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1.
J Biochem Mol Toxicol ; 34(7): e22491, 2020 Jul.
Article in English | MEDLINE | ID: mdl-32125059

ABSTRACT

A previous study reported that compound 5A, a caffeic acid phenethyl ester (CAPE) analog, exhibited obvious neuroprotective activity, in particular, compound 5A possessed higher stability and membrane permeability than CAPE. CAPE displays antitumour function; therefore, evaluating the antitumour effect of its analog with higher stability and membrane permeability is worthwhile. We first investigated the antitumour activity of compound 5A. We found that compound 5A significantly inhibited the proliferation of tumor cells and showed low cytotoxicity in normal cells. Furthermore, compound 5A was found to induce the cell cycle arrest and apoptosis of CNE2 cells. Through the prediction of SwissTargetPrediction and subsequent confirmation, epidermal growth factor receptor (EGFR) was identified as a target of compound 5A. Compound 5A also influenced the expression of genes downstream of EGFR in nasopharyngeal carcinoma (NPC) cells. Based on these findings, compound 5A inhibits the proliferation of NPC cells by targeting EGFR and may become a new candidate compound for NPC treatment.


Subject(s)
Antineoplastic Agents/pharmacology , Caffeic Acids/pharmacology , Cell Proliferation/drug effects , Nasopharyngeal Carcinoma/metabolism , Nasopharyngeal Neoplasms/metabolism , Phenylethyl Alcohol/analogs & derivatives , Apoptosis/drug effects , Cell Cycle Checkpoints/drug effects , Cell Survival/drug effects , ErbB Receptors/chemistry , ErbB Receptors/genetics , ErbB Receptors/metabolism , Fibroblasts/drug effects , Fibroblasts/metabolism , Gene Expression/drug effects , HeLa Cells , Humans , MCF-7 Cells , Nasopharyngeal Carcinoma/pathology , Nasopharyngeal Neoplasms/pathology , Phenylethyl Alcohol/pharmacology , Signal Transduction/drug effects
2.
Biol Pharm Bull ; 42(10): 1689-1693, 2019 Oct 01.
Article in English | MEDLINE | ID: mdl-31366853

ABSTRACT

Caffeic acid phenethyl ester (CAPE), an active polyphenolic component of honeybee propolis, has been demonstrated to have many medicinal properties. However, the antitumor effect and mechanism of CAPE on laryngeal carcinoma cells have not been examined. In this study, we treated HEp2 cells with various concentration of CAPE, and the results showed that CAPE can reduce the viability of HEp2 cells with IC50 values of 23.8 ± 0.7 µM for 72 h. Meanwhile, CAPE significantly inhibited activation of signal transducer and activator of transcription (Stat)3 in a concentration dependent manner in HEp2 cells and regulated the expression and transcription of Plk1. AG490, a specific Stat3 inhibitor, not only inhibited the activation and expression of Stat3, but also inhibited the expression of Plk1 in HEp2 cells, so Stat3 was probably involved in the regulation of Plk1 in HEp2 cells. In addition, treatment of CAPE leaded to a blockage of cell cycle in S phase in HEp2 cells. Therefore, CAPE inhibited the proliferation of HEp2 Cells probably by regulating Stat3/Plk1 pathway and inducing S phase arrest.


Subject(s)
Caffeic Acids/pharmacology , Cell Cycle Checkpoints/drug effects , Cell Cycle Proteins/metabolism , Laryngeal Neoplasms/metabolism , Phenylethyl Alcohol/analogs & derivatives , Propolis/chemistry , Protein Serine-Threonine Kinases/metabolism , Proto-Oncogene Proteins/metabolism , S Phase/drug effects , STAT3 Transcription Factor/metabolism , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/therapeutic use , Caffeic Acids/therapeutic use , Cell Line, Tumor , Cell Proliferation , Humans , Laryngeal Neoplasms/drug therapy , Phenylethyl Alcohol/pharmacology , Phenylethyl Alcohol/therapeutic use , Polyphenols/pharmacology , Polyphenols/therapeutic use , Polo-Like Kinase 1
3.
Article in Chinese | MEDLINE | ID: mdl-25330636

ABSTRACT

OBJECTIVE: To investigate the effect of nasal instillation of vitamin D3 on patients with allergic rhinitis symptoms including nasal itching, sneezing, clear nasal discharge, and nasal congestion. METHOD: Thirty subjects with allergic rhinitis proved by skin prick test (SPT) and 30 subjects with deviated septum alone were recrui ted and administrated with 300 000 IU of vitamin D3 by nasal instillation weekly. Seven days after the intervention, the four major symptoms including nasal itching, sneezing, clear nasal discharge, and nasal congestion were evaluated by score. RESULT: After intranasal instillation of vitamin D3, the symptoms in allergic rhinitis group in cluding nasal itching, sneezing, nasal discharge and nasal congestion, and serum 25-hydroxyvitamin D level has statistical differences (P < 0.05). CONCLUSION: Vitamin D3 could be well absorbed through nasal mucosa. It demonstrated to have significantly effect on serum 25-hydroxyvitamin D to improve the symptoms for patients with allergic rhinitis. Vitamin D3 may be a kind of adjuvant therapy for prevention and treatment of allergic rhinitis.


Subject(s)
Cholecalciferol/administration & dosage , Rhinitis, Allergic/drug therapy , Administration, Intranasal , Adult , Female , Humans , Male , Middle Aged , Young Adult
4.
Article in Chinese | MEDLINE | ID: mdl-24738313

ABSTRACT

OBJECTIVE: To explore the distribution of allergen tested by skin prick test (SPT) in about 5,843 allergic rhinitis patients in south Shanghai. METHOD: SPT test was conducted in 5,843 allergic rhinitis patients who came to our clinic from January 2007 to August 2012. The result was analyzed by age, sex and year. RESULT: The top three allergens by percentage are dermatophagoides pteronyssinus, dermatophagoides culinae and fungus among 15 common allergens. Incidence rate between male and female in each year had statistical significance, both of which showed no increasing trend with year. Incidence rates among different age groups aging from 6 to 17 years' old had no statistically significant difference, but statistically significant difference among different age groups existed in other age groups. Incidence rate showed increasing trend with year in age group of 40-65, which was not observed in other groups. The incidence rate showed decreasing trend with age in male and female, while the incidence rate in male was always higher than female. CONCLUSION: In south Shanghai, primary allergens causing allergic rhinitis are dermatophagoides pteronyssinus, dermatophagoides culinae and fungus. Statistically significant difference about allergic rhinitis existed in age and sex. SPT has important significance in diagnosis of allergens.


Subject(s)
Allergens/immunology , Rhinitis, Allergic/diagnosis , Rhinitis, Allergic/epidemiology , Adolescent , Adult , Aged , Aged, 80 and over , Child , Child, Preschool , China/epidemiology , Female , Humans , Male , Middle Aged , Rhinitis, Allergic/immunology , Skin Tests , Young Adult
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