C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity
The aims of the present study were to estimate the affinity between 3,5-(E)-bis(3-methoxy-4-hydroxybenzal)-4-piperidinone hydrochloride (C0818) and heat shock protein 90 (Hsp90) and to investigate the inhibitory effects of this compound on Hsp90 ATPase activity. Fluorescence spectroscopy was used to...
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| Format: | Article |
| Language: | English |
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Elsevier
2017-01-01
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| Series: | Acta Pharmaceutica Sinica B |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211383516300260 |
| _version_ | 1828466335980453888 |
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| author | Yingjuan Fan Yang Liu Lianru Zhang Fang Cai Liping Zhu Jianhua Xu |
| author_facet | Yingjuan Fan Yang Liu Lianru Zhang Fang Cai Liping Zhu Jianhua Xu |
| author_sort | Yingjuan Fan |
| collection | DOAJ |
| description | The aims of the present study were to estimate the affinity between 3,5-(E)-bis(3-methoxy-4-hydroxybenzal)-4-piperidinone hydrochloride (C0818) and heat shock protein 90 (Hsp90) and to investigate the inhibitory effects of this compound on Hsp90 ATPase activity. Fluorescence spectroscopy was used to examine the affinity between varying concentrations of C0818 and Hsp90, N-Hsp90, M-Hsp90 and C-Hsp90. Fluorescence intensities were recorded in the range of 290–510 nm at 293, 303 and 310 K, respectively. A colorimetric assay for inorganic phosphate (based on the formation of a phosphomolybdate complex and the subsequent reaction with malachite green) were used to examine the inhibitory effects of C0818 on Hsp90 ATPase activity. The equilibrium dissociation constant KD value of C0818 was found to be 23.412±0.943 μmol/L. The interaction between C0818 and Hsp90 was driven mainly by electrostatic interactions. C0818 showed the strongest affinity with C-Hsp90. These results conclusively demonstrate the inhibitory activity of C0818 on the activity of Hsp90 ATPase. |
| first_indexed | 2024-12-11T03:48:57Z |
| format | Article |
| id | doaj.art-cfa83402e5b145ab8e3994c3a4e1c5e1 |
| institution | Directory Open Access Journal |
| issn | 2211-3835 2211-3843 |
| language | English |
| last_indexed | 2024-12-11T03:48:57Z |
| publishDate | 2017-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Acta Pharmaceutica Sinica B |
| spelling | doaj.art-cfa83402e5b145ab8e3994c3a4e1c5e12022-12-22T01:21:58ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432017-01-0171919610.1016/j.apsb.2016.05.014C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activityYingjuan Fan0Yang Liu1Lianru Zhang2Fang Cai3Liping Zhu4Jianhua Xu5School of Pharmacy, Fujian Medical University, Fuzhou 350108, ChinaSchool of Pharmacy, Fujian Medical University, Fuzhou 350108, ChinaSchool of Life Science, Xiameng University, Xiamen 361005, ChinaSchool of Pharmacy, Fujian Medical University, Fuzhou 350108, ChinaSchool of Pharmacy, Fujian Medical University, Fuzhou 350108, ChinaSchool of Pharmacy, Fujian Medical University, Fuzhou 350108, ChinaThe aims of the present study were to estimate the affinity between 3,5-(E)-bis(3-methoxy-4-hydroxybenzal)-4-piperidinone hydrochloride (C0818) and heat shock protein 90 (Hsp90) and to investigate the inhibitory effects of this compound on Hsp90 ATPase activity. Fluorescence spectroscopy was used to examine the affinity between varying concentrations of C0818 and Hsp90, N-Hsp90, M-Hsp90 and C-Hsp90. Fluorescence intensities were recorded in the range of 290–510 nm at 293, 303 and 310 K, respectively. A colorimetric assay for inorganic phosphate (based on the formation of a phosphomolybdate complex and the subsequent reaction with malachite green) were used to examine the inhibitory effects of C0818 on Hsp90 ATPase activity. The equilibrium dissociation constant KD value of C0818 was found to be 23.412±0.943 μmol/L. The interaction between C0818 and Hsp90 was driven mainly by electrostatic interactions. C0818 showed the strongest affinity with C-Hsp90. These results conclusively demonstrate the inhibitory activity of C0818 on the activity of Hsp90 ATPase.http://www.sciencedirect.com/science/article/pii/S2211383516300260Curcumin derivativeHsp90ATPase activityFluorescence spectrometryInteraction |
| spellingShingle | Yingjuan Fan Yang Liu Lianru Zhang Fang Cai Liping Zhu Jianhua Xu C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity Acta Pharmaceutica Sinica B Curcumin derivative Hsp90 ATPase activity Fluorescence spectrometry Interaction |
| title | C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity |
| title_full | C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity |
| title_fullStr | C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity |
| title_full_unstemmed | C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity |
| title_short | C0818, a novel curcumin derivative, interacts with Hsp90 and inhibits Hsp90 ATPase activity |
| title_sort | c0818 a novel curcumin derivative interacts with hsp90 and inhibits hsp90 atpase activity |
| topic | Curcumin derivative Hsp90 ATPase activity Fluorescence spectrometry Interaction |
| url | http://www.sciencedirect.com/science/article/pii/S2211383516300260 |
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