3,3',5'-Tri-O-methylpiceatannol and 4,3',5'-tri-O-methylpiceatannol: improvements over piceatannol in bioactivity

Piceatannol (3,4,3',5'-tetrahydroxy-trans-stilbene) (NSC 365798) has recently been isolated and was subsequently synthesized for NCI tumor panel testing as a new antileukemic natural product from the seeds of Euphorbia lagascae. During the synthesis, a bioactive reaction mixture of several partially O-methylated piceatannol analogues was obtained. This mixture has now been maximized and subjected to bioactivity-directed fractionation, using brine shrimp lethality, to yield 3,3',5'-tri-O-methylpiceatannol (NSC 381281); this new compound has improved stability and better bioactivity in several systems than piceatannol itself. To confirm the structure, 5 was synthesized from vanillin. In addition, the isovanillin analogue, 4,3',5'-tri-O-methylpiceatannol (NSC 381864), another new compound, was synthesized and found to be bioactive.     

Preemptive analgesia for postoperative pain relief in lumbosacral spine surgeries: a randomized controlled trial.

BACKGROUND CONTEXT: Administration of analgesic medication, before the actual onset of painful stimulus, is more effective than that after the onset of painful stimulus. This is the principle of preemptive analgesia. Although it is often considered superior to other forms of analgesia, its role in postoperative pain relief after lumbosacral spinal surgery has not been fully investigated. PURPOSE: To analyze the efficacy of preemptive analgesia with a single caudal epidural injection for patients undergoing surgeries on the lumbosacral spine by the posterior approach. STUDY DESIGN/SETTING: Randomized, double-blinded and controlled clinical trial. PATIENT SAMPLE: Eighty-two patients who underwent discectomy in the lumbosacral spine by the posterior approach, with or without instrumentation, were randomized to the control group (n=40) and to the study group (n=42). METHODS: Patients in control group received a single caudal epidural injection of 20 ml of normal saline. Patients in study group received a single caudal epidural injection of 20 ml containing bupivacaine and tramadol as the active agents. The time interval between this injection and the surgical incision was never less than 20 minutes in either of the groups. This facilitated enough time for the drug to get fixed to the nerve roots, leading to effective preemptive analgesia. OUTCOME MEASURES: Patients were monitored for postoperative pain immediately after surgery when they had completely recovered and regained consciousness from general anesthesia, and subsequently 4, 8, 12 and 24 hours thereafter. Pain was quantified using the visual analog scale (VAS) and the verbal rating scale (VRS). The time at which supplemental analgesic medication was first demanded in the postoperative period by the patient was also noted. RESULTS: The two groups were comparable for age, sex, body weight and the type of surgery they underwent. Because the data did not have a normal Gaussian distribution, the one-tailed Mann-Whitney test, being a nonparametric test, was adopted for statistical analysis. Accordingly, VAS and VRS values at all time intervals were significantly lower (p<.0001) in the study group as compared with the control group. This indicated significantly better pain relief in the study group. There was also a significant delay (p=.0041) in the first demand for supplemental analgesic medication in the postoperative period in the study group. No complication specific to the procedure was noted except for the development of postoperative urinary retention, which was transient and appropriately managed with urinary catheterization. CONCLUSIONS: Preemptive analgesia with a single caudal epidural injection of bupivacaine and tramadol is a safe, simple and effective method for postoperative pain relief.     

Conformational changes in the IgG molecule of lepromatous sera using laser Raman spectroscopy

In the present work we report our studies on IgG separated from the serum of lepromatous patients and non-lepromatous leprosy cases using Laser Raman Spectroscopy. Striking spectral changes in LL cases have been observed in the following special regions: (a) the amide I and III, (b) the S-S and C-S stretching (c) the skeletal bending and (d) skeletal stretching regions. These changes indicate a decrease in the amount of beta-structure and a transition towards alpha-helical conformation.     

An unusual presentation of a recurrent neurofibroma in the hand

Neurofibromas in the hand are uncommon and constitute less than 5% of all hand tumours. Accurate diagnosis and appropriate management are important because malignant transformation has been reported, especially in Von Recklinghausen’s neurofibromatosis. We report a case of a large neurofibroma in the right hand of an 18-year-old girl of Afro-Caribbean origin. She was symptomatic with complaints of pain and weakness of grip. General examination revealed multiple café-au-lait spots on the trunk and one nodular swelling in the forearm. The swelling was excised through a palmar approach and histology proved it to be a neurofibroma. The case is being reported for its rarity and it emphasizes the importance of general examination. Histopathological examination is vital in excluding malignant transformation.     

Covered exstrophy: a rare variant

A case of covered exstrophy without sequestration of a bowel segment is reported. A 4-year-old female presented with dribbling of urine. Treatment to date has been simple excision of the covered membrane with functional closure of the bladder and bilateral posterior iliac osteotomies, with reconstruction of the bladder neck and genitalia to be performed at a later date. The embryogenesis of this rare variant, a review of the reported cases, and management options are discussed. Accepted: 6 November 1997     

Glutathione S-transferase isoenzymes in human lung tumors

In the present studies we have compared the levels of glutathione(GSH) and GSH-related enzymes in lung tumors and correspondingnormal tissues obtained from the same individuals. We have alsoimmunologically quantitated the relative amounts of glutathioneS-transferase (or GST-P) type antigen in tumors and adjacentnormal tissues from five patients. GST activities towards 1-chloro-2,4-dinitrobenzene (CDNB) and ethacrynic acid were found to beelevated in tumors from two out of five patients (patients #1and 4), whereas the activity towards these substrates was markedlysuppressed in the tumor tissue from one of the patients (#5).Immunotitration and Western blot studies using antibodies raisedagainst -type GST isoenzymes of human lung and placenta indicatedinduction of GST -type isoenzyme in tumors from patients #1and 4 and suppression of this isoenzyme in tumor from patient#5. The tumors from patients #2 and 3 did not show any increasein GST activity or GST -type antigen. Except for the tumor frompatient #5, the GSH content was higher in the tumors from otherpatients. GSH reductase activity was found to be elevated intumors of all the patients examined in this study. These resultsindicate that GSH and GSH related enzymes are differentiallyaltered in lung tumors and GSH levels and GST - or GST-P-typeisoenzyme(s) are not uniformly elevated in all tumors.