limits aloin A/B and related hydroxyanthracene derivatives in food to trace amounts ^{7Reference 7Commission Regulation (EU) 2021/468 · 2021Amending Annex III to Regulation (EC) No 1925/2006 as regards botanical species containing hydroxyanthracene derivatives (aloin A/B, aloe-emodin, emodin, danthron)View study →}. Modern decolourised/purified aloe products are formulated specifically to remove aloin. Any historical purgative “doses” are context, not a personal recommendation, and given the genotoxicity-class concern, self-dosing isolated aloin is not advisable.

References

1. Akao T, Che QM, Kobashi K, Hattori M, Namba T (1996). A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloe-emodin anthrone. Biological & Pharmaceutical Bulletin. https://pubmed.ncbi.nlm.nih.gov/8820926/
2. Hattori M, Kanda T, Shu YZ, Akao T, Kobashi K, Namba T (1988). Metabolism of barbaloin by intestinal bacteria. Chemical & Pharmaceutical Bulletin. https://pubmed.ncbi.nlm.nih.gov/3246014/
3. Patel DK, Patel K, Tahilyani V (2012). Barbaloin: a concise report of its pharmacological and analytical aspects. Asian Pacific Journal of Tropical Biomedicine. https://pubmed.ncbi.nlm.nih.gov/23569857/
4. Food and Drug Administration (2002). Status of certain additional over-the-counter drug category II and III active ingredients (aloe & cascara sagrada stimulant laxatives). Final rule. Federal Register 67(90):31125-7. https://pubmed.ncbi.nlm.nih.gov/12001972/
5. EFSA ANS Panel (2018). Safety of hydroxyanthracene derivatives for use in food. EFSA Journal. https://pubmed.ncbi.nlm.nih.gov/32625659/
6. Boudreau MD, Mellick PW, Olson GR, Felton RP, Thorn BT, Beland FA (2013). Clear evidence of carcinogenic activity by a whole-leaf extract of Aloe barbadensis miller (aloe vera) in F344/N rats. Toxicological Sciences. https://pubmed.ncbi.nlm.nih.gov/22968693/
7. Commission Regulation (EU) 2021/468 (2021). Amending Annex III to Regulation (EC) No 1925/2006 as regards botanical species containing hydroxyanthracene derivatives (aloin A/B, aloe-emodin, emodin, danthron). Official Journal of the European Union. https://eur-lex.europa.eu/legal-content/EN/TXT/?uri=CELEX:32021R0468
8. Pandiri AR, et al. (2011). Aloe vera non-decolorized whole leaf extract-induced large intestinal tumors in F344 rats share similar molecular pathways with human sporadic colorectal tumors. Toxicologic Pathology. https://pubmed.ncbi.nlm.nih.gov/21937742/
9. Boudreau MD, et al. (2017). Aloin, a component of the aloe vera plant leaf, induces pathological changes and modulates the composition of microbiota in the large intestines of F344/N male rats. Toxicological Sciences. https://pubmed.ncbi.nlm.nih.gov/28525602/
10. Nesslany F, et al. (2009). Aloe-emodin-induced DNA fragmentation in the mouse in vivo comet assay. Mutation Research. https://pubmed.ncbi.nlm.nih.gov/19559101/
11. Gokulan K, Kolluru P, Cerniglia CE, Khare S (2019). Dose-dependent effects of aloin on the intestinal bacterial community structure, short chain fatty acids metabolism and intestinal epithelial cell permeability. Frontiers in Microbiology. https://pubmed.ncbi.nlm.nih.gov/30972034/

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