Sigesbeckia pubescens
StarSigesbeckia pubescens
Synonyms: Sigesbeckia orientalis subsp. pubescens, Sigesbeckia pubescens f. eglandulosa, Sigesbeckia orientalis f. pubescens
Safety at a glance
No rule in our tables for this herb: pregnancy, breastfeeding, incompatible pairs (十八反 / 十九畏), herb–drug, dose ceiling. This is not a safety clearance.
Not graded — No toxicity grade is recorded. Most herbs in the catalogue carry none.
Traditionally used for
- Pain & joints
Western Herbalism Properties
Botanical Description
Sigesbeckia pubescens is an erect annual herb of the Asteraceae growing 30-100 cm tall, with stout, branching, densely glandular-pubescent and hairy stems that feel sticky to the touch. The opposite, broadly ovate to triangular-ovate leaves have coarsely serrate margins, a truncate to broadly cuneate base often decurrent on the winged petiole, and softly hairy surfaces with conspicuous trichomes. Small, yellow heads with both ray and disc florets are arranged in lax terminal corymbiform panicles; the diagnostic feature is the involucre of five long, spreading, glandular outer bracts that produce viscid drops, helping the achenes (which are curved and lack a pappus) cling to passing animals for dispersal. It is widely distributed across temperate and subtropical East Asia, including China, Korea and Japan, in forest margins, riverbanks, fields and disturbed ground.
Active Constituents
Kirenol
ent-Pimarane diterpenoidConcentration: Relative proportion of about 0.6 per cent in an ethanol extract of the aerial parts; kirenol is the assay marker the Chinese Pharmacopoeia sets for Siegesbeckiae Herba
The best-characterised constituent of the drug, carrying most of its anti-inflammatory and anti-arthritic activity in preclinical models. A 26-batch survey using DNA barcoding alongside UPLC-QTOF found kirenol in this species but in none of the Sigesbeckia orientalis batches tested, which is a practical reason not to treat the three official source species as interchangeable.
Darutoside
ent-Pimarane diterpenoid glycosideConcentration: Relative proportion of about 0.2 per cent in an ethanol extract of the aerial parts
Isolated from this species and its structure revised by Kim and colleagues in 1979. It contributes measurably to the anti-inflammatory and analgesic effect of the whole extract in rodent oedema and writhing models, and 16-O-acetyldarutoside serves alongside kirenol as a thin-layer chromatography identity standard for the drug.
Malonylkirenol esters (15-O-malonylkirenol and 16-O-malonylkirenol)
ent-Pimarane diterpenoid estersConcentration: Among the twelve marker compounds that discriminate the three official Siegesbeckiae Herba species by partial least squares discriminant analysis
Malonyl esters of kirenol, including a previously undescribed 15,16-di-O-malonylkirenol, isolated during chemical profiling of the drug. Their principal value at present is chemotaxonomic: they help distinguish this species from Sigesbeckia orientalis and Sigesbeckia glabrescens in decoction pieces where morphology no longer does.
Hesperidin
Flavanone glycosideConcentration: Relative proportion of about 0.01 per cent in an ethanol extract of the aerial parts
Reported for the first time in this species in 2021. Present at very low relative abundance but active in the same rodent inflammation and nociception models as kirenol and darutoside, contributing to suppression of COX-2 expression and inflammatory cell infiltration.
ent-Kaurane and ent-strobane diterpenoids
DiterpenoidsConcentration: Numerous minor congeners; over three hundred phytochemicals have been catalogued across the genus
A continuing series of minor diterpenoids described from the aerial parts. One of them, ent-16-beta,17-dihydroxy-kauran-19-oic acid, inhibits MDA-MB-231 breast cancer cell migration in a chemotaxis assay with an IC50 of 1.96 microM and suppressed lung metastasis in nude mice. These are structure-elucidation and screening findings; none has been taken into a human study.
⚠ Drug Interactions
Sigesbeckia orientalis or Sigesbeckia glabrescens dispensed as Siegesbeckiae Herba
The Chinese Pharmacopoeia allows Siegesbeckiae Herba to come from Sigesbeckia orientalis L., S. pubescens Makino or S. glabrescens Makino, so a prescription for the drug can be filled with any of the three. They are not equivalent. In a 26-batch DNA-barcoded chemical survey, none of the S. orientalis batches contained kirenol at all, despite kirenol being the Pharmacopoeia's own quality marker, and in a head-to-head comparison in DSS-induced colitis in mice, S. pubescens outperformed the other two species.
Clinical note: If a clinical effect is being attributed to this herb, record which of the three species the batch actually was. Batches supplied as S. orientalis may contain no kirenol, so a change of supplier can amount to a change of drug.
Methotrexate, TNF inhibitors and JAK inhibitors
Extract of this species suppresses proinflammatory chemokine production in interferon-gamma and TNF-alpha stimulated keratinocytes and dermal fibroblasts by modulating JAK2, STAT1 and STAT3 signalling, which is the pathway tofacitinib and its relatives target. Kirenol has separately been shown to act on the TWEAK/Fn14 axis in rheumatoid arthritis models. The herb is used clinically for exactly the conditions these drugs treat, so co-administration is likely in practice, and no study has examined it.
Clinical note: In a patient on a DMARD or a JAK inhibitor, document herb use and monitor for infection as you would for any added immunomodulator. Do not treat the herb as a substitute for the drug.
NSAIDs and selective COX-2 inhibitors
Ethanol extract of the aerial parts and its constituents kirenol, darutoside and hesperidin reduce COX-2 expression in inflamed rodent tissue and raise thermal pain thresholds. That is the same enzyme NSAIDs inhibit, though by suppressing expression rather than blocking the enzyme. Whether the effects are additive at achievable human doses has not been tested.
Clinical note: No reason to prohibit the combination, but if a patient reports good analgesia on both, taper one at a time. Watch for gastrointestinal upset, the herb's most commonly reported adverse effect.
Antihypertensive drugs
Hypertension is a documented traditional indication for Sigesbeckia species across Chinese and Korean practice, and raw unprocessed Siegesbeckiae Herba is used in Chinese medicine partly for that purpose. There is no controlled blood-pressure study of the herb in humans or, so far as the published record shows, a clean animal haemodynamic study, so this entry rests on traditional use rather than measured pharmacology.
Clinical note: Check blood pressure when starting or stopping the herb in a treated hypertensive. Do not present it as an evidence-based antihypertensive.
Dosage Calculator
⚖ Dosage Calculator
A weight-based mathematical estimate for Sigesbeckia pubescens. Not a prescription.
Evidence Tier
5 studies on recordRecorded studies by study design, strongest design at the top. This is a study-design tier only, not a GRADE rating: it does not weigh risk of bias, consistency or precision.
Systematic review / meta-analysis
0
Randomized controlled trial
0
Other clinical trial
0
Observational / case report
0
In vitro / animal
5
2 verified · 3 unverified
Show 5 studies
- Kirenol, darutoside and hesperidin contribute to the anti-inflammatory and analgesic activities of Siegesbeckia pubescens makino by inhibiting COX-2 expression and inflammatory cell infiltration
- Sigesbeckia pubescens makino alleviates ulcerative colitis in mice by modulating the Nrf2/Keap1 pathway
- Therapeutic Effects of Sigesbeckia pubescens Makino Against Atopic Dermatitis-Like Skin Inflammation Through the JAK2/STAT Signaling Pathway
- Neuroprotective Effects of Sigesbeckia pubescens Extract on Glutamate-Induced Oxidative Stress in HT22 Cells via Downregulation of MAPK/caspase-3 Pathways
- UPLC-QDA combined with pharmacology and chemometrics to analyze the correlation between the processing technology and color of Siegesbeckiae herba
Other / unclassified
0
Verified: design read from PubMed for a DOI that resolves to the cited paper Unverified: taken from the study's recorded description
Clinical Studies
Kirenol, darutoside and hesperidin contribute to the anti-inflammatory and analgesic activities of Siegesbeckia pubescens makino by inhibiting COX-2 expression and inflammatory cell infiltration
HPLC-DAD identified kirenol, darutoside and hesperidin in the ethanol extract at roughly 0.6, 0.2 and 0.01 per cent, hesperidin for the first time in this species. Extract and isolated constituents reduced xylene-induced ear oedema and complete Freund's adjuvant paw oedema in mice, raised the thermal pain threshold, cut acetic-acid writhing, lowered COX-2 expression in the inflamed tissue and blocked LPS-driven RAW264.7 migration. Rodent and cell work; there is no human trial of this herb.
Sigesbeckia pubescens makino alleviates ulcerative colitis in mice by modulating the Nrf2/Keap1 pathway
The three official Siegesbeckiae Herba species were compared head to head in C57BL/6 mice given 3 per cent dextran sulfate sodium for seven days. This species lowered the disease activity index, limited colon shortening and reduced histological damage relative to the model, acting through Nrf2/Keap1 activation with raised glutathione, lower malondialdehyde and upregulated HO-1 and NQO1. The species comparison is the important part: the three official sources are not equally active.
Therapeutic Effects of Sigesbeckia pubescens Makino Against Atopic Dermatitis-Like Skin Inflammation Through the JAK2/STAT Signaling Pathway
Oral extract reduced the severity of house dust mite induced dermatitis in NC/Nga mice, with lower serum inflammatory mediators, thinner epidermis, less mast cell infiltration and restored barrier function. In stimulated human keratinocytes and dermal fibroblasts it suppressed chemokine production through JAK2, STAT1 and STAT3. Preclinical only, but the mechanism is the reason for the JAK inhibitor caution recorded above.
Neuroprotective Effects of Sigesbeckia pubescens Extract on Glutamate-Induced Oxidative Stress in HT22 Cells via Downregulation of MAPK/caspase-3 Pathways
Extract raised viability of glutamate-stressed HT22 hippocampal cells dose-dependently, lowered reactive oxygen species and lactate dehydrogenase release, and attenuated phosphorylation of ERK1/2, JNK and p38 with reduced caspase-3 activation. A cell-line result offered here only as mechanistic background for the traditional use in stroke sequelae; it is not evidence of clinical neuroprotection.
UPLC-QDA combined with pharmacology and chemometrics to analyze the correlation between the processing technology and color of Siegesbeckiae herba
Colorimetry, UPLC-QDA fingerprinting and rodent analgesic, anti-inflammatory and osteoarthritis models were used together to compare processing methods for the drug. Material steamed nine times turned glossy black and performed best, which puts a modern measurement behind the classical nine-steamings-and-nine-dryings instruction. Relevant to dispensing: raw and repeatedly steamed material are not the same preparation.
Historical Texts
Xin Xiu Ben Cao (Tang Materia Medica)
Tang dynasty China, 659 CEBen Cao Tu Jing (Illustrated Classic of Materia Medica)
Northern Song China, 1061Ben Cao Gang Mu
Ming dynasty China, 1596References
- Tao G, Li Q, Xu S, Song W, Yang Z, Zhou Y, Gao L, Huang W, Li X, Ye Y. Rapid identification of chemical compositions from three species of Siegesbeckiae Herba by ultra-performance liquid chromatography-electrospray ionization-quadrupole time of flight-mass spectrometry in combination with deoxyribonucleic acid barcoding . Journal of Separation Science (2023) [DOI]
- Dar P, Wenqing C, Khalifa SAM, Chen J, Linghu K, Xiong W, El-Seedi HR, Yu H. 44-year journey (1980–2024): scientometric insights into Sigesbeckiae herba and update on its medicinal properties and phytochemicals profile . Chinese Medicine (2026) [DOI]
- Kim JH, Han KD, Yamasaki K, Tanaka O. Darutoside, a diterpenoid from Siegesbeckia pubescens and its structure revision . Phytochemistry (1979) [DOI]
- Wang J, Xie K, Wang Q, Li W, Fu H. Isolation and characterization of ent-pimarane diterpenoids from Sigesbeckia pubescens . Natural Product Research (2019) [DOI]
- Wang J, Liu R, Chen H, Chen A, Chen L. Ent-16β,17-dihydroxy-kauran-19-oic acid (DKA), a kaurane diterpenoid from Sigesbeckia pubescens(Makino) Makino, inhibits the migration of MDA-MB-231 breast cancer . Natural Product Research (2023) [DOI]
- Ibrahim SRM, Altyar AE, Sindi IA, El-Agamy DS, Abdallah HM, Mohamed SGA, Mohamed GA. Kirenol: A promising bioactive metabolite from siegesbeckia species: A detailed review . Journal of Ethnopharmacology (2021) [DOI]
This information is for educational purposes only and is not intended to replace professional medical advice. Always consult a qualified healthcare provider before using any herbal remedy, especially if you are pregnant, nursing, or taking medications.
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