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1.
J Plant Res ; 136(5): 587-612, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37452973

RESUMO

Asteraceae (synonym as Compositae) is one of the largest angiosperm families among flowering plants comprising one-tenth of all agri-horticultural species grown across various habitats except in Antarctica. These are commercially utilized as cut and loose flowers as well as pot and bedding plants in landscape gardens due to their unique floral traits. Consequently, ineffective seed setting and presence of an intraspecific reproductive barrier known as self-incompatibility (SI) severely reduces the effectiveness of hybridization and self-fertilization by traditional crossing. There have been very few detailed studies of pollen-stigma interactions in this family. Moreover, about 63% of Aster species can barely self-fertilize due to self-incompatibility (SI). The chrysanthemum (Chrysanthemum × morifolium) is one of the most economically important ornamental plants in the Asteraceae family which hugely shows incompatibility. Reasons for the low fertility and reproductive capacity of species are still indefinite or not clear. Hence, the temporal pattern of inheritance of self-incompatibility and its effect on reproductive biology needs to be investigated further to improve the breeding efficiency. This review highlights the self-incompatible (SI) system operating in important Astraceous (ornamental) crops which are adversely affected by this mechanism along with different physiological and molecular techniques involved in breaking down self-incompatibility.

2.
Chem Biol Interact ; 379: 110508, 2023 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-37150498

RESUMO

Tattooing is a very common fashion trend across all the ages and gender of the society worldwide. Although skin inflammatory diseases are very frequent among tattoo users because of the active chemical ingredients used in tattoo ink, yet no ingredient-specific toxicity study has been performed. Benzo(ghi)perylene (BgP) is one of the PAHs and an important ingredient of black tattoo ink that shows strong absorption in UVA and UVB radiation of sunlight. Therefore, understanding the hazardous potential of BgP especially under UVA exposure is important for the safety of skin of tattoo users by considering the fact that penetration of UVA is in the dermis region where tattoo ingredients reside. To evaluate the hazardous potential of BgP on human skin under UVA exposure, different experimental tools i.e., in-chemico, in-silico and in-vitro were utilized. Our results illustrated that BgP photosensitized under UVA (1.5 mW/cm2) irradiation shows a degradation pattern till 4 h exposure. Photosensitized BgP reduced significant cell viability (%) at 1 µg/ml concentration. However, the pretreatment of singlet and hydroxyl radical quenchers, restoration of cell viability observed, confirmed the role of type-I and type-II photodynamic reactions in phototoxicity of BgP. Further, intracellular uptake of BgP in HaCaT cells was estimated and confirmed by UHPLC analysis. Molecular docking of BgP with DNA and formation of γ-H2AX foci demonstrated the DNA intercalation and double-stranded DNA damaging potential of BgP. Furthermore, acridine orange and ethidium bromide (AO/EB) dual staining showed apoptotic cell death via photosensitized BgP under UVA irradiation. The above findings suggest that BgP reached the human skin cell and induced dermal toxicity via direct and indirect mode of DNA damage under UVA exposure finally promoting the skin cell death. Thus, BgP-containing tattoo ink may be hazardous and may induce skin damage and diseases, especially in presence of UVA radiation of sunlight. To minimize the risk of skin diseases from synthetic ingredients in tattoo ink, the study highlights the importance of developing eco-friendly and skin-friendly tattoo ingredients by companies.


Assuntos
Tatuagem , Humanos , Tatuagem/efeitos adversos , Simulação de Acoplamento Molecular , Raios Ultravioleta/efeitos adversos , Pele/metabolismo , Dano ao DNA , DNA/metabolismo
3.
Med Chem ; 19(8): 730-756, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36593699

RESUMO

The 1,3,4-thiadiazole nucleus has attracted the attention of medicinal chemists during the last decades due to its multiple pharmacological activities, such as antiviral, anticancer, antibacterial, and anticonvulsant activity. This scaffold's structural alteration could aid in developing novel therapeutically effective drugs. Incorporating this adaptable pharmacophore into a well-established medicinally active molecule results in hybrid molecules with diverse pharmacological effects. These encouraging reports suggested that this privileged skeleton should be thoroughly researched for medicinal purposes. Hence, an attempt has been made in this compilation to review the structure-activity relationships of numerous thiadiazole derivatives reported in the literature with varied pharmacological properties. This review provides an up-to-date explanation of the various synthesized 1,3,4- thiadiazole analogs and their pharmacological importance.


Assuntos
Farmacóforo , Tiadiazóis , Relação Estrutura-Atividade , Tiadiazóis/farmacologia , Tiadiazóis/química , Antibacterianos/farmacologia
5.
Saudi J Biol Sci ; 28(7): 3727-3734, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34220224

RESUMO

Reproductive drugs that include contraceptive and fertility drugs are used to manage reproductive health in both humans and animals. Contraceptive drugs are mainly used by humans for reversible contraception whereas fertility drugs are mainly used in animals to increase milk production, poultry products and meat production. Usage of these drugs has increased manifold in the last decade. These drugs are excreted through body fluids (mainly urine and milk) that lead to contamination of surface water, milk and animal produce. Consumption of such contaminated products or water results in reproductive disorders and different types of cancers in humans. This questionnaire-based study was designed and conducted involving gynecologists, pharmacies, medical stores and veterinarians in Patiala city and its adjoining areas in India to evaluate the quantitative and qualitative aspects of use of these drugs. A total of 150 survey points were identified with random sampling method. Data was analyzed using appropriate statistical tools. The results showed that contraceptive drugs constitute 86% of reproductive drugs usage in humans. Further, steroidal contraceptives constitute a huge 94.7% share of contraceptive drugs, and of these combined oral contraceptives have 79.79% share among which a combination is ethinylestradiol and levonorgestrel is the most popular (20.92%). The consumption of COCs is higher than that of progestin only pills (Z = 3.39) as well as estrogen only pills (Z = 4.30). In contrast, usage of non-hormonal fertility drugs (89%) dominates over the hormonal class (11%) in humans. The most widely used non-hormonal fertility drug is clomiphene citrate (73.87%). In animals, the prescription rate of hormonal fertility drugs is higher (83%) than the non-hormonal one, where in the most widely prescribed drug is buserelin acetate. These findings are in consonance with the similar studies carried out in US, Europe and Canada which suggest that reproductive drugs usage pattern is more or less similar across the globe. A careful control to discourage indiscriminate use of such drugs is the need of hour to prevent damage of environment and ultimately to the health of living beings.

6.
Saudi J Biol Sci ; 28(6): 3176-3182, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34121852

RESUMO

Although the pupation behavior of blowflies has been widely studied, this preliminary study was done on the vertical dispersal behavior (both ascending and descending) and fly emergence rate of third instar larvae of Chrysomya megacephala (Fabricius) to evaluate weather immature stages of blowflies survive burial and emerge out as adult. Third instar larvae of Chrysomya megacephala were placed at three different depths (5 cm, 25 cm and 45 cm) of soil under laboratory conditions to determine the impact of soil depth on the ascending and descending vertical dispersal behavior and the subsequent emergence of adults. The results of this study, although preliminary, but valuable to the field of forensic entomology because they provide new information about both ascending and descending vertical dispersal behavior of Chrysomya megacephala forensically important species of blowfly. In all the cases, maximum number of pupae recovered at the depth of 0 to 5 cm are 35.5 ± 4.5, 34 ± 1, 25 ± 5, when food was located at 5 cm, 25 cm and 45 cm depth respectively. This means that maximum no of larvae reached to the depth of 0 to 5 cm by ascending dispersal irrespective of at which depth they are placed. Paramount pupae were recovered from shallow burial depth of 0-5 cm in ascending dispersal and showed highest eclosion success i.e. 90.1% followed by 25 cm and 45 cm i.e. 71.7% and 55% respectively. While the number of pupae recovered as well as eclosion success was less in descending dispersal with an average of 62.8%, 39.25% and 33.9% at depths of 5, 25 and 45 cm respectively. This manifest if larvae disperse ascendingly, it increases their chance of survival.

7.
Saudi J Biol Sci ; 28(4): 2049-2055, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33911920

RESUMO

Egyptian flower mantis Blepharopsis mendica (Order: Mantodea) is a widespread mantis species throughout the southwest Palearctic region. The ecological and geographical distribution of such interesting species is rarely known. So, through this work, habitat suitability models for its distribution through Egyptian territory were created using MaxEnt software from 90 occurrence records. One topographic (altitude) and eleven bioclimatic variables influencing the species distribution were selected to generate the models. The predicted distribution in Egypt was focused on the Delta, South Sinai, the north-eastern part of the country, and some areas in the west including Siwa Oasis. Temporal analysis between the two periods (1900-1961) and (1961-2017) show current reduction of this species distribution through Delta and its surrounding areas, may be due to urbanization. On the other hand, it increases in newly protected areas of South Sinai. Under the future climate change scenario, the MaxEnt model predicted the habitat gains for B. mendica in RCP 2.6 for 2070 and loss of habitat in RCP 8.5 for the same year. Our results can be used as a basis for conserving this species not only in Egypt, but also throughout the whole of its range, also, it show how the using of geo-information could help in studying animal ecology.

8.
Int J Legal Med ; 135(3): 967-977, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33230566

RESUMO

Age determination of insects collected from vertebrate remains is an essential step in estimating time since colonization as related to the post-mortem interval. Long-established methods for making such estimates rely on determining age related to stage of development at the time of collection in relation to conditions experienced. However, such estimates are based on the completion of a stage of development. Methods allowing for more precise estimates of age (i.e., within a stage of development) are sorely needed. This study examined the potential of volatile organic compounds emitted by blow fly, Ch. rufifacies (Macquart), immatures to determine stage of development, which could potentially be used to estimate the age. Volatile organic compounds (VOCs) from the larval and pupal stages of Ch. rufifacies were collected by headspace solid-phase micro-extraction followed by gas chromatography-mass spectrometry (GC-MS). Analyses indicated 37 compounds shift quantitatively, as well as qualitatively, as the larvae and pupae age. Furthermore, compounds, such as 2-ethyl-1-hexanol, phenol, butanoic acid, hexadecanoic acid, octadecanoic acid, 2-methyl propanamide, and 2-methyl butanoic acid, serve as indicator compounds of specific stages within Ch. rufifacies development. This information could be important to determine if these compounds can be used in the field to predict the presence of certain developmental stages, in order to determine the potential of using volatile markers to estimate time of colonization.


Assuntos
Calliphoridae/química , Calliphoridae/crescimento & desenvolvimento , Entomologia Forense , Compostos Orgânicos Voláteis/análise , Animais , Cromatografia Gasosa-Espectrometria de Massas , Larva/química , Larva/crescimento & desenvolvimento , Pupa/química , Pupa/crescimento & desenvolvimento , Microextração em Fase Sólida
9.
J Forensic Sci ; 66(1): 236-244, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32966626

RESUMO

Calliphoridae are one of the most important insect groups encountered as evidence collected from a crime scene. Age determination of the immature stages of these necrophagous flies is an important step toward estimating the time of colonization and inferring a minimum postmortem interval (PMImin ) in most instances. To determine if the cuticular hydrocarbons could be used to establish whether the development stages yield characteristics profiles, allowing for age estimation, hydrocarbons were extracted from 1st and 2nd, as well as feeding and post-feeding 3rd instar Chrysomya rufifacies, the hairy maggot blow fly. Extracted hydrocarbons were analyzed using gas chromatography coupled to mass spectrometry with the aim to investigate the changes in chemical profiles of each larval stage. A total of 23 compounds were identified with most of them being alkanes (65%) with carbon chain lengths of 9-33 carbons, alkenes (18%), and methyl-branched alkanes (17%). All the hydrocarbons except pentadecane (C15), hexadecane (C16), and nonacosane (C29) showed significant differences in their expression throughout larval development. For 1st instars, nonane was the most abundant (17% of the total hydrocarbons content) compound. Accounting for 11% and 10% of the cuticular hydrocarbons, tricosane and pentacosane, respectively, were the notable hydrocarbons in 2nd instars. For post-feeding 3rd instars, hentriacontane and tritriacontane were present with relative abundances 18% and 15%, respectively. On average, there was a shift from low to high molecular weight hydrocarbons as the larvae aged. These results indicate the change in hydrocarbons makeup as larvae age and could potentially be used to determine the age of immature C. rufifacies and hence aid in PMImin estimations. However, future research is needed to validate these results under natural conditions in the field.


Assuntos
Calliphoridae/química , Calliphoridae/crescimento & desenvolvimento , Entomologia Forense/métodos , Hidrocarbonetos/análise , Larva/química , Larva/crescimento & desenvolvimento , Animais , Comportamento Alimentar , Cromatografia Gasosa-Espectrometria de Massas , Mudanças Depois da Morte
10.
Int J Radiat Biol ; 96(10): 1309-1316, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32659144

RESUMO

PURPOSE: The novelty in flower color or inflorescence form is recognized as a valuable trait in Chrysanthemum - a potential commercial flower crop with significant worth in global cut flower trade. This study was conducted to irradiate white and orange flowered cultivars of Chrysanthemum with an objective to identify and isolate desirable types representing novelty in flower color and inflorescence form from the irradiated populations. The terminal rooted cuttings of Chrysanthemum exposed to γ-irradiation at 10 or 15 Gy doses were found effective for inducing novel flower color variants in cultivars Thiching Queen and Purnima. The mutant progeny evolved with novel inflorescence traits of these cultivars will enrich the existing germplasm of Chrysanthemum for further utilization in breeding programs. MATERIALS AND METHODS: Two standard type Chrysanthemum cultivars, Thiching Queen and Purnima were exposed to varied doses of γ-rays (0, 5, 10, 15, and 20 Gy) using Cobalt 60 (60Co) as irradiation source for treating rooted cuttings. The irradiated mutant population was evaluated for likely variation in various vegetative and flowering characters compared to non-irradiated (control) plants. RESULTS: In Chrysanthemum cultivars Thiching Queen, seven and 'in Purnima', two flower color variants were isolated from the irradiated populations that were reportedly novel in color and desirable for commercial aspect. The leaf abnormalities were observed in mutant populations exhibiting variation in flower color, shape, and size of leaves. Certain floral abnormalities were also observed in inflorescence that reportedly progressed with increase in dosage of γ-rays irradiation. CONCLUSIONS: This study developed a gamma ray (60Co) induced mutagenesis protocol with potential application to develop novel and desirable mutants in Chrysanthemum.


Assuntos
Chrysanthemum/efeitos da radiação , Radioisótopos de Cobalto/efeitos adversos , Raios gama/efeitos adversos , Inflorescência/efeitos da radiação , Chrysanthemum/crescimento & desenvolvimento , Chrysanthemum/metabolismo , Relação Dose-Resposta à Radiação , Inflorescência/crescimento & desenvolvimento , Inflorescência/metabolismo , Dose Letal Mediana , Pigmentação/efeitos da radiação
11.
Physiol Mol Biol Plants ; 26(5): 1075-1085, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32377055

RESUMO

Hippophae rhamnoides L. provides an enormous range of medicinal and nutritional benefits. The significant abilities of this plant to survive in Himalayan high altitudes enticed our study to investigate its rhizosphere. Seventeen rhizobacterial strains were isolated from the rhizospheric soil and plant root nodules, belonging to genus Frankia, Azorhizobium, Bacillus, Paenibacillus, Brevibacillus and Pseudomonas, as identified by 16SrRNA sequencing. This varying bacterial population was further examined for the presence of root degrading enzymes pectinase and cellulase, which enable them to intrude the plant roots. Based on the growth and substrate utilization by these rhizobacteria on pectinase screening agar medium and Mandels and Reese agar medium, all the seventeen strains were identified as pectinase and cellulase producing rhizobacteria. The quantitative analysis by DNS method demonstrated varying enzyme activities, spot-lighting the physiological variation in the microbiome. The divergence in the enzyme activities shown by all the strains was analysed statistically, using the software ASSISTAT.

13.
Bioorg Med Chem Lett ; 29(16): 2208-2217, 2019 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-31272795

RESUMO

Targeting nuclear receptor RORγ is recognized to be beneficial in multiple autoimmune disorders. We disclosed new indole analogues as potent RORγ inverse agonists. RO-2 as one of the potent and orally bioavailable compounds was evaluated in various models of autoimmune disorder. It showed potent suppression of downstream markers of RORγt activity in murine and human primary cells, ex vivo PD assay and in multiple animal models of autoimmune diseases. The results indicate the potential of these indole analogues as orally bioavailable small molecule inverse agonists of RORγt, efficacious in various Th17 driven models of autoimmune disorders.


Assuntos
Doenças Autoimunes/tratamento farmacológico , Indóis/química , Membro 3 do Grupo F da Subfamília 1 de Receptores Nucleares/agonistas , Animais , Humanos , Camundongos , Modelos Moleculares , Relação Estrutura-Atividade
15.
Environ Sci Pollut Res Int ; 25(26): 25822-25839, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30039489

RESUMO

Industrial and municipal solid wastes, noise, pesticides, fertilizers and vehicular emission are visible pollutants responsible for environmental contamination and ill-effects on health of all living systems. But, environmental contamination due to drugs or medicines used for different purposes in humans and animals goes unseen largely and can affect the health of living system severely. During the last few decades, the usage of drugs has increased drastically, resulting in increased drug load in soil and water. Contraceptive and fertility drugs are extensively and effectively used in humans as well as animals for different purposes. Usage of these reproductive drugs in humans is increased manifold to manage reproductive problems and/or for birth control with changing lifestyles. These drugs are excreted in urine and faeces as metabolite or conjugated forms, leading to contamination of water, milk and animal produce, which are consumed directly by humans as well as animals. These drugs are not eliminated even by water treatment plant. Consumption of such contaminated water, milk, meat and poultry products results in reproductive disorders such as fertility loss in men and increase risk of different types of cancers in humans. Therefore, assessment of impact of environmental contamination by these drugs on living system is of paramount importance. The purpose of this review article is to provide a comprehensive analysis of various research and review reports on different contraceptive and fertility drugs used in human and animals, their occurrence in the environment and their ill-effects on living systems. The approaches to control this invisible menace have also been proposed.


Assuntos
Anticoncepcionais/química , Anticoncepcionais/toxicidade , Poluentes Ambientais/química , Poluentes Ambientais/toxicidade , Animais , Monitoramento Ambiental , Poluição Ambiental/prevenção & controle , Hormônios/química , Hormônios/toxicidade , Humanos
16.
J Complement Integr Med ; 16(1)2018 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-29933244

RESUMO

Background & methods We investigated the in vitro antioxidant and antifungal activity by agar disc diffusion assay of leaf extract of some stinging plants namely, Urtica dioica L., Tragia involucrate L., Carduus nutans L. and Mucuna pruriens (L.) DC., against pathogenic fungi causing infections/diseases. Results M. pruriens (Disc 4), T. involucrate (Disc 2), U. dioica (Disc 1) showed significant antifungal activity against all tested pathogens, while C. nutans (Disc 3) showed intermediate activity against only Chaetomium globosum (Cg). The leaf extract of M. Pruriens showed maximum total phenol content (~1004 µg g-1 dry wt) followed by T. involucrate, C. nutans and U. dioica. However, the ascorbate was observed highest in T. involucrate (~10.3 µg g-1 dry wt) followed by M. pruriens (~9.2 µg g-1 dry wt) but the difference was not significant (p ≤ 0.05). Likewise, M. pruriens showed maximum anthocyanin content (~0.3 µg g-1 dry wt). The activity of antioxidant enzymes revealed that M. Pruriens showed maximum ascorbate peroxidase (APX) activity, while the highest guaiacol peroxidase (GPX) and catalase (CAT) activities were observed in C. nutans and U. dioica, respectively. Conclusions M. Pruriens showed potential in vitro antioxidant and antifungal activity against studied pathogens that may be used for ethno-pharmacological uses.


Assuntos
Antifúngicos/farmacologia , Antioxidantes/farmacologia , Carduus/química , Fungos/efeitos dos fármacos , Mucuna/química , Extratos Vegetais/farmacologia , Técnicas In Vitro , Micoses/tratamento farmacológico , Extratos Vegetais/química , Urtica dioica/química
18.
Pharm Biol ; 55(1): 1833-1842, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28552029

RESUMO

CONTEXT: Effects of a radioprotective, standardized leaf extract (code SBL-1) from traditional medicinal plant, sea buckthorn [Hippophae rhamnoides L. (Elaeagnaceae)], on neurotransmitters and brain injuries in rats showing radiation-induced conditioned taste aversion (CTA), are not known. Understanding CTA in rats is important because its process is considered parallel to nausea and vomiting in humans. OBJECTIVE: This study investigated the levels of neurotransmitters, antioxidant defences and histological changes in rats showing radiation CTA, and their modification by SBL-1. MATERIALS AND METHODS: The inbred male Sprague-Dawley rats (age 65 days, weighing 190 ± 10 g) were used. Saccharin-preferring rats were selected using standard procedure and divided into groups. Group I (untreated control) was administered sterile water, group II was 60Co-γ-irradiated (2 Gy), and group III was administered SBL-1 before irradiation. Observations were recorded up to day 5. RESULTS: Irradiation (2 Gy) caused (i) non-recoverable CTA (≥ 64.7 ± 5.0%); (ii) degenerative changes in cerebral cortex, amygdala and hippocampus; (iii) increases in brain dopamine (DA, 63.4%), norepinephrine (NE, 157%), epinephrine (E, 233%), plasma NE (103%) and E (160%); and (iv) decreases in brain superoxide dismutase (67%), catalase (60%) and glutathione (51%). SBL-1 treatment (12 mg/kg body weight) 30 min before irradiation (i) countered brain injuries, (ii) reduced CTA (38.7 ± 3.0%, day 1) and (iii) normalized brain DA, NE, E, superoxide dismutase, catalase and CTA from day 3 onwards. DISCUSSION AND CONCLUSION: Radiation CTA was coupled with brain injuries, disturbances in neurotransmitters and antioxidant defences. SBL-1 pretreatment countered these disturbances, indicating neuroprotective action.


Assuntos
Suplementos Nutricionais , Hippophae/química , Neurônios/metabolismo , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Lesões Experimentais por Radiação/prevenção & controle , Protetores contra Radiação/uso terapêutico , Tonsila do Cerebelo/metabolismo , Tonsila do Cerebelo/patologia , Tonsila do Cerebelo/efeitos da radiação , Animais , Antioxidantes/química , Antioxidantes/normas , Antioxidantes/uso terapêutico , Comportamento Animal/efeitos da radiação , Química Encefálica/efeitos da radiação , Córtex Cerebral/metabolismo , Córtex Cerebral/patologia , Córtex Cerebral/efeitos da radiação , Radioisótopos de Cobalto , Condicionamento Clássico , Hipocampo/metabolismo , Hipocampo/patologia , Hipocampo/efeitos da radiação , Masculino , Neurônios/patologia , Neurônios/efeitos da radiação , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/normas , Fármacos Neuroprotetores/uso terapêutico , Estresse Oxidativo/efeitos da radiação , Extratos Vegetais/química , Extratos Vegetais/normas , Lesões Experimentais por Radiação/metabolismo , Lesões Experimentais por Radiação/patologia , Lesões Experimentais por Radiação/fisiopatologia , Protetores contra Radiação/química , Protetores contra Radiação/normas , Distribuição Aleatória , Ratos Sprague-Dawley , Distúrbios do Paladar/etiologia , Distúrbios do Paladar/prevenção & controle
19.
Bioorg Med Chem Lett ; 27(8): 1867-1873, 2017 04 15.
Artigo em Inglês | MEDLINE | ID: mdl-28279528

RESUMO

In a pursuit to identify reversible and selective BTK inhibitors, two series based on 7H-pyrrolo[2,3-d]pyrimidine and 1H-pyrrolo[2,3-b]pyridine as the hinge binding core, have been identified. Structure activity relationship (SAR) exploration led to identification of two advanced lead molecules, 11 and 13, which demonstrated desired BTK inhibitory potency in different cellular assays, excellent selectivity in a panel of 50 diverse kinases, favorable in vivo PK properties in mice and anti-arthritic effect in a mouse model of CIA.


Assuntos
Antirreumáticos/química , Antirreumáticos/uso terapêutico , Artrite Reumatoide/tratamento farmacológico , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/uso terapêutico , Proteínas Tirosina Quinases/antagonistas & inibidores , Piridinas/química , Piridinas/uso terapêutico , Pirróis/química , Pirróis/uso terapêutico , Tirosina Quinase da Agamaglobulinemia , Animais , Antirreumáticos/farmacocinética , Antirreumáticos/farmacologia , Artrite Reumatoide/enzimologia , Humanos , Masculino , Camundongos Endogâmicos C57BL , Simulação de Acoplamento Molecular , Inibidores de Proteínas Quinases/farmacocinética , Inibidores de Proteínas Quinases/farmacologia , Proteínas Tirosina Quinases/metabolismo , Piridinas/farmacocinética , Piridinas/farmacologia , Pirróis/farmacocinética , Pirróis/farmacologia , Relação Estrutura-Atividade
20.
Int Ophthalmol ; 37(4): 885-891, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27628585

RESUMO

PURPOSE: To report the pattern of ophthalmic manifestations associated with Paederus dermatitis (PD). SETTING: Department of Ophthalmology, Sri Guru Ram Das Institute of Medical Sciences and Research, Amritsar, India. DESIGN: Clinic-based retrospective study. METHODS: Medical charts of patients presenting to the eye clinic with clinical features consistent with the diagnosis of PD from May 1, 2014 to April 30, 2016 were retrospectively reviewed. Relevant demographic and clinical data of periocular and ocular findings were collected and analyzed. The patients with a history of chronic skin disorders or allergies were excluded from the study. RESULTS: A total of 56 patients were included in the study, of which 39 (69.6 %) were males. The age range was 4-65 years with a median of 27 years. On presentation, common subjective symptoms were burning sensation in 49 (87.5 %), itching in 37 (66.1 %), watering in 25 (44.6 %), foreign body sensation in 19 (33.9 %), blurring of vision in 17 (30.4 %), and photophobia in 12 (21.4 %) patients. Visual acuity at presentation was 20/20 in 39 (69.6 %) patients, between 20/30 and 20/80 in 9 (16.1 %) patients, and less than 20/80 in 8 (14.3 %) patients. Lid swelling, erythema, crusts, and vesicles were the common periocular findings; and conjunctival hyperemia, discharge, and corneal erosions were the common ocular findings. CONCLUSIONS: The current study shows that PD can cause significant ocular morbidity. Ophthalmologists, especially those who work in endemic areas, should be aware of this entity both in terms of management as well as for educating patients about the preventive measures.


Assuntos
Doenças da Túnica Conjuntiva/etiologia , Dermatite Irritante/complicações , Ceratite/etiologia , Acuidade Visual , Adolescente , Adulto , Idoso , Animais , Criança , Pré-Escolar , Besouros , Doenças da Túnica Conjuntiva/diagnóstico , Dermatite Irritante/diagnóstico , Feminino , Seguimentos , Humanos , Ceratite/diagnóstico , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Adulto Jovem
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