Mitragynine (1) is a major alkaloidal component in the Thai traditional medicinal herb, Mitragyna speciosa, and has been proven to exhibit analgesic activity mediated by opioid receptors. By utilizing this natural product as a lead compound, synthesis of some derivatives, evaluations of the structure-activity relationship, and surveys of the intrinsic activities and potencies on opioid receptors were performed with guinea pig ileum. The affinities of some compounds for mu-, delta-, and kappa-receptors were determined in a receptor binding assay. The essential structural moieties in the Corynanthe type indole alkaloids for inducing the opioid agonistic activity were also clarified. The oxidative derivatives of mitragynine, i.e., mitragynine pseudoindoxyl (2) and 7-hydroxymitragynine (12), were found as opioid agonists with higher potency than morphine in the experiment with guinea pig ileum. In addition, 2 induced an analgesic activity in the tail flick test in mice.
Background/Aims: Hospitalized patients with Crohn’s disease (CD) can develop severe nutritional deficits. However, the nutritional screening tools with the most utility for such patients are still unknown. Methods: Nutritional status of 40 CD patients was assessed on admission using several screening tools and laboratory tests. Their validity was evaluated in relation to length of hospital stay (LOS) and intestinal resection. Receiver operating characteristic analysis was performed to predict prolonged LOS (≥28 days). Results: Prolonged LOS was correlated with each of the following screening parameters: Subjective Global Assessment, Nutrition Risk Screening 2002 (NRS 2002), Onodera’s Prognostic Nutritional Index (O-PNI), Controlling Nutritional Status, serum albumin level, and weight loss. These parameters were not correlated with intestinal resection. Evaluation of prognostic yield showed cutoff values of serum albumin 3.3 g/dL (AUC 0.797, sensitivity 57.1%, specificity 89.5%) and O-PNI 36.5 (0.749, 71.4%, 73.7%). By combining the serum albumin cutoff value and NRS 2002 score, patients were divided into 4 groups, with a prolonged LOS rate of 68.2% in the group with the worst prognosis. Conclusions: A combination of serum albumin (given the simplicity of testing) and NRS 2002 as nutritional screening tools may be useful for hospitalized CD patients.
This study aimed to compare the nutritional status and energy expenditure of hospitalized patients with Crohn’s disease (CD) and those with ulcerative colitis (UC). Twenty-two hospitalized patients with CD and 18 patients with UC were enrolled in this study. We analyzed nutritional status upon admission by using nutritional screening tools including subjective global assessment, malnutrition universal screening tool, and laboratory tests. We measured resting energy expenditure (mREE) of the patients with indirect calorimetry and predicted resting energy expenditure (pREE) was calculated by using the Harris-Benedict equation. Results presented here indicate no significant difference in nutritional parameters and energy metabolism between CD and UC patients. In UC patients, a significant correlation was observed between mREE/body weight and disease activity detected by the Lichtiger and Seo indices. However, there was no correlation between mREE/body weight and Crohn’s disease activity index in CD patients. Inflammatory cytokine interleukin-6 levels correlated with mREE/pREE in CD and UC patients while tumor necrosis factor-α was not. In conclusion, energy expenditure significantly correlated with disease activity in UC patients but not in CD patients. These results indicate that establishing daily energy requirements based on disease activity of UC is imperative for improving the nutritional status of patients.
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