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Natural Antimicrobials Meet a Synthetic Antibiotic: Carvacrol/Thymol and Ciprofloxacin Cocrystals as a Promising Solid-State Route to Activity Enhancement
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2020-08-21 , DOI: 10.1021/acs.cgd.0c00900 Oleksii Shemchuk 1 , Simone d’Agostino 1 , Cecilia Fiore 1 , Vittorio Sambri 2, 3 , Silvia Zannoli 3 , Fabrizia Grepioni 1 , Dario Braga 1
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2020-08-21 , DOI: 10.1021/acs.cgd.0c00900 Oleksii Shemchuk 1 , Simone d’Agostino 1 , Cecilia Fiore 1 , Vittorio Sambri 2, 3 , Silvia Zannoli 3 , Fabrizia Grepioni 1 , Dario Braga 1
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The antibiotic ciprofloxacin (CIP) zwitterion has been cocrystallized via slurry and/or ball-milling with carvacrol (CAR) and thymol (THY), also known to exert antimicrobial activity, with the aim of improving the antibacterial activity of ciprofloxacin. In the case of CAR, the 1:4 cocrystal CIP·CAR4 appears to be the most stable phase, where the intermediate phases CIP·CAR3 and CIP·CAR2 have been isolated by stepwise loss of CAR. In the case of THY, the 1:2 cocrystal CIP·THY2 is the most stable, while the 1:4 cocrystal CIP·THY4 easily loses THY to yield the bisadduct. All cocrystals were structurally characterized by single crystal or powder diffraction: in both cocrystals sheets of CIP molecules are intercalated with layers of CAR and THY, respectively, that can be released stepwise upon heating as followed by DSC, TGA and variable temperature XRPD. Preliminary antimicrobial experiments provide encouraging evidence of the enhanced activity of the cocrystals CIP·CAR4 and CIP·THY2 against Escherichia coli (ATCC 25922) with respect to pure ciprofloxacin as well as to physical mixtures of ciprofloxacin with carvacrol or thymol.
中文翻译：
天然抗菌素与合成抗生素相遇：香芹酚/百里香酚和环丙沙星共晶体是提高活性的有前途的固态途径
抗生素环丙沙星（CIP）的两性离子通过与香芹酚（CAR）和百里香酚（THY）的浆液和/或球磨共结晶，也被称为具有抗菌活性，目的是提高环丙沙星的抗菌活性。在CAR的情况下，1：4共晶CIP·CAR 4似乎是最稳定的相，其中中间相CIP·CAR 3和CIP·CAR 2已通过CAR的逐步丢失而分离。在THY情况下，最稳定的1：2共晶CIP·THY 2，而最重要的是1：4共同晶CIP·THY 4容易失去THY来产生双加合物。所有共晶的结构均通过单晶或粉末衍射进行表征：在这两个共晶中，CIP分子的薄片分别插有CAR和THY层，可在加热后逐步释放，然后依次加热DSC，TGA和可变温度XRPD。初步的抗菌实验提供了令人鼓舞的证据，表明共晶CIP·CAR 4和CIP·THY 2对纯环丙沙星以及环丙沙星与香芹酚或百里酚的物理混合物的抗大肠杆菌活性（ATCC 25922）。
更新日期：2020-10-07
中文翻译：
天然抗菌素与合成抗生素相遇：香芹酚/百里香酚和环丙沙星共晶体是提高活性的有前途的固态途径
抗生素环丙沙星（CIP）的两性离子通过与香芹酚（CAR）和百里香酚（THY）的浆液和/或球磨共结晶，也被称为具有抗菌活性，目的是提高环丙沙星的抗菌活性。在CAR的情况下，1：4共晶CIP·CAR 4似乎是最稳定的相，其中中间相CIP·CAR 3和CIP·CAR 2已通过CAR的逐步丢失而分离。在THY情况下，最稳定的1：2共晶CIP·THY 2，而最重要的是1：4共同晶CIP·THY 4容易失去THY来产生双加合物。所有共晶的结构均通过单晶或粉末衍射进行表征：在这两个共晶中，CIP分子的薄片分别插有CAR和THY层，可在加热后逐步释放，然后依次加热DSC，TGA和可变温度XRPD。初步的抗菌实验提供了令人鼓舞的证据，表明共晶CIP·CAR 4和CIP·THY 2对纯环丙沙星以及环丙沙星与香芹酚或百里酚的物理混合物的抗大肠杆菌活性（ATCC 25922）。
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