Posted by PeterMartin on March 20, 2019, at 1:54:42
In reply to Re: TPPU (sEH inhibitor) for depression: [New], posted by PeterMartin on March 20, 2019, at 1:39:49
One more article from Jan 30 on this topic:
https://www.frontiersin.org/articles/10.3389/fphar.2019.00036/full
Role of Soluble Epoxide Hydrolase in Metabolism of PUFAs in Psychiatric and Neurological Disorders
---Many patients with depression become chronically ill, with several relapses or later recurrences, following initial short-term improvement or remission. Relapses occur at a rate of over 85 percent within a decade of an index depressive episode (Forte et al., 2015; Sim et al., 2015). Therefore, the prevention of relapse and recurrence is important in the management of depression. Taken together, it seems that sEH inhibitors could be prophylactic drugs to prevent or minimize relapses triggered by inflammation and/or stress in remitted patients with depression (Hashimoto, 2016; Ren et al., 2016). In addition, given the comorbidity of depressive symptoms in PD or DLB patients (Cummings, 1992; Takahashi et al., 2009; Goodarzi et al., 2016; Schapira et al., 2017), it is also likely that sEH inhibitors may serve as prophylactic drugs to prevent the progression of PD or DLB in patients.
Some natural compounds with sEH inhibitory action were reported. MMU [1,3-bis (4-methoxybenzyl)urea](Figure 2), the most abundant (45.3 μg/g dry root weight from the plant Pentadiplandra brazzeana), showed an IC50 of 92 nM via fluorescent assay and a Ki of 54 nM via radioactivity-based assay on human sEH (Kitamura et al., 2015). MMU is about 8-fold more potent than previously reported natural product sEH inhibitor honokiol (Lee et al., 2014; Kitamura et al., 2015; Figure 2). These findings may explain partly the pharmacological mechanisms of the traditional medicinal use of the root of P. brazzeana. Therefore, it is of interest to study whether the use of the root of P. brazzeana has beneficial effects in patients with psychiatric and neurological disorders.
poster:PeterMartin
thread:1103639
URL: http://www.dr-bob.org/babble/20190206/msgs/1103641.html