Alantolactona

Otros Nombres

(3aR,5S,8aR,9aR)-3a,5,6,7,8,8a,9,9a-Octahydro-5,8a-dimethyl-3-methylenenaphtho[2,3-b]furan-2(3H)-one(3aR,5S,8aR,9aR)-5,8a-dimethyl-3-methylidene-3a,5,6,7,8,8a,9,9a-octahydronaphtho[2,3-b]furan-2(3H)-one(3AR-(3aalpha,5beta,8abeta,9aalpha))-3a,5,6,7,8,8a,9,9a-octahydro-5,8a-dimethyl-3-methylenenaphtho(2,3-b)furan-2(3H)-one4alphaH-Eudesma-5,11(13)-dien-12-oic acid, 8beta-hydroxy-, gamma-lactone4αH-Eudesma-5,11(13)-dien-12-oic acid, 8β-hydroxy-, γ-lactone8b-Hydroxy-4aH-eudesm-5-en-12-oic acid, gamma-lactoneAlant camphorAlantolactone (6CI)ALLANTOLACTONEElecampane camphorEupatalHeleninHelenin (7CI)HelenineInula camphorNaphtho[2,3-b]furan-2(3H)-one, 3a,5,6,7,8,8a,9,9a-octahydro-5,8a-dimethyl-3-methylene-, (3aR,5S,8aR,9aR)-

Sinopsis

Alantolactone: A Comprehensive Reference

1. Identity and Chemical Characterization

Chemical Names and Classification

Alantolactone (abbreviated Ala or ALT) is a sesquiterpene lactone (STL) — a C15 terpenoid secondary metabolite produced by combining three isoprene units. More precisely, alantolactone is a eudesmane-type sesquiterpene lactone containing an α-methylene-γ-lactone moiety. This structural subclass is called a eudesmanolide, distinguishing it from guaianolides and germacranolides within the broader sesquiterpene lactone family.

Alantolactone is denoted by a molecular formula of C₁₅H₂₀O₂ and has a molecular weight of 232.32 g/mol. The compound is identified by CAS Registry Number 546-43-0. Its IUPAC systematic name is (3aS,6R,9aS,9bR)-3a,6-dimethyl-3-methylidene-3a,4,5,6,7,8,9,9b-octahydro-3H-benzo[e][1]benzofuran-2-one, though it is more commonly referred to in the literature as alantolactone, elecampane camphor, or helenin (the latter term historically also applied to a mixture of alantolactone and isoalantolactone). Alantolactone is described in chemical databases as an allergenic sesquiterpene lactone and may be encountered as a crystalline mixture with related alantolactones within the sesquiterpene group.

Botanical Sources

Alantolactone, a sesquiterpene lactone derived from plants of the Asteraceae family, has been extensively studied for its diverse pharmacological potential. The primary and best-studied botanical source is Inula helenium L. (elecampane), but the compound occurs across a broad range of plants within this family. Alantolactone can be isolated from Inula helenium, Inula racemosa, Inula royleana, Saussurea costus, Carpesium macrocephalum, Chrysanthemum indicum, Globba schomburgkii, Stevia lucida, and Telekia sp. An additional source confirmed in recent reviews is Ajania fruticulosa, Aucklandia lappa, Carpesium macrocephalum, Chrysanthemum indicum, Inula racemosa, I. helenium, Inula japonica, Inula royleana, and Saussurea costus.

Within I. helenium, alantolactone is concentrated predominantly in the root and rhizome. Alantolactone and isoalantolactone are the major active ingredients of Inulae Radix (the dried root recognized in the Chinese Pharmacopoeia). The root oil of Inula racemosa contains alantolactone, which is widely utilized as an anthelmintic, antiseptic, and expectorant, and also as a home remedy for boils and skin infections.

Related Compounds and Common Preparations

Alantolactone co-occurs in plant sources with structurally closely related sesquiterpene lactones. The natural products attributing to the antimicrobial activity observed in vitro were identified as alantolactone (1), isoalantolactone (2), igalan (3), and an unseparated mixture of dugesialactone (4) and alloalantolactone (5) as major compounds in Inula helenium root. Isoalantolactone is the most pharmacologically studied congener and epimer of alantolactone. In research and supplement contexts, the compound is encountered as:

Isolated pure compound — extracted and purified from Asteraceae roots for laboratory and preclinical research
Standardized root extract — hydro-ethanolic or ethanolic extracts of Inula helenium root, prepared to a known sesquiterpene lactone content
Crude root preparations — decoctions, teas, and tinctures used in traditional medicine systems
Dried root powder — used in traditional dose forms
Essential oil fraction — the root oil of several Inula species contains alantolactone as a key constituent

Emerging studies have reported several promising strategies to enhance the oral bioavailability of ALT, such as combining ALT with other herbs and using ALT-entrapped nanostructured carriers.

2. Traditional and Historical Use

Ancient Greek and Roman Traditions

Inula helenium, the plant containing alantolactone, carries a name that reaches deeply into classical antiquity. The Latin name of elecampane (Inula helenium) comes from the story of Helen of Troy, who was supposed to have carried the herb elecampane with her while being abducted from Sparta. Revered by the ancient Greeks and Romans, this herb was recommended for treating such diverse problems as indigestion, melancholy, sciatica, bronchitis, and asthma. The ancient Romans used the plant as both medicine and food. Hippocrates also used the plant to treat chronic skin eruptions and itching. The roots of the plant have been traditionally used as a diuretic in Europe, as a fragrance in Japan, and as a preservative in China.

Celtic and European Folk Traditions

The common name "elfwort" is connected to the belief in Celtic times that the herb possessed magical properties; elves were variously believed to favour the plant and also to reside within it. The common name "scabwort" came about from the use of the root, boiled well in vinegar, beaten and made into a salve with suet or oil of trotters for scabs or itch, including for use on sheep. The decoctions from the vinegar-boiled root were also applied to "putrid sores or cankers." It has a long history of use for "old coughs," especially in tuberculosis and for advanced lung conditions to help remove phlegm, such as bronchiectasis, pneumoconiosis, whooping cough, and bronchitis.

The common name "Horseheal" was derived from its use by veterinarians in treating pulmonary disorders in horses, while "Scabwort" came from the herb's reputed effectiveness in healing scabs on sheep. Elecampane root is also one of the ingredients used in the preparation of absinthe.

Ayurvedic Tradition

Ayurvedic medicine uses the same two species of elecampane root (Inula helenium and I. racemosa; known as pushkaramula), not only to clear the lungs but also as a lung rejuvenative tonic since it promotes the longevity of lung tissue. Reducing kapha and vata and increasing pitta, it is considered expectorant, antispasmodic, carminative, analgesic, and rejuvenative. Ayurveda uses Inula helenium for chronic bronchitis, asthma, cardiac asthma, pleurisy, dyspepsia, cough, rheumatism, skin eruptions, all kinds of pain especially that arising from chill, and animal bites. The Ayurvedic tradition uses elecampane for respiratory complaints and rheumatism as well as skin problems including bites and stings.

Traditional Chinese Medicine (TCM) and Tibetan Medicine

Radix Inulae is a commonly used traditional Chinese and Tibetan medicine, particularly valued for its gastric effects and antibacterial action. In traditional medicine systems like Traditional Chinese Medicine (TCM), alantolactone is utilized for its health benefits. The source plant, known as Xuanfuhua or Tujinggen in Chinese, has appeared in classical materia medica texts for centuries.

Inula racemosa is a plant species of the genus Inula distributed in the northwest belt and high-altitude areas of the Himalayas, and it is extensively utilized in the conventional medicinal systems of India, China, and Tibet to treat a variety of illnesses. Elecampane contains alantolactone, which has been used against intestinal parasites and is recognized for its anti-inflammatory properties.

American Indigenous Use

American Indians used the roots medicinally in infusions and decoctions to treat lung diseases. The herb was also naturalized in North America after European colonization, where it became incorporated into local herbal traditions.

3. Key Constituents and Active Compounds

Principal Phytochemicals

While this article focuses on alantolactone itself, it is important to note that the plant sources from which it is derived contain multiple bioactive constituents. In Inula helenium root, the major sesquiterpene lactones are alantolactone and isoalantolactone, along with smaller amounts of igalan, dugesialactone, and alloalantolactone. The root also contains up to 44% of the carbohydrate inulin as well as mucilage.

Structural Pharmacophore

The α-methylene group attached to the γ-lactone is considered the immunologic and pharmacological requisite of alantolactone and other sesquiterpene lactones. Such a group is known to be capable of undergoing "Michael-type addition" with the sulfhydryl group of cysteine. Alantolactone can also undergo addition with the imidazole group of histidine and with the ε-amino group of lysine, but not with the guanido group of arginine, the hydroxyl group of serine, or the thioether function of methionine. This reactivity toward nucleophilic amino acid side chains underlies both the pharmacological activity and the sensitizing (allergenic) potential of the molecule.

4. Established Mechanisms of Action

NF-κB Pathway Inhibition

One of the most consistently documented mechanisms is alantolactone's inhibition of the nuclear factor-κB (NF-κB) signaling pathway. Alantolactone is a eudesmane-type sesquiterpene lactone containing an α-methylene-γ-lactone moiety, and previous studies have shown that it inhibits the NF-κB signaling pathway by targeting the inhibitor of NF-κB (IκB) kinase. Besides antimicrobial activities against bacteria, fungi, and viruses, alantolactone has also demonstrated significant anti-inflammatory effects in various models by inhibiting NF-κB and MAPKs to decrease pro-inflammatory cytokines such as IL-1β, IL-6, and TNF-α.

STAT3 Inhibition

Alantolactone effectively suppressed both constitutive and inducible STAT3 activation, inhibited its translocation into the nucleus, and decreased its DNA binding activity. Further mechanistic study revealed that alantolactone abrogated STAT3 activation by promoting STAT3 glutathionylation. This glutathionylation mechanism represents a relatively novel way in which alantolactone modulates STAT3, distinct from direct binding to the SH2 domain.

MAPK Pathway Modulation

These findings suggested that alantolactone possesses anticancer activity via ROS-mediated mitochondrial dysfunction involving the MAPK pathway, and had an effect on the transcription factors NF-κB, AP-1, and STAT3.

Reactive Oxygen Species (ROS) and Oxidative Stress Induction in Cancer Cells

In A549 lung adenocarcinoma cells, alantolactone effectively inhibits proliferation and triggers oxidative stress–mediated apoptosis by inducing ER stress and mitochondrial dysfunction. This alantolactone-mediated apoptosis was inhibited by N-acetylcysteine (NAC) while the thiol oxidant diamide potentiated it, confirming the centrality of thiol chemistry and ROS generation in the compound's anticancer action in cell culture.

Nrf2 Antioxidant Pathway Activation

The antioxidant potential of alantolactone is attributed to activating the Nrf2 pathway, which leads to the induction of detoxifying and antioxidant enzymes. This is particularly relevant to its hepatoprotective and anti-inflammatory effects, where the compound appears to act as a dual regulator — inducing Nrf2-driven cytoprotection while suppressing NF-κB–driven inflammation.

Apoptosis Induction

The antitumor effects of alantolactone have been demonstrated in vitro and in vivo via inducing intrinsic apoptosis, oxidative stress, ER stress, cell cycle arrest, and inhibiting autophagy and STAT3 phosphorylation, which are also involved in its combination or synergy with other antitumor drugs. In breast cancer MCF-7 cells, alantolactone induced apoptosis by regulating the protein expression levels of Bcl-2, Bcl-2-associated X protein (Bax), p53, caspase-3, and caspase-12, which are associated with the apoptotic pathway, and suppressed colony formation and migration by regulating the protein expression of MMP-2, MMP-7, and MMP-9.

PI3K/Akt Signaling

In addition to NF-κB and STAT3, alantolactone has been shown to modulate the PI3K/Akt pathway. ATL treatment attenuated neurologic deficits, inhibited neuronal apoptosis and inflammatory reaction, promoted polarization of microglia toward the M2 phenotype, and activated the PI3K/Akt signaling pathway in a rat model of subarachnoid hemorrhage.

L-type Voltage-Gated Calcium Channel Inhibition

The antihypertensive activity of alantolactone involves inhibition of L-type voltage-gated calcium channels (VGCCs), leading to reduced calcium influx in vascular smooth muscle cells and ultimately suppression of vascular contraction.

TNF-R1 Modulation

Alantolactone selectively down-regulated the expression of tumor necrosis factor (TNF) receptor 1 (TNF-R1) in human lung adenocarcinoma A549 cells. Alantolactone did not affect the expression of three adaptor proteins recruited to TNF-R1. The down-regulation of TNF-R1 expression by alantolactone was suppressed by an inhibitor of TNF-α-converting enzyme, and alantolactone increased the soluble forms of TNF-R1 that were released into the culture medium as an ectodomain. Structure-activity relationship analysis of eight eudesmane derivatives revealed that the α-methylene-γ-lactone moiety was needed to promote TNF-R1 ectodomain shedding.

Quorum Sensing Inhibition

A study investigated the quorum quenching and biofilm inhibition properties of alantolactone against Pseudomonas aeruginosa PAO1. The production of key virulence factors and biofilm components were affected in bacteria when treated with sub-minimum inhibitory concentrations (sub-MIC) of alantolactone, and the anti-infective potential was corroborated in an in vivo model with improved survival of infected Caenorhabditis elegans and reduced bacterial colonization.

5. Scientific Evidence by Area of Use

5.1 Anticancer Activity

Evidence level: Predominantly preclinical (in vitro and animal); no clinical human trials identified.

Alantolactone is a natural compound extracted from traditional Chinese medicine Inula helenium L. with therapeutic potential in the treatment of various diseases. In vitro and in vivo studies have indicated cytotoxic effects of alantolactone on various cancers, including liver cancer, colorectal cancer, and breast cancer. The inhibitory effects of alantolactone depend on several cancer-associated signaling pathways and abnormal regulatory factors in cancer cells.

Lung cancer: In A549 lung adenocarcinoma cells, alantolactone effectively inhibits proliferation and triggers oxidative stress–mediated apoptosis by inducing ER stress and mitochondrial dysfunction. Alantolactone could significantly enhance the anticancer effects of the chemotherapy drug gemcitabine on A549 cells and NCI-H520 cells through inhibiting the activation of AKT/glycogen synthase kinase (GSK)-3β and endoplasmic reticulum (ER) stress pathways.

Breast cancer: The anticancer effects of alantolactone on the human breast cancer cell line MCF-7 were investigated in vitro. Cell viability was reduced significantly compared with that of control cells. Cell signaling pathway analysis confirmed that alantolactone increased the phosphorylation of p38 and decreased the nuclear expression levels of p65 and Nrf2. A separate study reported that alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells.

Glioblastoma: Glioblastoma multiforme (GBM) is one of the most refractory CNS neoplasms, and current treatments have poor effects in GBM patients. Alantolactone has a wide range of pharmacological activities, and its anti-tumor effect has received increasing attention in this context. Research demonstrated potent antitumor activity against GBM by targeting IKKβ kinase activity and interrupting NF-κB/COX-2-mediated signaling cascades.

Prostate cancer: Alantolactone exerts anticancer activity in different types of cancers. One study investigated the relationship between alantolactone and cancer stem cells (CSCs) in prostate cancer (PCa) metastasis and the molecular mechanisms involved in the progression of PCa.

Cervical cancer: Alantolactone exhibits potent anti-inflammatory and anticancer activities. Researchers investigated the mechanism of alantolactone in reducing the proliferation, migration, and invasion of HeLa and SiHa cervical cancer cells as well as its promotion of mitochondrial damage and autophagy.

Other cancer cell lines: Alantolactone demonstrates antiproliferative effects on several cancer cell lines, including colon, melanoma, ovary, prostate, lung, and leukemia cell lines. Alantolactone isolated from Inula helenium provides effective inhibitory activity for cell growth against MK-1, HeLa, B16F10, and K562 cell lines.

Limitation: All findings described above are from cell culture models or rodent models. Further basic and clinical research must validate the safety, pharmacodynamics, and therapeutic efficacy of alantolactone in humans. No completed clinical trials in humans have been identified in the peer-reviewed literature for any oncology indication.

5.2 Anti-Inflammatory Activity

Evidence level: Robust preclinical (in vitro and animal); no human clinical trials.

Besides antimicrobial activities against bacteria, fungi, and viruses, alantolactone has demonstrated significant anti-inflammatory effects in various models by inhibiting NF-κB and MAPKs to decrease pro-inflammatory cytokines such as IL-1β, IL-6, and TNF-α.

Psoriasis model: A study aimed to evaluate the antipsoriatic potential of alantolactone in vitro and in vivo. The results showed that alantolactone significantly attenuated IL-17A, IL-22, oncostatin M, IL-1α, and TNF-α cytokine-induced hyperproliferation in HaCaT keratinocytes. M5 cytokines significantly upregulated mRNA levels of TNF-α, IL-6, IL-1β, and IL-8, but alantolactone attenuated the upregulation of these inflammatory cytokines. In addition, alantolactone was found to inhibit STAT3 phosphorylation and NF-κB p65 nuclear translocation in HaCaT keratinocytes.

Skeletal muscle inflammation / insulin resistance: Protective effects of alantolactone, a sesquiterpene lactone isolated from Inula helenium, were observed against glucose intolerance and insulin resistance induced by prolonged exposure to IL-6. Alantolactone has been reported to have anti-inflammatory and anti-cancer effects through IL-6-induced STAT3 signaling pathway.

5.3 Antimicrobial Activity

Evidence level: Preclinical in vitro; some in vivo animal data; no human clinical trials.

In Irish ethnomedical literature, Inula helenium L. (elecampane) is often indicated for respiratory and dermal ailments, a traditional use that has been explored in laboratory settings. The natural products attributing to antimicrobial activity observed in vitro were identified as alantolactone (1), isoalantolactone (2), igalan (3), and an unseparated mixture of dugesialactone (4) and alloalantolactone (5) as major compounds. The findings suggest that the geographical origin of the plant does not influence the anti-bacterial potency nor the chemical composition of traditional elecampane root.

Antibacterial activity has been documented against Staphylococcus aureus and Mycobacterium tuberculosis in laboratory studies. Antibacterial activities of alantolactone have been reported against Mycobacterium tuberculosis and Staphylococcus aureus. Against Pseudomonas aeruginosa, alantolactone operates via a quorum-quenching mechanism rather than direct bactericidal activity: a study investigated the quorum quenching and biofilm inhibition properties of alantolactone against P. aeruginosa PAO1, and the production of key virulence factors and biofilm components were affected in bacteria when treated with sub-MIC of alantolactone.

5.4 Antifungal Activity

Evidence level: In vitro; preliminary.

Alantolactone, the major active sesquiterpene lactone component of Inula helenium, has pleiotropic activity, including neuroprotective, antiviral, and anti-inflammatory, as well as antibacterial activities. In addition, alantolactone has demonstrated fungistatic activity against Fusarium solani in vitro, a fungal pathogen for plants and humans, at concentrations above 100 μg/mL. Research has also specifically examined activity against Candida albicans biofilms, driven by the clinical challenge of drug-resistant fungal infections.

5.5 Anthelmintic (Antiparasitic) Activity

Evidence level: Traditional use supported by limited laboratory data; no modern human clinical trials.

Elecampane contains alantolactone, which has been used against intestinal parasites. Traditional uses include killing worms that can live in the intestine, including hookworm, roundworm, threadworm, and whipworm. Studies on alantolactone and isoalantolactone showed larvicidal activities, and the compound presents a capability as a skin sensitizer. This anthelmintic property has historically been one of the primary uses of the parent plant.

5.6 Antiviral Activity

Evidence level: In vitro only; preliminary.

Alantolactone, a eudesmanolide sesquiterpene lactone derived from Inula helenium, has been reported to exhibit potent antiviral activity against Hepatitis C Virus (HCV), with an EC₅₀ value of less than 3 μM. These findings come from in vitro studies and have not been translated to clinical settings.

5.7 Neuroprotective Activity

Evidence level: Animal model studies only; no human clinical trials.

Alantolactone has neuroprotective activity through attenuating oxidative stress and inflammation, besides its modulation of glucose and lipid metabolism.

Traumatic brain injury and subarachnoid hemorrhage: In a rat subarachnoid hemorrhage model, alantolactone treatment attenuated neurologic deficits, inhibited neuronal apoptosis and inflammatory reaction, promoted polarization of microglia toward the M2 phenotype, and activated the PI3K/Akt signaling pathway. This was the first study to demonstrate the role of alantolactone in a subarachnoid hemorrhage model and to demonstrate its anti-apoptosis and anti-inflammatory properties after SAH.

5.8 Metabolic Effects: Glucose and Lipid Homeostasis

Evidence level: Cell culture and animal model studies; no human clinical trials.

Non-alcoholic fatty liver disease (NAFLD): C57BL/6 mice were fed a high-fat diet (HFD) to induce NAFLD. After 16 weeks, alantolactone was administered by gavage to observe its effect on NAFLD. RNA sequencing of liver tissues was performed to investigate the mechanism. In vitro, mouse cell line AML-12 was pretreated with alantolactone to resist palmitic acid-induced inflammation, oxidative stress, and fibrosis. Alantolactone significantly inhibited inflammation, fibrosis, and oxidative stress in HFD-induced mice, as well as in palmitic acid-induced AML-12 cells. Mechanistic studies showed that the effect of alantolactone was related to the induction of Nrf2 and the inhibition of NF-κB.

Lipid homeostasis: One study used luciferase reporter screening to identify alantolactone as a natural compound that can inhibit the promoter activity of APOC3. Alantolactone decreased APOC3 expression at both mRNA and protein levels. Pretreatment of L02 liver cells with oxLDL to investigate lipid homeostasis showed that alantolactone attenuated oxLDL-induced foam cell formation by reducing total cholesterol (TC) and triglyceride (TG) contents. Furthermore, these results could be reversed by overexpressing APOC3 protein. Alantolactone inhibited tyrosine phosphorylation (Tyr705pho) of STAT3 to down-regulate APOC3 expression.

Insulin resistance: Protective effects of alantolactone, a sesquiterpene lactone isolated from Inula helenium, were observed against glucose intolerance and insulin resistance induced by prolonged exposure of IL-6 in a cell culture experimental system. In streptozotocin-induced diabetic mice, alantolactone inhibited high glucose-induced proinflammatory cytokine production by inhibiting the NF-κB pathway.

5.9 Antihypertensive Activity

Evidence level: Mechanistic in vitro data only.

Research suggests that the antihypertensive activity of alantolactone involves inhibition of L-type voltage-gated calcium channels, leading to reduced calcium influx in vascular smooth muscle cells and ultimately suppression of vascular contraction. No clinical data in humans are available.

5.10 Skin Conditions (Psoriasis)

Evidence level: In vitro keratinocyte models and mouse model; no human clinical trials.

Psoriasis is an immune-mediated inflammatory disease affecting 2% to 3% of the world population. Alantolactone, a sesquiterpene lactone isolated from Inula helenium and Radix inulae, has several biological effects, including antifungal, anthelmintic, antimicrobial, anti-inflammatory, antitrypanosomal, and anticancer properties. A study aimed to evaluate the antipsoriatic potential of alantolactone in vitro and in vivo. The results demonstrated suppression of psoriasis-relevant cytokines and inhibition of STAT3 and NF-κB pathways in keratinocyte cell models and in an imiquimod-induced mouse model of psoriasis.

6. Body Systems Associated with Alantolactone

Immune system: Modulation of NF-κB, STAT3, and MAPK inflammatory signaling; suppression of TNF-α, IL-1β, IL-6, and IL-8
Oncology / cell cycle: Apoptosis induction, cell cycle arrest, inhibition of cancer cell migration and invasion across multiple tumor types (cell culture/animal data only)
Central nervous system: Neuroprotection in traumatic brain injury and subarachnoid hemorrhage models via PI3K/Akt activation and NF-κB suppression
Hepatic / metabolic: Attenuation of NAFLD-associated inflammation and fibrosis; modulation of lipid metabolism via APOC3 and STAT3; reduction of glucose intolerance in inflammatory contexts
Cardiovascular: Inhibition of L-type calcium channels in vascular smooth muscle; suppression of APOC3-related dyslipidemia
Gastrointestinal / parasitology: Traditional and experimental anthelmintic activity against intestinal parasites
Respiratory: Historically used as an expectorant and for respiratory infections; contemporary in vitro antimycobacterial data
Skin / integumentary: Anti-inflammatory and antiproliferative activity in psoriasis models; historical use for dermatoses
Infectious disease: Antibacterial (including anti-staphylococcal and anti-tubercular), antifungal, antiviral (HCV in vitro), and anti-Pseudomonas quorum-quenching activities

7. Dosage Forms and Reported Doses

There are currently no established clinical dosage guidelines for isolated alantolactone in humans, as no completed human clinical trials have been published. The following doses and forms appear in primary sources:

Elecampane root (traditional/herbal): The root of the plant is utilized in various forms, typically in dosages of 1.5 to 4 grams three times daily. A typical dosage of elecampane root is 1.5 to 4 grams three times daily, either in capsule form or boiled in water as tea. These doses refer to the whole root or its preparation; the actual alantolactone content will vary by extraction method and plant source.
In vivo animal studies: In a mouse NAFLD model, C57BL/6 mice were fed a high-fat diet for 16 weeks, after which alantolactone was administered by gavage to observe its effect. Specific milligram-per-kilogram doses were not extracted from abstract-level data available.
In vitro studies: In a psoriasis model study, HaCaT keratinocytes were treated with alantolactone at concentrations of 1.25, 2.5, and 5 μM.
Antiviral activity: Alantolactone has been reported to exhibit potent antiviral activity against Hepatitis C Virus (HCV) with an EC₅₀ value of less than 3 μM in cell-based assays.
Antifungal activity: Alantolactone demonstrated fungistatic activity against Fusarium solani in vitro at concentrations above 100 μg/mL.

Although published data support the safety and efficacy of Saussurea costus (a key alantolactone source), the active constituents, physiological pathways, pharmacokinetics, bioavailability, and consequences to human health are not known with ample detail. Optimizing delivery methods to enhance bioavailability remains a critical focus of current research.

8. Safety Considerations

Allergic Contact Dermatitis

Alantolactone is one of the best-characterized plant-derived contact allergens. Alantolactone and isoalantolactone are two moderate allergens from Inula helenium L. Only alantolactone showed a significant sensitizing response in vivo and in vitro in epicutaneously sensitized mice, without using Freund's complete adjuvant. Isoalantolactone did not show any sensitizing capacity in the murine model studied. Comparison of in vitro lymphocyte proliferation and in vivo allergenic capacity showed a good correlation and clearly demonstrated that, of the two sesquiterpene lactones, alantolactone is the better sensitizer.

The mechanism of sensitization is well characterized: an adduct of alantolactone with guinea pig skin proteins induces, in guinea pigs, a state of delayed hypersensitivity to alantolactone and cross-reaction to other natural or synthetic α-methylene-γ-butyrolactones, as assessed by epicutaneous tests to the haptens. This cross-reactivity has clinical relevance for individuals with Asteraceae/Compositae sensitivity: samples of alantolactone that have undergone addition reactions with amino acid side chains no longer produce allergic eczematous contact dermatitis, as measured by patch test, confirming that the intact α-methylene-γ-lactone group is required for sensitization.

Asteraceae Family Cross-Reactivity

Individuals who have demonstrated sensitivity to alantolactone may react to other plants within the Asteraceae family due to the presence of related sesquiterpene lactones. Elecampane may cause hypersensitivity reactions in patients with an existing allergy to plants in the Asteraceae family.

Systemic Toxicity at High Doses

Elecampane (the primary source of alantolactone) is possibly safe for most adults in conventional doses, but large amounts of elecampane are possibly unsafe. Large amounts can cause vomiting, diarrhea, spasms, and paralysis. These effects are attributed to the bioactive sesquiterpene lactone constituents, including alantolactone, at high systemic exposure.

Absence of Human Pharmacokinetic Data

Although published data support the safety and efficacy of alantolactone's source plants, the active constituents, physiological pathways, pharmacokinetics, bioavailability, and consequences to human health are not known with ample detail. Therefore, active constituents including alantolactone could be used in clinical trials for treating different types of diseases. Until such trials are completed, the absorption, distribution, metabolism, and excretion (ADME) profile in humans remains incompletely characterized.

Pregnancy and Lactation

Information regarding safety and efficacy of elecampane and its constituents in pregnancy and lactation is lacking. No human data are available.

Drug Interactions

Another aspect of research that must be addressed for clinical use is the interaction of alantolactone with other drugs, and the outcomes of both in vitro and preclinical studies must be critically analyzed and incorporated into practical uses. Formal drug–drug interaction studies in humans have not been reported.

Clinical Trials Status

Clinical trials evaluating the use of elecampane are lacking; however, in vitro research focuses on potential application in chemotherapy and immunotherapy. Antibacterial, cardiovascular, and hypoglycemic effects have also been suggested. The same gap applies specifically to isolated alantolactone: the entirety of published evidence remains at the preclinical stage as of mid-2025.

9. Current Research Landscape and Future Directions

Given the role of inflammation in the pathogenesis of numerous chronic diseases, alantolactone is a remarkable natural compound with immense therapeutic potential, demonstrating various pharmacological activities, including anticancer, anti-inflammatory, antibacterial, antioxidant, insecticidal, neuroprotective, and lipid metabolism-modulating properties.

Alantolactone is known for its wide spectrum of biological effects, including antimicrobial, antifungal, antiviral, and anthelmintic activities; anti-inflammatory activities; and antiproliferative effects on several cancer cell lines. It has received extensive attention, causing in-depth research in medicinal chemistry, and numerous novel alantolactone derivatives have been synthesized through different strategies.

Research suggests that various biochemical pathways are involved in the bioactivity of alantolactone, such as STAT3, MAPK/NF-κB, and YAP1/TAZ pathways for anticancer; proinflammatory cytokines NF-κB and STAT3 signaling for anti-inflammatory; the Nrf2 pathway for antioxidant; L-type voltage-gated calcium channels for antihypertensive; enhanced reactive oxygen species production for antifungal properties; and potential to alter lipid metabolism via suppression of IL-6-stimulated TLR-4 expression.

Alantolactone's wide spectrum of biological effects has led to in-depth research in medicinal chemistry, and numerous previously undescribed alantolactone derivatives have been synthesized through different strategies with the aim of improving potency, selectivity, and pharmacokinetic properties.

References

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Quimioterapia (reducción de efectos secundarios)Científico
Alantolactone is a sesquiterpene lactone from Elecampane (Inula helenium) root with documented expectorant, antitussive, and antimicrobial properties relevant to respiratory health. It relaxes tracheal smooth muscle and has shown activity against respiratory pathogens including Mycobacterium tuberculosis.

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