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Biomedical subjects

K K Bhopale

Publications and source records attributed to K K Bhopale.

16 recordsLinked to original sources
PubMed1996

A simple quantitative in vitro macrophage migration assay.

An in vitro macrophage chemotaxis model using mouse peritoneal non-elicited resident macrophage cells and chemotaxins containing mediators of non-specific elicitors such as oyster glycogen or sodium caseinate has been described. Macrophage cells accumulation in mouse peritoneal cavity was maximum at 48 hr after injecting (i.p.) oyster glycogen (2.5%) or sodium caseinate (12%), 0.5 ml/mouse. Chemotaxins containing mediators were prepared from these mice by peritoneal lavage and termed as routine 'diluted' cocktail and 'concentrated (3 times)' cocktail. Chemotaxis assays were carried out in a modified Boyden chamber using a 48-well microchemotaxis assembly. In vitro results showed higher macrophage chemotaxis response against the 'concentrated' cocktails as compared to routine 'diluted' cocktail. Macrophages exhibited cell density dependent increase in the responsiveness to chemoattractant and macrophage cell density of 4 x 10(6) per ml concentration in the upperwell was found to be optimum. Macrophage responsiveness was seen better with sodium caseinate cocktail as compared to oyster glycogen in vitro as well as in vivo. DMSO (Dimethyl Sulphoxide) solvent (0.25% conc.) did not interfere with normal macrophage chemotaxis. Both CO2 incubator (5% CO2 in air) and BOD incubator with humidified chamber favoured chemotaxis. In vitro test system described can be used as a model to study the effect of anti-inflammatory compounds directly on the macrophage chemotaxis.

Animals↗
PubMed1995

A comparative study of experimental caecal amoebiasis and the evaluation of amoebicides.

Caecal amoebiasis models (mouse, hamster and rat) were compared for amoebic infection and chemotherapeutic evaluation using a pathogenic strain of Entamoeba histolytica of human origin. Caecal infection in the hamster was of the acute type, with a large number of amoebae in the caecal tissue, whereas the amoebae in rats were seen in the lumen, on the mucosal surface. Amoebic lesions in the mouse caecum were of moderate severity. The mouse model responded to both metronidazole (tissue amoebicide) and diloxanide furoate (luminal amoebicide), whereas the hamster model only responded well to metronidazole and the rat model only to diloxanide furoate. Using the mouse as a primary screening model, a new oxadiazole compound, BTI 2405E, was found to have tissue and luminal amoebicidal activity. In rodent caecal models, a single dose of BTI 2405E was found to be more effective than one of metronidazole or diloxanide furoate. The mouse model appears to be the most useful for primary screening of anti-amoebic compounds.

Amebicides↗
PubMed1993

Activity of a new oxadiazole compound, against experimental infections with Entamoeba histolytica and Giardia lamblia in animal models.

BTI 2286E(+/-)-E-3-(4-methylsulphinylstyryl)-1,2,4-oxadiazole has demonstrated potent amoebicidal activity in a single-dose treatment against Entamoeba histolytica infection in the livers of golden hamsters and the caeca of mice, hamsters and rats. It has intra luminal activity against Entamoeba criceti, a natural infection in golden hamster, and anti-giardial activity against Giardia lamblia infection in suckling mice. BTI 2286E is more potent than metronidazole in extra intestinal, intra luminal amoebiasis models and has significant advantages in that it is non-mutagenic in the Ames test and has a shorter duration of effective treatment.

Amebicides↗
PubMed1993

Pharmacokinetics and amoebicidal activity of (+-)-(E)-3-(4- methylsulphinylstyryl)-1,2,4-oxadiazole (BTI 2286E) and its sulphone metabolite (BTI 2571E) in the golden hamster, Mesocricetus auratus.

BTI 2286E is a 1,2,4-oxadiazole with amoebicidal activity. Three groups of golden hamsters received single doses of BTI 2286E or its sulphone metabolite BTI 2571E as either BTI 2286E 60 mg/kg po or BTI 2571E 60 mg/kg po or BTI 2571E 60 mg/kg ip. Blood samples were collected up to 8 h post-dose and plasma concentrations of BTI 2286E and BTI 2571E were assayed by HPLC. BTI 2286E was rapidly absorbed, extensively metabolized during first pass and rapidly eliminated with a plasma elimination half-life of 1.32 h. Conversion to BTI 2571E was the major pathway of elimination. BTI 2571E had approximately 40% bioavailability after oral administration. After intraperitoneal administration its absorption was slow and prolonged, with an apparent elimination half-life of 2.77 h, considerably longer than the elimination half-life of 0.67 h observed when BTI 2571E was formed as a metabolite, in vivo. The amoebicidal activity of both the compounds was evaluated in the acute hamster hepatic model of amoebiasis. Both BTI 2286E and BTI 2571E were administered as single graded po or ip dose, and their dose-response profiles were characterized. BTI 2571E exhibited poor activity after oral administration (ED50 70 mg/kg) probably due to poor bioavailability, but after intraperitoneal administration its activity (ED50 40 mg/kg) was comparable to that of BTI 2286E after po or ip administration.

Administration, Oral↗
PubMed1993

Comparative pharmacokinetics and amoebicidal activity of metronidazole and satranidazole in the golden hamster, Mesocricetus auratus.

The pharmacokinetic properties of metronidazole and satranidazole were studied in the golden hamster (Mesocricetus auratus), at a dose of 80 mg/kg po. Blood and liver samples were collected at frequent time intervals and assayed for metronidazole and satranidazole by HPLC. Satranidazole exhibited significantly higher plasma concentrations than metronidazole at 1 and 2 h post-dose, but the comparative Cmax values were not significantly different. The satranidazole plasma elimination half-life of 1.01 h was significantly shorter than the corresponding metronidazole half-life of 3.62 h. The comparative liver pharmacokinetic parameters Cmax, Tmax and T1/2 did not differ significantly. Satranidazole however exhibited significantly higher liver concentrations at 1 h post-dose and Cmax and AUC0-infinity values were approximately 35% higher. The in-vivo amoebicidal activity of both compounds was evaluated in the acute hamster hepatic model of amoebiasis. Both metronidazole and satranidazole were administered as single graded doses po, and their dose-response profiles were characterized. Satranidazole demonstrated significantly greater amoebicidal activity than metronidazole with an ED50 value of 19.5 mg/kg, compared to an ED50 value of 45 mg/kg for metronidazole. These data suggest that higher plasma and liver concentrations of satranidazole and greater intrinsic potency probably contribute to superior amoebicidal activity in the hamster model of hepatic infection.

Administration, Oral↗
PubMed1983

Comparative studies on the amoebicidal activity of known 5-nitroimidazole derivatives and CG 10213-Go in golden hamsters, Mesocricetus auratus, infected in the liver or caecum or both with trophozoites of Entamoeba histolytica.

CG 10213-Go, a 5-nitroimidazole derivative synthesized at the CIBA-Geigy Research Centre, Bombay, proved superior to such currently used 5-nitroimidazole derivatives as metronidazole, ornidazole, secnidazole, tinidazole and nimorazole, against experimental amoebic infections of the liver and caecum in a golden hamster model. CG 10213-Go is now undergoing clinical trials.

Amebicides↗
PubMed1981

Serum protein profile of mice during infection with single and repeated doses of Hymenolepis nana eggs.

Significant alterations in serum protein of mice following Hymenolepis nana infection were observed. These changes were recorded as decrease in albumin, increase in gamma globulin and a temporary rise in alpha-1, alpha-2 and beta globulins. The decrease in albumin and increase in gamma globulin occurred as early as on 1st day after infection. The alpha-1 and alpha-2 globulins did not show definite profile during infection. The beta globulin predominantly increased till the day 20 post infection and thereafter generally decreased. Repeated infection did not enhance any further alterations in serum protein. There was no significant correlation between infection dose levels and serum protein changes.

Alpha-Globulins↗
PubMed1981

The stimulation of immunity to Hymenolepis mana in mice exposed to low-level infections.

Mice infected with as few as ten eggs of Hymenolepis nana are highly resistant to a challenge infection. Repeated low-level infection can stimulate immunity which is as strong as stimulated by a single large infection. Elimination of the challenge infection occurs to an equal extent in all groups regardless of the size of the immunizing infection. ?

Animals↗