Angelicin

Angelicin at a Glance

Angelicin — also called isopsoralen — is the simplest angular furanocoumarin, the bent structural counterpart to the linear psoralens. Its furan ring is fused at the 7,8 position of the coumarin core rather than the 6,7 position, and that single geometric difference governs almost everything distinctive about the molecule. It occurs in the carrot family (angelica, parsnip, hogweed) and the legume family (babchi, Bituminaria), and it takes its name from the genus Angelica.

Like all furanocoumarins, angelicin absorbs ultraviolet-A light and can then bind covalently to DNA. But because of its angular shape it forms mostly single-strand monoadducts rather than the interstrand cross-links that linear psoralens such as bergapten and psoralen produce ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}. This makes it less phototoxic than the linear congeners — cells repair monoadducts more readily — yet it remains genuinely photoreactive and photo-mutagenic, which is why it carries a moderate safety flag rather than a low one.

Beyond its photobiology, isolated angelicin has been studied fairly widely in cells and rodents: anti-inflammatory effects in airway and lung-injury models, anticancer activity in vitro, induction of fetal haemoglobin, antibacterial/bone effects in periodontitis models, and analgesic/antidiarrhoeal signals. All of this is preclinical — there are no human clinical trials of the isolated molecule.

Angular vs. Linear: Why Angelicin Cross-Links Less

The defining fact about angelicin is structural. Coumarin’s furan ring can fuse in two ways:

• Linear furanocoumarins (psoralen, bergapten / 5-MOP, xanthotoxin / 8-MOP, imperatorin) are straight. Under UVA their two photoreactive double bonds sit on opposite ends of a rod-like molecule that intercalates neatly between DNA base pairs, so they can photobind a pyrimidine on each strand — producing interstrand cross-links as well as monoadducts ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}.
• Angular furanocoumarins (angelicin, and its methyl relatives) are bent by the 7,8 furan fusion. That kink is sterically incompatible with reaching across both strands, so angelicin forms predominantly monofunctional monoadducts ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}.

The practical consequence runs in both directions. Cross-links are the more cytotoxic and more mutagenic lesion, and they are harder to repair — so angelicin’s monoadduct-only chemistry makes it markedly less phototoxic than psoralen or 8-MOP ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}. That is precisely what drove mid-twentieth-century interest in angular furanocoumarins as potentially safer photochemotherapy agents. But “less” is not “none”: monoadducts are still mutagenic lesions, and furanocoumarin mixtures carrying angelicin remain photo-genotoxic under UVA ^{9Reference 9Raquet N · 2014Application of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixturesView study →}. Angelicin is therefore the safer-but-still-hazardous member of the family — the reason its badge is moderate, not low.

What It's Used For

The isolated molecule has a broad but uniformly preclinical evidence base. The most developed signal is anti-inflammatory (it reaches whole-animal models); the rest is in-vitro or early rodent work.

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. Every row here is preclinical, so none scores high; read the per-row basis.

01Anti-Inflammatory (Airway & Lung)Promising48%Two mouse models (LPS lung injury, OVA asthma) + defined MAPK/NF-κB mechanism ^{2,3Reference 2Liu F et al. · 2013Angelicin regulates LPS-induced inflammation via inhibiting MAPK/NF-κB pathwaysView study →Reference 3Wei D et al. · 2016AnimalEffects of Angelicin on Ovalbumin (OVA)-Induced Airway Inflammation in a Mouse Model of AsthmaView study →}

02AnticancerShaky40%Multiple cell lines + tubulin/HDAC8 mechanism; one lung-xenograft ^{4,5Reference 4I-Hsiao C et al. · 2023Angelicin inhibits the growth and migration of triple-negative breast cancer cellsView study →Reference 5Mira A · 2015In vitroIn vitro Cytotoxic Activities and Molecular Mechanisms of Angelica shikokiana Extract and its Isolated CompoundsView study →}

03Fetal-Haemoglobin InductionShaky30%In-vitro γ-globin/HbF induction in K562 & erythroid progenitors ^{6Reference 6Lampronti I et al. · 2003Accumulation of gamma-globin mRNA in human erythroid cells treated with angelicinView study →}

04Antibacterial & Bone (Periodontitis)Shaky30%P. gingivalis MIC/biofilm + mouse periodontitis, osteogenic markers ^{7Reference 7Li X et al. · 2018New Application of Psoralen and Angelicin on Periodontitis With Anti-bacterial, Anti-inflammatory, and Osteogenesis EffectsView study →}

05Analgesic & AntidiarrhoealShaky26%Rodent writhing/diarrhoea assays + COX/µ-opioid docking ^{8Reference 8Bagchi S et al. · 2025AnimalExploring the Analgesic and Antidiarrheal Properties of Angelicin Through Cyclooxygenase Inhibition and µ-Opioid Receptor Interaction: In Vivo and In Silico StudiesView study →}

06Photochemotherapy (Angular PUVA)Shaky22%Mechanistic/historical; monoadduct DNA photobinding ^{1,9Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →Reference 9Raquet N · 2014Application of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixturesView study →}

Mechanisms

The DNA-monoadduct row is the anchor: the same photochemistry that underlies any phototherapeutic use is also the source of the genotoxicity that caps the safety rating.

Pharmacokinetics

Dedicated human pharmacokinetic data for isolated angelicin are sparse. As a small, lipophilic furanocoumarin it is absorbed orally and metabolised by hepatic cytochrome P450 enzymes, with glucuronidation of hydroxylated metabolites; systemic exposure of the parent is generally low and variable, which — as with most furanocoumarins — undercuts the high in-vitro concentrations (often 50–150 µM) used in the anticancer and HbF studies ^{4,6Reference 4I-Hsiao C et al. · 2023Angelicin inhibits the growth and migration of triple-negative breast cancer cellsView study →Reference 6Lampronti I et al. · 2003Accumulation of gamma-globin mRNA in human erythroid cells treated with angelicinView study →}. The pharmacologically load-bearing PK point is a class effect on drug metabolism: furanocoumarins are classic mechanism-based (“suicide”) inhibitors of cytochrome P450 — the linear congener 8-methoxypsoralen potently inactivates human CYP2A6 ^{10Reference 10Koenigs LL et al. · 1997Mechanism-based inactivation of human liver cytochrome P450 2A6 by 8-methoxypsoralenView study →}, and the grapefruit furanocoumarins inhibit intestinal CYP3A4. Angelicin belongs to this family, so a plausible interaction risk exists even though angelicin-specific human inhibition constants are not well characterised (see Toxicity).

Clinical Trials

There are no clinical trials of isolated angelicin. The entire human-relevant record is indirect — dietary and topical exposure to furanocoumarin-rich plants, and the historical PUVA experience with linear psoralens (a different subclass). All angelicin-specific data are cell-culture or rodent.

Last checked: July 2026.

Isolate vs. Plant Studies

The angelicin literature is unusually isolate-heavy — a strength for attribution, a caveat for real-world relevance. The anti-inflammatory, anticancer, HbF, antibacterial and analgesic findings all use the purified molecule ^{2,3,4,5,6,7,8Reference 2Liu F et al. · 2013Angelicin regulates LPS-induced inflammation via inhibiting MAPK/NF-κB pathwaysView study →Reference 3Wei D et al. · 2016AnimalEffects of Angelicin on Ovalbumin (OVA)-Induced Airway Inflammation in a Mouse Model of AsthmaView study →Reference 4I-Hsiao C et al. · 2023Angelicin inhibits the growth and migration of triple-negative breast cancer cellsView study →Reference 5Mira A · 2015In vitroIn vitro Cytotoxic Activities and Molecular Mechanisms of Angelica shikokiana Extract and its Isolated CompoundsView study →Reference 6Lampronti I et al. · 2003Accumulation of gamma-globin mRNA in human erythroid cells treated with angelicinView study →Reference 7Li X et al. · 2018New Application of Psoralen and Angelicin on Periodontitis With Anti-bacterial, Anti-inflammatory, and Osteogenesis EffectsView study →Reference 8Bagchi S et al. · 2025AnimalExploring the Analgesic and Antidiarrheal Properties of Angelicin Through Cyclooxygenase Inhibition and µ-Opioid Receptor Interaction: In Vivo and In Silico StudiesView study →}, so the effects can be assigned to angelicin itself rather than to a plant matrix. The catch is the mirror image: humans almost never encounter isolated angelicin. Real exposure is as one furanocoumarin among many in babchi, angelica, parsnip or fig — mixtures in which linear psoralens (bergapten, xanthotoxin) usually dominate the phototoxic burden, and where content swings enormously with species, chemotype and plant part ^{1,9Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →Reference 9Raquet N · 2014Application of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixturesView study →}. So the isolate data establish what angelicin can do at defined concentrations, but transfer poorly to any particular plant preparation.

Its Role in Plants

Furanocoumarins are chemical-defence compounds. Plants build them from the phenylpropanoid pathway: umbelliferone is prenylated and cyclised to the linear precursor for psoralens, or — via a separate prenylation and the enzyme angelicin synthase (a CYP71AJ-family P450) acting on columbianetin — to the angular angelicin ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}. Both branches serve defence: furanocoumarins are phototoxic to insect herbivores and antimicrobial to pathogens.

The angular branch is thought to be an evolutionary escalation. Some specialist insects (for example black swallowtail larvae) evolved P450 enzymes that detoxify linear furanocoumarins; angular furanocoumarins such as angelicin are poorer substrates and can even inhibit those detoxifying enzymes, so producing angelicin helps a plant stay ahead of herbivores that have already adapted to its linear defences ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}. This is plant ecology, not human pharmacology — a molecule’s job as a plant toxin does not predict its value as a medicine.

Prevalence in Nature

Angelicin occurs across two plant families in particular. In the carrot family (Apiaceae) it is found in garden angelica (Angelica archangelica) and other Angelica species, parsnip (Pastinaca sativa) and hogweeds (Heracleum spp.); in the legume family (Fabaceae) it is a constituent of babchi (Psoralea corylifolia, the source of “bakuchi” in Ayurveda) and pitch trefoil (Bituminaria bituminosa). It also appears in figs (Ficus carica) of the Moraceae ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}.

Reported concentrations vary by orders of magnitude with species, tissue and season — on the order of a few tenths of a percent of dry weight in babchi fruit, higher figures reported (seasonally) in fig, and trace levels in some Angelica tissues ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}. Because these figures come from heterogeneous methods and preparations, they are best read as rough ranges, not fixed contents (see the compound’s gaps tracker).

Discovery & Synthesis

Angelicin has been recognised as a constituent of Angelica since the nineteenth century, and its name derives directly from that genus; a precise first-isolation citation is not well documented in the modern literature. Its defining chemistry — the angular 7,8-furan fusion that distinguishes it from linear psoralen — was characterised as furanocoumarin photobiology matured through the mid-twentieth century, when angular furanocoumarins were investigated as potentially less-phototoxic photochemotherapy agents ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →}. Angelicin is accessible by total synthesis (angular furanocoumarins are built by furan-annulation of a hydroxycoumarin), but because it is not a bulk commercial drug, laboratory supply is typically by extraction from babchi or other furanocoumarin-rich plants or by standard synthetic routes, and it is sold mainly as a research chemical rather than manufactured at drug scale.

Patents: not yet researched.

Toxicity & Safety

Angelicin’s moderate flag is earned by its photochemistry, not by ordinary oral toxicity. It is the less dangerous member of the furanocoumarin family — but “less” than the potent skin toxin 8-MOP still leaves a real, UV-dependent hazard.

Safety at a Glance

⚠️ Moderate toxicityPhotosensitivity

• Less phototoxic than linear psoralens. The angular shape forms mostly repairable DNA monoadducts, not the interstrand cross-links that make psoralen/8-MOP strongly phototoxic.
• Still photo-genotoxic under UVA. Angelicin remains photo-mutagenic; furanocoumarin mixtures containing it cause phytophotodermatitis (blistering, hyperpigmentation) after skin contact plus sun.
• Furanocoumarin CYP-inhibition risk. As a member of a class of mechanism-based P450 inhibitors (the “grapefruit effect”), angelicin-rich plant exposure may alter metabolism of CYP3A4/CYP2A6 substrates; angelicin-specific human data are limited.
• No human safety characterisation of the isolate. No trials, no defined dose, no reproductive-toxicity dataset for pure angelicin.

Full Safety & Interactions Detail

Phototoxicity & photo-genotoxicity. Angelicin absorbs UVA and photobinds DNA. Because it forms monoadducts rather than cross-links, cells repair the damage more readily and it is less phototoxic than psoralen or 8-methoxypsoralen ^{1Reference 1Mahendra CK et al. · 2020Angelicin—A Furocoumarin Compound With Vast Biological PotentialView study →} — but it is not benign: angelicin is photo-mutagenic, and furocoumarin mixtures based on an Angelica archangelica pattern (which includes angelicin) are demonstrably photo-genotoxic (photo-mutagenic and -clastogenic) under UVA ^{9Reference 9Raquet N · 2014Application of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixturesView study →}. In practical terms, skin contact with angelicin-containing plants followed by sunlight can provoke phytophotodermatitis — the burning, blistering and lingering hyperpigmentation caused by furanocoumarin-rich plants such as hogweed, parsnip and figs. Sun exposure after handling these plants is the main real-world caution.

Drug-metabolism interactions. Furanocoumarins are the archetypal mechanism-based inhibitors of cytochrome P450 — the basis of the grapefruit-juice drug interaction, where furanocoumarins inhibit intestinal CYP3A4 and raise blood levels of many oral drugs; 8-methoxypsoralen is a potent inactivator of CYP2A6 ^{10Reference 10Koenigs LL et al. · 1997Mechanism-based inactivation of human liver cytochrome P450 2A6 by 8-methoxypsoralenView study →}. Angelicin belongs to this family and can be expected to share the liability qualitatively, so concentrated angelicin/furanocoumarin exposure alongside CYP3A4- or CYP2A6-metabolised medicines is a plausible interaction — though angelicin-specific inhibition constants and clinical relevance are not well established.

Reproductive/developmental note (prose only). No dedicated reproductive-toxicity dataset exists for isolated angelicin. Given the genotoxic potential of photoactivated furanocoumarins, caution is reasonable, but pregnancy/lactation decisions belong to the herb or product page where intake is actually decided, not to this molecule page.

What is not known. This is a phytochemistry-level safety summary. There is no repeat-dose, carcinogenicity or comprehensive interaction package for pure angelicin in humans; absence of a listed harm here is not evidence of safety.

Dosage

There is no established human dose for angelicin. It is a research compound and an incidental dietary/topical exposure from furanocoumarin-bearing plants, not a dosed supplement — the studies above use isolated angelicin at cell-culture concentrations (commonly 25–150 µM) or animal doses in the range of a few to tens of mg/kg ^{2,3,4,6Reference 2Liu F et al. · 2013Angelicin regulates LPS-induced inflammation via inhibiting MAPK/NF-κB pathwaysView study →Reference 3Wei D et al. · 2016AnimalEffects of Angelicin on Ovalbumin (OVA)-Induced Airway Inflammation in a Mouse Model of AsthmaView study →Reference 4I-Hsiao C et al. · 2023Angelicin inhibits the growth and migration of triple-negative breast cancer cellsView study →Reference 6Lampronti I et al. · 2003Accumulation of gamma-globin mRNA in human erythroid cells treated with angelicinView study →}. Any photochemotherapy interest is historical and investigational and would depend on controlled UVA dosing, not on an oral “dose” of the compound. These are figures from research, not a personal recommendation.

References

1. Mahendra CK, Tan LTH, Lee WL, et al. (2020). Angelicin—A Furocoumarin Compound With Vast Biological Potential. Frontiers in Pharmacology. https://pubmed.ncbi.nlm.nih.gov/32372949/
2. Liu F, Sun GQ, Gao HY, et al. (2013). Angelicin regulates LPS-induced inflammation via inhibiting MAPK/NF-κB pathways. Journal of Surgical Research. https://pubmed.ncbi.nlm.nih.gov/23816246/
3. Wei D, Guo XY, Lin LN, et al. (2016). Effects of Angelicin on Ovalbumin (OVA)-Induced Airway Inflammation in a Mouse Model of Asthma. Inflammation. https://pubmed.ncbi.nlm.nih.gov/27581277/
4. I-Hsiao C, Chien-Yu C, Yu-Hsuan L, I-Fen C (2023). Angelicin inhibits the growth and migration of triple-negative breast cancer cells. Pakistan Journal of Pharmaceutical Sciences. https://pubmed.ncbi.nlm.nih.gov/36967496/
5. Mira A, Shimizu K (2015). In vitro Cytotoxic Activities and Molecular Mechanisms of Angelica shikokiana Extract and its Isolated Compounds. Pharmacognosy Magazine. https://pubmed.ncbi.nlm.nih.gov/27013795/
6. Lampronti I, Bianchi N, Borgatti M, Fibach E, Prus E, Gambari R (2003). Accumulation of gamma-globin mRNA in human erythroid cells treated with angelicin. European Journal of Haematology. https://pubmed.ncbi.nlm.nih.gov/12930320/
7. Li X, Yu C, Hu Y, et al. (2018). New Application of Psoralen and Angelicin on Periodontitis With Anti-bacterial, Anti-inflammatory, and Osteogenesis Effects. Frontiers in Cellular and Infection Microbiology. https://pubmed.ncbi.nlm.nih.gov/29922598/
8. Bagchi S, Khatun MM, et al. (2025). Exploring the Analgesic and Antidiarrheal Properties of Angelicin Through Cyclooxygenase Inhibition and µ-Opioid Receptor Interaction: In Vivo and In Silico Studies. Drug Development Research. https://doi.org/10.1002/ddr.70201
9. Raquet N, Schrenk D (2014). Application of the equivalency factor concept to the phototoxicity and -genotoxicity of furocoumarin mixtures. Food and Chemical Toxicology. https://pubmed.ncbi.nlm.nih.gov/24680798/
10. Koenigs LL, Peter RM, Thompson SJ, Rettie AE, Trager WF (1997). Mechanism-based inactivation of human liver cytochrome P450 2A6 by 8-methoxypsoralen. Drug Metabolism and Disposition. https://pubmed.ncbi.nlm.nih.gov/9394031/

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