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Enhancement of water solubility and anti-tuberculosis activities by a novel artemisinin derivative
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Ning ZHANG1, Yang LIU2, Ye LI2, *, Ping HU1, 2, *
Acta Pharmaceutica Sinica | 2019, 54(1) : 36 - 40
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Acta Pharmaceutica Sinica | 2019, 54(1): 36-40
• Special Reports: Promoting the Dissolution of Poorly Soluble Drugs •
Enhancement of water solubility and anti-tuberculosis activities by a novel artemisinin derivative
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Ning ZHANG1, Yang LIU2, Ye LI2, *, Ping HU1, 2, *
Affiliations
  • 1. School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, China
  • 2. Shanxi Chinese Medicine Research Institute, Xi'an 710003, China
Published: 2019-01-12 doi: 10.16438/j.0513-4870.2018-0876
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Artemisinin and its derivatives have been proved for their anti-tuberculosis activities, despite its low water solubility which hampered its efficacy and corresponding formulation development. In this study we designed and synthesized a novel artemisinin analog by conjugating an arginine through a succinic acid linker. This design not only enhanced the water solubility of the artemisinin, but also increased the efficacy of the molecule towards tuberculosis bacteria due to disruption by arginine. The results showed that the solubility of the synthesized derivatives A-2 and A-3 increased 19.8-27.8 folds compared to artemisinin. In vitro cytotoxicity experiment showed that compound A-3 had negligible toxicity to THP-1 cells up to 1 mg·mL-1, the minimal inhibitory concentration (MIC) of A-2 and A-3 was 20 and 10 μg·mL-1, respectively, which was 5 or 10 times lower than that of artemisinin. Intracellular bacteria inhibition experiment showed that compound A-3 at lower concentrations such as 100 or 200 μg·mL-1 significantly inhibited the growth of tuberculosis bacteria (P < 0.05 or P < 0.01), which efficacy was stronger than artemisinin at the concentration of 100 μg·mL-1. These results strongly suggested that compound A-3 was a potential anti-tuberculosis lead compound.

artemisinin  /  derivative  /  tuberculosis  /  arginine  /  solubility
Ning ZHANG, Yang LIU, Ye LI, Ping HU. Enhancement of water solubility and anti-tuberculosis activities by a novel artemisinin derivative[J]. Acta Pharmaceutica Sinica, 2019 , 54 (1) : 36 -40 . DOI: 10.16438/j.0513-4870.2018-0876
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Article Info
doi: 10.16438/j.0513-4870.2018-0876
  • Receive Date：2018-09-25
  • Online Date：2026-01-26
  • Published：2019-01-12
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History
  • Received：2018-09-25
  • Revised：2018-11-06
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    1. School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, China
    2. Shanxi Chinese Medicine Research Institute, Xi'an 710003, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
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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