Eriocalyxin B Biological Activity: A Review on Its Mechanism of Action

Natural products, a rich source of bioactive chemical compounds, have served humans as a safer drug of choice since times. Eriocalyxin B, an ent-Kaurene diterpenoid, has been extracted from a traditional Chinese herb Isodon eriocalyx. Experimental data support the anticancer and anti-inflammatory activities of EriB. This natural entity exhibits anticancer effects against breast, pancreatic, leukemia, ovarian, lung, bladder, and colorectal cancer. EriB has capability to inhibit the proliferation of cancer cells by prompting apoptosis, arresting cell cycle, and modulating cell signaling pathways. The regulation of signaling pathways in cancerous cells by EriB involves the modulation of various apoptosis-related factors (Bak, Bax, caspases, XIAP, survivin, and Beclin-1), transcriptional factors (nuclear factor kappa B [NF-κB], STAT3, Janus-activated kinase 2, Notch, AP-1, and lκBα), enzymes (cyclooxygenase 2, matrix metalloproteinase 2 [MMP-2], MMP-9, and poly (ADP-ribose) polymerase), cytokines, and protein kinases (mitogen-activated protein kinase and ERK1/2). This review proposes that EriB supplies a novel opportunity for the cure of cancer but supplementary investigations along with preclinical trials are obligatory to effectively figure out its biological and pharmacological applications.

Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells

We have designed and synthesized 6 ent-Kaurane-type diterpenoid derivatives containing α,β-unsaturated ketone moieties. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, L6) by MTT assay. All the tested compounds exhibited comparable or higher activity than DDP and eriocalyxin B. Compounds 16, 17 and 18 are promising anti-tumor leads due to their cytotoxic potencies and higher selectivity, with SI values of 161.06, 47.80 and 128.20, respectively.

Functional roles of eriocalyxin B in zebrafish revealed by transcriptome analysis

Eriocalyxin B (EriB) is a naturalent-kaurane diterpenoid obtained fromIsodon eriocalyxvar.laxiflora(family Lamiaceae), which exerted multiple biological activities (e.g.anti-tumor and anti-inflammatory)viathe alteration of gene expression and signaling transduction.