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5 results on '"Qunfa Huang"'

1. A011, a novel small-molecule ligand of σ2 receptor, potently suppresses breast cancer progression via endoplasmic reticulum stress and autophagy

Author

Yuyun Li, Xiaoyang Xie, Shiyi Liao, Zhanwei Zeng, Siyan Li, Baocheng Xie, Qunfa Huang, Huan Zhou, Chenhui Zhou, Jiantao Lin, Yunsheng Huang, and Daohua Xu

Subjects
Breast cancer, Sigma-2 receptor, Endoplasmic reticulum stress, Autophagy, Apoptosis, Therapeutics. Pharmacology, RM1-950
Abstract

Breast cancer has surpassed lung cancer to become the most commonly diagnosed cancer in women worldwide. Sigma-2 (σ2) receptor is considered to be a potential therapeutic target for breast cancer because of its high expression in breast cancer cells and low expression in normal breast cells. Many σ2 ligands have been reported to have excellent anticancer activity, but their mechanism of action has not been fully elucidated. We discovered that A011 had high affinity and selectivity for σ2 receptor, reduced proliferation in five cancer cell lines, and significantly inhibited the monoclonal formation ability of MCF-7 cells. Furthermore, A011 rapidly increased the levels of intracellular Ca2+ and reactive oxygen species and induced autophagy. Molecular pharmacology studies revealed that A011 induced endoplasmic reticulum stress, activated the PERK-eIF2α-CHOP pathway and inhibited the activation of the PI3K-Akt-mTOR pathway, leading to cell apoptosis. In an in vivo tumor model, A011 showed obvious anti-tumor activity and no significant toxicity. More importantly, our study demonstrated for the first time that endoplasmic reticulum stress is the main mechanism of anti-cancer effects for σ2 ligands, at least for A011. A011 may potentially be useful as a therapeutic agent for treating breast cancer.

Published
2022
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2. A011, a novel small-molecule ligand of σ

Author

Yuyun, Li, Xiaoyang, Xie, Shiyi, Liao, Zhanwei, Zeng, Siyan, Li, Baocheng, Xie, Qunfa, Huang, Huan, Zhou, Chenhui, Zhou, Jiantao, Lin, Yunsheng, Huang, and Daohua, Xu

Subjects
Phosphatidylinositol 3-Kinases, Cell Line, Tumor, Autophagy, Humans, Apoptosis, Breast Neoplasms, Female, Endoplasmic Reticulum Stress, Ligands, Signal Transduction
Abstract

Breast cancer has surpassed lung cancer to become the most commonly diagnosed cancer in women worldwide. Sigma-2 (σ

Published
2022

3. Protective effects of crocin against endogenous Aβ-induced neurotoxicity in N2a/APP695swe cells

Author

Jinwen Li, Jikun Du, Yuanhua Li, Li Li, Daibo Song, Baohong Li, Qunfa Huang, and Jierong Liu

Subjects
Pharmacology, Amyloid beta-Peptides, Neurotoxicity, Endogeny, Apoptosis, medicine.disease, Neuroprotection, Carotenoids, 030227 psychiatry, Crocin, Pathogenesis, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Neuroprotective Agents, chemistry, Annexin, Alzheimer Disease, medicine, Humans, Phosphorylation, Cytotoxicity, 030217 neurology & neurosurgery
Abstract

Alzheimer’s disease (AD) is a most common neurodegenerative disorder worldwide. Because of its complex pathogenesis, the prevention and therapies of AD still are a severe challenge. Evidence suggested that crocin, the major component of saffron, exhibited neuroprotective effects in AD. As such, in this study, N2a/APP695swe cells were enrolled to investigate the effects of crocin on endogenous Aβ-induced neurotoxicity. Crocin (100 and 200 μM) could ameliorate cytotoxicity according to CCK-8 assay and reduce apoptosis in line with Hoechst 33,342 staining and Annexin V-FITC/PI double staining in N2a/APP695swe cells. Reduced ROS generation and elevated MMP were found in N2a/APP695swe cells treated with crocin (100 and 200 μM). Additionally, crocin at concentrations of 100 and 200 μM inhibited the release of cytochrome and attenuated caspases-3 activity in N2a/APP695swe cells. Furthermore, succinylation, crotonylation, 2-hydroxyisobutyrylation, malonylation, and phosphorylation were significantly reduced, while a slight increase of acetylation was found in 100-μM crocin treated N2a/APP695swe cells. Taken together, crocin may be a promising natural product candidate for the effective cure of AD.

Published
2021

4. Nuclear-Targeted TAT-PZLL-D3 Co-Delivery DOX and p53 for Chemotherapy Resistance of SCLC

Author

Zhijiang He, Qunfa Huang, Li Li, Dawei Zhang, Jian-Tao Lin, Hua Chen, Tianshou Cao, and Dan Wang

Subjects
A549 cell, Drug, Co delivery, Materials science, viruses, Mechanical Engineering, media_common.quotation_subject, 02 engineering and technology, Transfection, 010402 general chemistry, 021001 nanoscience & nanotechnology, Condensed Matter Physics, 01 natural sciences, 0104 chemical sciences, Mechanics of Materials, Apoptosis, Confocal laser scanning microscopy, Cancer research, General Materials Science, 0210 nano-technology, Gene, Chemotherapy resistance, media_common
Abstract

Small cell lung cancer (SCLC) accounts for 13% ~ 15% of lung cancer. It is a subtype with high malignancy and poor prognosis. Almost all patients with SCLC will inevitably have drug resistance and tumor recurrence, which has become an urgent problem in the treatment of SCLC. Nuclear-targeted drug delivery system, which enables intra-nuclear release of anticancer drugs, is expected to address this challenge. In this study, based on transactivator of transcription (TAT)’s active transport property to the nucleus, we developed a high-efficiency nucleus-targeted co-delivery vector that delivers genes and drugs directly into the nucleus of A549 cells. The system is based on a poly-(N-ε-carbobenzyloxy-L-lysine) (PZLL) and dendritic polyamidoamine (PAMAM) block copolymer (PZLL-D3) with TAT modified on the surface of carrier. In vitro studies showed that DOX and p53 could can be effectively transported to the nucleus and kill the cancer cells. Thus, such deliver system would bypass the drug resistance and tumor recurrence problem.

Published
2021

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