1. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  2. Glycosidase Reactive Oxygen Species (ROS)
  3. Guavinoside B

Guavinoside B is an orally active α-glucosidase inhibitor with an IC50 of 0.21 mM. Guavinoside B upregulates the expressions of Nrf2, GCLC and NQO1 induced by Acetaminophen (HY-66005), downregulates the expression of p-JNK, and reduces intracellular ROS levels. Guavinoside B decreases serum TNF-α levels induced by Acetaminophen, alleviates hepatocellular infiltration and necrosis, and improves liver-related biochemical parameters. Guavinoside B is applicable to the research of diabetes and Acetaminophen-induced liver injury.

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Guavinoside B

Guavinoside B Chemical Structure

CAS No. : 372955-18-5

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Description

Guavinoside B is an orally active α-glucosidase inhibitor with an IC50 of 0.21 mM. Guavinoside B upregulates the expressions of Nrf2, GCLC and NQO1 induced by Acetaminophen (HY-66005), downregulates the expression of p-JNK, and reduces intracellular ROS levels. Guavinoside B decreases serum TNF-α levels induced by Acetaminophen, alleviates hepatocellular infiltration and necrosis, and improves liver-related biochemical parameters. Guavinoside B is applicable to the research of diabetes and Acetaminophen-induced liver injury[1][2].

IC50 & Target[1]

α‑glucosidase

0.21 mM (IC50)

In Vitro

Guavinoside B potently inhibits purified α-glucosidase enzyme activity with an IC50 of 0.21 mM[1].
Guavinoside B (3.3-100 μM; 24 h) does not affect the viability of HepG2 cells, either with or without 5 mM Acetaminophen (HY-66005) treatment[2].
Guavinoside B (3.3-30 μM; 16 h) reduces Acetaminophen-induced intracellular ROS accumulation by 28.6% in HepG2 cells, with weaker, non-significant effects at 3.3 and 10 μM[2].
Guavinoside B (10-30 μM; 16 h) upregulates Nrf2 and GCLC mRNA expression in untreated HepG2 cells, and (3.3-30 μM; 16 h) upregulates Nrf2, GCLC, and NQO1 mRNA expression in Acetaminophen-treated HepG2 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[2]

Cell Line: HepG2 (human hepatocellular carcinoma cells)
Concentration: 3.3, 10, 30 μM (alone; co-treated with 5 mM Acetaminophen)
Incubation Time: 16 h
Result: Increased mRNA expression levels of Nrf2 and GCLC at 10 and 30 μM when used alone.
Showed no impact on NQO1 mRNA expression when used alone.
Increased mRNA expression levels of Nrf2, GCLC, and NQO1 at 3.3, 10, and 30 μM when used with Acetaminophen.

Western Blot Analysis[2]

Cell Line: HepG2 (human hepatocellular carcinoma cells)
Concentration: 3.3, 10, 30 μM (alone; co-treated with 5 mM Acetaminophen)
Incubation Time: 16 h
Result: Increased protein expression levels of Nrf2, GCLC, and NQO1 at 3.3, 10, and 30 μM when used alone.
Increased protein expression levels of Nrf2, GCLC, and NQO1 at 3.3, 10, and 30 μM when used with Acetaminophen compared to the Acetaminophen-only group.
In Vivo

Guavinoside B (100 mg/kg/d; p.o.; daily; 7 consecutive days) exerts potent hepatoprotective effects against Acetaminophen (HY-66005)-induced liver injury in male C57BL/6 mice by activating Nrf2 signaling and inhibiting JNK phosphorylation, reducing serum TNF-α by 22.7%, and normalizing key hepatic oxidative stress and liver function biomarkers[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 7 weeks old) injected with Acetaminophen[2]
Dosage: 100 mg/kg/d
Administration: p.o.; daily; 7 consecutive days
Result: Markedly alleviated Acetaminophen-induced hepatic pathological changes, including reduced hepatocyte necrosis and inflammation around central venous lesions.
Significantly reduced serum AST and ALT levels.
Significantly reduced hepatic ROS and MDA levels, and reversed Acetaminophen-induced depletion of hepatic GSH and SOD.
Significantly increased hepatic mRNA expression of SOD1 and GPx1.
Significantly up-regulated hepatic mRNA and protein expression levels of Nrf2, GCLC, and NQO1.
Significantly reduced serum TNF-α levels from 35.3 pg/mL (Acetaminophen-only group) to 27.3 pg/mL, and significantly inhibited Acetaminophen-induced JNK phosphorylation in liver tissue.
Molecular Weight

572.51

Formula

C28H28O13

CAS No.
SMILES

O=C(C1=CC=CC=C1)C2=C(C(C)=C(C(C)=C2O)O[C@@H]3O[C@@H]([C@H]([C@@H]([C@H]3O)O)O)COC(C4=CC(O)=C(C(O)=C4)O)=O)O

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Guavinoside B
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HY-N17855
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