Drug intelligence / Profile preview

calceolarioside B

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Calceolarioside B is a **natural phenylethanoid glycoside** extracted from traditional Chinese medicinal plants, particularly *Akebia quinata* (Mutong) and *Stauntonia hexaphylla*. It is a **hydroxycinnamic acid derivative** with the molecular formula C23H26O11 and molecular weight of 478.45 g/mol. The compound demonstrates multiple biological activities including **antiviral**, **anti-inflammatory**, **immunomodulatory**, and **aldose reductase inhibitory** properties. Notably, calceolarioside B has shown significant activity against **SARS-CoV-2 Omicron BA.2 variant** by binding to the spike protein receptor-binding domain (RBD) with high affinity (KD = 11 μM), thereby inhibiting viral entry into host cells by blocking ACE2 receptor binding. The compound also exhibits **anti-inflammatory effects** by reducing IL-6 expression (43.18% reduction) and promoting macrophage phenotype switching from pro-inflammatory M1 to anti-inflammatory M2 phenotype. Additionally, it demonstrates **aldose reductase inhibition** (IC50 = 23.99 μM) and **DPPH radical scavenging activity** (IC50 = 94.60 μM), suggesting potential antioxidant properties. Calceolarioside B has been investigated for **anti-proliferation properties** against prostate cancer cell lines and shows promise as a dual-function inhibitor with both direct antiviral and immunomodulatory activities.

Other names
Calceolarioside Bdesrhamnosyl isoacteoside105471-98-5
02

Targets

AKR1B1 (Aldose Reductase)Mpro (3C-like proteinase of SARS-CoV-2)BA.2 RBD (SARS-CoV-2 Omicron BA.2 spike receptor-binding domain)

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