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Table 4 The pharmacological activities and mechanisms of the extracts and pure compounds from Fagopyrum dibotrys

From: Towards a better understanding of Fagopyrum dibotrys: a systematic review

Pharmacological activities Components Experimental models Administration design Effects
Anti-inflammatory Ethanolic extract FCA-induced AA rat model 40, 80 or 1600 mg/kg, 21 days (qd), i.g. Decrease the plasma viscosity and reduce the production of IL-1 and TNF-a
Procyanidin B1 LPS-induced THP-1 50, 100, 150 or 200 mg/L,18 h Negative modulation Toll-like receptor-MyD88 signaling pathway
Ethanolic extract AA-induced irritable bowel syndrome rat model 6 or 24 g/kg, 14 days (qd), i.g. Reduce intestinal inflammation via regulating tight junction proteins
Ethanolic extract FCA-induced SD rats 40, 80 or 160 mg/kg, 21 days (qd), i.g. Reduce the production of IL-1 and TNF-a
Luteolin LPS-induced BALB/c mice 0.5 or 1 mg/kg, 2 h, i.p. Inhibit HMGB1 and the production of TNF-a and NO
Chrysoeriol TPA-induced ear edema mouse model and LPS-stimulated RAW264.7 cells 0.5 or 1 mg/ear, 30 min, skin 10, 20 or 30 µM ,1 h Inhibit JAK2/STA T3 and IκB/p65 NF-κB pathways
Isorhamnetin LPS-induced HGFs 10, 20 or 40 µM, 24 h Inhibit LPS-induced inflammation in HGFs by activating Nrf2 pathway
Tricin LPS-induces hPBMCs 15 µM, 24 h Anti-inflammatory via a mechanism involving the TLR4/NF-κB/STAT cascade
Protocatechuic acid RA-FLSs were obtained via collagenase digestion 5, 10, 20, or 40 µM, 24 or 48 h Ameliorate RA-FLSs via inhibiting the NF-κB and Akt/mTOR signalling pathways
Hecogenin 2,4-Dinitrofluorobenzenein-induced BALB/c mice 50, 75 or 100 mg/mice Ameliorate inflammation by inhibiting TNF-a and IL-12
Procyanidin B2 Paraquat-induced SD rats 25, 50 and 100 mg/kg,
3 days (qd), i.g.
Suppress the activation of NLRP3 inflammasome
Anti-cancer Ethanolic extract Ketamine-induced SD rats 6, 3, 1.5 g/kg 6 days (qd), i.g. Decrease the excessive expression of TNF-α, ICAM-1, NF-κB p65 and MIP2M mRNA
Extract HeLa, DU145, H460, MCF-7, K562, HCT116, HepG2, U2OS, T98G cells 15, 30, 45, 60 or 120 µg/mL, 48, 72 or 96 h Inhibit the proliferation of cells derived from certain organs
Ethanolic extract Hela cell 2, 10, 50, 250 g/mL, 12, 24, 48 or 72 h Promote the expression of apoptotic Bax and inhibiting the expression of Bcl-2
β-Sitosterol MCF-7 cell 5, 10, 20 or 30 µM, 48 h Preferentially binds with specific β-tubulin isotypes (βII and βIII)
Rhamnetin MCF-7 cell 5, 10, 15 or 25 µM, 24, 48 or 72 h Induce apoptosis in MCF-7 cells via the
miR‑34a/Notch‑1 pathway
Isorhamnetin PANC-1 cell 10–100 mol/L, 48 h Decrease the phosphorylation levels of MEK and ERK in the Ras/MAPK pathway
Genkwanin HT-29 or sr-480 0.1, 1.0, 5.0 or 10.0 ng/mL, overnight Inhibit cancer cells proliferation
Afzelin LNCaP or PC-3 0.1, 1.0 or 10.0 µg/mL, 72 h Inhibition of LIM domain kinase 1 expression
Anti-oxidant Crude aqueous acetone extract DPPH 2-1000 g/mL, 30 min DPPH radical scavenging
Hesperidin APAP-induced Wister rats 100 or 200 mg/kg, 14 days (qd), i.g. Decrease caspase-3, caspase-9, NF-κB, iNOS, Kim-1 and increase Bcl-2
Ferulic acid ABTS and DPPH 1–10 µM, N/A Enhance the scavenging of ABTS and DPPH radicals
Procyanidin B2 HL-60 20 or 200 µM, 1 h Exerts antioxidant by interacting with H2O2
Anti-bacterial Ethanolic extract Pneumococcus-induced KunMing mice 0.76, 0.38, 0.19, 0.098 or 0.049 g/kg,7 days (qd), i.g. Prevent ethanol-induced acute liver injury via blocking CYP2El-mediated ethanol bioactivation and scavenging free radical
Superfine powder Fagopyrum dibotryis Gram-negative bacteria-induced KunMing mice 1.75, 1.25, 0.75 g/kg, 7 days (qd), i.g. Against Gram-negative bacteria
Emodin TSB and TSA used for H. parasuis growth 32 or 64 µg/ mL, 24 h Influence conformation of
membrane protein
Anti-viral Ethanolic extract H3N2-induced chicken embryo 10, 5 or 2.5 mg/mL, 12 or 24 h Inhibit viral proliferation
Genkwanin ASFV Ba71V 40 µM, 96 h Reduce ASFV early and late proteins and viral DNA synthesis
Tricin H1N1pdm, H1N1, H3N2 3.3–30 µM, 8 h Decrease the expression of viral protein and messenger RNA
Ursolic acid RV SA11 10, 20, 30, 40 µM, 24 h Decrease VP6 and NSP2 viral proteins
Procyanidin B1 Vesicular stomatitis and HCV-induced Huh-7 12.5, 25, 50 or 100 µM, 1 h Suppress HCV RNA synthesis
Procyanidin B2 FCV-F9 and MNV-1 1 or 0.5 mg/mL, 3, 6, 24 h Causes structural changes of the P domain of VLPs, leading to HNoV inactivation
Anti-diabetic Ethanolic extract Streptozotocin-induced KunMing mice 50, 100, or 200 mg/kg, 6 weeks (qd), i.g. Hypoglycemic via Crease TG, TC, LDL-C, MDA and HOMA-IR. Decrease HDL-C, SOD, CAT, GSH-Px and ISI
Ursolic acid Metabolic syndrome patient 150 mg/day, 12 weeks Reduce body weight, BMI, waist circumference and fasting glucose, increase insulin sensitivity
Procyanidin C1 ATCC CL173 1, 10 or 20 µM, 48 h Act as a potential insulin action enhancer through the AKT-eNOS pathway in mature adipocytes
Gallic acid and P-coumaric acid STZ-induced Rattus norvegicus 20 mg/kg and 40 mg/kg, 6 weeks (qd), i.g. Decrease the level of TNF-α and increased the levels of PPARγ mRNA and adiponectin