Total synthesis of (-)-blepharocalyxin D.
[reaction: see text] The Prins cyclization strategy was successfully applied in the total synthesis of (-)-blepharocalyxin D, a cytotoxic dimeric diarylheptanoid isolated from Alpinia blepharocalyx.
Biomedical subjects
Publications and source records attributed to Eun Lee.
[reaction: see text] The Prins cyclization strategy was successfully applied in the total synthesis of (-)-blepharocalyxin D, a cytotoxic dimeric diarylheptanoid isolated from Alpinia blepharocalyx.
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Many researchers have used cue reactivity paradigm to study alcohol craving. But the difference of craving response to drinks between alcoholic patients and social drinkers was little evaluated. To investigate characteristics of alcohol-related visual cues which induce alcohol craving in alcoholism, we examined the response of subjects to alcohol-related cues considering qualitative aspects. The authors developed 27 photographs related to alcohol as candidate visual cues. Thirty five patients with alcohol dependence, 35 heavy drinkers and 35 social drinkers were shown these pictures and asked to rate these 6 pictures in order of inducing alcohol craving the most. 'A glass of Soju' and 'A Party scene' were chosen as the alcohol-related visual cues which induced craving the most in the patients and heavy drinkers, respectively. The results suggest that the patients with alcohol dependence are more absorbed by alcohol without drinking context such as an atmosphere or situation involving drinking. Heavy drinkers may experience craving in anticipation of being in a drinking situation.
To investigate the nature of emotional experience in schizophrenia, we examined emotional responses to affective stimuli. Twenty-one outpatients with schizophrenia (9 paranoid, 12 nonparanoid) and 20 normal controls rated the arousal and valence that they experienced from the presentation of 60 pictures. Schizophrenia patients displayed less emotional responsivity to the positive stimuli and they displayed diverse responsivity to the negative stimuli, which depended upon arousal level. Further analysis, using schizophrenia subtype, indicated that nonparanoid patients reported increased negative responsivity and decreased positive responsivity, regardless of arousal level. However, paranoid schizophrenia patients showed enhanced self-reported experiences of emotion to the low arousing stimuli and diminished responsivity to the high arousing stimuli. This pattern was robust to the negative stimuli. These findings suggest that paranoid schizophrenia patients might suffer from aberrantly flattened responses to negative emotional stimuli, and that this may account for paranoid tendency and secondary social isolation in paranoid schizophrenia.
To explore whether or not patients with schizophrenia display a more profound impairment of negative emotion processing, we assessed the implicit evaluation of positive and negative emotional stimuli. Twenty patients with schizophrenia (9 paranoid, 11 non-paranoid) and 22 normal controls were instructed to classify emotional pictures according to the intrinsic valence if the pictures were black and white. If the stimuli were color-filtered, participants were instructed to press the positive/negative response key according to the extrinsic valence (assigned valence of color). The error rates of the color-filtered stimuli were used as dependent measures. Normal controls made more errors on trials of the positive pictures when the correct response was the negative response key than when the correct response was the positive response key. The reverse was true on trials of the negative pictures. Patients with schizophrenia, especially paranoid schizophrenia, committed more errors in trials of the positive pictures when the correct response key was the negative response key. However, the reverse was not true on trials of the negative pictures. These findings suggest that patients with paranoid schizophrenia might suffer from an impaired ability to evaluate negative emotions and have a loosening of association within their negative emotional networks.
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Major depressive disorder and alcohol dependence are common and serious mental illnesses. There is a great interest in discovering useful treatments for both mood symptoms and alcohol abuse in those patients with depressive disorders and comorbid alcohol dependence. The primary purpose of this study was to evaluate the effectiveness and tolerability of mirtazapine for the treatment of patients with alcohol dependence comorbid with a depressive disorder in an open label, naturalistic multicentre treatment setting. The 17-item Hamilton Depression Rating Scale (HDRS), the Hamilton Anxiety Rating Scale (HARS) and the Clinical Global Impression-Severity (CGI-S) scale were measured at baseline and at weeks 4 and 8 for the assessment of treatment effectiveness. Alcohol craving was measured using the Obsessive Compulsive Drinking Scale (OCDS) and the Visual Analog Scale for Craving (VAS). This study showed a statistically significant reduction of the scores on the HDRS (13.9+/-7.3, p<0.0001), HARS (10.8+/-7.2, p<0.0001) and the CGI-S (1.7+/-1.0, p<0.0001) from baseline to the endpoint (week 8). The OCDS and VAS scores were also decreased significantly by 42.3% and 53.2% (9.0+/-10.0, p<0.0001; 2.5+/-2.4, p<0.0001, respectively). The number of patients with a 50% reduction or more in the HDRS and HARS scores was 103 (72.0%) and 106 (74.1%) at the endpoint, respectively. Adverse events related to mirtazapine were observed in 10% or more of the patients in this study. In conclusion, the results from this naturalistic study suggest that the use of mirtazapine for the patients with alcohol dependence comorbid with depressive disorder is accompanied by clinical improvement in their mood and alcohol craving.
[Carbohydrate structure: see text] The original macrodiolide structure proposed for feigrisolide C was incorrect. The true structure of feigrisolide C was identified as (2'S,3'S,6'R,8'R)-homononactoyl (2R,3R,6S,8S)-nonactic acid, which was confirmed by total synthesis.
(+)-SCH 351448 (Na+ salt A) was synthesized employing ring-closing olefin metathesis reaction of an open diene diester intermediate for construction of the 28-membered macrodiolide structure. The open diene diester was prepared from the monomeric hydroxy carboxylic acid and two different olefin fragments. The monomeric hydroxy acid was synthesized via Julia-Julia coupling reaction of intermediates derived from the same olefinic fragments. Oxane units in these fragments were prepared by radical cyclization reactions of beta-alkoxyacrylates. Analogous SCH 351448 salts incorporating other mono- and divalent cations may be prepared. Under acidic conditions, SCH 351448 (Na+ salt A) was the most stable complex, but SCH 351448 (Ca2+ salt) and (Na+ salt B) appear to be physiologically important species.
A radical cyclization of beta-alkoxyvinyl sulfoxides-Pummerer rearrangement-allylation protocol was successfully applied to the synthesis of the threo/cis/threo/cis/erythro bis-oxolane moiety in rolliniastatin 1 (1), rollimembrin (2), and membranacin (3).
[reaction: see text] Possible structures of feigrisolide C were synthesized via ring-closing olefin metathesis reaction of a diester derivative prepared from 8-epi-nonactic acid, but physical characteristics of the synthetic samples did not match with those of the natural sample of feigrisolide C.
The goal of this study was to measure the interindividual reproducibility of glutamate quantification in 1.5-T (1)H MRS of human brains. To determine the effective echo time (TE) for glutamate quantification, spectra from a phantom and 12 participants were obtained with TE = 30, 35, 40, and 144 ms (repetition time (TR) = 2000 ms and volume of interest = 4 cm(3)). The average Cramer-Rao lower bounds for glutamate quantification using LCModel was lowest in two experiments when TE = 40 ms.Twenty-one subjects participated in experiments that measured interindividual reproducibility of glutamate quantification. Spectra were acquired with TR = 6000 ms and TE = 40 ms. Results showed that the coefficients of variance were 11.0 and 13.1% in the anterior cingulate cortex and insula, respectively. This suggests that glutamate can be reproducibly measured from 1.5-T (1)H MRS with long TR, effective TE, and the LCModel.
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[reaction: see text] Tetrahydrofuranyl allyl carbinols may be prepared stereoselectively via radical cyclization of beta-alkoxyvinyl sulfoxides, Pummerer rearrangement, and reaction with allylstannane.
Homolasonolide A and 10-desmethyllasonolide A are biologically less active than lasonolide A. The ethyl ester analogue of lasonolide A exhibited higher activity than the parent compound in some biological test.
Total synthesis of SCH 351448 was accomplished employing the ring-closing olefin metathesis reaction for the preparation of the 28-membered macrodiolide.
Chiral secondary alcohols may be prepared from primary alcohols via asymmetric C-H insertion reactions of alpha'-alkoxy-alpha-diazoketones catalyzed by rhodium(II)(2R,3R)-3-phenylcholestane-2-carboxylate.