Table 7.
Dosage, experimental model, pharmacological action and mechanism of Atractylodis Rhizoma extracts.
| Pharmacology | Pharmacological effects | Substances and dosages | Experimental model | Mechanisms | Ref. |
|---|---|---|---|---|---|
| Improving gastrointestinal function | Stimulating gastric emptying or small intestinal motility | The extract (500 or 1000 mg/kg) and β-eudesmol (50 or 100 mg/kg) | Atropine-, dopamine-, 5-hydroxytryptamine-treated mice | Inhibiting the dopamine D2 and 5-HT3 receptor | Kimura and Sumiyoshi (2012) |
| Inhibiting of gastric ulcer | n-butanol extract 0.18 g/kg |
Rats | Improving blood circulation in ulcer, promoting DNA, RNA and protein synthesis | Piao and Piao (1996) | |
| Anti-gastrointestinal mucosal injury | Atractylenolide I (ATL-I) 5 and 10 μM | IEC-6 cell | Promoting IEC-6 cell proliferation and migration; increasing polyamines content, and enhancing TRPC1 and PLC-γ1 mRNA and protein expression | Song et al. (2017) | |
| Resisting gastric ulcer | Hinesol IC50: 5.8*105 M |
Porcine gastric membrane vesicles | Inhibiting H+, K+-ATPase and Mg2+-ATPase and Ca2+-ATPase activity | Satoh et al. (2000) | |
| Anti-gastric ulcer | A. lancea 2.5 g/kg | Acetic acid imitated rats | The gastroprotective effects were mediated by up-regulating trefoil factor 2 and epidermal growth factor | Yu et al. (2015) | |
| Immunomodulatory activity | Immunostimulatory effects | The boiling water extract 1.0 mg/mL |
Murine normal colonic epithelial MCE301 cells | Inducing secretion of granulocyte colony-stimulating factor | Shimato et al. (2018) |
| Immunomodulatory activity | Acidic polysaccharide (ALP-3) 50, 100, 250, 500, 1000, 2000 μg/mL | Murine RAW264.7 macrophage cell line | Stimulating macrophage proliferation, and stimulating phagocytic, NO and cytokines production on RAW264.7 cells | Qin et al. (2019) | |
| Intestinal immune system modulating activity | ALP-1 and ALP-3 50, 100, 250, 500, 1000, 2000 μg/mL | Peyer's patch cells | Activating T cells in Peyer patch cells and promoting the production of CSF | Qin et al. (2019) | |
| Intestinal immune system modulating activity | Polysaccharides 100 μg/mL |
Peyer's patch cells | Regulating intestinal immune system | Yu et al. (1998) | |
| Anti-tumor activity | Inhibitory effect on human gastric cancer cells | Water extract of the A. lancea 0.0625, 0.125, 0.25, 0.5, and 1 mg/mL | BGC-823 and SGC-7901 cells | Inhibiting the growth of BGC-823 and SGC-7901 cells | Zhao et al. (2014) |
| Anti-leukemia | Atractylenolide I (ATL-I) 3.13–100 μg/mL | Human K562 CML, U937 AML and Jurkat T lymphoma cells | Inducing apoptosis and differentiation of macrophage lineage | Huang et al. (2016) | |
| Anti-melanoma effects | Atractylenolide I (ATL-I) 40, 60, 80, 100, 120, 150 μM | Human A375, Hs294T and SK-MEL-5 melanoma cells | Inhibiting phospho-janus kinase 2, phospho-signal transducer and activator of transcription 3, matrix metalloproteinase-2 and -9 | Fu et al. (2018) | |
| Antimelanoma effects | Atractylenolide II (ATL-II) 12.5, 25 mg/kg | B16 xenograft mouse | Suppressing STAT3 activation and tumor growth | Fu et al. (2014) | |
| Antigastric carcinoma | ATL-II 50, 100, 200, 400 μM | Human gastric carcinoma cell lines HGC-27 and AGS | Modulating Akt/ERK signaling pathway to inhibit cell proliferation, motility and inducing apoptosis | Tian and Yu (2017) | |
| Antitumor activity | Atractylenolide III (ATL-III) 1, 10, 100 μM | HMC-1 cell | Inhibiting mast cell proliferation, phosphorylated signal transducer, IL-13, proinflammatory cytokines and activator of transcription | Yoou et al. (2017) | |
| Antitumor activity | ATL-III 100 μM | LAD2 human mast cell | Inhibiting mast cell proliferation and the production of inflammatory cytokine | Yoou et al. (2017) | |
| Antitumor activity | Hinesol 5, 10, 25, 50, 100 μM | Human leukemia HL-60 cells | Hinesol induced apoptosis through the JNK signaling pathway in HL-60 cells | Masuda et al. (2015) | |
| Anti-cholangiocarcinoma | β-eudesmol IC50: 39.33 mg/mL |
The CCA cell lines, and normal human cell line | Promoting cell cycle arrest at G1 phase, and inducing cell apoptosis through activation of caspase-3/7 | Kotawong et al. (2018) | |
| Anti-hepatocellular carcinoma | β-eudesmol IC50: 16.51 ± 1.21–24.57 ± 2.75 μg/mL |
B16–F10 and HepG2 cell lines | Inducing tumor cell death by caspase-mediated apoptosis pathways | Bomfim et al. (2013) | |
| Anti-multiple myeloma cells | β-sitosterol 0, 6.25, 12.5, 25, 50, 100 mM | Human multiple myeloma U266 and MM1S cell | Increasing the sub-G1 apoptotic population, activating caspase-9 and -3 | Sook et al. (2014) | |
| Anti-tumor activity | β-eudesmol 10–100 mM | HeLa, SGC-7901, and BEL-7402 | Inhibiting angiogenesis by suppressing CREB activation in the growth factor signaling pathway | Ma et al. (2008) | |
| Inhibiting of Cholangiocarcinoma | β-eudesmol (0, 1, 10, 30, 100 μM), dicoumarol (1 μM), 5-FU (0, 3, 10, 30, 100 μM), DOX (0, 0.1, 0.01, 1, 10 μM) | Human CCA cell line, KKU-100 | Enhancing chemotherapeutic effects of 5-fluorouracil and doxorubicin in the high NQO1-expressing human CCA cell line, NQO1-KKU-100 | Srijiwangsa et al. (2018) | |
| Inhibiting of lung and colon cancer | β-eudesmol 5–100 μM | Human lung (A549) cells, colon (HT29 and Caco-2) cells | Inhibiting proliferation of tumor cells and superoxide production; inhibiting adhesion and migration of A549 and HT29 cell | Sghaier et al. (2016) | |
| Anti-angiogenic mechanism and anti-tumor activity | β-eudesmol (2.5–5 mg/kg) | Implanting H22 and S180 mice tumor cells into oxters of 7-week-old KM mice | Suppressing CREB activation in growth factor signaling pathway | Ma et al. (2008) | |
| Inhibiting angiogenesis | β-eudesmol 10–100 μM | Porcine brain microvascular endothelial cells, human dermal microvascular endothelial cells | The blockade of the ERK signaling pathway | Tsuneki et al. (2005) | |
| Anti-inflammatory activity | Anti-inflammatory effects in vitro | AR methanol extract 100 μg/mL | Murine macrophage-like cell line RAW264.7 cells | Inhibiting the production of NO | Shimato et al. (2018) |
| Anti-inflammatory effect | ATL-III 1–100 μM, LPS 1 μg/mL | The murine macrophage cell line RAW264.7 | Suppressing the release of NO, PGE2, TNF-α and IL-6 related to the NF-κB- and MAPK signaling pathways | Ji et al. (2016) | |
| Improving intestinal inflammation and cooccurring dysmotility | Atractylodin 10.0 mg/kg | Diarrheaprominent rats were established by acetic acid and restraint stress; constipation-prominent rats were established by cool water | Reducing pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 in the plasma and inhibiting the expression of inflammatory mediators iNOS and NF-κB in jejunal segments in both CP and DP rats. | Yu et al. (2017) | |
| Anti-inflammatory effects | Water extracts of A. lancea rhizomes 100, 200 mg/kg | Male C57BL/6 mice | Inducing the hepatic expression of CYP3A | Yuan et al. (2017) | |
| Alleviating LPS-induced inflammatory responses | Atractylodin 40 or 80 mg/kg | Lipopolysaccharide (LPS)-induced inflammatory rates | Suppression of nucleotide-binding domain-like receptor protein 3 inflammasome and toll-like receptor 4 activation | Tang et al. (2018) | |
| Ameliorate colitis | β-sitosterol and stigmasterol 0.4% | Dextran sulfate sodium (DSS)-induced colitis in C57BL/6J male mice | Suppressing the activation of inflammatory master regulator NF-κB. Stigmasterol significantly lowered colonic inflammation score and the expression of cyclooxygenase-2 and colony stimulating factor-1 | Feng et al. (2017) | |
| Anti-bacterial activity | Antimycotic effect | AR 0.5–10.0% | Trichophyton tonsuraus, Microsporum gypseum et al. | This drug had apparent fungi action | Yin et al. (2000) |
| Combating multidrug resistant strains | Stigmasterol 1 μg/disc, or in combination (1 μg/disc ampicillin + 1 μg/disc stigmasterol) | 2 g-positive bacteria and 2 g-negative bacteria | Synergistic effects of stigmasterol and ampicillin against β-lactamase producing clinical isolates | Yenn et al. (2017) | |
| Other activities | Protective effects of acute lung injury | LPS + AO-I (5, 10 and 20 mg/kg), LPS + VGX-1027 (0.5 mg/mouse) | LPS-induced acute lung injury mouse model | Inhibiting of TLR4 expression and NF-κB activation | Zhang et al. (2015) |
| Antiasthmatic properties | Stigmasterol 10–100 mg/kg | Ovalbumin-induced Guinea pigs | Reducing the proliferation of eosinophils, lymphocytes, and monocytes while reducing peribronchiolar, perivascular, and alveolar infiltration of inflammatory cells | Antwi et al. (2017) | |
| Treatment of hallucinations of dementia | Atractylenolide III 0.03, 0.15, 0.75 mg/kg; β-eudesmol 0.4, 2.0, 10 mg/kg |
1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (DOI)-induced head-twitch mice | Active constituents contributing to the anti-hallucination effects of Byaku- and So-jutsu against serotonin receptors | Murayama et al. (2014) | |
| Neuroprotective activity | Atractylenolide III 0.6, 1.2 and 2.4 mg/kg/day | Chronic high-dose homocysteine administration induced learning and memory impairment in rats | Decreasing homocysteine-induced reactive oxygen species formation and restored homocysteine-induced decrease of phosphorylated protein kinase C expression level | Zhao et al. (2015) | |
| Autonomic nerve activity | β-eudesmol 1.6, 1.8, 2.3, 2.4 ng/mL | Male Wistar rats (300–350 g) | Suppressing ASNA, partly through TRPA1 and the afferent vagus nerve | Ohara et al. (2018) | |
| Influenza A virus treatment | Atractylon treatment at doses of 10–40 mg/kg | Influenza a virus (IAV) caused pneumonia in mice | Upregulating the expression of Τoll-like receptor 7, MyD88, tumor necrosis factor receptor-associated factor 6 and IFN-β mRNA but downregulating NF-κB p65 protein expression in the lung tissues of IAV-infected mice | Cheng et al. (2016) | |
| Anti-diabetic activity | Metformin 200 mg/kg, stigmasterol 50, 100 mg/kg | Rat L6 cells | Enhancing the GLUT4 expression in L6 cells, skeletal muscle and white adipose tissue | Wang et al. (2017) | |
| Anti-obesity effect | the ethanol extract of Atractylodes lancea rhizome (250, 500 mg/kg) | A high-fat diet-induced obesity mice | Atractylodin showed the highest lipase inhibitory activity | Jiao et al. (2014) | |
| Anti-allergic activities | AR ethanol extracts 200 mg/day | Male NC/Nga mice | Inhibiting 5-LOX from RBL-1 cells | Lim et al. (2012) |