Toxicological assessment of Capparis spinosa L. seed’s oil

Introduction. Herbal medicines are unique therapeutic agents that represent multicomponent complexes of biologically active substances. They have low toxicity, a wide spectrum of therapeutic action with a minimum of side effects and a relatively low cost. Capparis spinosa L. has been widely used in traditional medicine for the treatment of various diseases and health conditions. Material and methods. An assessment of the toxicometric parameters of Capparis spinosa L. seed’s oil was done by a single oral and dermal exposure, the average lethal doses have been calculated for both routes, sensitivity by sex has been studied. The local irritant, skin resorptive, effect on the mucous membranes of the eyes of experimental animals was investigated. Sensitizing activity was studied according to the complex sensitization scheme. Processing of the results was carried out by the method of variation statistics. Standard errors and other indicators were calculated using the Litchfield-Wilcoxon probabilistic analysis method modified by Prozorovsky. The difference in mean values was estimated using Student’s t-test. Results. The acute toxicity of the oil was not expressed, death of animals was not observed. Average lethal dose for a single oral exposure was above 7000 mg/kg and dermal more than 3000 mg/kg. Sensitivity by sex in an acute experiment has not been established. The oil had a mild irritating effect on the mucous membranes of the eyes. It did not show skin-irritating, resorptive-toxic and sensitizing effects. Conclusion. Capparis spinosa L seed’s oil belongs to the 4th hazard class (low hazard) according to the hygienic classification and safety requirements of substances.

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TOXICOLOGICAL EVALUATION OF INDOMETHACIN AS A RISK FACTOR FOR WORKERS’ HEALTH

Hygiene and Sanitation ◽

10.18821/0016-9900-2019-98-5-503-508 ◽

2019 ◽

Vol 98 (5) ◽

pp. 503-508

Author(s):

N. A. Martynova ◽

Larisa G. Gorokhova ◽

V. A. Shtaiger

Keyword(s):

Blood Serum ◽

Guinea Pigs ◽

Muscle Relaxation ◽

Lethal Dose ◽

The Body ◽

Male Rats ◽

Hazard Class ◽

Toxicological Evaluation ◽

Mucous Membranes ◽

Ulcerogenic Effect

Introduction. The toxicity of indomethacin was studied for its hygienic regulation. Material and methods. The toxic properties of indomethacin in the experiments on out-bred and linear mice, rats, Guinea pigs and rabbits contained in standard vivarium conditions and quarantined have been studied. In the experiments, various modes (single, repeated, chronic) and ways of exposure (intragastric, inhalation, epicutaneous) were modeled. The average lethal dose (LD50) of Indomethacin and the threshold of a single acute action (Limac) were determined; irritant effect on the skin and mucous membranes, cumulative and allergenic activity were revealed. In subacute and chronic intake to the body, the main target organs were determined on the based of the results of biochemical and hematological studies. Results. DL50 for male rats, females and male mice, when introduced into the stomach, were have been established to be 20, 15 and 25.6 mg/kg respectively. It refers to the substances of hazard class 2. DL50 in the intraperitoneal introduction for the rats accounted for 13.8 mg/kg, for Guinea pigs - 500 mg/kg. The clinical picture of acute poisoning in mice and rats was characterized by low mobility, decreasing breathing, ataxia, muscle relaxation, anorexia, diarrhea, ulceration with the perforation of the intestines, and the death on the 2-4th days after the poisoning. In the experiments on Guinea pigs, the ulcerogenic effect was not detected. Local irritant effect on the skin and mucous membranes of the eyes was not revealed. It has a marked skin-resorptive action causing ulcerogenic effect and the death of the animals after 6 applications. The introduction of verospiron to the rats in a dose of 25 mg/kg simultaneously with the application of indomethacin ointment on the skin prevented the ulcer development in the gastrointestinal tract and the death of the animals. No sensitizing effect was detected. It has an average cumulative ability: the cumulation coefficient amounted to 2.6. In a subacute experiment, there was a decrease in the body temperature and summation-threshold index, an increase in the vertical motor activity and a threshold of pain sensitivity. During the study of blood serum an increase in AcAt activity, a rise of chlorides in the blood serum and their decrease in the urine, and an increase in the number of erythrocytes and hemoglobin in peripheral blood were revealed. In the pathomorphological study, there was an increase in the coefficients of liver mass and ulceration of the stomach and intestines. The threshold of acute inhalation action accounted for 0.52 mg/m3 (by the reduction of the summation-threshold index and the content of sodium and chlorides in the urine). Conclusion. The maximum permissible concentration of indomethacin in the air of the working area was of 0.05 mg/m3 with the mark “special protection of the skin and eyes”, hazard class 1, aerosol.

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TOXICOLOGICAL ASSESSMENT OF BIO PREPARATION OILDESTRUCTOR «LENOIL»® – NORD, SHP

Токсикологический вестник ◽

10.36946/0869-7922-2017-3-58-60 ◽

2017 ◽

pp. 58-60

Author(s):

T. Yu. Korshunova ◽

O. N. Loginov

Keyword(s):

Lethal Dose ◽

Petroleum Products ◽

Hazardous Substances ◽

Delayed Type Hypersensitivity ◽

Contaminated Sites ◽

Biological Product ◽

Hazard Class ◽

Polluted Soils ◽

Toxicological Assessment ◽

Repeated Applications

Based on experimental results, toxicological assessment of the biological product oil-destructor «Lenoil»® – NORD, SHP is reported.. The biological product is intended for cleaning of oil-polluted soils and water objects at low positive temperatures. It was found out that the median lethal dose (LD50) at intragastric intake amounts to more than 5000 mg/kg, therefore the biological product refers to hazard class 4 (low hazardous substances). The biological product does not cause signs of irritation of respiratory tracts, but is able to induce slight irritation of eye mucous membranes and skin ( repeated applications).The biological product has no sensitizing action when reproducing a delayed-type hypersensitivity reaction. The biological product oil-destructor “Lenoil»® – NORD, SHP can be used for its intended purpose, i.e. to accelerate the destruction of oil and petroleum products during the remediation of oil-contaminated sites. At work the personnel must be provided with special clothing and personal protective equipment and observe hygiene and sanitary norms.

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Acute toxicity of an insecticidal little containing ivermectin and fipronil for white mice

Veterinaria Kubani ◽

10.33861/2071-8020-2020-6-31-32 ◽

2020 ◽

pp. 31-32

Author(s):

Mikhail A. Levchenko ◽

◽

Natalia A. Sennikova ◽

Keyword(s):

Acute Toxicity ◽

Lethal Dose ◽

Live Weight ◽

Acute Oral Toxicity ◽

Oral Toxicity ◽

Toxicological Assessment ◽

Russian Research Institute ◽

Veterinary Entomology ◽

Russian Research

Toxicological assessment is a mandatory research step in the development of new insecticidal drugs. At the All-Russian Research Institute of Veterinary Entomology and Arachnology, a prototype of the insecticidal bait Mukhnet IF was obtained with an active ingredient content of 0.06% ivermectin and 0.015% fipronil, which showed a highly effective effect against houseflies. This work presents the results of the study of acute oral toxicity of the above agent. For this, male white mice with a live weight of 16-26 g were selected. They were kept on a starvation diet for one day in individual houses with water. The drug was given in mg/kg body weight the next day. A total of 33 doses have been tested, ranging from 100 mg/kg to 40,000 mg/kg. The animals were observed for 14 days. According to the research results, it was revealed that at doses up to 20,000 mg/kg there were no signs of intoxication, but when tested at 25,000 mg/kg in some mice, these signs were noted, and at 30,000, 35,000 and 40,000 mg/kg deaths were recorded 20±10, 45±30 and 60±20%, respectively. It was not possible to test the drug over the last above dose due to incomplete eaten by mice. According to the degree of danger for warm-blooded animals, the drug belongs to the 4th class of low-hazard drugs (average lethal dose of 5000 mg/kg or more) in accordance with the classification of GOST 12.1.007-76. When analyzing the literature data on the toxicological characteristics of preparations containing ivermectin and chlorfenapyr, it was revealed that the insecticidal agent in its acute toxicity for warm-blooded animals is comparable to known analogues.

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DECONTAMINATION OF VETERINARY SURVEILLANCE OBJECTS BY NEW GENERATION MEDICINE

Vestnik of the Russian agricultural science ◽

10.30850/vrsn/2019/2/64-67 ◽

1970 ◽

pp. 64-67

Author(s):

М. S. Saypullaev ◽

А. U. Koychuev ◽

Т. B. Mirzoeva

Keyword(s):

Staphylococcus Aureus ◽

Inhalation Exposure ◽

Gram Negative Bacteria ◽

Hazard Class ◽

E Coli ◽

Highly Efficient ◽

Mucous Membranes ◽

Environmentally Safe ◽

New Generation ◽

And Staphylococcus Aureus

The successful conduct of disinfection measures largely depends on the availability of veterinary practice a highly efficient, environmentally safe disinfectants. In this regard, finding new highly efficient disinfectant remains relevant. Studies found that the "Polied" (OOO "Razvitie XXI Vek, Russia) can be attributed to the highly efficient and environmentally friendly means. Solutions "Polied" have a high disinfectant activity against smooth and rough surfaces in the laboratory against gram-positive, gram-negative bacteria, mycobacteria and spores of microorganisms. Studies have established that solutions should be "Polied" obezzarajivatmi E. coli (EA 1257) concentrations of 0.1% on smooth surfaces and Staphylococcus aureus concentration of 0.05% in 1 hour from the calculation of 0.25-0.3 litres/m2. Disinfection of rough test surfaces against Escherichia coli and Staphylococcus aureus occurred after treatment with 0,3% solution of 3-hour exposure, at a rate of 0.5 l/m2. It was also found that 1.0% solution "Polied" fully obezzarazhivatel test the surface of mycobacteria (PCs-5) and at double the 0.6% concentration for 24 hours. Disinfection of rough test surfaces contaminated with spores of B. cereus (PCs 96) was achieved with a 4.0% solution at twice the irrigation rate of 0.5 l/m2 at an exposure of 24 hours. Toxicity solutions of the drug "Polied" refer to "moderate" threat (hazard class 3) and low-hazard substances (4 hazard class) when applied to the skin, mucous membranes of the eyes, and inhalation exposure on the respiratory system.

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Features of Bioaccumulation and Toxic Effects of Copper (II) Oxide Nanoparticles Under Repeated Oral Exposure in Rats

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210728163901 ◽

2021 ◽

Vol 09 ◽

Author(s):

Mark Sergeevich Stepankov ◽

Marina Aleksandrovna Zemlyanova ◽

Nina Vladimirovna Zaitseva ◽

Anna Mikhailovna Ignatova ◽

Alena Evgenievna Nikolaeva

Keyword(s):

Surface Area ◽

Pore Volume ◽

Mesangial Cells ◽

Lethal Dose ◽

Toxic Effects ◽

Oral Exposure ◽

Oxide Nanoparticles ◽

Brown Pigment ◽

Cuo Nps ◽

Hematological Analysis

Background: Currently, the range of copper (II) oxide nanoparticles’ (CuO NPs) applications is expanding and the global production of CuO NPs is increasing. In this regard, the risk of exposure of the population to this nanomaterial increases. Objective: The aim of the study is to investigate the patterns of bioaccumulation and toxic effects of CuO NPs after multiple oral exposures. Methods: The particle size was determined by scanning electron microscopy and dynamic laser light scattering. Specific surface area was measured by the method of Brunauer, Emmett, Teller. Total pore volume - by the method of Barrett, Joyner, Khalenda. Twenty-four hours after the final exposure, blood samples were taken for biochemical and hematological analysis, and internal organs were taken to determine their mass, copper concentration and histological analysis. The study was carried out in comparison with copper (II) oxide microparticles (CuO MPs). Results: In terms of size, surface area, and pore volume, the studied copper (II) oxide sample is a nanomaterial. The median lethal dose of CuO NPs was 13187.5 mg/kg of body weight. Bioaccumulation occurs in the stomach, blood, intestines, liver, lungs, kidneys and brain. Pathomorphological changes in the liver are manifested in the form of necrosis, degeneration, hepatitis; kidney - proliferation of mesangial cells, dystrophy; stomach - gastritis; small intestine - hyperplasia, enteritis; large intestine - colitis; lungs - hyperplasia, abscess, pneumonia, bronchitis, vasculitis. Clumps of brown pigment were detected in the kidneys, stomach and lungs. The mass of the stomach and intestines increased, the mass of the liver, kidneys and lungs decreased. Pathomorphological changes in organs are likely to cause an increase in the levels of activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, lactate dehydrogenase, amylase, malondialdehyde concentration and a decrease in plasma antioxidant activity. The proportion of segmented neutrophils, the number of leukocytes are raised, the proportion of lymphocytes is reduced. Conclusion: The degree of bioaccumulation and toxicity of CuO NPs are more expressed in relation to CuO MPs.

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COMPOSITION OF BIOLOGICALLY ACTIVE SUBSTANCES OF THE HORSE CHESTNUT (AECULUS HIPPOCASTANUM L.)

ÈKOBIOTEH ◽

10.31163/2618-964x-2021-4-1-33-39 ◽

2021 ◽

Vol 4 (1) ◽

pp. 33-39

Author(s):

V.P. Kurchenko ◽

◽

N.V. Sushinskaya ◽

K.I. Maiorava ◽

E.I. Tarun ◽

...

Keyword(s):

Fatty Acids ◽

Antioxidant Activity ◽

Phenolic Compounds ◽

Biologically Active Substances ◽

Biologically Active ◽

Horse Chestnut ◽

Hazard Class ◽

Active Substances

The study of the composition of biologically active substances, alcoholic extracts from flowers of Aeculus hippocastanum L. According to the results of HPLC-MS and GC-MS analyzes, the extract contains the main amounts of phenolic compounds: quercetin, epicatechin, kaempferol. In addition, the extract contains fatty acids and their esters, alcohols, 3-deoxy-d-manno lactone, 1,2,3,5-cyclohexantethrol, α-methyl-mannofuranoside, γ sitosterol. Antioxidant activity of an extract from flowers of A. hippocastanum is associated with the peculiarities of the compositionof biologically active substances. The toxological-hygienic assessment of flowers of this species in acute and subacute experiments showed that it belongs to the 4th hazard class (low hazard).

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Acute toxicity of nanosized beet pectin

Kazan medical journal ◽

10.17750/kmj2015-208 ◽

2015 ◽

Vol 96 (2) ◽

pp. 208-213

Author(s):

N Yu Alimzhanov ◽

I Sh Chakeev ◽

Sh Zh Zhorobekova ◽

I O Kudaybergenova ◽

B N Lepshin

Keyword(s):

Acute Toxicity ◽

Structural Changes ◽

Least Squares Method ◽

Histological Study ◽

Lethal Dose ◽

Study Drug ◽

Biological Properties ◽

Probit Analysis ◽

Pectin Substance ◽

Hazard Class

Aim. To determine the acute toxicity and hazard class of nanosized low-esterified beet pectin.Methods. To study the acute toxicity of substances, Kerber’s method was used. Probit analysis for different values of lethal dose calculated by least squares method, as well as morphologic studies, statistical analysis (non-parametric methods - Wilcoxon-Mann-Whitney test) were used. Pectin toxicity was studies on 40 mature Wistar rats of both gender and body weight of 160-230 g.Results. Enteral administration of 12 000 mg/kg of pectin did not affect the general condition and did not lead to lethal outcome. The following values of lethal doses were calculated using probit analysis: LD16=34 990.6542056074≈35 g/kg, LD50=74 242.9906542057≈74 g/kg, LD84=113 495.327102804≈113 g/kg, LD100=133 121.495327103≈133 g/kg. Histological study of rat organ tissues that received 12 000 mg/kg of pectin showed no structural changes in tissues of examined organs. Study drug - nanosized low molecular weight pectin, might be referred to hazard class IV (low hazard substances) according to GOST 12.1.007-76. and classification K.K. Sidorov Pectin substance may be considered as practically nontoxic drug (LD50 >10,000 mg/kg), which corresponds to Class V compounds according to Hodge and Sterner classification and classification by K.K. Sidorov.Conclusion. The results indicate complete safety of nanosized forms of pectin, which opens up prospects for further studies of the biological properties of this substance.

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ANALYSIS OF RELATIONSHIPS BETWEEN THE CAPACITY OF CHEMICALS TO THE CUMULATION AND THE STRUCTURE OF THEIR MOLECULES

Hygiene and Sanitation ◽

10.18821/0016-9900-2017-96-10-970-975 ◽

2019 ◽

Vol 96 (10) ◽

pp. 970-974

Author(s):

Nina V. Kharchevnikova ◽

Z. I. Zholdakova ◽

V. I. Zhurko ◽

D. Yu. Fedortsova ◽

V. G. Blinova

Keyword(s):

Lethal Dose ◽

Practical Interest ◽

Training Dataset ◽

Jsm Method ◽

Hazard Class ◽

Structural Class ◽

Chemical Hazard ◽

Leave One Out ◽

The Relationship

The relationships between the capacity of chemicals to cumulate a toxic effect (functional cumulation) and the structure of their molecules were investigated. In the process of substantiation of safe levels (MAC) of substances in water this capacity is characterized by the cumulation hazard class (later in the text - hazard class). This class is stated to be depend on the value of the relationship between the mean lethal dose of the acute experiment and the threshold dose of the chronic experiment. The experimental study of a huge amount of new chemicals in the chronic experiments is a very difficult task, thus the study of the possibility to predict the hazard class of a chemical is of great scientific and practical interest. By using a logical combinatorial method JSM, named in honor of an English logic J.S. Mill, the structural groups in molecules, determining the appurtenance of these chemicals to a hazard class were identified and the possibility of the prediction of the hazard class of a chemical belonging to a definite structural array, containing such structural group were investigated. The training dataset (583 compounds) was automatically derived from the database WATERTOX, containing the data on acute and chronic toxicity for about 2000 substances. The results suggest the JSM method to be limitedly applicable for the determination of a hazard class of an untested chemical using this heterogeneous training dataset because we were unable to unambiguously derive the list of chemicals belonging to the class of moderately hazard substances. The chemical in some cases was predicted to belong to one or other of the neighboring classes. However taking in mind this uncertainty, the accuracy of the method evaluated, when using the “leave-one-out” method was 78%. Nevertheless the JSM method enables us to find structural subgroups “responsible” for the functional cumulation. The relation of the hazard class of a chemical belonging to a definite structural class with its structure and the possibility of the prediction of an untested chemical hazard class are demonstrated. The prognosis of the hazard classes for chemicals belonging to several structural sets including the anthraquinone derivatives, phthalimides, perfluorated aliphatic compounds, chlorosubstituted phenols, phenylureas is performed.

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RECENTES AVANÇOS NA FUNCIONALIZAÇÃO SELETIVA DE QUINOLINAS

Química Nova ◽

10.21577/0100-4042.20170701 ◽

2021 ◽

Author(s):

Dartagnan Ferreira ◽

Valter Murie ◽

Thiago Santos ◽

Paulo Vieira ◽

Giuliano Clososki

Keyword(s):

Wide Spectrum ◽

Structural Diversity ◽

Biological Properties ◽

Biologically Active ◽

Chemical Transformations ◽

Heterocyclic Molecules ◽

Point Of Interest ◽

Selective Functionalization ◽

Biological Interest ◽

Approved Drugs

RECENT ADVANCES IN SELECTIVE FUNCTIONALIZATION OF QUINOLINES. Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.

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ANTI-MYCOBACTERIAL ACTIVITY OF CAPPARIS SPINOSA L. EXTRACT AGAINST CLINICAL ISOLATES OF MYCOBACTERIUM TUBERCULOSIS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i8.17629 ◽

2017 ◽

Vol 10 (8) ◽

pp. 181 ◽

Cited By ~ 1

Author(s):

Azadeh Ehsanifar ◽

Nadia Kazemipoor ◽

Bahman Fouladi

Keyword(s):

Methanol Extract ◽

Lethal Dose ◽

Reference Sample ◽

Inhibitory Effect ◽

Maximum Efficiency ◽

Clinical Samples ◽

Health Issues ◽

Capparis Spinosa ◽

The Impact ◽

Microbial Effects

Objective: Tuberculosis (TB) has been one of the biggest global health issues for decades. Emerging forms of the disease; however, after many years since the discovery of the last effective treatment for this disease, the emerging forms of it have made scientists worried about the disease. Most herbs have anti-microbial properties; however, there was no research on the impact of fruit Capparis spinosa on TB. This study was conducted to evaluate the anti-microbial effects of bacterial C. spinosa.Methods: In this study, methanolic extract at maximum efficiency to maintain existing substances was prepared by the freeze dryer device and to determine the minimum inhibitory concentration of bacteria’s growth. The proportional method was used on 7 clinical samples and one reference sample H37RV with its six concentrations (80-50-25-10-1-0/2 mg/ml). In addition, to determine the effects of plant extracts in combination with rifampin, all samples were tested by the supplement combination or cover combination of these two materials. All tests were performed twice. The methanol extract of the plant at the concentration of 25 mg/mL in all samples has inhibitory effect on the growth.Results: In study, clinical samples with a lethal dose of RIFAMPIN, it was shown that none of the samples have drug resistance. The results have revealed that the methanol extract has an anti-mycobacterial effect.Conclusion: The results of this study indicate that Capparis spinosa possess considerable anti-mycobacterial properties in the laboratory. These results can be used as a background for further future studies on this species.

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