Synthesis of Indole-Containing 2-Thiobarbituric Acid Derivatives

The synthesis of barbituric acid derivatives containing α-phenylskatyl residues substituted at C(5) is described. The initial compound was α-phenylnorgramine, which had been previously successfully used for the alkylation of a series of CH-acids, in particular, for the synthesis of diethyl-1H-indol-3-yl(phenyl)methylmalonate. This compound has been used to obtain a series of 2-thiobarbituric acid derivatives, which are expected to possess antioxidant, membrane protector, and radioprotector properties.__________Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 1, pp. 29 – 33, January, 2005.     

Bacterial lipase and high-fat diets in canine exocrine pancreatic insufficiency: A new therapy of steatorrhea?

BACKGROUND & AIMS: Nutrients and properties of lipases affect survival of lipolytic activity during aboral gastrointestinal transit. Whether different doses and formulations of bacterial lipase and diets affect steatorrhea was tested in pancreatic-insufficient dogs. METHODS: A dose of 0-600,000 IU of powdered and 135,000 and 300,000 IU of liquid bacterial lipase was given with a standard meal to 5 dogs with ligated pancreatic ducts. In 4 dogs, 0 or 300,000 IU (normal 6-hour postprandial amount) of powder bacterial lipase was also given with five meals containing 850 kcal with different nutrient caloric densities (mixture design). Coefficients of fat absorption during 72- hour fecal balance studies were used to assess treatments. RESULTS: With the standard meal, powder bacterial lipase reduced steatorrhea in a dose-dependent manner (P = 0.03), and 135,000 and 300,000 IU of the liquid form decreased steatorrhea more than powder bacterial lipase (P = 0.017 and 0.057, respectively). Coefficients of fat absorption with 300,000 IU of powder bacterial lipase correlated (r2 = 0.79; P < 0.001) with increasing proportions of fat calories in diets. CONCLUSIONS: Liquid bacterial lipase decreases steatorrhea more than powder, and 300,000 IU of powder bacterial lipase ingested with high-fat meals corrects canine pancreatic steatorrhea. The combination of adequate mixing of small amounts (milligrams) of bacterial lipase and high-fat meals abolishes canine steatorrhea and may abolish human pancreatic steatorrhea. (Gastroenterology 1997 Jun;112(6):2048-55)     

T-cells of virus-infected mice produce a lymphokine which activates the autoreactivity of intact mouse lymphocytes.

The role of lymphokines was estimated in induction of autoreactive T-cells during Langat virus infection in mice. It was shown that in vitro cultured splenocytes from virus-infected animal containing autoreactive lymphocytes (ARL) spontaneously produce a lymphokine which is capable to activate the autoreactivity of lymphocytes derived from the spleen of intact syngeneic mice. The capacity of this lymphokine to activate the autoreactivity of acceptor cells within 2 hr was demonstrated by local graft-versus host reaction (GVHR) in the donor-recipient system. According to their surface markers (theta-antigen expression, absence of immunoglobulins) the lymphokine activating autoreactivity (LAA) producers may belong to T-lymphocyte population. Autoreactivity could be induced by the lymphokine only if the LAA producers and acceptors were compatible by the major histocompatibility complex antigens.     

A randomized controlled trial of electromagnetic therapy in the primary care management of venous leg ulceration

OBJECTIVE: The aim was to establish the potential efficacy, tolerabilityand side-effect profile of electromagnetic therapy as an adjunctto conventional dressings in the treatment of venous leg ulcers. METHOD: A prospective, randomized, double blind controlled clinicaltrial was carried out in a dedicated leg ulcer clinic basedin one urban general practice. Nineteen patients with leg ulcersof confirmed venous aetiology were assessed. The main outcomemeasures were rate and scale of venous leg ulcer healing, changesin patient-reported pain levels, quality of life, degree ofmobility, side effect profile and acceptability to patientsand staff. RESULTS: Sixty-eight per cent of patients attending this dedicated clinicachieved improvements in the size of their ulcer (4, 21%, healedfully) and in reduced pain levels (P < 0.05) during the trial,despite the chronicity of ulcer histories. Patients treatedwith electromagnetic therapy at 800 Hz were found at day 50to have significantly greater healing (P < 0.05) and paincontrol (P < 0.05) than placebo therapy or treatment with600 Hz. All patients reported improved mobility at the end ofthe study. The electromagnetic therapy was well tolerated bypatients, with no differences between groups in reporting adverseevents, and proved acceptable to staff. CONCLUSION: Despite the small numbers in this pilot study, electromagnetictherapy provided significant gains in the healing of venousleg ulcers and reduction in pain. Keywords. Electromagnetic therapy, RCT, leg ulcers, primary care.