Xanthium strumarium subsp. sibiricum. X. strumarium 苍 耳 子  Cāng ĕr zĭ  Cocklebur   Family: Compositae

PART USED: Fruit- harvested early Autumn when fruit has ripened.
   FLAVOR: Pungent, bitter, pleasant CHANNELS: Lung  TOXICITY: Slightly toxic[1,4]
FUNCTIONS- Common herb for sinusitis and rhinitis.
GROUP: Wind Damp Dispersing
1. Disperses Wind and dispels Dampness.[4] Alleviates rheumatism, stops pain.[1]
2. Open up nasal passages.[4] Antiallergenic.[3]
3. Dispels exterior Wind.[4]
4. Relieves constipation.
INDICATIONS
1. Sinusitis.[1] Colds.[1] Rhinitis, headache, allergic rhinitis. Acute sinusitus with hot feeling, headache, running sticky mucus.[3] Chronic sinusitis with running nose with not so much yellow or sticky mucus and pulse slightly fast.[3] Rhinitis with allergy conditions- difficult to treat sometimes works, and sometimes not- also need to strengthen body energy.[3] Any nasal or sinus problem with a thick, viscous discharge and related headache.[4]
2. Wind Damp painful obstruction.[1,4] Rheumatic pain.
3. Headache due to external Wind perverse Energy; Headache feels very sharp and extends to back of neck,[4] on windy days symptoms become worse.[3]
4. Skin disorders with itching.[4] Pruritus.[1] Itching.
5. Leprosy.[1]
CONTRAINDICATIONS: Headache or painful obstruction due to Blood deficiency. Overdosage may cause nausea, vomiting, lowering of blood pressure and abdominal pain.[3,4]
COMBINATIONS
PREPARATIONS: Decoction. Seeds 6-9 g.[1] Whole plant 15-30 g.[1] External use, a suitable amount may be steeped, and the solution used for bathing the affected parts.[1] Fruits 3-9 g.[2,4]Good quality is large, round, nad yellow green.
    
苍 耳 草 Cāng ĕr cǎo  Leaves and stem
   FLAVOR: Pungent, bitter  TOXICITY: Slightly toxic[4]
ACTIONS
1. Expels Wind.[4]
2. Clears Heat.[4] Relieves toxicity.[4]
INDICATIONS
1. Wind Damp painful obstruction with spasms and pain in the extremities.[4]
2. Deep rooted skin lesions and pruritus.[4]
PREPARATIONS: Generally used topically; when taken internally the dosage is 6-15 g.[4] It should not be taken internally long-term, and should not be prescribed for those who are very weak.[4]
DESCRIPTION: Annual herb.
References
Inner Path can not take any responsibility for any adverse effects from the use of plants. Always seek advice from a professional before using a plant medicinally.
Constituents
Research

Biological activities of xanthatin from Xanthium strumarium leaves.
Nibret E, Youns M, Krauth-Siegel RL, Wink M.
Abstract
The objective of the present work was to evaluate the biological activities of the major bioactive compound, xanthatin, and other compounds from Xanthium strumarium (Asteraceae) leaves. Inhibition of bloodstream forms of Trypanosoma brucei brucei and leukaemia HL-60 cell proliferation was assessed using resazurin as a vital stain. Xanthatin was found to be the major and most active compound against T. b. brucei with an IC(50) value of 2.63 µg/mL and a selectivity index of 20. The possible mode of action of xanthatin was further evaluated. Xanthatin showed antiinflammatory activity by inhibiting both PGE(2) synthesis (24% inhibition) and 5-lipoxygenase activity (92% inhibition) at concentrations of 100 µg/mL and 97 µg/mL, respectively. Xanthatin exhibited weak irreversible inhibition of parasite specific trypanothione reductase. Unlike xanthatin, diminazene aceturate and ethidium bromide showed strong DNA intercalation with IC(50) values of 26.04  µg/mL and 44.70 µg/mL, respectively. Substantial induction of caspase 3/7 activity in MIA PaCa-2 cells was observed after 6 h of treatment with 100 µg/mL of xanthatin. All these data taken together suggest that xanthatin exerts its biological activity by inducing apoptosis and inhibiting both PGE(2) synthesis and 5-lipoxygenase activity thereby avoiding unwanted inflammation commonly observed in diseases such as trypanosomiasis.
PMID: 21953905 DOI: 10.1002/ptr.3651 Phytother Res. 2011 Dec;25(12):1883-90. doi: 10.1002/ptr.3651. Epub 2011 Sep 23. ncbi.nlm.nih.gov

Xanthatin and xanthinosin from the burs of Xanthium strumarium L. as potential anticancer agents.
Ramírez-Erosa I, Huang Y, Hickie RA, Sutherland RG, Barl B.
Abstract
Xanthatin and xanthinosin, 2 sesquiterpene lactones isolated from the burs of Xanthiun strumarium L. (cocklebur), showed moderate to high in vitro cytotoxic activity in the human cancer cell lines WiDr ATCC (colon), MDA-MB-231 ATCC (breast), and NCI-417 (lung). Xanthatin and xanthinosin were purified as the result of a multi-screening bioassay-guided study of wild plant species of the family Asteraceae, collected from various sites in Saskatchewan, Canada. Seventy-five extracts at a single concentration of 100 microg/mL were evaluated for in vitro cytotoxicity to the human cancer cell lines used. The chloroform extract of Carduus nutans L. (nodding thistle) aerial parts (IC50, 9.3 microg/mL) and the hexane extract of Echinacea angustifolia DC. (narrow-leaved purple coneflower) root (IC50, 4.0 microg/mL) were moderately to highly cytotoxic to the lung cancer cell line. The chloroform extracts of X. strumarium L. burs and Tanacetum vulgare L. (tansy) aerial parts exhibited the highest cytotoxicity for all cell lines tested; their IC50 values, obtained from multidose testing, ranged from 0.1 to 6.2 microg/mL (X. strumarium) and from 2.4 to 9.1 microg/mL (T. vulgare). Further purification of the chloroform fraction of X. strumarium yielded xanthatin and xanthinosin in high yields. This is the first time that these compounds have been reported in the burs of X. strumarium. Their IC50 values are also reported herein.
PMID: 18066118 DOI: 10.1139/Y07-104 Can J Physiol Pharmacol. 2007 Nov;85(11):1160-72. ncbi.nlm.nih.gov

Xanthium strumarium L. extracts produce DNA damage mediated by cytotoxicity in in vitro assays but does not induce micronucleus in mice.
Piloto Ferrer J, Cozzi R, Cornetta T, Stano P, Fiore M, Degrassi F, De Salvia R, Remigio A, Francisco M, Quiñones O, Valdivia D, González ML, Pérez C, Sánchez-Lamar A.
Abstract
Xanthium strumarium L. is a member of the Asteraceae commonly used in Cuba, mainly as diuretic. Some toxic properties of this plant have also been reported and, to date, very little is known about its genotoxic properties. The present work aims was to evaluate the potential cytotoxic and genotoxic risk of whole extract from Xanthium strumarium L. whole extract of aerial parts. No positive response was observed in a battery of four Salmonella typhimurium strains, when exposed to concentrations up to 5 mg/plate, with and without mammalian metabolic activation (liver microsomal S9 fraction from Wistar rats). In CHO cells, high concentrations (25-100 μg/mL) revealed significant reduction in cell viability. Results from sister chromatid exchanges, chromosome aberrations, and comet assay showed that X. strumarium extract is genotoxic at the highest concentration used, when clear cytotoxic effects were also observed. On the contrary, no increase in micronuclei frequency in bone marrow cells was observed when the extract was orally administered to mice (100, 500, and 2000 mg/Kg doses). The data presented here constitute the most complete study on the genotoxic potential of X. strumarium L. and show that the extract can induce in vitro DNA damage at cytotoxic concentrations.
PMID: 25025061 PMCID: PMC4082875 DOI: 10.1155/2014/575197 Biomed Res Int. 2014;2014:575197. doi: 10.1155/2014/575197. Epub 2014 Jun 15. ncbi.nlm.nih.gov

Inhibition of melanogenesis by Xanthium strumarium L.
Li H, Min YS, Park KC, Kim DS.
Abstract
Xanthium strumarium L. (Asteraceae) is traditionally used in Korea to treat skin diseases. In this study, we investigated the effects of a X. strumarium stem extract on melanin synthesis. It inhibited melanin synthesis in a concentration-dependent manner, but it did not directly inhibit tyrosinase, the rate-limiting melanogenic enzyme, and instead downregulated microphthalmia-associated transcription factor (MITF) and tyrosinase expression. MITF, the master regulator of pigmentation, is a target of the Wnt signaling pathway, which includes glycogen synthase kinase 3β (GSK3β) and β-catenin. Hence, the influence of X. strumarium stem extract on GSK3β and β-catenin was further investigated. X. strumarium induced GSK3β phosphorylation (inactivation), but the level of β-catenin did not change. Moreover, a specific GSK3β inhibitor restored X. strumarium-induced melanin reduction. Hence, we suggest that X. strumarium inhibits melanin synthesis through downregulation of tyrosinase via GSK3β phosphorylation.
PMID: 22484949 DOI: 10.1271/bbb.110894 Biosci Biotechnol Biochem. 2012;76(4):767-71. Epub 2012 Apr 7. ncbi.nlm.nih.gov Hepatotoxicity of kaurene glycosides from Xanthium strumarium L. fruits in mice.
Wang Y, Han T, Xue LM, Han P, Zhang QY, Huang BK, Zhang H, Ming QL, Peng W, Qin LP.
Abstract
The fruit of Xanthium strumarium L. (Cang-Er-Zi) is a traditional Chinese medicine that is used in curing nasal diseases and headache according to the Chinese Pharmacopoeia. However, clinical utilization of Xanthium strumarium is relatively limited because of its toxicity. The present investigation was carried out to evaluate the toxic effects on acute liver injury in mice of the two kaurene glycosides (atractyloside and carbxyatractyloside), which are main toxic constituents isolated from Fructus Xanthii on acute liver injury in mice. Histopathological examinations revealed that there were not obviously visible injury in lungs, heart, spleen, and the central nervous system in the mice by intraperitoneal injection of atractyloside (ATR, at the doses 50,125 and 200 mg/kg) and carbxyatractyloside (CATR, at the doses 50,100 and 150 mg/kg) for 5 days. However, it revealed extensive liver injuries compared with the normal group. In the determination of enzyme levels in serum, intraperitoneal injection of ATR and CATR resulted in significantly elevated serum alanine aminotransferase (ALT), asparate aminotransferase (AST), alkaline phosphatase (ALP) activities compared to controls. In the hepatic oxidative stress level, antioxidant-related enzyme activity assays showed that ATR and CATR administration significantly increased hepatic malondialdehyde (MDA) concentration, as well as decreased superoxide dismutase (SOD), catalase (CAT) activities and glutathione (GSH) concentration, and this was in good agreement with the results of serum aminotransferase activity and histopathological examinations. Taken together, our results demonstrate that kaurene glycosides induce hepatotoxicity in mice by way of its induction of oxidative stress as lipid peroxidation in liver, which merited further studies. Therefore, these toxic constituents explain, at least in part, the hepatotoxicity of X. strumarium L. in traditional medicine.
PMID: 21699085 Pharmazie. 2011 Jun;66(6):445-9. ncbi.nlm.nih.gov

MAPK/AP-1-Targeted Anti-Inflammatory Activities of Xanthium strumarium.
Hossen MJ, Kim MY, Cho JY.
Abstract
Xanthium strumarium L. (Asteraceae), a traditional Chinese medicine, is prescribed to treat arthritis, bronchitis, and rhinitis. Although the plant has been used for many years, the mechanism by which it ameliorates various inflammatory diseases is not yet fully understood. To explore the anti-inflammatory mechanism of methanol extracts of X. strumarium (Xs-ME) and its therapeutic potential, we used lipopolysaccharide (LPS)-stimulated murine macrophage-like RAW264.7 cells and human monocyte-like U937 cells as well as a LPS/D-galactosamine (GalN)-induced acute hepatitis mouse model. To find the target inflammatory pathway, we used holistic immunoblotting analysis, reporter gene assays, and mRNA analysis. Xs-ME significantly suppressed the up-regulation of both the activator protein (AP)-1-mediated luciferase activity and the production of LPS-induced proinflammatory cytokines, including interleukin (IL)-1[Formula: see text], IL-6, and tumor necrosis factor (TNF)-[Formula: see text]. Moreover, Xs-ME strongly inhibited the phosphorylation of mitogen-activated protein kinase (MAPK) in LPS-stimulated RAW264.7 and U937 cells. Additionally, these results highlighted the hepatoprotective and curative effects of Xs-ME in a mouse model of LPS/D-GalN-induced acute liver injury, as assessed by elevated serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT), and histological damage. Therefore, our results strongly suggest that the ethnopharmacological roles of Xs-ME in hepatitis and other inflammatory diseases might result from its inhibitory activities on the inflammatory signaling of MAPK and AP-1.
PMID: 27627914 DOI: 10.1142/S0192415X16500622 Am J Chin Med. 2016;44(6):1111-1125. Epub 2016 Sep 15. Am J Chin Med. 2016;44(6):1111-1125. Epub 2016 Sep 15. ncbi.nlm.nih.gov