Hasil untuk "Toxicology. Poisons"

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DOAJ Open Access 2025
Evaluation of hematological parameters and alterations in burned patients

Afsona Parveen, Parthib Dey, Prithviraj Karak

Background: Burn injuries, categorized into four degrees, are common in-home accidents caused by heat, cold, electricity, chemicals, radiation, and friction. This study aims to determine the ideal parameters for burn patients and regulate their hematological parameters to ensure appropriate care and overall well-being. Materials and Methods: From 148 victims’ examinations only 40 patient case histories have been examined. Investigations are conducted into determination of various hematological parameters. Statistic investigation of those parameters represented by bar diagrams to compute t-values and p values. Results: The study involved 40 adult burn patients, with a mean age of 31.05±12.05. Women were more affected than men, with thermal burn being the most common. The mean TBSA was 22.0±13%, with a higher rate of 2nd degree burn. On Statistical analysis of hematological parameters showed negative “t” statistic values, with hemoglobin showing the highest value t-value (2.20). Age-based comparisons showed a decrease in Hb and RBC, with platelets, WBC, neutrophils, and ESR significantly reduced. Positive correlations were found for PCV (0.183, p=0.217), Hb (0.299, p<0.05), RBC (0.297, p<0.05), lymphocytes (0.213, p=0.145), monocytes (0.063, p=0.687), and eosinophils (0.190, p=0.198). Conclusion: Hematological characteristics, bleeding profiles, and renal and hepatic dysfunction are all brought on by burn injuries. For medical teams to forecast prognosis and treatment response, biochemical marker estimation is essential. Burn patients frequently have decreased platelet counts, higher TLC, and lower hemoglobin levels. For better results, liver, kidney, serum electrolyte, and CBC monitoring are crucial.

Therapeutics. Pharmacology, Toxicology. Poisons
DOAJ Open Access 2025
Serum TLR2 and S100B in Substance Abuse: A Clinical Perspective

Babak Mostafazadeh, Mahtab Ramezani, Leila Simani et al.

Background: Substance abuse leads to blood-brain barrier dysfunction and activation of neuro-inflammatory pathways. However, the contribution of serum levels of Toll-like receptor 2 (TLR-2) and S100 calcium-binding protein B (S100B) to neuropsychological outcomes has not been clearly established. This study aims to explore the relationship between TLR-2 and S100B serum concentrations in individuals with substance abuse and their potential influence on neuropsychological results, specifically regarding the functioning of the frontal lobe. Methods: This study involved 28 individuals who were diagnosed with substance abuse at Loghman Hakim Hospital’s Toxicology Unit in 2022. Serum TLR-2 concentration and S100B levels, as neuroinflammatory markers, and the frontal assessment battery (FAB), as executive function markers, were measured. Results: Substance abuse patients exhibited elevated levels of both TLR-2 and S100B. In drug addicts, a strong positive relationship was detected between serum levels of TLR-2 and S100B (r=0.742, P=0.0021) levels. Nevertheless, no significant relationship was found between FAB scores and serum concentrations of S100B and TLR-2. Conclusion: This study reveals increased serum TLR-2 and S100B levels in individuals with substance abuse. However, these elevated levels did not appear to be associated with risk factors related to substance abuse or frontal lobe function.

Medicine (General), Toxicology. Poisons
DOAJ Open Access 2025
Pollution by antimicrobials and antibiotic resistance genes in East Africa: Occurrence, sources, and potential environmental implications

Miraji Hossein, Asha Shabani Ripanda

The escalating burden of antimicrobial pollution in East Africa poses severe threats to public health, environmental integrity, and economic stability. Environmental compartments such as soil and water serve as reservoirs for these pollutants such as antimicrobials and antibiotic resistance genes, creating selective pressure that accelerates the emergence of antimicrobial resistance (AMR). These dynamic fosters the proliferation of multidrug-resistant pathogens, or ''superbugs,'' complicating infection management and amplifying health risks in a region already challenged by inadequate healthcare and sanitation infrastructure. Furthermore, pollution by antimicrobials and antibiotic resistance genes critically disrupts ecological processes, such as nutrient cycling and organic matter degradation, diminishing soil fertility, water quality, and agricultural productivity, thereby threatening food security and overall ecological health. Current surveillance efforts, including the Global Antimicrobial Resistance and Use Surveillance System (GLASS) and the East Africa Public Health Laboratory Networking Project (EAPHLNP), have made strides in tracking AMR trends and guiding policy decisions. However, these efforts remain insufficient to address the growing crisis. This study highlights the urgent need for integrated strategies, including stringent antibiotic usage regulations, advanced wastewater treatment technologies, and comprehensive environmental surveillance. Therefore, there is a need to address the intersections of health, agriculture, and environment, to mitigate AMR and its far-reaching consequences to ensure public health safety and sustainability.

Toxicology. Poisons
DOAJ Open Access 2025
Retrospective analysis of clinical laboratory parameters in Han Wistar rat controls

Rupert Kellner, Alexander Amberg, Frank Bringezu et al.

IntroductionDespite the availability of control animal data sets from toxicological studies, the influence of external factors, such as age of animals, test site and study conditions, on clinical laboratory parameters in rats is only sparsely characterized.ObjectiveIn order to analyze the covariates of study design, we leveraged the largest available curated collection of control animal data from toxicological studies, sourced from five European pharmaceutical companies. We investigated the influence of external factors on commonly measured clinical chemistry, enzyme activity and hematology parameters in Han Wistar rats of both sexes.Materials and Methods457,605 control group clinical laboratory data points from 1,288 legacy toxicity studies on Han Wistar rats were curated and analyzed by ANOVA and partial eta squared to discern their effect sizes.ResultsOur analysis revealed that bodyweight, used as a surrogate for age in rats, significantly influences some parameters, while demonstrating stability in others. Descriptive statistics and tolerance intervals are provided for 20-g body weight class intervals. The effect size of these body weight classes, as calculated by partial eta squared, is large for parameters that change during development (e.g., phosphate or alkaline phosphatase) but was negligible for more stable parameters (e.g., calcium and alanine aminotransferase). For parameters which are less dependent on body weight class, the relative influence of other factors, namely, the company providing the study data, as well as study year is more prominent. These factors likely act as summary factors for various influences such as changes in analytical protocols, diet or housing conditions.ConclusionThis analysis provides a comprehensive overview of parameter variability and offers critical guidance for parameters which need to be controlled when utilizing historical control data to establish reference intervals or generate virtual control groups.

Toxicology. Poisons
DOAJ Open Access 2024
Bioaccumulation of Organic and Inorganic Pollutants in Fish from Thermaikos Gulf: Preliminary Human Health Risk Assessment Assisted by a Computational Approach

Konstantinos M. Kasiotis, Effrosyni Zafeiraki, Electra Manea-Karga et al.

The monitoring of contaminants in fish species is pivotal for fishes’ health and reproduction, as well as for human health. In the specific work, three major categories of contaminants, pesticides, pharmaceuticals, and macro and trace elements, were investigated in two major fish species, <i>Dicentrarchus labrax</i> and <i>Solea solea</i>, collected from Thermaikos Gulf, in Greece. To achieve this goal, three analytical methods using LC-MS/MS, GC-MS/MS, and ICP-MS were developed, validated, and applied to the collected fish samples. The results indicated a very low prevalence of caffeine and acetaminophen, both not exceeding 3.8 μg/kg fish. Similarly, thiabendazole, cypermethrin, and tricyclazole (pesticides) were found in a concentration range of 0.9 to 13.7 μg/kg fish, while in one <i>D. labrax</i> sample, traces of the metabolite of organochlorine pesticide DDT, <i>o,p’</i>-DDE were detected. Al, Mn, Fe, Zn, and Sr were the predominant trace elements in a concentration range of 500–20,000 μg/kg fish. Macro elements levels varied from 280 to 5405 mg/kg fish. Health risk assessment did not unveil an unacceptable risk for the human health of adults, apart from one sample presenting Hg above the regulatory levels. On the contrary, for children, the calculated hazard quotient values for Hg in all cases and for two As detections were higher than the threshold value of 1, indicating a potential risk.

Therapeutics. Pharmacology, Toxicology. Poisons
DOAJ Open Access 2023
In vitro safety assessment of alkyl lactate esters in human umbilical vein endothelial cells (HUVECs)

Fatemeh Javaheri-Ghezeldizaj, Maryam Ghaffari, Jafar Ezzati Nazhad Dolatabadi et al.

Safety assessment requires information on both the chronic and acute effects of chemicals. Chemical materials such as food additives have become one of the most critical and compelling issues in the continuing debate on food safety. Calcium lactate (CL) and Sodium lactate (SL) are approved chemicals used in various products. The present study, in vitro study, was designed to evaluate the cyto-genotoxicity effects of CL and SL on human umbilical vein endothelial cells (HUVECs). The cytotoxicity effect of these additives was determined by MTT and Annexin V-FITC apoptosis assays. Besides, genotoxicity parameters such as morphological change of DNA and DNA fragmentation were studied with DAPI staining and DNA ladder assays, respectively. The results showed that the growth of HUVECs decreased upon treatment with CL at higher concentrations, but SL did not significantly alter HUVECs cell number. Annexin V-FITC apoptosis assays revealed that CL could induce cell death based on necrosis rather than apoptosis. In SL, the early and late apoptosis was not considerable in treated cells. Exposure to CL and SL did not lead to morphological change and DNA fragmentation in the HUVECs cell line. Overall, it is concluded from these results that CL and SL have not been cytotoxic and genotoxic effects in low concentrations in human umbilical vein endothelial cells in vitro.

Toxicology. Poisons
CrossRef Open Access 2023
Data from Nek4 Status Differentially Alters Sensitivity to Distinct Microtubule Poisons

Jason Doles, Michael T. Hemann

<div>Abstract<p>Microtubule poisons are widely used in cancer treatment, but the factors determining the relative efficacy of different drugs in this class remain obscure. In this study, we identified the NIMA kinase Nek4 in a genetic screen for mediators of the response to Taxol, a chemotherapeutic agent that stabilizes microtubules. After Taxol treatment, Nek4 promoted microtubule outgrowth, whereas Nek4 deficiency impaired G<sub>2</sub>-M arrest and decreased formation of mitotic-like asters. In contrast, Nek4 deficiency sensitized cells to vincristine, which destabilizes microtubules. Therefore, Nek4 deficiency may either antagonize or agonize the effects of microtubule poisons, depending on how they affect microtubule polymerization. Of note, <i>Nek4</i> gene maps to a commonly deleted locus in non-small cell lung cancer. Thus, Nek4 deletion in this disease may rationalize the use of particular types of microtubule poisons for lung cancer therapy. Cancer Res; 70(3); 1033–41</p></div>

DOAJ Open Access 2022
Pectin with various degrees of esterification differentially alters gut microbiota and metabolome of healthy adults

Wenqi Huang, Qingying Fang, Linlin Fan et al.

Abstract Pectin with various degrees of esterification (DE) leads to different food processing directions and has the distinct potential for modulating human health. Investigations of pectin–gut microbiota interactions may contribute towards better understanding of the structure–function mechanism. In this study, in vitro batch fermentation (artificial colon model) was used to illustrate the differential impacts of pectin with different DE on the gut microbiota and metabolome of healthy adults. The results indicated that low‐esterified pectin L13 showed better‐sustained abilities in terms of the diversity of microbiota and promoted the abundance of Clostridiaceae and Lachnospiraceae at family levels, and Bacteroides and Lachnospira at genus levels. High‐esterified pectin H121 induced less Enterococcus and Clostridium. Data from untargeted metabolomics revealed the alterations of intracellular metabolites including fatty acids, amino acids, and organic molecules by various types of pectins. Inositol was the unique intracellular metabolite that was significantly upregulated by low‐esterified pectin L13. All types of pectins could increase the level of acetic acid, but butyric acid was only enriched by pectin L13.

Food processing and manufacture, Toxicology. Poisons
DOAJ Open Access 2022
Accidental lead in contaminated pipe-borne water and dietary furan intake perturbs rats’ hepatorenal function altering oxidative, inflammatory, and apoptotic balance

Solomon E. Owumi, Uche O. Arunsi, Omolola M. Oyewumi et al.

Abstract Inadvertent exposure to furan and Pb is associated with hepatorenal abnormalities in humans and animals. It is perceived that these two chemical species may work in synergy to orchestrate liver and kidney damage. Against this background, we investigated the combined effect of furan and incremental lead (Pb) exposure on hepatorenal dysfunction. Wistar rats (n = 30; 150 g) were treated for 28 days accordingly: Control; FUR (8 mg/kg), PbAc (100 µg/L), FUR + PbAc1 (8 mg/kg FUR + 1 µg/L PbAc); FUR + PbAc1 (8 mg/kg FUR + 10 µg/L PbAc), and FUR + PbAc1 (8 mg/kg FUR + 100 µg/L PbAc). Biomarkers of hepatorenal function, oxidative stress, inflammation, DNA damage, and apoptosis were examined. Furan and incrementally Pb exposure increased the levels of hepatorenal biomarkers and oxidative and pro-inflammatory mediators, including lipid peroxidation, reactive oxygen and nitrogen species, and interleukin-1 beta. Increased DNA damage, caspases- 9 and -3, and atypical histoarchitecture of the hepatorenal tissues exemplified furan and Pb treatment-related perturbations. Furthermore, the levels of antioxidants and IL-10 were also suppressed. Furan and Pb dose-dependently exacerbated hepatorenal derangements by altering the redox and inflammatory rheostats, worsened DNA damage, and related apoptotic onset that may potentiate hepatorenal disorders in humans and animals. The findings validate the synergistic effect of furan and Pb in the pathophysiology of kidney and liver disorders.

Therapeutics. Pharmacology, Toxicology. Poisons
DOAJ Open Access 2022
Recent advances on the structure identification of components in food

Min Zhao, Jin‐Long Tian

Abstract With the rapid development of food industry, people pay more and more attention to the health benefits of food‐active molecules. The active function of food molecules depends on the chemical structure. So how to determine the chemical composition of food becomes very important. Based on this, this paper mainly expounds the structural analysis methods and specific processes of food chemical components, as well as the difficulties encountered in the determination of structure, and summarizes the latest research trends of food structural analysis. The purpose is to let more scholars understand the structure analysis process of the chemical substance basis of food, and provide a reference for the healthy development of food.

Food processing and manufacture, Toxicology. Poisons
DOAJ Open Access 2022
Aggregation-prone A53T mutant of α-synuclein exaggerates methamphetamine neurotoxicity in SH-SY5Y cells: Protective role of cellular cholesterol

Sho Aoki, Takeshi Funakoshi, Toshihiko Aki et al.

The aim of this study is to examine the effects of wild type as well as a mutant (A53T) form of α-synuclein (α-syn) on neuronal cells exposed to methamphetamine (METH). SH-SY5Y human dopaminergic neuronal cells stably expressing exogenously added wild type (WT) or A53T α-syn were established for this purpose. Among the three types of cells, parental, WT α-syn-overexpressing, and A53T α-syn overexpressing SH-SY5Y cells (hereafter referred to as SH-SY5Y, WT SH-SY5Y, and A53T SH-SY5Y, respectively), only A53T SH-SY5Y cells showed significant loss of cell viability after exposure to 2 mM METH for 24 h. Transcriptome analysis using DNA microarray showed that METH induced genes for cholesterol biosynthesis in all of these three cell lines, suggesting that METH upregulates cellular cholesterol biosynthesis independently from cellular α-syn levels. Visualization of the cellular localization of free cholesterol showed that METH induces an aberrant intracellular accumulation of free cholesterol in all three cell lines. In addition, we observed the aggregation of α-syn into cytoplasmic granules, which was more apparent with A53T α-syn than WT α-syn, in cells exposed to METH. Furthermore, the cell death observed in METH-treated A53T SH-SY5Y cells was exaggerated by the addition of 2-hydroxypropyl-β-cyclodextrin (CD), a substance used to extract cholesterol from cells. These results suggest that the aggregation of A53T α-syn in METH-treated cells should be involved in cell death. The upregulation of cellular biosynthesis and cholesterol accumulation by METH should play a protective role against A53T α-syn neurotoxicity in METH-treated SH-SY5Y cells.

Toxicology. Poisons
DOAJ Open Access 2018
Radical containing combustion derived particulate matter enhance pulmonary Th17 inflammation via the aryl hydrocarbon receptor

Sridhar Jaligama, Vivek S. Patel, Pingli Wang et al.

Abstract Background Pollutant particles containing environmentally persistent free radicals (EPFRs) are formed during many combustion processes (e.g. thermal remediation of hazardous wastes, diesel/gasoline combustion, wood smoke, cigarette smoke, etc.). Our previous studies demonstrated that acute exposure to EPFRs results in dendritic cell maturation and Th17-biased pulmonary immune responses. Further, in a mouse model of asthma, these responses were enhanced suggesting exposure to EPFRs as a risk factor for the development and/or exacerbation of asthma. The aryl hydrocarbon receptor (AHR) has been shown to play a role in the differentiation of Th17 cells. In the current study, we determined whether exposure to EPFRs results in Th17 polarization in an AHR dependent manner. Results Exposure to EPFRs resulted in Th17 and IL17A dependent pulmonary immune responses including airway neutrophilia. EPFR exposure caused a significant increase in pulmonary Th17 cytokines such as IL6, IL17A, IL22, IL1β, KC, MCP-1, IL31 and IL33. To understand the role of AHR activation in EPFR-induced Th17 inflammation, A549 epithelial cells and mouse bone marrow-derived dendritic cells (BMDCs) were exposed to EPFRs and expression of Cyp1a1 and Cyp1b1, markers for AHR activation, was measured. A significant increase in Cyp1a1 and Cyp1b1 gene expression was observed in pulmonary epithelial cells and BMDCs in an oxidative stress and AHR dependent manner. Further, in vivo exposure of mice to EPFRs resulted in oxidative stress and increased Cyp1a1 and Cyp1b1 pulmonary gene expression. To further confirm the role of AHR activation in pulmonary Th17 immune responses, mice were exposed to EPFRs in the presence or absence of AHR antagonist. EPFR exposure resulted in a significant increase in pulmonary Th17 cells and neutrophilic inflammation, whereas a significant decrease in the percentage of Th17 cells and neutrophilic inflammation was observed in mice treated with AHR antagonist. Conclusion Exposure to EPFRs results in AHR activation and induction of Cyp1a1 and in vitro this is dependent on oxidative stress. Further, our in vivo studies demonstrated a role for AHR in EPFR-induced pulmonary Th17 responses including neutrophilic inflammation.

Toxicology. Poisons, Industrial hygiene. Industrial welfare
DOAJ Open Access 2018
Phylogenetic Comparative Methods can Provide Important Insights into the Evolution of Toxic Weaponry

Kevin Arbuckle

The literature on chemical weaponry of organisms is vast and provides a rich understanding of the composition and mechanisms of the toxins and other components involved. However, an ecological or evolutionary perspective has often been lacking and is largely limited to (1) molecular evolutionary studies of particular toxins (lacking an ecological view); (2) comparisons across different species that ignore phylogenetic relatedness (lacking an evolutionary view); or (3) descriptive studies of venom composition and toxicology that contain post hoc and untested ecological or evolutionary interpretations (a common event but essentially uninformative speculation). Conveniently, comparative biologists have prolifically been developing and using a wide range of phylogenetic comparative methods that allow us to explicitly address many ecological and evolutionary questions relating to venoms and poisons. Nevertheless, these analytical tools and approaches are rarely used and poorly known by biological toxinologists and toxicologists. In this review I aim to (1) introduce phylogenetic comparative methods to the latter audience; (2) highlight the range of questions that can be addressed using them; and (3) encourage biological toxinologists and toxicologists to either seek out adequate training in comparative biology or seek collaboration with comparative biologists to reap the fruits of a powerful interdisciplinary approach to the field.

DOAJ Open Access 2015
Exposure to bisphenol A and gender differences: from rodents to humans evidences and hypothesis about the health effects

Lidia Caporossi, Bruno Papaleo

Bisphenol A (BPA) interacts with the endocrine system and seems to produce different effects in relation to gender. The objective of the study was to clarify the possible health effects of exposure to BPA in relation to gender. A literature search was performed using three different search engines: Medline, PubMed and Scopus. Data on both animals and humans showed that BPA acts as a xenoestrogen and interacts with the androgens’ metabolism, producing different outcomes: uterotropic effects, decreasing sperm production, stimulation of prolactin release. Gender difference plays a key role in understanding the real toxic effects, the BPA serum concentrations were, all the time, higher in male subjects, possibly due to the difference in androgen-related enzyme activity levels, compared with the healthly female subjects, to equal levels of exposure; while higher BPA levels in women have been associated with a variety of conditions including obesity, endometrial hyperplasia, recurrent miscarriages, and polycystic ovarian syndrome. The data collected are sufficiently robust to raise concerns about the potentially deleterious impact of BPA on humans, even with some methodological limitations; the different impact of BPA in men and in women is documented and of a certain interest. In toxicology it is necessary to assess effects in relation to gender differences, in order to set up prevention plans in the work environment targeting the specific risk.

Therapeutics. Pharmacology, Toxicology. Poisons
DOAJ Open Access 2015
A Comparative Study of the Effects of Cumin and Mefenamic Acid Capsules on Menstrual Bleeding in IUD Users: A Randomized Triple Blind Clinical Trial

NM Rajabi, M Modarres, GH Amin et al.

Background: Unusual menstrual bleeding is one of the most common side effects of IUD. Objective: Considering public enthusiasm to the use of herbal medicine, this study conducted to compare the effects of cumin and mefenamic acid capsules on menstrual bleeding in IUD users. Methods: This crossover triple-blind randomized clnical trial study was performed on 100 IUD users who came to 6 health centers in Karaj. Research took place in three stages. In the first stage menstrual bleeding was measured by using Hygam table. In the second stage all participants were randomly allocated to mefenamic acid and cumin groups. They took capsules for two consecutive cycle. In the third stage each research unit received the same treatment of the opposite group with replacing the medicine for two more consecutive cycle. Menstrual bleeding was assessed by using Hygam table for 5 cycle. Considering that the maximum efficacy time for cumin was 24 hours and for Mefenamic acid was6 to 8 hours, the use of drugs in 7 days during menstruation, had no effect on subsequent cycles. Data, was analyse by Chi-square and Fisherchr('39')s exact test, paired t-test, Wilcoxon. Results: The mean of menstrual bleeding was 154.26±60.08 and after treatment was 106.68±45.38 and 105.8±40.56 in the mefenamic acid and cumin groups. There was a significant difference in decrease of pain intensity in both groups (p<0.001). There wasn’t a significant difference in decrease of pain intensity between two groups. Conclusion: This study showed that cumin same as mefenamic acid capsules can decrease menstrual bleeding effectively. Therefore it is recommended to use it in the treatment of menstrual bleeding in IUD users.

Therapeutics. Pharmacology, Toxicology. Poisons
S2 Open Access 2011
Clinical Review: Emergency management of acute poisoning

D. J. V. Hoving, D. Veale, G. Müller

Abstract Acutely poisoned patients are commonly encountered in Emergency Centres. Acute poisoning (accidental or intentional) requires accurate assessment and prompt therapy. The necessity to prevent cross contamination during the initial evaluation should be emphasized. Early identification of the involved toxin/s is crucial and the majority will be identified by a thorough history and physical examination. An ABC-approach should be followed ensuring a protected airway, adequate ventilation and hemodynamic stability. Supportive and symptomatic care remains the cornerstone of treatment. A stepwise approach may be followed to decrease the bioavailability of toxins. Indications, contra-indications, risks and dosage regimens are describe for decontamination procedures including both termination of topical exposures and decreasing exposure to ingested toxins. Furthermore, procedures to increase the elimination of toxins and a short section covering specific toxins and their antidotes are also included. The aim of this commissioned review was to establish concise guidelines for the initial management of the acutely poisoned patient in the Emergency Centre. The American Academy of Clinical Toxicology and the European Association of Poisons Centres and Clinical Toxicologists are the international leaders in the field of toxicology and the guidelines in their position papers were generally followed. Most of the dosage regimes are according to the South African Medicines Formulary.

28 sitasi en Medicine
DOAJ Open Access 2011
Comparative Effects of α-, β-, and γ-Carbolines on Platelet Aggregation and Lipid Membranes

Hironori Tsuchiya

Cigarette smoking and alcohol consumption possibly affect platelet functions. To verify the hypothesis that some α-, β-, and γ-carboline components in cigarette smoke and alcoholic beverages may change platelet aggregability, their effects on human platelets were determined by aggregometry together with investigating their membrane effects by turbidimetry. Carbolines inhibited platelet aggregation induced by five agents with the potency being 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole > 3-amino-1-methyl-5H-pyrido[4,3-b]indole > 1-methyl-9H-pyrido[3,4-b]indole. The most potent 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole showed 50% aggregation-inhibitory concentrations of 6–172 μM. Both γ-carbolines interacted with phosphatidylcholine membranes to lower the lipid phase transition temperature with the potency correlating to the antiplatelet activity, suggesting that the interaction with platelet membranes to increase their fluidity underlies antiplatelet effects. Given their possible concentration and accumulation in platelets, γ- and β-carbolines would provide cigarette smokers and alcohol drinkers with reduced platelet aggregability, and they may be responsible for the occurrence of hemorrhagic diseases associated with heavy smoking and alcoholics.

Toxicology. Poisons

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