Erianin inhibits human cervical cancer cell through regulation of tumor protein p53 via the extracellular signal‑regulated kinase signaling pathway

Abstract

Erianin, a natural bibenzyl compound, is present in Dendrobium chrysotoxum Lindl. (commonly known as Shihu in China), which is used as an antipyretic and analgesic in traditional Chinese medicine, and has been reported to exert inhibitory effects on cancer cells in vitro. Cervical cancer is the third-most common cancer in women worldwide, and has the highest morbidity rate of gynecological malignancies. Thus, the identification of effective chemotherapeutical agents to treat this disease is urgent. The aim of the present study was to elucidate the biological functions and molecular mechanism of erianin on HeLa cells. Cellular proliferation was assessed using an MTT assay and flow cytometry assay with propidium iodide (PI) staining. Apoptosis rates were observed using a high content screening system via annexin V-fluorescein isothiocyanate/PI double staining, and measured by flow cytometry. The protein levels of tumor protein p53, extracellular signal-regulated kinase 1/2 (ERK1/2), caspase-3, B-cell lymphoma-2 (Bcl-2) and Bcl-2-associated X (Bax) were assessed by western blot analysis. Erianin inhibited the growth of HeLa cells and induced apoptosis in a dose- and time-dependent manner, inducing cell cycle arrest at the G2/M stage. Erianin treatment also increased the expression of Bax and caspase-3, but decreased levels of Bcl-2 and phosphorylated-ERK1/2. Cells treated with paclitaxel were regarded as the positive group. Together, the results of the present study indicated that erianin could be considered as an effective drug candidate; in HeLa cells it inhibited cellular proliferation and promoted apoptosis via regulation of the ERK1/2 signaling and mitochondrial-based apoptosis pathways. Thus, erianin has the promise to be developed further for cervical cancer therapy.

Erianin suppresses hepatocellular carcinoma cells through down-regulation of PI3K/AKT, p38 and ERK MAPK signaling pathways

“…Erianin [2-Methoxy-5-(2-(3,4,5-trimethoxyphenyl)-ethyl)-phenol], a natural bibenzyl compound derived from Dendrobium chrysotoxum Lindl., has been used as a herbal drug for thousands of years in traditional Chinese medicine (TCM) due to its antipyretic and analgesic effects [13]. Previous phytochemical studies have reported that erianin possessed multiple pharmacological activities, including antioxidative, antitumor activity [14]. In addition, erianin has been reported to inhibit cell proliferation and induce apoptosis in human promyelocytic leukemia HL-60 cells, and human cervical cancer HeLa cells via PI3K/Akt, ERK signaling and mitochondria-based apoptosis pathways [15].…”

Transcriptomic analyses reveal putative genes associated with bibenzyl biosynthesis in the traditional Chinese herb Dendrobium officinale

“…Bibenzyl compounds are composed of various formulas, with a pair of benzyl radicals. Of them, the erianin and gigantol are structurally similar, and they are represented as bibenzyl compounds [46,47,40,49]. As a result, in this study, the contents of erianin and gigantol were measured as representatives of bibenzyl compounds.…”

“…The Dendrobium plants are highly prized and have been used as traditional Chinese herbal medicine for many years, but the bioactive constituents of authenticating Dendrobium drugs are complex, including polysaccharides, alkaloids, flavonoids and bibenzyl compounds [43][44]. Polysaccharides perform immunomodulatory and hepatoprotective activities while bibenzyl compounds exhibit antioxidant, anticancer and immunomodulatory activities [18,19,45,16,46,47]. Several studies have been conducted on the identification of putative genes involved in polysaccharide biosynthesis [9,41,48].…”

Transcriptomic Analyses Shed Light on Critical Genes Associated with Bibenzyl Biosynthesis in Dendrobium officinale

“…The bioactive constituents include polysaccharides, alkaloids, flavonoids, and bibenzyl compounds and are complex to authenticate for drug development [ 43 , 44 ]. Polysaccharides perform immunomodulatory and hepato-protective activities, while bibenzyl compounds exhibit antioxidant, anticancer, and immunomodulatory activities [ 45 , 46 , 47 ]. Several studies have been conducted to identify putative genes involved in polysaccharide biosynthesis [ 9 , 40 , 48 ].…”