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Screening of some Nigerian plants for molluscicidal activity.

Methanolic (MEOH), evaporated crude water (ECW) and unevaporated crude water (UECW) extracts of 25 Nigerian plants, used for different medicinal and domestic purposes were screened for molluscacidal activity on laboratory-reared Lymnaea natalensis Krauss. Seven of the plants were not active; extracts from 18 (72 per cent) of the plants, some of which are renowned fish poisons, had molluscicidal activity. These were Acacia nilotica, Aristolochia albida, Balanites aegyptiaca, Blighia sapida, Boswellia dalzielii, Detarium microcarpum, Gnidia kraussiana, Kigelia africana, Nauclea latifolia, Opilia celtidefolia, Parkia clappertoniana, Polygonum limbatum, Pseudocedrela kotschyi, Sclerocarya birrea, Securidaca longipedunculata, Ximenia americana, Vetiveria nigritana and Ziziphus abyssinica. The LC50 of these extracts were determined. It is strongly recommended that the toxic effects of these extracts against fish, cercariae, snail eggs and mammals be further investigated so as to determine the right concentration, especially for use in fish ponds.

Animals↗

Lipase activity measured in serum by a continuous-monitoring pH-Stat technique--an update.

Using recent knowledge regarding the roles of colipase, bile acids, Ca2+, and emulsifiers, we optimized a previously published pH-Stat method for lipase (EC 3.1.1.3) activity measurements. The recommended assay conditions are: olive oil/triolein, 100 mL/L; sodium glycocholate, 35 mmol/L; Ca2+, 8.5 mmol/L; and colipase, 6.0 mg/L. The sample volume is 0.10 mL, the reaction pH 9.0, the temperature 30 degrees C, and the concentration of titrant 15 mmol/L. Hydroxypropyl methylcellulose, 20 g/L, replaces acacia as emulsifier to avoid inhibition by excess Ca2+. The standard curve is linear to greater than 4566 U/L. The reference interval with olive oil as substrate is 30-235 U/L. Lipase activities with triolein substrate are 9.9% greater than with olive oil. Interference by pancreatic carboxylesterase (EC 3.1.1.1) activity is inhibited by incubating the sample with diisopropylfluorophosphate. Results correlate well with those by the optimized SingleVial method of Boehringer Mannheim Diagnostics (r = 0.997) and the immunochemical assay of Beckman Instruments, Inc. (r = 0.995). Correlation with the aca method (E.I. DuPont de Nemours & Company) is less satisfactory (r = 0.892), probably owing to lack of colipase in the latter method.

Adult↗

Chimeric protein: abrin B chain-trypsin inhibitor conjugate as a new antitumor agent.

Abrin B chain and trypsin inhibitor isolated from Acacia confusa (ACTI) were covalently linked to form a chimeric protein (ANB-ACTI) with N-succinimidyl-3-(-2-pyridyldithio)propionate. The chimeric protein had 31% of trypsin inhibitory activity of ACTI and 7% of hemagglutinating activity of abrin B chain, but no inhibition on protein biosynthesis. ANB-ACTI had strong inhibitory effects on the growth of sarcoma 180 cells and Hela cell culture while the mixture of an equivalent amount of free abrin B chain and ACTI did not. The results suggests that abrin B chain of chimeric protein may act as a vector to carry ACTI into the tumor cells. ACTI into the tumor cells. ACTI in the chimeric protein potentiates its antitumor activity as well as its resistance to tryptic digestion.

Abrin↗

Multiple puncture tuberculin tests: relationship of false negative responses to variations in dried tuberculin coating.

Multiple puncture dried tuberculin tests compare favourably with the standard Mantoux test provided the tips of the metal prongs are thinly and uniformly coated with tuberculin. Unfortunately, surface tension, varying viscosity of the acacia solutions, and deeper dipping depths lead to increased quantities of tuberculin materials adhering to the metal prongs which results in thickening and retraction of the materials on the metal. Solutions of tuberculin in buffered phosphate produce thin and uniform coatings provided adequate cleaning of the metal--especially degreasing--is carried out. In the absence of this the coating layer may fragment. However, provided the distal 0.6-0.8 mm is covered, sufficient tuberculin will be deposited intradermally.

False Negative Reactions↗

Preliminary evaluation of some wild and cultivated plants for snail control in Machakos District, Kenya.

Fifty local medicinal, agricultural and wild growing deciduous plants, representing 49 species, 46 genera and 22 families, were screened as water extracts at 1:1000 concentration for molluscicidal activity against Biomphalaria pfeifferi in Machakos District, Kenya. Forty-seven of the 50 (94%) plants and 106 of the 134 (79%) plant materials (roots, stems, leaves, fruits, flowers and seeds) were molluscicidal. The leaves of Pappea capensis (Sapindaceae), Steganotaenia araliacea (Umbelliferae), Zornia setosa subsp. obvata (Papilionaceae) and Terminalia kilimandscharica (Combretaceae), the flower pods of Hyptis pectinata (Labiatae), the seeds of Acacia nilotica (Mimosaceae) and the fruits and roots of Solanum nigrum (Solanaceae) gave 100% kill. Another 15 species produced mortality rates between 53% and 87%. Plants were evaluated for possible use in local snail control programmes by considering their growing characteristics, habitat requirements, toxicity in non-target organisms, abundance in the study area and competing uses.

Animals↗

Cholesteryl octanoate breath test. Preliminary studies on a new noninvasive test of human pancreatic exocrine function.

A new breath test for noninvasive assessment of pancreatic exocrine function in humans was developed. The test is based on the hydrolysis of cholesteryl-[1-14C]octanoate by pancreatic carboxyl ester lipase (cholesterol esterase) with subsequent absorption and hepatic metabolism of the liberated octanoate to 14CO2. The rate at which 14CO2 appears in breath appeared to be proportional to the rate of hydrolysis. The substrate is administered as a gum acacia stabilized emulsion of vegetable oil (18 g) containing cholesteryl octanoate (2 g; 4.4 microCi) dispersed in a 500-ml isotonic meal. Tests were performed in 6 healthy volunteers and 11 patients with pancreatic disease with varying degrees of steatorrhea. In healthy subjects, 14CO2 output was rapid with peak output occurring at 60-90 min in all subjects; cumulative output in 4 h averaged 30%. Duplicate studies indicated that the time-course of 14CO2 recovery was reproducible. The pattern of 14CO2 output in patients with pancreatic disease varied widely. Patients without steatorrhea (fecal fat less than or equal to 7 g/day) or with mild steatorrhea (fecal fat 7-11 g/day) had normal or near normal patterns of 14CO2 output, whereas patients with moderate or severe steatorrhea (fecal fat greater than 11 g/day) expired 14CO2 at a rate one-third to one-tenth that of the healthy volunteers. Addition of pancreatic enzyme supplementation to the test meal increased 14CO2 output in 6 of 6 patients with moderate or severe steatorrhea, suggesting that the activity of pancreatic carboxyl ester lipase was rate limiting in these patients. In an additional study in a healthy volunteer, 14CO2 and 13CO2 were measured simultaneously in breath after ingestion of a test meal containing cholesteryl-[1-13C]octanoate and 14C-octanoate. 14CO2 was expired more rapidly than 13CO2, suggesting that hydrolysis of the substrate may also be rate limiting in healthy volunteers. These studies indicate that severe pancreatic exocrine dysfunction can be detected with a simple breath test in 60-90 min.

Adult↗

Antitumor lectin-trypsin inhibitor conjugate.

Concanavalin A (Con A) and trypsin inhibitor isolated from Acacia confusa were covalently linked with N-succinimidyl-3-(2-pyridyldithio)propionate. Con A-A. confusa trypsin inhibitor (ACTI) conjugate covalently bound (Con A-ACTI) retained about 42% of the trypsin inhibitory activity present in the native ACTI and had a higher hemagglutinating activity than did the native Con A. Con A-ACTI had a greater resistance to tryptic digestion than did the mixture of Con A and ACTI. The conjugate entered sarcoma 180 tumor cells, whereas the free ACTI did not. A single dose of the conjugate injected ip into noninbred N:NIH(S) white mice bearing sarcoma 180 had a remarkable effect of increasing the survival of tumor-bearing mice, while the mixture of an equivalent dose of free Con A and ACTI was not effective.

Animals↗

North American pollinosis due to insect-pollinated plants.

In warmer regions of North America many newly introduced plants are cultivated widely and others are becoming aggresive naturalized weeds. A large number are insect-pollinated and shed considerable quantities of airborne pollen. Levels of allergenicity based on skin test data, numbers of patients having immediate hypersensitivity and localities where airborne pollen grains have been identified are presented for each genus of entomophilous plants considered incitants of pollinosis. Among the most relevant are Acacia, Brassica, Citrus, Ligustrum, Olea and Schinus.

Air Pollution↗

Effects of acidic phospholipids, nucleotides, and heparin on the activity of lipase from rat liver lysosomes.

Purification and characterization of endogenous lipid factors that stimulate rat liver lysosomal lipase has led to the identification of cardiolipin, phosphatidylserine, and phosphatidic acid as stimulators of this activity. Bovine heart cardiolipin (half-maximal stimulation at 1.5 x 10(-4) m) and bovine brain phosphatidylserine (half-maximal stimulation at 9.5 x 10(-4) m) were the most potent of the phospholipids from other sources tested. The major rate-enhancing effect of phosphatidylserine is expressed as a 35-fold increase in the apparent V(max) of the enzyme. The effect is produced by acid phospholipids specifically, since in no case was there greater than a twofold stimulation by synthetic detergents, zwitterionic phospholipids, taurocholic acid, or gum acacia. The observed degree of stimulation depends upon the detergent used to disperse tripalmitin substrate and the relative concentrations of factor and detergent in reaction mixtures. The concentration of phosphatidylserine to produce half-maximal stimulation is directly dependent upon the Triton X-100 concentration, but the effects of this detergent on cardiolipin stimulation are more complex. Enzyme activity is inhibited 50% by 1 mm nucleoside triphosphate and 2.5 mm ADP, 80% by 1 mm PP(i), 100% by 20 U/ml heparin and 0.25 mg/ml chondroitin sulfate, and 80% by 10 mm sulfate ion. Inhibition is partially prevented by phosphatidylserine.

Animals↗

Functional closure of the ductus venosus during early postnatal life in the dog.

Radiographic contrast studies of the ductus venosus performed in 12 pups between the 60th day of intrauterine life and the 5th day after birth indicated that blood flow through the ductus venosus had ceased between the 2nd and 3rd days of extrauterine life. The time of functional closure was not identical with the time of morphologic closure. The functional closure of the ductus venosus was a gradual process and was related to an increase in liver perfusion through the portal vein branches. Both in specimens injected with a radiopaque gum acacia mass and in a corrosion cast of umbilical vein and portal system of the liver, persistence of the lumen of the ductus venosus up to the time of its functional closure was confirmed. The rate of closure in the dog was discussed in relation to that in man and the horse, pig, goat, and sheep.

Animals↗

[Ecology of opportunistic fungi].

As most of the pathogenic fungi, opportunistic fungi have a saprophytic life in the soil. The knowledge of their life in natural conditions may allow to avoid their proliferation in the vicinity of man. Examples of ecology were taken among Aspergilli and mycetoma-inducing fungi. The ecology of these fungi was studied in Senegal-Mauritania where mycetoma is fairly frequent and well studied. Cultures of L. senegalensis and L. tompkinsii were very often isolated from dry thorns of acacias or other thorn trees. M. mycetomi, the most frequent mycetoma-inducing fungus, was very difficult to culture from wood or soil specimens. A special selective sulphide medium had to be used. Some strains of M. mycetomi were isolated from specimens taken off the surface of termitaria.

Aspergillus↗

In vivo mutagenic effect of methyldopa. 1. Dominant lethal test in male mice.

The dominant lethal test was used to evaluate the mutagenic potential of methyldopa, an antihypertensive drug, in male mice. In the series treated, animals were exposed to 480 or 960 mg/kg of the drug as a suspension in 1% gum acacia via the oral route. A separate group of males served as control. Following treatment each male of the control, as as well as the treated series, was mated to two untreated virgin females each week for a period of 6 consecutive weeks. All mated females were sacrificed on the 10th day of separation and their ovaries and uterine contents were examined. Corpora lutea, implantations and resorptions were recorded. The drug treatment did not impair the mating capacity and fertility. Pre- and post-implantation losses were assessed. Higher incidences of post-implantation losses and abortion, and lower incidences of total implantations particularly at higher dose levels clearly reveal a dominant lethal effect of the drug.

Abortion, Spontaneous↗

Dissolution of meprobamate from various tablet formulations.

The effect of some formulation variables on the release of meprobamate from compressed tablets has been investigated. Possible interaction among the various variables was also studied. As a diluent, lactose produced a better dissolution rate than did starch. Tablets made with starch paste as the binder produced a faster release of meprobamate than those made with gelatin solution. Acacia proved to be the best disintegrating agent when compared to microcrystalline cellulose or starch, especially when the formulation already contained starch as the diluent. Under these conditions, microcrystalline cellulose was a better disintegrating agent than starch. Magnesium stearate or talc when used as a lubricant did not reduce the rate of release of meprobamate. Formulations containing a large proportion of starch (about 50%) did not produce a fast release of meprobamate.

Excipients↗

Stability of aqueous suspensions of disulfiram.

The stability of disulfiram in aqueous suspension is reported. Aqueous suspensions of disulfiram were prepared from bulk powder and from disulfiram tablets. Acacia and sodium benzoate were present in the suspension, the final concentration of which was 25 mg/ml disulfiram. Suspensions were stored in amber bottles under fluorescent light at 24 degrees C for 178 days (tablets) and 295 days (bulk powder). Samples were taken at various intervals during storage and assayed by high-pressure liquid chromatography (HPLC) and a modified NF method. Both types of suspension were stable. Potency remained constant, and no new peaks appeared in the chromatograph. Physical integrity of the suspensions was maintained. The suspension made from tablets contained less foam and air than the one made from bulk powder; both types were easily dispersible. A degradation product of disulfiram, diethyldithiocarbamic acid, did not interfere with the assay. The HPLC assay method was more reproducible than the modified NF method. Aqueous suspensions of disulfiram are stable at room temperature for the indicated time periods, and the HPLC assay method for disulfiram is reproducible and accurate.

Chromatography, High Pressure Liquid↗

Effect of guar gum on the dissolution rate of ephedrine hydrochloride and sulphadimidine tablets.

The effect of guar gum as a binder was studied in comparison with other commonly used binders namely: gun acacia, Carbopol 934, sodium carboxymethyl cellulose and Explotab on the disintegration time and the dissolution rate of tablets containing ephedrine hydrochloride and sulphadimidine. The results revealed that the solubility of the drug as well as the concentration and the type of binder affect both the disintegration time and the dissolution rate of the tablet.

Ephedrine↗

[Reproductive and developmental toxicity studies of T-3761 in rats].

We carried out reproductive and developmental toxicity studies (i.e. fertility study, teratological study, and perinatal and postnatal study) of T-3761, a new quinolone derivative, in S.D. rats. T-3761 was administered orally at the dose of 60, 300 and 1,500 mg/kg/day as suspension in 5% acacia solution. 1. Fertility study T-3761 was administered to male rats for 9 weeks prior to mating and to female rats for 2 weeks prior to mating and until day 7 of gestation. In parent rats, soft stools, slight depression of body weight gain and increase in water intake were observed at the dose of 1,500 mg/kg. Cecum weight was increased at the dose of 300 mg/kg and more in male and at the dose of 1,500 mg/kg in female. No effects on reproductive performance were discernible in the T-3761 treated groups. In fetuses, external, skeletal and visceral examinations revealed no teratological abnormalities. Slightly retarded ossification, however, was observed at the dose of 1,500 mg/kg. From these findings, the no-effect dose of T-3761 in fertility study was considered to be 300 mg/kg/day for parent rats and fetuses. 2. Teratological study T-3761 was administered from day 7 to day 17 of gestation. In dams, soft stools, transient decrease in food intake, increase in water intake, depression of body weight gain and increase in cecum weight were observed at the dose of 1,500 mg/kg. In fetuses, slight increase in incidence of ventricular septal defect and slightly retarded ossification were observed at the dose of 1,500 mg/kg. In the postnatal examination, there were no effects in the T-3761 treated groups. From these findings, the no-effect dose of T-3761 in teratological study was considered to be 300 mg/kg/day for dams and next generations. 3. Perinatal and postnatal study T-3761 was administered from day 17 of gestation to day 21 of lactation. In dams, cecum weight was increased at the dose of 300 mg/kg and more. And soft stools, transient decrease in food intake, increase in water intake, transient depression of body weight gain and slight extension of gestation period were observed at the dose of 1,500 mg/kg. In the postnatal examination, there were no effects in the T-3761 treated groups. From these findings, the no-effect dose of T-3761 in perinatal and postnatal study was considered to be 300 mg/kg/day for dams and more than 1,500 mg/kg/day for next generations.

Animals↗

Lipase production by Aspergillus niger under various growth conditions using solid state fermentation.

Ricinus seed litters were chosen as a cheap carbon source for lipase production by A. niger under solid state fermentation (SSF). Maximum lipase production was achieved upon using an enriched (potassium citrate and casein) waste at pH 7.8 and 30 degrees C for 8 days incubation. Nitrogen sources as NH4Cl, NH4NO3, (NH4)2SO4, urea and amino acids repressed the lipolytic activity. The chloride salts of Ba2+, Co2+, Cu2+, Fe3+, Hg2+, K+, Mg2+, Mn2+, Na+ and Sn2+ inhibited, while Zn+2 did not affect lipase production. Compounds containing hydrolyzable ester group, such as Tween(s), were found to inhibit lipase activity. When the effect of different additives such as EDTA, gum acacia, span(s), mineral and vitamins, were studied, it was found that they all exhibit decreased lipase production by the tested fungus.

Ammonium Chloride↗

[Intravascular persistence, tissue storage and excretion of hydroxyethyl starch (HAS)].

Hydroxyethyl starch is a derivative of amylopectin, the branched glycogen-like alpha-1,4-glucose polymer, the amylase hydrolysis of which is retarded by hydroxyethylation. If 70 to 90 per cent of the glucose polymer units contain hydroxyethyl groups, the intravascular persistence and urinary excretion of hydroxyethyl starch of a molecular weight of 435,000 is similar to that of Dextran 70. Hydroxyethyl starch and Dextran 70 are stored briefly in reticuloendothelial and hepatic cells, and cause swelling and vacuolation of renal tubules with little alteration of renal function. Elimination of hydroxyethyl starch from sites of tissue storage is much faster than elimination of the non-metabolized polymers acacia and polyvinylpyrrolidone. The distribution and excretion kinetics of hydroxyethyl starch are thus appropriate for a plasma substitute.

Animals↗