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The combined anti-HIV-1 effect of chloroquine and antiretroviral drugs in vitro
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Si-ying XIANG1, 2, Min CHEN2, 3, Huan CHEN2, 3, Rong-hua LUO2, Liu-meng YANG2, Chen QING1, Yong-tang ZHENG2, *
Acta Pharmaceutica Sinica | 2018, 53(2) : 227 - 235
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Acta Pharmaceutica Sinica | 2018, 53(2): 227-235
• ORIGINAL ARTICLES·Pharmacology •
The combined anti-HIV-1 effect of chloroquine and antiretroviral drugs in vitro
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Si-ying XIANG1, 2, Min CHEN2, 3, Huan CHEN2, 3, Rong-hua LUO2, Liu-meng YANG2, Chen QING1, Yong-tang ZHENG2, *
Affiliations
  • 1. School of Pharmaceutical Science and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, China
  • 2. Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
  • 3. University of Chinese Academy of Sciences, Beijing 100039, China
Published: 2018-02-12 doi: 10.16438/j.0513-4870.2017-0853
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The study is aimed to evaluate the anti-HIV-1 effect of chloroquine in combination with antihuman immunodeficiency virus (HIV) drugs, and inhibition of plasmacytoid dendritic cells (pDC) activation and type Ⅰ interferon (IFN-I) production by Toll-like receptor 7 (TLR7) agonist stimulation. We investigated the anti-HIV-1ⅢB, HIV-1KM018 activity of chloroquine and chloroquine combined with rategrivir (RAL), enfuvirtide (T-20), indinavir (IDV) and efavirenz (EFV) in vitro by luciferase activity assay system and ELISA method for p24 antigen. We measured the effect of chloroquine on the activation of pDC in combination with RAL and IDV, respectively. Quantitative PCR was used to evaluate the activity of chloroquine in combination with RAL and IDV in the upregulation of interferon (IFN)-α and IFN-β. Chloroquine showed less cytotoxicity to C8166, TZM-bl and PBMC cells, and the 50% cytotoxic concentration values were 85.02 ±0.28, 73.67 ±5.10 and 91.84 ±4.10 μmol·L-1, respectively. The anti-HIV-1ⅢB activity of chloroquine combination with RAL, T-20, IDV and EFV were moderate in synergy, strong in synergy, additive and moderate antagonism, respectively. The anti-HIV-1KM018 activity of chloroquine in combination with RAL, IDV were moderate synergy, minor synergy. There was no significant difference between the chloroquine monotherapy and chloroquine combined with RAL, IDV in the down-regulation of pDC activation and IFN-α, IFN-β expression levels. We have found that chloroquine combined with different anti-HIV drugs represent different degrees of synergism, antagonism or additive anti-HIV-1 effect. Chloroquine in combination with RAL and IDV did not have influence on the inhibitory effect of chloroquine on pDC activation and type Ⅰ interferon secretion induced by TLR7 agonist. The results suggest that chloroquine may be used to enhance the therapeutic activities of anti-HIV medicines.

chloroquine  /  human immunodeficiency virus-1  /  combination therapy  /  plasmacytoid dendritic cells activation
Si-ying XIANG, Min CHEN, Huan CHEN, Rong-hua LUO, Liu-meng YANG, Chen QING, Yong-tang ZHENG. The combined anti-HIV-1 effect of chloroquine and antiretroviral drugs in vitro[J]. Acta Pharmaceutica Sinica, 2018 , 53 (2) : 227 -235 . DOI: 10.16438/j.0513-4870.2017-0853
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Article Info
doi: 10.16438/j.0513-4870.2017-0853
  • Receive Date：2017-08-30
  • Online Date：2026-01-15
  • Published：2018-02-12
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History
  • Received：2017-08-30
  • Revised：2017-10-10
Funding
Affiliations
    1. School of Pharmaceutical Science and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, China
    2. Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
    3. University of Chinese Academy of Sciences, Beijing 100039, China
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表12种不同金属材料的力学参数
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小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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