Antidepressant-like effects of a novel curcumin derivative J147: Involvement of 5-HT1A receptor

Lian, Lejing; Xu, Ying; Zhang, Jianbo; Yu, Yong; Zhu, Naping; Guan, Xiaofei; Huang, Hui; Chen, Ruijie; Chen, Jie; Shi, Guangming; Pan, Jianchun

doi:10.1016/j.neuropharm.2018.04.003

Cited by 41 publications

(20 citation statements)

References 43 publications

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“…In summary, the findings acquired from the mechanistic studies indicated that compounds 4a , 4b , 4e and 4f presented significant antidepressant-like activities and 5-HT 1A , 5-HT 2A/2C and 5-HT 3 receptors seem to contribute to these effects. These results supported the previous literature pointing out the role of serotonergic system and 5-HT 1A , 5-HT 2A/2C and 5-HT 3 receptors [ 56 , 57 , 58 , 59 ] in the pharmacological mechanisms of various compounds possessing antidepressant efficacy. Actually, additional radioligand binding studies will help to confirm the involvement of these three serotonergic receptors as molecular targets of compounds 4a , 4b , 4e and 4f .…”

Section: Resultssupporting

confidence: 92%

Synthesis of Novel Benzazole Derivatives and Evaluation of Their Antidepressant-Like Activities with Possible Underlying Mechanisms

et al. 2018

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Novel benzazole derivative compounds 4a–4h were obtained by the reaction of corresponding 2-(benzazol-2-ylthio)acetohydrazide and appropriate 4-substituted benzaldehydes. The chemical structures of the synthesized compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR and LCMS spectroscopic methods. Antidepressant-like effects of the compounds were evaluated by tail suspension test (TST) and modified forced swimming tests (MFST). Moreover, locomotor activities of the animals were assessed by an activity cage apparatus. In the series, compounds 4a, 4b, 4e and 4f (at 50 mg/kg) significantly decreased the immobility time of mice in both of the TST and MFST. The same compounds prolonged the swimming time of animals in MFST without any change in the climbing duration. These data indicated that compounds 4a, 4b, 4e and 4f possess significant antidepressant-like activities. Moreover, pre-treatments with p-chloro-phenylalanine methyl ester (an inhibitor of serotonin synthesis), NAN-190 (a 5-HT1A antagonist), ketanserin (a 5-HT2A/2C antagonist), and ondansetron (a 5-HT3 antagonist) reversed the exhibited pharmacological effects. Results of the mechanistic studies suggested the involvement of serotonergic system and contributions of 5-HT1A, 5-HT2A/2C and 5-HT3 receptors to the antidepressant-like effects of compounds 4a, 4b, 4e and 4f. Furthermore, unchanged locomotor activity of mice following the administrations of these four derivatives confirmed that the presented antidepressant-like effects are specific.

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Section: Resultssupporting

confidence: 92%

Synthesis of Novel Benzazole Derivatives and Evaluation of Their Antidepressant-Like Activities with Possible Underlying Mechanisms

et al. 2018

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“…The obtained results are in line with previous reports on strong antidepressant-like effect of repeated curcumin administration (10 mg/kg bw, via gavage) in a CMS model (Jiang et al, 2013;Liu et al, 2014). Furthermore, curcumin and its derivatives in stressed animals are known to decrease the serum corticosterone levels and modulate the sensitivity of serotonin receptors of type 5-HT 1A , 5-HT 1B and 5-HT 7 (Li et al, 2009;Lian et al, 2018).…”

Section: Discussionsupporting

confidence: 91%

“…Our previous data about the MWM task discussed its correlation with the impairment in the hippocampus (Vasileva et al, 2017) which was confirmed in the present study as the model of chronic stress provoked learning disabilities and memory impairments. The mitigation of such stress-induced alternations by salidroside and curcumin presented that these substances could also act at the hippocampal brain area and could modulate the BDNF levels in conditions of stress (Lian et al, 2018;Liu et al, 2014;Yang et al, 2014).…”

Section: Discussionmentioning

confidence: 99%

Antidepressant-like effect of salidroside and curcumin on the immunoreactivity of rats subjected to a chronic mild stress model

Vasileva

Saracheva

Ivanovska

et al. 2018

Food and Chemical Toxicology

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Deregulated cytokines' production is found in depressed patients. Salidroside and curcumin both have been described with potential antidepressant-like activities. The present study investigated the effect of pure salidroside, curcumin and their combination on the immunoreactivity of animals, subjected to a chronic mild stress (CMS) model, followed by lipopolysaccharide (LPS)-induced inflammation. Wistar male rats were separated in the following six groups: control, CMS model, fluoxetine (2.5 mg/kg, oral), salidroside (5 mg/kg, oral), curcumin (20 mg/kg, oral) and salidroside + curcumin (5 mg/kg + 20 mg/kg, oral). Changes in glucose preference, spatial learning and exploratory behavior were recorded. The IL-6 levels in the rats' sera and of the TNF-α levels in the rats' sera and the brain tissue homogenate were evaluated. The groups exposed to stress and treated with fluoxetine, salidroside, curcumin or salidroside + curcumin showed increase in the glucose preference and locomotor activity, as well as, decrease in the escape latency and the cytokines' levels compared to the CMS model group. The chronic stress induced behavioral alternations and increased cytokines' levels in rats which were reversed by administration of salidroside and curcumin, suggesting antidepressant-like effects comparable to that of fluoxetine and potential synergistic interaction regarding the anti-inflammatory and anti-stress effects.

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“…18 reports that J147 improves the depression-like behavior in mouse models caused by chronic stress, and its mechanism may involve the regulation of cAMP/pCREB/ BDNF pathway.…”

Section: Resultsmentioning

confidence: 99%

“…Several reports suggest that J147 can reverse memory deficits, enhance the production of new brain cells, and retard the progression of Alzheimer's disease in rats 16,17 .Related the study of molecular mechanisms have found that J147 combines with the proteins mitochondrial proteins via ATP synthase, there by promoting aging cells, mice and fruit flies to look younger 17 . Besides, Lian et al 18 reports that J147 improves the depression-like behavior in mouse models caused by chronic stress, and its mechanism may involve the regulation of cAMP/pCREB/ BDNF pathway.…”

mentioning

confidence: 99%

A curcumin derivative J147 ameliorates diabetic peripheral neuropathy in streptozotocin (STZ)-induced DPN rat models through negative regulation AMPK on TRPA1

Cao

Zhang

et al. 2018

Acta Cir. Bras.

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A curcumin derivative J147 ameliorates diabetic peripheral neuropathy in streptozotocin (STZ)-induced DPN rat models through negative regulation AMPK on TRPA1 1 8-Experimental SurgeryActa Cir Bras. 2018;33(6):533-541 AbstractPurpose: To investigate the specific molecular mechanisms and effects of curcumin derivative J147 on diabetic peripheral neuropathy (DPN). Methods: We constructed streptozotocin (STZ)-induced DPN rat models to detected mechanical withdrawal threshold (MWT) in vivo using Von Frey filaments. In vitro, we measured cell viability and apoptosis, adenosine 5'-monophosphate-activated protein kinase (AMPK) and transient receptor potential A1 (TRPA1) expression using MTT, flow cytometry, qRT-PCR and western blot. Then, TRPA1 expression level and calcium reaction level were assessed in agonist AICAR treated RSC96cells. Results:The results showed that J147reduced MWT in vivo, increased the mRNA and protein level of AMPK, reduced TRPA1 expression and calcium reaction level in AITCR treated RSC96 cells, and had no obvious effect on cell viability and apoptosis. 18 reports that J147 improves the depression-like behavior in mouse models caused by chronic stress, and its mechanism may involve the regulation of cAMP/pCREB/ BDNF pathway.Due to curcumin can relieve diabetic peripheral neuropathic pain 14 , we aimed to investigate the specific molecular mechanisms and effects of J147 on DPN through the establishment of DPN rat models, cell viability and apoptosis assay in this study. ■ Methods DPN rat modelsEthical Guidelines were approved by the Ethical Committee of Shanxi University of Traditional Chinese Medicine.The 30 adult male SPF rats (weighing 200 ± 20g) were obtained from Institute of Laboratory Animal Science, Chinese Academy of Medical Science (Beijing, China). They were housed in stainless steel squirrel cages with food and water available ad libitum. The breeding room was kept at 20°C, 70% humidity and 12 h of light.SPF rats were weighed after fasting for 12 h, and streptozotocin(STZ) solution (Solarbio, Beijing, China) was injected intraperitoneally at 50 mg/kg weight. After 4 h of injection, the rats resumed their diet ■ IntroductionDiabetic peripheral neuropathy (DPN) is one of the major disability factors and the most common chronic neurological complications in diabetes 1 . The clinical manifestations of this disease are distal symmetric pain with paresthesia, like numbness, ant walking, insect crawling, fever, electric shock, and motor neurological disorders 2,3 .Further, severe DPN patients may develop lower extremity arthropathy and ulcers 2 . In addition, there will be DPN in 30-50% diabetic patients by 2025 according to the prediction from WHO 4 . Therefore, in order to ameliorate the patient's clinical symptoms and control the development of DPN, the comprehensive treatments are used, such as control of blood glucose, oral Duloxetine and Pregabalin, interventional therapy and surgical treatment [5][6][7][8] . Regardless, the exact pathogenesis of DPN is not fully understood until now. ...

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Antidepressant-like effects of a novel curcumin derivative J147: Involvement of 5-HT1A receptor

Cited by 41 publications

References 43 publications

Synthesis of Novel Benzazole Derivatives and Evaluation of Their Antidepressant-Like Activities with Possible Underlying Mechanisms

Synthesis of Novel Benzazole Derivatives and Evaluation of Their Antidepressant-Like Activities with Possible Underlying Mechanisms

Antidepressant-like effect of salidroside and curcumin on the immunoreactivity of rats subjected to a chronic mild stress model

A curcumin derivative J147 ameliorates diabetic peripheral neuropathy in streptozotocin (STZ)-induced DPN rat models through negative regulation AMPK on TRPA1

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