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1.
Bioorg Med Chem Lett ; 30(12): 127169, 2020 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-32273217

RESUMO

The purinergic P2X7 receptor (P2X7R) is an adenosine triphosphate (ATP) ligand-gated cationic channel receptor. P2X7R is closely associated with various inflammatory, immune, cancer, neurological, musculoskeletal and cardiovascular disorders. P2X7R is an interesting therapeutic target as well as molecular imaging target. This brief digest highlights the radioligands targeting P2X7R recently developed in drug discovery and molecular imaging agent development.


Assuntos
Sondas Moleculares/química , Radioisótopos/química , Receptores Purinérgicos P2X7/análise , Animais , Descoberta de Drogas , Humanos , Marcação por Isótopo , Ligantes , Imagem Molecular , Tomografia por Emissão de Pósitrons , Receptores Purinérgicos P2X7/metabolismo
2.
Zhongguo Zhong Yao Za Zhi ; 45(20): 4812-4818, 2020 Oct.
Artigo em Zh | MEDLINE | ID: mdl-33350251

RESUMO

The molecular marker-assisted breeding is one of the important methods to cultivate excellent germplasms of Chinese medicinal materials by combining modern molecular biology with traditional genetic breeding. The main target of breeding is to make the biological characters of Chinese medicinal materials stable and the yield and medicinal component of it controllable, and ensure that the medicinal materials produced have the characteristics of "excellent shape, high quality and high effect". Compared with traditional breeding that prefers to the selection of phenotypic traits, the molecular marker-assisted breeding also emphasizes genotype screening. It mainly includes five fields, namely the construction of genetic linkage maps, the positioning of quantitative trait locus(QTL), the analysis of genetic diversities, the identification of varieties and hybrid germplasm purity, and the application of molecular marker-assisted selection. At present, SCoT, ISSR, SSR and SNP are the main DNA markers used in the studies of marker-assisted breeding of Chinese medicinal materials. With the rapid development of high-throughput sequencing technology, genome-wide association(GWAS) and molecular design breeding will become the hotspots of Chinese medicinal materials breeding in the future. In this paper, we review current studies excellent germplasm selection of Chinese medicinal materials using molecular marker-assisted breeding and future development prospects. It is suggested to accelerate the breeding of traditional Chinese medicinal materials using molecular pharmacognosy theory and methods, in order to provide theoretical guidance for breeding, protection and sustainable utilization of traditional Chinese medicinal materials.


Assuntos
Estudo de Associação Genômica Ampla , Polimorfismo de Nucleotídeo Único , Povo Asiático , Cruzamento , Marcadores Genéticos/genética , Humanos , Polimorfismo de Nucleotídeo Único/genética
3.
Zhongguo Zhong Yao Za Zhi ; 45(18): 4392-4397, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164367

RESUMO

Songling Xuemaikang Capsules is a Chinese patent medicine mainly made of the Chineses medicine Puerariae Lobatae Radix and leaves of Pinus massoniana. During its production, a large amount of herb extraction residues would be treated as wastes, resulting in resource wasting and serious environmental pollution. In order to solve this problem, we took the hydrolysates of Puerariae Lobatae Radix, P. massoniana leaves, and whole herb residues of Songling Xuemaikang Capsules as the fermentation substrate to explore the ability of Rhodosporidium toruloides to produce microbial lipid. The results showed that the R. toruloides could produce lipid with use of the residues from Songling Xuemaikang Capsules, and the lipid contents reached 33.6%. The lipid products had similar fatty acid composition profiles to those of vegetable oils. Herb residues were converted into fermentation substrates in this study, and were recycled into the production of high value-added compounds to realize the transformation of the wastes, laying the foundation for the sustainable utilization of herb residues.


Assuntos
Medicamentos de Ervas Chinesas , Pueraria , Cápsulas , Lipídeos
4.
Zhongguo Zhong Yao Za Zhi ; 45(17): 4158-4162, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164401

RESUMO

The enzyme linked immunosorbent assay of aflatoxin has been adopted in Chinese Pharmacopoeia(2020 edition). Based on high-throughput screening of monoclonal antibodies technology, monoclonal antibodies that can specifically recognize the aflatoxin B_1 and the total amount of aflatoxin B_1, B_2, G_1, and G_2 in Chinese herbal medicines were prepared. By optimizing the concentration of coating antibody, enzyme-labeled antigen, and the reaction system of enzyme-linked immunosorbent assay, the enzyme linked immunosorbent assay(ELISA) were developed for detection of aflatoxins in Chinese herbal medicines, decoction pieces, and preparation of Chinese medicine. In this method, the recovery test of actual samples is 60%-120%, and the relative standard deviation is less than 15%. In addition, in view of the complicated and expensive pretreatment methods for the determination of aflatoxin in Chinese herbal medicine, we developed a highly efficient pretreatment method of liquid-liquid extraction of aflatoxin in Chinese herbal medicine without immunoaffinity column. As an effective method for the detection of aflatoxin, the ELISA can effectively reduce the aflatoxins testing cost of traditional Chinese medicine, and promote the detection ability at earlier stages of production, and strengthen the quality supervision of traditional Chinese medicine.


Assuntos
Aflatoxinas , Medicamentos de Ervas Chinesas , Aflatoxina B1 , Anticorpos Monoclonais , Contaminação de Medicamentos , Ensaio de Imunoadsorção Enzimática
5.
Zhongguo Zhong Yao Za Zhi ; 45(18): 4510-4518, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164382

RESUMO

The names, basic sources, medicinal parts, efficacy and standards of the medicinal materials in Euphorbiaceae were systematically collated and analyzed by the textual research for Yao medicine monographs in this paper. The results showed that there were great differences in the names, basic sources, medicinal parts and efficacy of some medicinal materials recorded in different literatures. There were 19 genera and 60 species(including varieties) of Euphorbiaceae of Yao medicine, involving 50 kinds of medicinal materials. Among them, there were 42 kinds of single basic sources medicine, 8 kinds of multi basic sources medicine, 28 kinds of root medicine, 26 kinds of whole plant medicine, 25 kinds of unique Yao medicine, accounting for 50%, 11 kinds of cross with Chinese medicinal materials, accounting for 22%. There were 21 kinds of Yao medicine standards at all levels, but only 1 kind of Laoban medicine and 2 kinds of Yao medicine standards. The Yao medicine in Euphorbiaceae could be named by means of transliteration of Yao language/Yao language transliteration/Chinese medicine name, Laoban medicine, plant morphology, medicinal properties, color and smell of medicine, while the medicinal parts and efficacy of the same medicinal name were different from those of traditional Chinese medicine. Therefore, the name and basic sources of the medicinal materials in Euphorbiaceae were not standardized, and the quality standard is not perfect. The above results provided a reference for the construction and improvement of quality standard system, the promotion of the production of medicinal materials and clinical medication standards, and the further development and utilization of Euphorbiaceae.


Assuntos
Medicamentos de Ervas Chinesas , Euphorbiaceae , Plantas Medicinais , Humanos , Medicina Tradicional Chinesa , Registros , Padrões de Referência
6.
Zhongguo Zhong Yao Za Zhi ; 45(19): 4545-4554, 2020 Oct.
Artigo em Zh | MEDLINE | ID: mdl-33164417

RESUMO

In the theories of empirical identification of "arguments on quality" and "five elephants and seven originals", color is regarded as one of the important indicators in the quality evaluation of Chinese medicine. The color of medicinal material including the surface color, the internal color, and the color after processing is caused by the pigment in the cells, which is a characteristic of the "optimal shape". Most pigments have a wide range of pharmacological activities such as anti-oxidation, anti-tumor, anti-atherosclerosis, prevention of coronary heart disease, protection of cardiovascular function, enhancement of immunity, etc. Therefore, the "optimal color" of medicinal materials is unified with the "high quality". This article systematically reviews the research status of "quality discrimination by color", the correlation between L~*, a~*, b~* color space and active ingredients such as alkaloids, flavonoids, terpenes, etc. to explain the "quality discrimination by color" in quantitative characterization. We also summary the research progress on the biosynthesis and regulation of the main pigment components of traditional Chinese medicine, and analyze the biological causes that affect the accumulation of the main pigments. We aim to provide a reference for the theory "quality discrimination by color" in biological knowledge to establish a modern quality control system for Chinese herbal medicines.


Assuntos
Medicamentos de Ervas Chinesas , Cor , Flavonoides , Medicina Tradicional Chinesa , Controle de Qualidade
7.
Zhongguo Zhong Yao Za Zhi ; 45(20): 4867-4874, 2020 Oct.
Artigo em Zh | MEDLINE | ID: mdl-33350258

RESUMO

"Dao-di herbs" is the original comprehensive index for the quality evaluation of traditional Chinese medicine, which has the characteristics of high quality and good effect. After more than 30 years of development, a large number of data, including text data, image data and other types, have been generated in the modern research on Dao-di herbs. It has the characteristics of large quantity, variety, scattered content and different structure, and the data types of each feature are isolated or less interrelated. Based on the literature published in CNKI journal database since 1999-2019, the data collection, selection and collation of 34 kinds of Dao-di herbs characteristics, micro characteristics, ecological characteristics and genetic characteristics were carried out. Using the knowledge base construction technology and combining these characteristics of the characteristics data of the herbs, the above characteristics data were standardized and regarded as a part of the knowledge base of the herbs. Based on a large number of data, this paper analyzes the knowledge composition, research status, comparison between modern and traditional producing areas of traditional Chinese medicine, and takes Salvia miltiorrhiza as an example to compare the ecological characteristics of modern and traditional producing areas. The construction of the knowledge base will facilitate the mining and utilization of the scientific data of Dao-di herbs, and provide resource management and basic guarantee for the transformation and promotion of scientific and technological achievements of Dao-di herbs.


Assuntos
Medicamentos de Ervas Chinesas , Plantas Medicinais , Descoberta do Conhecimento , Medicina Tradicional Chinesa , Tecnologia
8.
Zhongguo Zhong Yao Za Zhi ; 45(20): 4957-4963, 2020 Oct.
Artigo em Zh | MEDLINE | ID: mdl-33350269

RESUMO

In order to evaluate the quality of different varieties of Maca(Lepidium meyenii), the main chemical components in Maca were investigated and a method for simultaneous determination of the main chemical components in Maca was established. UPLC-UV-Q-TOF-MS technology and reference materials were used to identify the structures of 19 main components in Maca. Seven compounds with UV absorption and high contents were selected to establish a simultaneous concentration determination method. The method was employed with a Waters Acquity I-Class~(TM) liquid chromatographic system coupled with a PDA detector and a Waters Acquity Cortecs C_(18)~+ column(2.1 mm×100 mm, 1.6 µm), and acetonitrile-0.2% phosphoric acid water was used as mobile phase(0.45 mL·min~(-1)). The detection wavelength was 195 nm and the column temperature was maintained at 40 ℃. There was efficient separation of seven compounds, p-hydroxybenzylglucosinolate, benzylglucosinolate, N-benzyl-9Z,12Z,15Z-octadecatrienamid, N-benzyl-9Z,12Z-octadecadienamide, N-(3-methoxybenzyl)-hexadecanamide, N-benzyl-hexadecanamide, and N-benzyl-9Z-octadecenamide. The stan-dard calibration curves were good(R~2>0.999). The precision, stability and repeatability were also good. The linearity ranges were 0.197-4.980 µg·mL~(-1) to 193.67-796.8 µg·mL~(-1), and the average recovery rate was 96.71%-103.9%. The average concentration of glucosinolates and macamides in Maca were 1.20% and 0.20%, respectively. Among four kinds of Maca grown in China, the concentration of glucosinolates in yellow Maca and black Maca were relatively high(1.55%), followed by white Maca(0.93%), and purple Maca(0.76%). The concentration of macamides in yellow, purple and white Maca was similar(0.23%-0.29%), however black Maca had significantly lower concentration(0.15%). Peru Maca tested in this study had the lowest concentration of these compounds. This qua-lity evaluation method was fast, accurate, and comprehensively reflects the concentration of the main chemical components in Maca, which provides a useful reference for the quality control and evaluation of Maca.


Assuntos
Lepidium , China , Extratos Vegetais/análise
9.
Zhongguo Zhong Yao Za Zhi ; 45(18): 4519-4527, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164383

RESUMO

In this paper, the name, origin and producing area of Sojae Semen Nigrum were studied to provide the basis for the selection of medicinal varieties of Sojae Semen Nigrum. The textual research of this herbal was carried out through the textual research of ancient and modern literature and the comparative study of botany, combined with agricultural archaeology and the investigation of adulterant products. Before Qin Dynasty, the Sojae Semen Nigrums had not been selected, and the edible beans should only be Glycine soja. From Qin to the Northern and Southern dynasties, the Sojae Semen Nigrums G. max were selected,but the medicinal Sojae Semen Nigrum was G. soja. After Tang Dynasty, Sojae Semen Nigrums were recorded more, the medicinal Sojae Semen Nigrums referred to G. soja,G. max and G. gracilis. In modern times, G. soja was hardly to use as the medicine. The harvest time is August or September, and there are many processing methods, such as frying, making tofu, making Semen Sojae Praeparatum, boiling, boiling with auxiliary materials, germination, etc. The quality evaluation of Sojae Semen Nigrum was consistent in past dynasties, and it was considered that "it is better for those who are tight and small". Before Tang Dynasty, the better should only be G. soja. After the Qing Dynasty, the better should be green cotyledon varieties of G. max,which are recommended. In addition, there are many varieties of Sojae Semen Nigrum. It is hoped that that the scientific researchers of traditional Chinese medicine can use modern technology to distinguish the efficacy of Sojae Semen Nigrum with green and yellow cotyledon, and make a comparison between large and small Sojae Semen Nigrum. The results provide scientific basis for the selection of medicinal varieties of Sojae Semen Nigrum.


Assuntos
Medicamentos de Ervas Chinesas , Glycine max , China , Medicina Tradicional Chinesa , Sementes/química , Glycine max/química
10.
Zhongguo Zhong Yao Za Zhi ; 45(17): 4031-4040, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164386

RESUMO

In order to guide the standardized planting and scientific harvesting of Artemisia argyi var. argyi 'Qiai', effects of diffe-rent planting density, leaf position and leaf age on the growth and quality of A. argyi var. argyi 'Qiai' were studied in this paper. The results showed that appropriate sparse planting could increase stem diameter, compact leaf spacing, increase the leaf size, reduce the rate of withered leaves and increase the number of effective leaves. Dense planting can significantly increase the yield of A. argyi var. argyi 'Qiai' per Mu(1 Mu≈667 m~2) and the output rate of moxa, but reduce the yield per plant and the number of effective leaves. With the decrease of leaf position and the increase of leaf age, the leaf size and the weight of one hundred leaves increased at first and then decreased, the density of non-glandular hair field of the lower epidermis and the output rate of moxa decreased. With the increase of planting density, the contents of eucalyptus oleoresin, camphor, α-platyclone, and cyanidin decreased gradually, the contents of chlorogenic acid, isochlorogenic acid B, isochlorogenic acid A and isochlorogenic acid C in the leaves of A. argyi var. argyi 'Qiai' increased gradually, while the contents of borneol, bornyl acetate and isozelanin increased at first and then decreased significantly. With the decrease of leaf position and the increase of leaf age, the contents of volatile oil, phenolic acid and flavonoid in A. argyi var. argyi 'Qiai' decreased gradually. PCA analysis can divide the leaf quality characteristics of A. argyi var. argyi 'Qiai' into two parts: the middle and upper 10-30 days leaf age, the middle and lower 40-50 days above leaf age. Based on the above factors, the planting density of 28 000 plants/Mu(row spacing of 10 cm×20 cm) can be selected for cultivation of A. argyi var. argyi 'Qiai' rhizome, and the effective plants in the field are about 142 800 plants/Mu. In terms of harvesting, it is suggested that the A. argyi var. argyi 'Qiai' should be harvested on "March 3 rd" and "May 5 th" of the lunar calendar. If it is the traditionally harvested at one time in May, the A. argyi var. argyi 'Qiai' should be divided into two parts: the middle and upper leaves, the middle and lower leaves, so as to achieve high quality and high price of A. argyi var. argyi 'Qiai' leaves and improve the economic benefits of A. argyi var. argyi 'Qiai' planting.


Assuntos
Artemisia , Medicamentos de Ervas Chinesas , Óleos Voláteis , Flavonoides , Folhas de Planta
11.
Zhongguo Zhong Yao Za Zhi ; 45(17): 4041-4050, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164387

RESUMO

To solve the problems of the unclear planting period and the traditional flat planting of Artemisia argyi var.argyi 'Qiai', such as the serious dead leaves in the middle and lower parts of the plant and the low yield and low quality in the field, the effects of different planting period and ridge pattern on yield and quality of A. argyi var.argyi 'Qiai' were studied. The results showed that the growth and development of A. argyi var.argyi 'Qiai' was better when planted in autumn and winter, and the ridge directions had little effect on the growth and yield of A. argyi var.argyi 'Qiai', while the ridge width had a significant effect. Compared the traditional wide ridge planting mode(the width of the ridge is 160 cm) with the ridge width of 80 cm, 60 cm and 40 cm, the results showed that the density per unit area, the number of effective plants, and the rate of dead leaves were decreased, while the number of productive leaves per plant, the number of lateral branches, and the total yield per plant were increased, the total yield was decreased. The output rates of moxa in the leaves of A. argyi var.argyi 'Qiai' decreased with the planting time postponed and the width of planting ridge increased. The contents of volatile oil, 1,8-oxido-p-menthane, camphor and borneol in A. argyi var.argyi 'Qiai' reach to the highest when planted in autumn and winter and the ridge width was 80 cm. In addition, the contents of total flavonoids, kaempferol, jeceosidin and eupatilin flavonoids in the leaves of A. argyi var.argyi 'Qiai' gradually decreased as the planting period postponed and the ridge width increased. The results show that the A. argyi var.argyi 'Qiai' should be planted in autumn and winter, and the double row ridge planting mode with width of 60-80 cm is more suitable for the cultivation and production of A. argyi var.argyi 'Qiai' in Qichun County of Hubei Province. This study will provide a theoretical basis and guidance for higher yield and quality in cultivation of A. argyi var.argyi 'Qiai' in Qichun county.


Assuntos
Artemisia , Medicamentos de Ervas Chinesas , Óleos Voláteis , Folhas de Planta
12.
Zhongguo Zhong Yao Za Zhi ; 45(17): 4057-4064, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164389

RESUMO

The chemical component information of samples was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS). The leaves and flosses of Artemisia argyi and A. stolonifera from different places, were distinguished by principal component analysis(PCA) and orthogonal partial least squares discriminant analysis(OPLS-DA). Then, compounds with significant differences(P<0.01) in abundance were screened out according to their VIP values and t-test. Eighteen components in all samples have been filtered and identified, including flavonoids and chlorogenic acids, the content of the 12 of which were measured by UPLC-UV, which are different in presence and content. Hispidulin in A. argyi is not detected in A. stolonifera. Schaftaside, isochlorogenic acid B, and isochlorogenic acid C are differential compounds of A. argyi and A. stolonifera leaves. Isochlorogenic acid A, isochlorogenic acid C and jaceosidin are differential compounds of A. argyi and A. stolonifera floss. There are significant differences in the contents of jaceosidin and schaftoside in the four famous A. argyi. In addition, the content of isochlorogenic acid A in wild A. stolonifera is higher than that in cultivated A. stolonifera. The results of the study successfully clarified the differences between A. stolonifera and A. argyi, and provided theoretical and data references for the further development and utilization of A. stolonifera.


Assuntos
Artemisia , Medicamentos de Ervas Chinesas , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Espectrometria de Massas
13.
Zhongguo Zhong Yao Za Zhi ; 45(17): 4081-4088, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164392

RESUMO

Jiuniucao in Qizhou, known as "Qiai", was precious and expensive in the Ming and Qing Dynasties. But the authentic plant of Jiuniucao is not mentioned in the Ben Cao Tu Jing and other medical books in the Song, Ming and Qing Dynasties. In history, mugwort leaf originates from many species of plants, Jiuniucao may be one of it. So this paper is to identify the original plant of Jiuniucao and clarify the historical origin of Jiuniucao and mugwort leaf. The textual research and geographical origin analysis of Jiuniucao in ancient literature was conducted. Then field investigation and sampling of Jiuniucao in Qizhou was proceeded, combing with feature comparison of Jiuniucao and Artemisia specimen in the Herbarium of Institute of Botany, Chinese Academy of Sciences. The study concluded that A. stolonifera is the authentic Jiuniucao for medical use. Jiuniucao was also an important original plant of mugwort leaf and it is worth further development and utilization.


Assuntos
Artemisia , Medicamentos de Ervas Chinesas , Livros , China , Humanos , Medicina Tradicional Chinesa , Projetos de Pesquisa
14.
Zhongguo Zhong Yao Za Zhi ; 45(17): 4071-4080, 2020 Sep.
Artigo em Zh | MEDLINE | ID: mdl-33164391

RESUMO

Moxa floss is the main material of moxibustion, which plays a therapeutic role through the thermal effect of combustion. In this paper, TG/DSC thermal analysis method was used to study the characteristic parameters of combustion heat of moxa floss produced in Qichun, and the thermal therapeutic effect and mechanism of moxibustion were studied through moxibustion OA animal model. The results show that the combustion process of moxa floss can be divided into three stages: drying, combustion oxidation and carbonization, and ash burnout. The combustion properties of moxa floss are between herbaceous and woody, and tend to be woody, with flammable, slow and lasting combustion characteristics. Moxibustion can relieve the pathological state of knee joint synovium to a certain extent, reduce knee joint swelling and blood stasis in OA rats, reduce interstitial edema, and improve local inflammation. The mechanism and target point of moxibustion treatment for OA may be up-regulating TRPM3 gene to activate ion channels, affecting calcium metabolism and reducing OA swelling degree; down-regulation of GAPDH affects glucose metabolism of knee synovial cells and mediates anti-inflammatory effect. Down-regulation of pain-related gene MMP24 is helpful to relieve OA pain. Up-regulation of CTNNB1 activates Wnt/ß-catenin signaling pathway and affects differentiation and regeneration of OA chondrocytes. This study reveals the pyrolysis characteristics of moxa floss for the first time and discusses the biological effect and possible mechanism of moxibustion heat, providing new ideas for the quality evaluation of moxa floss and the mechanism of moxibustion therapy.


Assuntos
Moxibustão , Osteoartrite , Animais , Modelos Animais de Doenças , Temperatura Alta , Oxirredução , Ratos
15.
Zhongguo Zhong Yao Za Zhi ; 45(19): 4606-4616, 2020 Oct.
Artigo em Zh | MEDLINE | ID: mdl-33164424

RESUMO

Prunus mume "Langmei" is a relict tree species, which fruit has good medicinal value. To understand the biosynthesis pathway of citric acid, the Illumina HiSeq XTen high-throughput sequencing technology was used to get the transcriptome from "Langmei". A total of 38 936 unigenes were obtained by assembling the fruit transcripts, of which 28 311 unigenes were successfully annotated in public databases, 15 193 unigenes were mapped to 265 KEGG metabolic pathways, and 18 908 unigenes were classified into 59 GO functional subclasses, 103 unigenes encoding 15 key enzymes involved in citric acid synthesis pathway were identified and analyzed. The structural model of citrate synthetase in "Langmei" showed that it was a homodimer and the secondary structure of each monomer was mainly composed of alpha helixes. Moreover, the residues in the active site of the citrate synthetase were highly conserved. This study provides a valuable resource for identifying candidate genes involved in the citric acid biosynthesis pathway, and will promote the development and sustainable utilization of genetic resources of "Langmei".


Assuntos
Ácido Cítrico , Frutas , Frutas/genética , Perfilação da Expressão Gênica , Sequenciamento de Nucleotídeos em Larga Escala , Transcriptoma
16.
Cell Tissue Res ; 377(3): 459-467, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31222501

RESUMO

Enteroendocrine cells are endocrine-like cells found in the luminal epithelia of the digestive tract. These cells have been described in most animal phyla. In echinoderms, the cells have been described mainly in organisms of the class Asteroidea (sea stars) and Holothuroidea (sea cucumbers). Here, we describe what is known about the enteroendocrine cells of the Echinodermata, including the cell types, their distribution in the digestive tract, their neuropeptide content and their regeneration and compare them to what has been found in other animal species, mainly in vertebrates. We also discuss the newly described view of enteroendocrine cells as chemical sensors of the intestinal lumen and provide some histological evidence that similar functions might be found within the echinoderms. Finally, we describe the temporal regeneration of the enteroendocrine cells in the holothurian intestine.


Assuntos
Equinodermos/anatomia & histologia , Células Enteroendócrinas , Trato Gastrointestinal , Animais , Células Enteroendócrinas/citologia , Células Enteroendócrinas/metabolismo , Trato Gastrointestinal/citologia , Trato Gastrointestinal/fisiologia , Neuropeptídeos/metabolismo , Regeneração
17.
Bioorg Med Chem Lett ; 29(10): 1177-1181, 2019 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-30922660

RESUMO

To develop PET tracers for imaging of Alzheimer's disease, a new carbon-11-labeled AMPAR allosteric modulator 4-cyclopropyl-7-(3-[11C]methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide ([11C]8) has been synthesized. The reference standard 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide (8) and its corresponding desmethylated precursor 4-cyclopropyl-7-(3-hydroxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide (9) were synthesized from 4-methoxyabiline and chlorosulfonyl isocyanate in eight and nine steps with 3% and 1% overall chemical yield, respectively. The target tracer [11C]8 was prepared from the precursor 9 with [11C]CH3OTf through O-[11C]methylation and isolated by HPLC combined with SPE in 10-15% radiochemical yield, based on [11C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the molar activity (AM) at EOB was 370-740 GBq/µmol with a total synthesis time of 35-40-minutes from EOB.


Assuntos
Doença de Alzheimer/diagnóstico por imagem , Compostos Radiofarmacêuticos/síntese química , Regulação Alostérica , Radioisótopos de Carbono/química , Cromatografia Líquida de Alta Pressão , Humanos , Marcação por Isótopo , Tomografia por Emissão de Pósitrons , Compostos Radiofarmacêuticos/análise , Compostos Radiofarmacêuticos/isolamento & purificação , Extração em Fase Sólida , Tiadiazinas/análise , Tiadiazinas/síntese química , Tiadiazinas/isolamento & purificação
18.
Bioorg Med Chem Lett ; 29(13): 1654-1659, 2019 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-31047754

RESUMO

To develop PET tracers for imaging of neuroinflammation, new carbon-11-labeled sEH/PDE4 dual inhibitors have been synthesized. The reference standard N-(4-methoxy-2-(trifluoromethyl)benzyl)benzamide (1) and its corresponding desmethylated precursor N-(4-hydroxy-2-(trifluoromethyl)benzyl)benzamide (2) were synthesized from (4-methoxy-2-(trifluoromethyl)phenyl)methanamine and benzoic acid in one and two steps with 84% and 49% overall chemical yield, respectively. The standard N-(4-methoxy-2-(trifluoromethyl)benzyl)-1-propionylpiperidine-4-carboxamide (MPPA, 4) and its precursor N-(4-hydroxy-2-(trifluoromethyl)benzyl)-1-propionylpiperidine-4-carboxamide (5) were synthesized from methyl 4-piperidinecarboxylate, propionyl chloride and (4-methoxy-2-(trifluoromethyl)phenyl)methanamine in two and three steps with 62% and 34% overall chemical yield, respectively. The target tracers N-(4-[11C]methoxy-2-(trifluoromethyl)benzyl)benzamide ([11C]1) and N-(4-[11C]methoxy-2-(trifluoromethyl)benzyl)-1-propionylpiperidine-4-carboxamide ([11C]MPPA, [11C]4) were prepared from their corresponding precursors 2 and 5 with [11C]CH3OTf through O-[11C]methylation and isolated by HPLC combined with SPE in 25-35% radiochemical yield, based on [11C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the molar activity (AM) at EOB was 370-740 GBq/µmol with a total synthesis time of 35-40-minutes from EOB.


Assuntos
Radioisótopos de Carbono/química , Inflamação/tratamento farmacológico , Doenças do Sistema Nervoso/tratamento farmacológico , Inibidores da Fosfodiesterase 4/uso terapêutico , Tomografia por Emissão de Pósitrons/métodos , Humanos , Inibidores da Fosfodiesterase 4/farmacologia
19.
Bioorg Med Chem Lett ; 29(12): 1476-1480, 2019 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-31005444

RESUMO

The reference standards halo-GSK1482160 (F-, Br-, and I-) and their corresponding precursors desmethyl-halo-GSK1482160 (F-, Br-, and I-) were synthesized from (S)-1-methyl-5-oxopyrrolidine-2-carboxylic acid or (S)-5-oxopyrrolidine-2-carboxylic acid and 2-halo-3-(trifluoromethyl)benzylamine (F-, Br-, and I-) in one step with 45-93% yields. The target tracers [11C]halo-GSK1482160 (F-, Br-, and I-) were prepared from desmethyl-halo-GSK1482160 (F-, Br-, and I-) with [11C]CH3OTf under basic conditions (NaOH-Na2CO3, solid, w/w 1:2) through N-[11C]methylation and isolated by HPLC combined with SPE in 40-50% decay corrected radiochemical yield. The radiochemical purity was >99%, and the molar activity (AM) at end of bombardment (EOB) was 370-740 GBq/µmol. The potency of halo-GSK1482160 (F-, Br-, and I-) in comparison with GSK1482160 (Cl-) was determined by a radioligand competitive binding assay using [11C]GSK1482160, and the binding affinity Ki values for halo-GSK1482160 (F-, Br-, and I-) and GSK1482160 (Cl-) are 54.2, 2.5, 1.9 and 3.1 nM, respectively.


Assuntos
Ensaio Radioligante/métodos , Compostos Radiofarmacêuticos/síntese química , Humanos
20.
Bioorg Med Chem Lett ; 28(13): 2234-2238, 2018 07 15.
Artigo em Inglês | MEDLINE | ID: mdl-29859907

RESUMO

The reference standards methyl 3-((2,2-difluoro-5H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]imidazol-6-yl)carbamoyl)benzoate (5a) and N-(2,2-difluoro-5H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]imidazol-6-yl)-3-methoxybenzamide (5c), and their corresponding desmethylated precursors 3-((2,2-difluoro-5H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]imidazol-6-yl)carbamoyl)benzoic acid (6a) and N-(2,2-difluoro-5H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]imidazol-6-yl)-3-hydroxybenzamide (6b), were synthesized from 5-amino-2,2-difluoro-1,3-benzodioxole and 3-substituted benzoic acids in 5 and 6 steps with 33% and 11%, 30% and 7% overall chemical yield, respectively. Carbon-11-labeled casein kinase 1 (CK1) inhibitors, [11C]methyl 3-((2,2-difluoro-5H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]imidazol-6-yl)carbamoyl)benzoate ([11C]5a) and N-(2,2-difluoro-5H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]imidazol-6-yl)-3-[11C]methoxybenzamide ([11C]5c), were prepared from their O-desmethylated precursor 6a or 6b with [11C]CH3OTf through O-[11C]methylation and isolated by HPLC combined with SPE in 40-45% radiochemical yield, based on [11C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the molar activity (MA) at EOB was 370-740 GBq/µmol with a total synthesis time of ∼40-min from EOB.


Assuntos
Benzimidazóis/síntese química , Benzoatos/síntese química , Caseína Quinase I/antagonistas & inibidores , Inibidores de Proteínas Quinases/síntese química , Compostos Radiofarmacêuticos/síntese química , Doença de Alzheimer/diagnóstico por imagem , Benzamidas/síntese química , Benzamidas/química , Benzimidazóis/química , Benzoatos/química , Radioisótopos de Carbono , Interações Hidrofóbicas e Hidrofílicas , Tomografia por Emissão de Pósitrons , Inibidores de Proteínas Quinases/química , Compostos Radiofarmacêuticos/química
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