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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