Triterpenes

Other Names

C30 isoprenoidsC30 terpenesC30 terpenoidsHexaprenyl compoundsNortriterpenesOxidosqualene-derived terpenesPentacyclic triterpenoidsPhytosterols (triterpene subclass)Plant isoprenoids (C30)Plant sterols (triterpene subclass)Sapogenins (triterpene aglycones)Six-isoprene-unit terpenesSqualene-derived terpenesSterols (triterpene subclass)Tetracyclic triterpenoidsTetranortriterpenoidsTriterpeneTriterpene glycosidesTriterpene saponinsTriterpenoidTriterpenoid glycosidesTriterpenoid saponinsTriterpenoids

Synopsis

Triterpenes: A Comprehensive Reference

1. Identity: Chemical and Botanical Overview

Triterpenes are a subclass of terpenes with a fundamental skeleton of 30 carbons (C30). They are a diverse group of natural organic compounds found widely in plants, fungi, and some animals, and are a subclass of terpenes derived from a common five-carbon building block called isoprene. Biogenetically, triterpenes are derived from isoprene and are composed of six isoprene units or three terpene units, with one isoprene unit consisting of five carbon atoms.

Triterpenes are characterized by a basic chemical structure derived from squalene, a 30-carbon precursor molecule. This C30 hydrocarbon backbone undergoes various cyclization and modification reactions, leading to a vast array of distinct structures. Nearly 200 different triterpene skeletons exist, categorized by their ring count, with pentacyclic (five-ring) structures being common. The vast majority of triterpenes are composed of tetra- and pentacyclic compounds that are modified by splitting off and attaching carbon atoms and by incorporating heteroatoms such as nitrogen.

Triterpenoids are oxygen-containing derivatives or degradation products of the naturally occurring compound triterpene; however, the terms triterpenoid and triterpene are sometimes used interchangeably. Plants frequently accumulate glycosylated versions of these chemicals, known as triterpenoid saponins, which are composed of hydrophobic triterpenoid aglycones termed sapogenin and one or more hydrophilic sugar moieties.

Principal Structural Classes

Oleanane-type: Includes oleanolic acid (3β-hydroxyolean-12-en-28-oic acid) and glycyrrhizin (from licorice). These belong to the oleanane subclass of pentacyclic triterpenoids.
Ursane-type: Ursolic acid (3β-hydroxy-urs-12-en-28-oic acid) is a close structural isomer of oleanolic acid and betulinic acid, all belonging to the natural pentacyclic triterpenoid carboxylic acids.
Lupane-type: Betulinic acid (a pentacyclic triterpenoid) is found in the bark of plane, birch, and eucalyptus trees and has emerged as a compound of significant interest due to its potential therapeutic applications.
Dammarane-type: Dammarane-type triterpenoids (DTT) are widely distributed in various medicinal plants and have generated great interest in drug research and development; they are the main bioactive ingredients abundant in Araliaceae plants such as Panax ginseng, P. notoginseng, and P. quinquefolium.
Lanostane-type: Found prominently in fungi, including the ganoderic acids of Ganoderma lucidum.
Cucurbitane-type: Cucurbitanes are a group of triterpenes named for their occurrence in plants of the Cucurbitaceae family, such as cucumbers, melons, and gourds.
Boswellic acids (β-pentacyclic triterpene acids): The β-pentacyclic triterpene acids in Boswellia serrata include 3-acetyl-11-keto-β-boswellic acid (AKBBA), 11-keto-β-boswellic acid (KBBA), β-boswellic acid (BBA), and 3-acetyl-β-boswellic acid (ABBA), which represent the major bioactive boswellic acids in the gum resin.
Squalene: One of the most important triterpenoids is squalene, from which other triterpenoids are synthesized; squalene is also produced in animals and serves as a precursor to all steroids, including cholesterol.

Natural Sources

Triterpenes are found in a wide variety of natural sources and are found extensively in various parts of plants, including leaves, stems, roots, fruits, seeds, and bark. Common fruits and vegetables such as apples, pears, mangoes, green peppers, strawberries, mulberries, guavas, and olives contain pentacyclic triterpenes; aromatic herbs like basil, oregano, rosemary, and lavender are also known sources; medicinal plants and fungi are particularly rich in triterpenes — for example, ginseng contains ginsenosides and Reishi mushrooms (Ganoderma lucidum) are a source of numerous triterpenes.

Raisins are rich in oleanolic acid, while dried cranberries, blueberries, and cherries are high in oleanolic and ursolic acids; plants such as holy basil, thyme, lavender, catnip, and peppermint leaves are also good sources of ursolic acid. The bark of the birch tree is recognized for its high content of betulin, another triterpene. Reishi contains a number of triterpenes, with the most prevalent being ganoderic acids, sterols, and lucidenic acids; there are actually over 140 triterpenes in reishi alone that can be found in the fruiting bodies, spores, and mycelia.

Squalene is most famously obtained from shark liver oil, where it is present in high concentrations; however, it is also found in a variety of plant sources including olive oil, amaranth seed, rice bran, and wheat germ.

Common Forms and Preparations

Triterpenes can be present in plants as secondary plant substances either in free form or as aglycones of triterpene saponins. While traditional preparation methods such as decoctions, teas, and coffee remain available, Western markets increasingly favor standardized extracts in tablet and capsule formulations. Due to their lipid-like nature, triterpenes require specific extraction methods, such as alcohol-based processes, to be effectively obtained from sources like mushrooms. Advances in extraction technologies, such as ultrasound and microwave-assisted methods, have improved the bioavailability and efficacy of compounds.

While consumption of triterpene-rich foods in Asian, African, and South American countries has been widely popular, in the Western world, their targeted application as food supplements started later, with the estimated individual average human consumption of triterpenes calculated as approximately 250–400 mg per day, based on the country.

2. Traditional and Historical Use

Triterpenoids have been used in traditional medicine for centuries, with various cultures utilizing plants rich in these compounds to treat a multitude of ailments; for example, the ancient Greeks and Romans used extracts from plants containing triterpenoid saponins for their medicinal properties. Historically, triterpenes have been used for centuries in traditional medicine systems such as Ayurvedic and Traditional Chinese Medicine to address a wide range of ailments, from skin conditions to promoting vitality.

Historically, triterpene-rich extracts such as those from Ganoderma lucidum (Reishi mushroom), Centella asiatica (Gotu kola), and olives have been used in traditional medicine across Asia, Africa, and the Mediterranean for promoting general health and longevity.

Traditional Chinese Medicine

For more than 2,000 years, Ganoderma lucidum, known traditionally as "lingzhi" or "reishi," has been valued in Asian medicine and has recently garnered attention in Western medical practice. Akebia, whose triterpene saponins are common in the Lardizabalaceae family, is recorded in the ancient Shen Nong Ben Cao Jing (The Classic of Herbal Medicine) and was traditionally used in diuresis-inducing and stranguria treatments. Glycyrrhizic acid (glycyrrhizin) is a main substance of licorice, which is one of the most important substances utilized as traditional medicine for almost 2,000 years.

Ayurvedic Medicine

Boswellic acids, the triterpenes present in the gum resins of Boswellia serrata (family Burseraceae), have been traditionally used in the Ayurvedic system of medicine as an antioxidant and anti-inflammatory agent to manage diseases such as rheumatoid arthritis, chronic bronchitis, asthma, and chronic inflammatory bowel diseases and osteoarthritis. In Ayurvedic medicine, the triterpene-rich extract of the neem tree (Azadirachta indica) is used to treat various ailments, including skin conditions and infections.

Traditional Uses of Specific Triterpenes

Historical remedies often incorporated triterpenes to promote wound healing, reduce fevers, and relieve pain; for example, the saponins in licorice have been celebrated for their soothing effects on the digestive and respiratory tracts, while ginseng's triterpenoid content was believed to support vitality.

For centuries, Centella asiatica (commonly referred to as Pegaga or Gotu kola) has served as a medicinal herb in China, India, and various other regions of Asia and is commonly used as an herbal medicine but can also be eaten fresh in salads, cooked as a vegetable, or blended into drinks.

Oleogum resins from Boswellia species are used in traditional medicine in India and African countries for the treatment of a variety of diseases. Protium species, among the most common genera in South America, include the important species known as "breu," whose gum and oil-resins are used as a tonic and stimulant and for the treatment of ulcers and inflammation.

3. Key Constituents and Mechanisms of Action

Biosynthesis

The biosynthesis of triterpenes involves the mevalonate pathway, which is responsible for producing isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP), the basic building blocks of isoprenoids; the triterpene synthase enzyme catalyzes the cyclization of squalene, a 30-carbon isoprenoid, to form various triterpene skeletons.

Principal Active Compounds

Oleanolic acid (OA) and Ursolic acid (UA): Oleanolic acid and its isomer ursolic acid fall under the ubiquitous class of pentacyclic triterpenoid bioactives mainly present in medicinal plants, herbs, fruit, and vegetables. UA and its derivatives possess a wide range of pharmacological effects, including antidiabetic, antiosteoporotic, hypocholesterolemic, hepatoprotective, neuroprotective, antiviral, anti-inflammatory, and antifungal activities, with very low toxicity.

Betulinic acid (BA): Betulinic acid has a range of well-documented pharmacological and biological effects, including antibacterial, immunomodulatory, diuretic, antiviral, antiparasitic, antidiabetic, and anticancer activities.

Boswellic acids: The major bioactive boswellic acids in Boswellia serrata gum resin include AKBBA, KBBA, BBA, and ABBA; among these, AKBBA was found to be a potent inhibitor of leukotriene-mediated inflammatory pathways and 5-lipoxygenase (5-LO) activities.

Ginsenosides: Ginseng is well known for its triterpenoid saponins, called ginsenosides, which contribute to its adaptogenic properties. The plant contains a complex of ginsenosides, triterpene saponins, including Rb1, Rb2, Rc, Rd, Re, Rf, and Rg1.

Glycyrrhizin (Glycyrrhizinic acid): Glycyrrhizinic acid is a triterpenoid saponin obtained from the root and rhizome extracts of licorice (Glycyrrhiza glabra), commonly used as a sweetener, being reported as at least 30 times sweeter than sucrose. The concentration of glycyrrhizin varies from species to species; commercially used G. glabra, G. inflata, and G. uralensis species contain up to 2–25% (dry weight) of glycyrrhizin.

Centella asiatica triterpenes: Numerous studies have reported that the main active components of C. asiatica are pentacyclic triterpenes; the extract contains four major triterpenoids: asiatic acid (AA), madecassic acid (MA), asiaticoside (AD), and madecassoside (MD).

Ganoderic acids (Reishi/Lingzhi): The bioactive constituents of G. lucidum encompass various compounds including polysaccharides, triterpenes, germanium, amino acids, sterols, lipids, antioxidants, B-complex vitamins, and minerals including iron, calcium, and zinc.

Corosolic acid: A large number of studies have reported the beneficial antidiabetic, anti-inflammatory, and anti-tumor effects of corosolic acid, a pentacyclic triterpenoid extracted mainly from banaba leaves (Lagerstroemia speciosa) and loquat (Eriobotrya japonica).

Established Mechanisms of Action

Pentacyclic triterpenes are renowned for their pleiotropic bioactivities, exhibiting anti-inflammatory, anticancer, antiviral, antimicrobial, antidiabetic, and hepatoprotective properties. Mechanistically, they modulate key signaling cascades — including NF-κB, PI3K/Akt, and PPAR pathways — induce apoptosis in transformed cells, scavenge reactive oxygen species, and inhibit enzymes implicated in metabolic disorders.

NF-κB inhibition: The pentacyclic triterpenoids (PTs) are multifunctional molecules having the ability to inhibit NF-κB signaling, and have attracted attention due to their ability to interact with multiple biological targets. Nuclear factor-kappaB (NF-κB) and STAT3 have emerged as major regulators of inflammation, cellular transformation, and tumor cell survival, proliferation, invasion, angiogenesis, and metastasis.

5-Lipoxygenase inhibition: The anti-inflammatory mechanism of boswellic acids is different from that of NSAIDs and is related to components of the immune system; the most evident action is the inhibition of 5-lipoxygenase; however, other factors such as cytokines (interleukins and TNF-alpha) and the complement system are also candidates, and leukocyte elastase and oxygen radicals are also targets.

Antidiabetic mechanisms: Oleanolic acid, ursolic acid, and betulinic acid act as hypoglycemic and anti-obesity agents mainly through: (i) reducing the absorption of glucose; (ii) decreasing endogenous glucose production; (iii) increasing insulin sensitivity; (iv) improving lipid homeostasis; and (v) promoting body weight regulation.

Reishi/Ganoderic acid mechanisms: Triterpenes like ganoderic acids inhibit 5-lipoxygenase and cyclooxygenase pathways, reducing inflammatory mediators, and also modulate T-helper cell differentiation toward Th1 responses. Triterpenes in G. lucidum may lower blood pressure by inhibiting angiotensin-converting enzyme (ACE) and improve lipid profiles through antioxidant upregulation.

Centella asiatica mechanisms: The phytopharmaceutical Centella asiatica, a traditional Ayurvedic medicine, contains triterpenes considered principally responsible for its anti-inflammatory effects; the triterpene glycoside madecassoside reduced NO, PGE2, TNF-α, IL-1β, and IL-6 in vitro via inhibition of protein and mRNA levels of iNOS and COX-2, in addition to NF-κB and DNA binding.

Collagen synthesis: Scientific evidence has demonstrated that C. asiatica formulations rich in the glycosides madecassoside and asiaticoside have been proved to possess pharmacological activities related to enhancing collagen synthesis, wound healing, and skin protection. The extract from the fresh and dried leaves and stems of Centella asiatica contains triterpenic derivatives (madecassic acid, asiatic acid, and asiaticoside), which have been shown to promote epithelialization and have anticellulitic and vasotonic activity.

4. Scientific Evidence by Area of Use

4.1 Anti-Inflammatory Effects

A systematic review synthesized evidence regarding the anti-inflammatory activity of G. lucidum triterpenes based on studies from the last two decades, searching PubMed, Medline, and Embase (2003–2025) for original in vitro and in vivo (non-clinical) studies; clinical trials, reviews, and multi-species extracts were excluded. All 23 included studies reported significant anti-inflammatory effects via reduction in pro-inflammatory markers (TNF-α, IL-1β, IL-6), primarily through downregulation of MAPK and TLR-4/NF-κB signaling pathways; meta-analysis of in vitro data confirmed significant reductions in NO levels (−3.29 [95% CI: −5.21, −1.37]; p = 0.0008), IL-6 (−3.51 [−4.73, −2.29]; p < 0.00001), and TNF-α (−2.20 [−2.93, −1.48]; p < 0.00001). However, the structural complexity and isomer diversity of these compounds remain significant barriers to pharmacological standardization, and future research must prioritize clinical translation by investigating compound synergism, bioavailability, and long-term toxicity profiles, which were notably absent in current non-clinical literature.

Licorice extract — encompassing 3 triterpenes and 13 flavonoids — exhibits evident anti-inflammatory properties mainly by decreasing TNF, MMPs, PGE2, and free radicals, which also explained its traditional applications in stimulating digestive system functions, eliminating phlegm, relieving coughing, and alleviating pain in Traditional Chinese Medicine.

Evidence strength: Most anti-inflammatory data for triterpenes derive from in vitro and animal studies. Robust human clinical trials remain limited.

4.2 Musculoskeletal and Joint Health (Boswellic Acids)

In multiple randomized, double-blind, placebo-controlled trials involving osteoarthritis (OA) patients, several Boswellia serrata-derived formulations enriched in boswellic acids — such as Boswel®, Aflapin®, and 5-Loxin® — were found to significantly improve pain scores, joint stiffness, and functional impairment; some formulations also demonstrated the ability to reduce inflammatory markers (e.g., TNF-α, IL-6, CRP) and matrix metalloproteinases (MMPs).

A double-blind, placebo-controlled human trial evaluated a standardized oral supplementation of Boswellin®, an extract of Boswellia serrata containing AKBBA with β-boswellic acid; 48 patients with osteoarthritis of the knee were randomized and allocated to the extract or placebo groups and administered intervention for 120 days; results revealed that extract treatment significantly improved physical function by reducing pain and stiffness compared with placebo. Radiographic assessments showed improved knee joint gap and reduced osteophytes confirming the efficacy of treatment; the extract also significantly reduced serum levels of high-sensitive C-reactive protein; no serious adverse events were reported.

In a meta-analysis including seven clinical trials involving 545 patients, Boswellia and its extract were reported to have a positive effect on relieving pain and stiffness and improving joint function.

Though the number of cases is small in related clinical studies, their results are convincing and supported by preclinical data; these studies include rheumatoid arthritis, osteoarthritis, chronic colitis, ulcerative colitis, collagenous colitis, Crohn's disease, and bronchial asthma; it cannot be expected that there is cure from these diseases, but at least improvement of symptoms in about 60–70% of cases has been observed.

Despite the substantial progress in preclinical studies, clinical research has not kept pace, particularly in the form of RCTs utilizing purified boswellic acids; most existing clinical studies have employed Boswellia serrata extract as the intervention, which contains a complex mixture of metabolites with undefined boswellic acid content; this complexity makes it difficult to attribute therapeutic effects specifically to boswellic acids, thereby limiting the translation of mechanistic findings to human applications.

Evidence strength: Moderate for osteoarthritis (multiple RCTs with small-to-medium sample sizes). Evidence for IBD and asthma is preliminary (pilot studies).

4.3 Immune Modulation

A randomized, double-blinded, placebo-controlled clinical trial was conducted to investigate the efficacy and safety of Reishi β-glucan in healthy adult volunteers aged 18 to 55; participants self-administered interventions or placebos daily for 84 days; results showed that subjects receiving Reishi β-glucan exhibited significant enhancement in various immune cell populations, including CD3+, CD4+, CD8+ T-lymphocytes, as well as improvement in the CD4/CD8 ratio and natural killer cell counts when compared to the placebo group; additionally, a statistically significant difference was observed in serum immunoglobulin A levels and natural killer cell cytotoxicity between groups.

The intervention was found to be safe and well tolerated, with no statistically significant changes observed in markers of kidney or liver function in either group; the study provides evidence for the ability of Reishi β-glucan to modulate immune responses in healthy adults, thereby potentially bolstering their defense against opportunistic infections.

However, previous trials on Ganoderma lucidum have been limited by small sample sizes, inconsistent methodologies, and variable supplement formulations, necessitating a comprehensive synthesis of evidence.

Evidence strength: Preliminary; most human trials on immunomodulation involve small populations and are focused on surrogate markers rather than clinical endpoints.

4.4 Anticancer and Chemopreventive Properties

A PubMed-indexed review examined the potential of triterpenes, derived from traditional medicine and diet, for their ability to suppress inflammatory pathways linked to tumorigenesis; these triterpenes include avicins, betulinic acid, boswellic acid, celastrol, diosgenin, madecassic acid, maslinic acid, momordin, saikosaponins, platycodon, pristimerin, ursolic acid, and withanolide.

Plant-derived natural products show high therapeutic potential in the management of various types of cancer; among different classes of phytocompounds, pentacyclic triterpenoids have been in the spotlight of research; ursolic acid and its structural isomer oleanolic acid represent compounds intensively studied and tested in vitro and in vivo for their anticancer and chemopreventive properties.

Evidence consistently highlights the importance of natural and synthetic triterpenoids, which have the potential for use in both chemoprevention and therapy of various cancers with several common molecular targets; the evidence for the ability of triterpenoids to suppress various key steps of tumor initiation, progression, and promotion clearly vindicates their traditional use in the treatment of inflammatory diseases/cancers, though these remain to be further validated once results of ongoing clinical studies are available.

Corosolic acid has revealed anti-tumor effects in various types of cancer such as colorectal, gastric, renal, liver, lung, brain, and prostate.

Evidence strength: Predominantly in vitro and animal-model data. As of the available literature, clinical anticancer efficacy in humans has not been definitively established for isolated triterpenes. Ongoing clinical trials are in progress.

4.5 Antidiabetic and Metabolic Effects

Oleanolic acid, ursolic acid, and betulinic acid are three triterpenic acids with potential effects for the treatment of type 2 diabetes; mechanistic studies showed that these act as hypoglycemic and anti-obesity agents mainly through reducing glucose absorption, decreasing endogenous glucose production, increasing insulin sensitivity, improving lipid homeostasis, and promoting body weight regulation; besides these promising effects, they are also believed to protect against diabetes-related comorbidities due to their anti-atherogenic, anti-inflammatory, and anti-oxidant properties.

Evidence strength: Strong mechanistic and animal-study data; limited and preliminary human clinical evidence specifically for isolated triterpenic acids in type 2 diabetes.

4.6 Hepatoprotective Effects

Glycyrrhizic acid has been used clinically for more than 20 years in patients with chronic hepatitis in China and Japan and shows a satisfactory therapeutic effect in many other diseases. The hepatoprotective mechanism of glycyrrhizic acid is due to its aglycone, glycyrrhetic acid, which inhibits both free radical generation as well as lipid peroxidation; 18α-GA has anti-hepatofibrosis effect and is frequently used as a hepatoprotective agent.

The most characteristic ingredients of G. lucidum are polysaccharides and triterpenoids, which have been extensively studied in animals and have not been linked to liver injury; reviews of hepatoprotective activity of mushrooms focused largely on in vivo studies of G. lucidum effects in animal models of hepatotoxicity suggest that the polysaccharides and triterpenoids are the active principles, while stressing the need for clinical trials in humans.

Evidence strength: Glycyrrhizin has clinical use data from Asian (particularly Japanese) clinical practice for chronic hepatitis; other triterpenes have predominantly preclinical evidence.

4.7 Skin Health and Wound Healing

The extract from the fresh and dried leaves and stems of Centella asiatica contains triterpenic derivatives (madecassic acid, asiatic acid, and asiaticoside), which have been shown to promote epithelialization and have anticellulitic and vasotonic activity. Madecassoside is widely distributed in the heart, liver, spleen, lung, brain, stomach, skin, and kidney through oral dosing, reaching maximum levels within 5–15 min after oral administration.

In dermatological conditions such as eczema and psoriasis, boswellic acid-based treatments were reported to alleviate erythema, scaling, and pruritus with good tolerability.

Evidence strength: Good evidence from human dermatological studies for Centella asiatica triterpenes in wound healing and skin conditions; boswellic acid evidence in dermatology is more limited.

4.8 Antimicrobial Properties

Ursolic acid, oleanolic acid, and betulinic acid are three hydroxyl pentacyclic triterpenoic acids naturally found in a large variety of vegetarian foods, medicinal herbs, and plants that have been investigated for antibacterial activity; no antibacterial activity was observed for betulinic acid, while oleanolic acid and more particularly ursolic acid did show a moderate to good antibacterial activity, but limited to Gram-positive bacteria.

Despite many preclinical studies, there are currently negligible clinical trials using these compounds for antibacterial responses.

Evidence strength: Preliminary; limited to in vitro studies with no clinical trial data to support human antibacterial use.

5. Body Systems and Health Areas

Musculoskeletal system: Joint pain, osteoarthritis, rheumatoid arthritis (boswellic acids — clinical evidence)
Immune system: Immunomodulation, natural killer cell activity (G. lucidum triterpenes and β-glucans — early clinical evidence)
Gastrointestinal system: Ulcerative colitis, Crohn's disease, gastritis, gastric ulcers (boswellic acids, glycyrrhizin — pilot clinical evidence)
Hepatic system: Hepatoprotection, hepatitis (glycyrrhizin — established clinical use in Asia; other triterpenes — animal/in vitro data)
Cardiovascular system: Research interest in G. lucidum has grown due to its demonstrated ability to safely influence several cardiovascular disease risk factors.
Metabolic/Endocrine system: Blood glucose regulation, lipid homeostasis, insulin sensitivity (oleanolic acid, ursolic acid, betulinic acid — mechanistic and animal evidence)
Integumentary system (Skin): Wound healing, collagen synthesis, eczema, psoriasis (Centella asiatica triterpenes — human evidence)
Respiratory system: Bronchial asthma (boswellic acids — pilot clinical evidence)
General biological activities documented include cytotoxic, hepatoprotective, hypocholesterolemic, and hypolipidemic activities.

6. Dosage Forms and Reported Study Dosages

Boswellia serrata extract (boswellic acids): In a double-blind, placebo-controlled trial of Boswellin® in 48 patients with knee osteoarthritis, the extract containing AKBBA and β-boswellic acid was administered for a period of 120 days.

Centella asiatica — Total Triterpene Fraction (TTFCA): TTFCA, a purified triterpene mixture, was well tolerated at all of the following doses in microcirculation studies: 30 or 60 mg daily for 7 days; 30 or 60 mg administered twice daily for 6 months; and 60 mg twice daily for 12 months; two studies used TTFCA at 180 mg daily for 12 months, and TTFCA was well tolerated at this highest reported dose.

Centella asiatica — whole herb/extract: The recommended dose of this herb, which is consumed in India and Sri Lanka as a healthy addition to the diet, is between 0.5 and 1.5 g dried leaf daily.

Glycyrrhizin (licorice): The acceptable daily intake (ADI) for glycyrrhizin is suggested to be 0.2 mg/kg/day. Pharmacokinetic research shows that the licorice constituent glycyrrhizin, taken in a dosage of 150 mg orally twice daily for 14 days, modestly decreases the area under the concentration-time curve of midazolam by about 20%.

Ganoderma lucidum (Reishi) extract: Human trials with 1.5–3 g daily reishi extract for 8–12 weeks have shown 20–30% increases in immune cell activity markers.

Dietary intake: The estimated individual average human consumption of triterpenes from food is approximately 250–400 mg per day, based on the country.

Despite potent in vitro and in vivo efficacy, clinical translation of many triterpenes has been hampered by poor water solubility and limited bioavailability; recent efforts have focused on semi-synthetic derivatisation, inclusion complexes with cyclodextrins, and nanoparticulate delivery systems to enhance pharmacokinetics.

7. Safety Considerations and Interactions

General Safety Profile

Pentacyclic triterpenoids are components of routine foodstuffs and are relatively nontoxic; these properties provide fertile ground for the development of PT-based phytopharmaceuticals.

Boswellic Acids

The number and severity of side effects with boswellic acid extracts is extremely low; the most reported complaints are gastrointestinal symptoms; allergic reactions are rare; most authors report that treatment with Boswellia extracts is well tolerated and the registered side effects in extract- and placebo-treated groups are similar.

Centella asiatica

Centella asiatica is an edible plant and the Botanical Safety Handbook classifies it as a Class 1 herb that can safely be consumed when used appropriately; the widespread use of Centella as a dietary supplement and the available human studies support its safety. Despite its presence in dietary supplements in the United States, there are no reports of adverse events associated with Centella asiatica found in the FDA CFSAN Adverse Event Reporting System. In a study involving 48 subjects, one case each of constipation, abdominal bloating, and itchiness were reported following 750 mg or 1,000 mg daily of a hydroethanolic extract; topical administration of Centella asiatica extracts and triterpenes is reported to cause contact dermatitis in some individuals.

Ganoderma lucidum (Reishi)

In view of the extensive worldwide use of Ganoderma lucidum and Lingzhi, clinically apparent liver injury from its use must be extremely rare; its likelihood score is D (possible rare cause of clinically apparent liver injury). Lingzhi is well tolerated and has not been associated with serum aminotransferase elevations during therapy, but has been implicated in rare single instances of acute liver injury, although in most reports other diagnoses were not adequately excluded. The mechanism and the ingredient responsible for the liver injury have not been identified; the most characteristic ingredients — polysaccharides and triterpenoids — have been extensively studied in animals and have not been linked to liver injury.

Glycyrrhizin / Licorice

Licorice root has been used in daily doses from 760 mg to 15 g for ulcer and gastritis; higher doses given for extended periods may pose a risk of hypokalemia; the acceptable daily intake (ADI) for glycyrrhizin is suggested to be 0.2 mg/kg/day. Use during pregnancy should be avoided; licorice exhibits estrogenic activity and has reputed abortifacient effects. Negative effects on pubertal maturation, neuroendocrine function, cognition, and behavior of children born to women who consumed high amounts of licorice during pregnancy have been documented.

Drug Interactions — Glycyrrhizin

Pharmacokinetic research shows that the licorice constituent glycyrrhizin, taken at a dosage of 150 mg orally twice daily for 14 days, modestly decreases the area under the concentration-time curve of midazolam by about 20%; midazolam is a substrate of cytochrome P450 3A4 (CYP3A4), suggesting that glycyrrhizin modestly induces CYP3A4 activity. Licorice extract from G. glabra species appears to inhibit CYP3A4-induced metabolism of testosterone in vitro; this is thought to be due to its constituent glabridin, which is a moderate CYP3A4 inhibitor in vitro and not present in other licorice species.

Drug Interactions — Reishi

Reishi can enhance the anticoagulant effects of warfarin, heparin, and aspirin, potentially increasing bleeding risk; patients taking blood thinners should monitor INR levels closely before supplementation.

Bioavailability Limitations

Pentacyclic triterpenes have been subjected to numerous studies that have revealed various biological activities; however, due to their high lipophilicity, which is considered to exert a significant influence on their bioavailability, their current use is limited. Triterpenic acids are a widespread class of phytocompounds possessing valuable therapeutic properties; they are a subclass of triterpenes bearing a characteristic lipophilic structure that imprints unfavorable in vivo properties which subsequently limit their applications.

References

Health Conditions

Health conditions that Triterpenes may help support.

No conditions available.

Body Systems

Body systems that Triterpenes may help support.

No body systems available.