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1.
Zhongguo Zhong Yao Za Zhi ; 45(7): 1620-1626, 2020 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-32489041

RESUMO

By analyzing the effects of light intensity on the growth, physiological and biochemical characteristics of Chrysanthemum indicum, the light intensity suitable for the growth of Ch. indicum was revealed, which provided a reference for the planting of Ch. indicum. There were five treatment groups of Ch. indicum, which was planted under 100%, 80%, 60%, 40% and 20% all natural light intensity conditions, respectively. In the meantime, these indicators of photosynthetic physiology, such as relative growth, photosynthetic pigment content, photosynthetic parameters, and chlorophyll fluorescence parameters etc. were measured in the peak period of growth of Ch. indicum as well as related indicators of the protective enzyme system, and the ultrastructure of chloroplast was observed with the use of transmission electron microscope technique. In our study, the results showed that the leaves of Ch. indicum occurred yellow phenomenon in different degrees when Ch. indicum was placed at more than 80% of the total natural light intensity condition, the height and stem diameter of plant reached the maximum at 60% of the total natural light intensity. More importantly, the number of branches of Ch. indicum was significantly increased under the total natural light intensity of more than 60%. Both the content of photosynthetic pigment and net photosynthetic rate were negatively correlated with light intensity, while photosynthetic parameters and chlorophyll fluorescence parameters showed a trend of rising first and then decreasing with the decrease of light intensity. The physiological indexes of Ch.indicum including stomatal conductivity, intracellular CO_2 concentration, transpiration rate, water use efficiency and actual photochemical quantum yield of PS Ⅱ had been determined, and the results showed that all of them were at the highest level under 60% total natural light intensity condition. The chloroplast structure of Ch. indicum was not obviously abnormal under 60% and 80% total natural light intensity treatments, but the stroma lamella was broken under 100% total natural light intensity, and not only the number of chloroplast, but also the number and volume of starch grains were decreased significantly under 20% and 40% total natural light intensity. With the decrease of light intensity, the enzymes activities of SOD and CAT decreased, the activity of POD increased in the early stage and decreased in the later stage, and the content of MDA showed a decreasing trend. The analysis of results indicated that the Ch. indicum can grow under 20%-100% total natural light intensity, but the best growth condition was under 60% total natural light intensity.


Assuntos
Chrysanthemum , Clorofila , Cloroplastos , Luz , Fotossíntese , Folhas de Planta
2.
Angew Chem Int Ed Engl ; 59(46): 20604-20611, 2020 11 09.
Artigo em Inglês | MEDLINE | ID: mdl-32700406

RESUMO

Signal transduction in living systems is the conversion of information into a chemical change, and is the principal process by which cells communicate. In nature, these functions are encoded in non-equilibrium (bio)chemical reaction networks (CRNs) controlled by enzymes. However, man-made catalytically controlled networks are rare. We incorporated catalysis into an artificial fuel-driven out-of-equilibrium CRN, where the forward (ester formation) and backward (ester hydrolysis) reactions are controlled by varying the ratio of two organocatalysts: pyridine and imidazole. This catalytic regulation enables full control over ester yield and lifetime. This fuel-driven strategy was expanded to a responsive polymer system, where transient polymer conformation and aggregation are controlled through fuel and catalyst levels. Altogether, we show that organocatalysis can be used to control a man-made fuel-driven system and induce a change in a macromolecular superstructure, as in natural non-equilibrium systems.

3.
Zhongguo Zhong Yao Za Zhi ; 44(15): 3246-3252, 2019 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-31602879

RESUMO

Inula japonica was used as the research object, "3414" fertilization experiment were conducted to study the effects of nitrogen,phosphorus and potassium formula fertilizer on the growth and chemical composition content of I. japonica. The characteristics of fertilizer requirement were preliminarily revealed and the study provided fertilization guidance for artificial cultivation of I. japonica. The results showed that different nitrogen,phosphorus and potassium formula fertilizers had significant effects on plant morphology,physiological and biochemical indexes,dry matter accumulation and chemical composition content. The growth indexes and chemical components of I. japonica showed an upward trend with the increase of fertilization amount,especially the nitrogen fertilizer was the most significant. The indicators were analyzed by membership function. After comprehensive evaluation,the optimal nitrogen,phosphorus and potassium formula fertilization level was N3 P2 K2,namely high level nitrogen fertilizer,medium level phosphorus fertilizer and potassium fertilizer. I. japonica is a high fertilizer demand plant,and the rational fertilization scheme is " applying nitrogen fertilizer again and applying phosphorus and potassium fertilizer properly".


Assuntos
Fertilizantes , Inula/crescimento & desenvolvimento , Nitrogênio/química , Fósforo/química , Potássio/química , Inula/química
4.
Zhongguo Zhong Yao Za Zhi ; 43(8): 1579-1587, 2018 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-29751703

RESUMO

The contents of 22 kinds of mineral elements in different parts of Changium smyrnioides and in the rhizosphere soil of 10 different populations were determined by microwave digestion-inductively coupled plasma atomic emission spectrometry (ICP-AES). The characteristics of mineral elements in the plants and the soil of main distribution area of Ch. smyrnioides was analyzed and the mechanism of the quality formation of Ch. smyrnioides was explored to provide the basis for the quality evaluation and cultivation regulation of Ch. smyrnioides.The results showed that the quality of soil environment was better in the main distribution area of Ch. smyrnioides, the content of trace elements was higher, the contents of P and K were lower and the contents of mineral elements in the soil of each distribution area was significantly different. The three elements of Se, P and K are significantly accumulated in the root of Ch. smyrnioides. There were significant differences in the total contents of mineral elements in the roots of Ch. smyrnioides in different producing areas. The contents of mineral elements in different parts of Ch. smyrnioides were significantly different. Ch.smyrnioides of the main distribution area of Ch. smyrnioides belonged to the safety level, the distribution of mineral elements in the plants can be used as an indicator of the quality of medicinal herbs.


Assuntos
Apiaceae , Plantas Medicinais , Oligoelementos , Minerais , Rizosfera , Solo
5.
Zhongguo Zhong Yao Za Zhi ; 43(12): 2480-2488, 2018 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-29950064

RESUMO

The effects of four kinds of different plant populations on the soil physical and chemical properties and soil enzyme activities of Salvia miltiorrhiza were analyzed by setting up four kinds of mixed planting groups, such as S. miltiorrhiza and Cassia obtusifolia, Capsicum annuum, Perilla frutescens and Zea mays. And through the root isolation treatment, we preliminarily explored the formation mechanism of the four kinds of matching plants of soil physical and chemical properties and soil enzyme activities of S. miltiorrhiza, and chose the matching plants suitable for the establishment of the compound population with S. miltiorrhiza,and provided the basis for constructing high efficiency compound planting pattern of S. miltiorrhiza. The results showed that there were significant differences in soil physical and chemical properties and soil enzyme activitiesof Salvia miltiorrhiza in different compound population mixed.The combination of C. obtusifolia, P. frutescens, Z. mays and S. miltiorrhiza mixed planting were all reduced the soil cation exchange capacity and soil enzyme activities, and increased the soil electric conductivity. The compound planting of P. frutescens and S. miltiorrhiza increased the soil cation exchange capacity and soil enzyme activities, and reduced the soil electric conductivity. Therefore,The compound planting population of P. frutescens and S. miltiorrhiza is conducive to improve soil physical and chemical properties and increase soil microbial activity, which is the best collocation species of S. miltiorrhiza.


Assuntos
Enzimas/química , Salvia miltiorrhiza/crescimento & desenvolvimento , Microbiologia do Solo , Solo/química
6.
Zhongguo Zhong Yao Za Zhi ; 43(9): 1818-1824, 2018 May.
Artigo em Chinês | MEDLINE | ID: mdl-29902891

RESUMO

The effects of four kinds of different plant populations on the morphology, the dry matter accumulation, active ingredient content and antioxidant activty in vitro of Salvia miltiorrhiza were analyzed by setting up four kinds of mixed planting groups, such as S. miltiorrhiza and Cassia obtusifolia, Capsicum annuum, Perilla frutescens and Zea mays. And through the root isolation treatment, we preliminarily explored the formation mechanism of the four kinds of matching plants of the yield and quality of S. miltiorrhiza, and chose the matching plants suitable for the establishment of the compound population with S. miltiorrhiza,and provided the basis for constructing high efficiency compound planting pattern of S. miltiorrhiza. The results showed that there were significant differences in plant morphology, dry matter accumulation of root, active ingredient content and antioxidant activty in vitro of S. miltiorrhiza in different compound population mixed. The growth and yield of S. miltiorrhiza were unfavorable to the combination planting of Cassia obtusifolia, Z. mays and Salvia miltiorrhiza.The compound planting of P. frutescens and S. miltiorrhiza significantly promoted the growth of S. miltiorrhiza, but significantly reduced the quality of S. miltiorrhiza.The yield and quality of S. miltiorrhiza were significantly improved by the combination of C. annuum and S. miltiorrhiza. Therefore, among the four plants of C. obtusifolia, C. annuum, P. frutescens, and Z. mays, the P. frutescens of Solanaceae is the best matching species for the construction of compound planting group with S. miltiorrhiza.


Assuntos
Capsicum , Salvia miltiorrhiza , Raízes de Plantas
7.
Anesth Analg ; 125(6): 2123-2133, 2017 12.
Artigo em Inglês | MEDLINE | ID: mdl-28787346

RESUMO

BACKGROUND: The spared nerve injury (SNI) model is a new animal model that can mimic several characteristics of clinical neuropathic pain. Opioids are recommended as treatment of neuropathic pain. Therefore, the present study was conducted to investigate the antinociceptive effects of endomorphin-1 (EM-1) and endomorphin-2 (EM-2) given centrally and peripherally in the SNI model of neuropathic pain in mice. METHODS: The SNI model was made in mice by sparing the sural nerve intact, when the other 2 of 3 terminal branches of the sciatic nerve (common peroneal and tibial nerves) were tightly ligated and cut. Von Frey monofilaments were used to measure the SNI-induced mechanical allodynia-like behavior. The antiallodynic effects of EM-1 and EM-2 were determined after central and peripheral administration in the SNI model of neuropathic pain. Also, the specific opioid receptor antagonists were used to determine the opioid mechanisms of EMs involved in neuropathic pain. Values were expressed as the mean ± standard deviation. RESULTS: Our results showed that the SNI mice developed prolonged mechanical allodynia-like behavior in ipsilateral paw after surgery, with the withdrawal threshold value being 0.061 ± 0.02 g after 14 days. EM-1 and EM-2 produced significant antiallodynic effects in ipsilateral paw after intracerebroventricular (i.c.v.) administration, more effective than that of morphine. The peak withdrawal thresholds of 10 nmol EM-1 and EM-2 determined at 5 minutes after injection were 0.92 ± 0.36 and 0.87 ± 0.33 g, respectively, higher than that of morphine (0.46 ± 0.20 g). Moreover, both EMs (10 nmol, i.c.v.) exerted significant antiallodynic effects in the contralateral paw, whereas no significant antinociceptive activity was seen after i.c.v. administration of morphine with equimolar dose. It was noteworthy that EM-1 and EM-2 produced antinociception through distinct µ1- and µ2-opioid receptor subtypes, and the EM-2-induced antiallodynia contained an additional component that was mediated by the release of endogenous dynorphin A, acting on κ-opioid receptor. In addition, the antiallodynic activities of peripheral administration of EM-1, EM-2, and morphine were also investigated. Intraplantar, but not subcutaneous administration of EM-1 and EM-2 also exhibited potent antinociception, establishing the peripheral and local effects. Both µ1- and µ2-opioid receptor subtypes, but not the δ- or κ-opioid receptors were involved in the peripheral antiallodynia of EMs. CONCLUSIONS: The present investigation demonstrated that both EM-1 and EM-2 given centrally and peripherally produced potent antiallodynic activities in SNI mice, and differential opioid mechanisms were involved.


Assuntos
Analgésicos Opioides/administração & dosagem , Hiperalgesia/tratamento farmacológico , Neuralgia/tratamento farmacológico , Oligopeptídeos/administração & dosagem , Nervo Sural/efeitos dos fármacos , Animais , Modelos Animais de Doenças , Hiperalgesia/patologia , Masculino , Camundongos , Neuralgia/patologia , Medição da Dor/efeitos dos fármacos , Medição da Dor/métodos , Nervo Fibular/efeitos dos fármacos , Nervo Fibular/patologia , Nervo Sural/patologia , Nervo Tibial/efeitos dos fármacos , Nervo Tibial/patologia , Resultado do Tratamento
8.
Pharm Biol ; 55(1): 581-589, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27937676

RESUMO

CONTEXT: Changium smyrnioides Wolff (Apiaceae) is an endangered medicinal plant with numerous pharmacological uses. OBJECTIVE: To investigate the effect of light intensity levels on the growth and accumulation of secondary metabolites of C. smyrnioides, cultivated seedlings were subjected to different relative light intensities via sun-shading. MATERIALS AND METHODS: Changium smyrnioides seedlings were subjected to five irradiance treatments (100, 60.54, 44.84, 31.39, and 10.56% sunlight) in glasshouse for 9 months. Enzymatic and non-enzymatic antioxidants with spectrophotometric method, photosynthetic parameters with Li-6400XT, dry matter accumulation and active component contents in the root with spectrophotometric and HPLC method were analyzed. RESULTS: With an increase in relative light intensity levels, activities of enzymatic and non-enzymatic antioxidants, and malondialdehyde (MDA) contents were increased overall, while net photosynthetic rate (Pn) and dry matter accumulation patter first increased and then declined. The highest net photosynthetic rate (30.68 µmol/m2·s) and dry root weight (5.07 g) were achieved under 60.54% sunlight. Lower relative light intensity levels stimulated the accumulation levels of bioactive compounds in the roots so that the highest contents of mannitol (1.35%) and choline (405.58 µg/g) were recorded under 31.39% sunlight, and the highest polysaccharide content (10.80%) were achieved under 44.84% sunlight. With a decrease in the relative light intensity levels, the water-soluble component content increased first and then decreased. DISCUSSION AND CONCLUSION: The results revealed that 31.39-60.54% sunlight serve as appropriate relative light intensity conditions for cultivated C. smyrnioides.


Assuntos
Apiaceae/efeitos dos fármacos , Raízes de Plantas/efeitos da radiação , Plântula/efeitos da radiação , Luz Solar , Antioxidantes/metabolismo , Apiaceae/crescimento & desenvolvimento , Apiaceae/metabolismo , Biomassa , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta à Radiação , Enzimas/metabolismo , Fotossíntese/efeitos da radiação , Fitoterapia , Proteínas de Plantas/metabolismo , Raízes de Plantas/crescimento & desenvolvimento , Raízes de Plantas/metabolismo , Plantas Medicinais , Polissacarídeos/metabolismo , Plântula/crescimento & desenvolvimento , Plântula/metabolismo , Espectrofotometria , Fatores de Tempo , Água/metabolismo
9.
Zhongguo Zhong Yao Za Zhi ; 40(17): 3391-4, 2015 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-26978978

RESUMO

There is time-honored history and culture of medicinal plant cultivation in China. In the present review, the medicinal plant cultivation history in china was summarized, its current situation and question were analyzed, and the prospects of medicinal plant cultivation research were pointed out, with the purpose of accelerating the growth of medicinal plant cultivation research.


Assuntos
Medicamentos de Ervas Chinesas/química , Materia Medica/química , Materia Medica/economia , Plantas Medicinais/crescimento & desenvolvimento , China , Medicamentos de Ervas Chinesas/história , História do Século XV , História do Século XVI , História do Século XVII , História do Século XVIII , História do Século XIX , História do Século XX , História do Século XXI , História Antiga , História Medieval , Materia Medica/história , Medicina Tradicional Chinesa/história , Medicina Tradicional Chinesa/tendências , Plantas Medicinais/química
10.
Zhongguo Zhong Yao Za Zhi ; 40(22): 4389-94, 2015 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-27097412

RESUMO

Twelve populations of Inula lineariifolia were used as materials to measure morphological characteristics, photosynthetic parameters and chemical constituents. It aims to provide a theoretical basis for germplasm resources evaluation. The results showed that I. lineariifolia had relatively rich morphological diversity, there were significant differences of morphological characteristics, photosynthetic parameters and chemical constituents among populations. There was positive correlation on morphological characteristics and P(n). Twelve populations were divided into three-type. The three populations of Xuyi, Mingguang and Fengyang were of narrower-longer leaf, bigger biomass,better photosynthetic and higher chemical constituents. Then they were classified for a similar group. It proved that the three populations were more suitable for cultivation and promotion.


Assuntos
Inula/crescimento & desenvolvimento , Inula/metabolismo , Fotossíntese , Biomassa , China , Flores/química , Flores/crescimento & desenvolvimento , Flores/metabolismo , Inula/química , Inula/classificação , Folhas de Planta/química , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/metabolismo , Caules de Planta/química , Caules de Planta/crescimento & desenvolvimento , Caules de Planta/metabolismo
11.
Zhongguo Zhong Yao Za Zhi ; 40(23): 4585-90, 2015 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-27141667

RESUMO

In order to explore reasonable artificial cultivation pattern of Thesium chinense, the biological characteristics and nutrients change in the process of winter dormancy of T. chinense was studied. The phenological period of T. chinense was observed by using fixed-point notation and the starch grains changes were determined dynamically by PAS-vanadium iron hematoxylin staixjing method. Soluble sugar and starch content were measured by anthrone-sulfuric acid method and amylase activity was determined by DN'S method. The results showed that the normal life cycle of T. chinense was two years. T. chinense was growing by seed in the first year, but growing by the root neck bud in the second year. During the process of dormancy, starch and soluble sugar could mutual transformation in different periods. T. chinense had sufficient carbohydrate to maintain growth and also a lot of small molecules to improve their ability to fight against adversity.


Assuntos
Dormência de Plantas , Santalaceae/crescimento & desenvolvimento , Folhas de Planta/química , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/metabolismo , Raízes de Plantas/química , Raízes de Plantas/crescimento & desenvolvimento , Raízes de Plantas/metabolismo , Caules de Planta/química , Caules de Planta/crescimento & desenvolvimento , Caules de Planta/metabolismo , Santalaceae/química , Santalaceae/metabolismo , Estações do Ano , Amido/análise , Amido/metabolismo
12.
Zhongguo Zhong Yao Za Zhi ; 40(4): 624-8, 2015 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-26137680

RESUMO

In order to establish the quality classification criteria of Paeonia suffruticosa seeds, thirty-one batches of P. suffruticosa seeds from different provenances were selected. The seed rooting rate, seed germination rate, seed purity, seed viability, 1,000-seed weight and moisture content were determined and analyzed through SPSS 20.0 software. Seed rooting rate, seed germination rate and seed purity were selected as the main index for classification, while 1,000-seed weight, seed viability and moisture content could be used as important references. The seed quality grading of P. suffruticosa was set as three grades. The seed quality of each grade should meet following requirements: For the first grade seeds, seed rooting rate ≥ 80%, seed germination rate ≥ 80%, seed purity ≥ 90%, seed viability ≥ 80%, 1,000-seed weight ≥ 250 g, moisture content, ≤ 10. For the second grade seeds, seed rooting rate ≥ 50%, seed germination rate ≥ 60%, seed purity ≥ 70%, seed viability ≥ 75%, 1,000-seed weight ≥ 225 g, moisture content ≤ 10. For the third grade seeds, seed rooting rate ≥ 20%, seed germination rate ≥ 45%, seed purity ≥ 60%, seed viability ≥ 45%, 1,000-seed weight ≥ 205 g, moisture content ≤ 10. The quality classification criteria of P. suffruticosa seeds have been initially established.


Assuntos
Medicamentos de Ervas Chinesas/química , Paeonia/química , Sementes/classificação , China , Germinação , Paeonia/classificação , Paeonia/crescimento & desenvolvimento , Sementes/química , Sementes/crescimento & desenvolvimento
13.
Zhongguo Zhong Yao Za Zhi ; 39(21): 4180-5, 2014 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-25775790

RESUMO

In order to optimize the testing methods for Paeonia suffruticosa seed quality, and provide basis for establishing seed testing rules and seed quality standard of P. suffruticosa. The seed quality of P. suffruticosa from different producing areas was measured based on the related seed testing regulations. The seed testing methods for quality items of P. suffruticosa was established preliminarily. The samples weight of P. suffruticosa was at least 7 000 g for purity analysis and was at least 700 g for test. The phenotypic observation and size measurement were used for authenticity testing. The 1 000-seed weight was determined by 100-seed method, and the water content was carried out by low temperature drying method (10 hours). After soaking in distilled water for 24 h, the seeds was treated with different temperature stratifications of day and night (25 degrees C/20 degrees C, day/night) in the dark for 60 d. After soaking in the liquor of GA3 300 mg x L(-1) for 24 h, the P. suffruticos seeds were cultured in wet sand at 15 degrees C for 12-60 days for germination testing. Seed viability was tested by TlC method.


Assuntos
Paeonia/crescimento & desenvolvimento , Sementes/fisiologia , Germinação , Luz , Controle de Qualidade , Temperatura
14.
Zhongguo Zhong Yao Za Zhi ; 39(23): 4544-7, 2014 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-25911798

RESUMO

To separate and identify chemical signals which induce Thesium chinense haustorium formation, the components of T. chinense roots secretion collected with XAD-4 resin were detected by GC-MS. The effect of DMBQ as exogenous signals to induce haustorium formation in T. chinense was studied. Fifty-three compounds of 9 types had been detected, including hydrocarbons, esters, organic acids, ketones, alcohols, nitrogen containing compounds, phenolic acids, aldehyde and quinine. It is worth noting that the 2, 5-di-tert-butyl-1,4-benzoquinone has the core structure of 1,4-benzoquinone, which may play an important role in the parasitic relationship of Prunella vulgaris and T. chinense: DMBQ worked effectively on inducing haustoria, but induction effects vary widely in different concentrations. DMBQ with the concentration of 1 µmol x L(-1) showed the best effect of the inducing ability with a ratio of 110.52 when treated to induce haustoria.


Assuntos
Magnoliopsida/química , Raízes de Plantas/química , Cromatografia Gasosa-Espectrometria de Massas , Interações Hospedeiro-Parasita , Magnoliopsida/fisiologia , Raízes de Plantas/fisiologia , Prunella/química , Prunella/fisiologia
15.
Peptides ; 171: 171116, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37951356

RESUMO

Previously, we have investigated three C-terminal esterified endomorphin-2 (EM-2) analogs EM-2-Me, EM-2-Et and EM-2-Bu with methyl, ethyl and tert-butyl ester modifications, respectively. These analogs produced significant antinociception in acute pain at the spinal and supraspinal levels, with reduced tolerance and gastrointestinal side effects. The present study was undertaken to determine the analgesic effects and opioid mechanisms of these three analogs in the formalin pain test. Our results demonstrated that intracerebroventricular (i.c.v.) administration of 0.67-20 nmol EM-2 analogs EM-2-Me, EM-2-Et and EM-2-Bu produced dose-dependent antinociceptive effects in both phase Ⅰ and phase Ⅱ of formalin pain. EM-2-Me and EM-2-Bu displayed more potent antinociception than morphine. Especially, EM-2-Bu exhibited the highest antinociception in phase Ⅱ of formalin pain, with the ED50 value being 2.1 nmol. Naloxone (80 nmol, i.c.v.) completely antagonized the antinociceptive effects of EM-2-Me, EM-2-Et and EM-2-Bu (20 nmol, i.c.v.) in both phase I and phase Ⅱ of formalin pain, suggesting a central opioid mechanism. Nevertheless, the antinociception induced by EM-2-Me might be involved in the release of dynorphin A, which subsequently acted on κ- opioid receptor. EM-2-Bu produced the antinociception probably by the direct activation of both µ- and δ-opioid receptors. EM-2-Me, EM-2-Et and EM-2-Bu also produced significant analgesic effects after peripheral administration, and the central opioid receptors were involved. Furthermore, EM-2-Bu had no influence on the locomotor activity after i.c.v. injection. The present investigation demonstrated that C-terminal esterified modifications of EM-2 will be beneficial for developing novel therapeutics in formalin pain.


Assuntos
Analgésicos Opioides , Dor , Animais , Camundongos , Analgésicos Opioides/farmacologia , Esterificação , Mercaptoetanol , Dor/tratamento farmacológico , Receptores Opioides , Receptores Opioides kappa , Receptores Opioides mu/metabolismo , Relação Dose-Resposta a Droga
17.
Br J Pharmacol ; 181(8): 1268-1289, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37990825

RESUMO

BACKGROUND AND PURPOSE: Endomorphins have shown great promise as pharmaceutics for the treatment of pain. We have previously confirmed that novel endomorphin analogues CEMR-1 and CEMR-2 behaved as potent µ agonists and displayed potent antinociceptive activities at the supraspinal and peripheral levels. The present study was undertaken to evaluate the antinociceptive properties of CEMR-1 and CEMR-2 following intrathecal (i.t.) administration. Furthermore, their antinociceptive tolerance and opioid-like side effects were also determined. EXPERIMENTAL APPROACH: The spinal antinociceptive effects of CEMR-1 and CEMR-2 were determined in a series of pain models, including acute radiant heat paw withdrawal test, spared nerve injury-induced neuropathic pain, complete Freund's adjuvant-induced inflammatory pain, visceral pain and formalin pain. Antinociceptive tolerance was evaluated in radiant heat paw withdrawal test. KEY RESULTS: Spinal administration of CEMR-1 and CEMR-2 produced potent and prolonged antinociceptive effects in acute pain. CEMR-1 and CEMR-2 may produce their antinociception through distinct µ receptor subtypes. These two analogues also exhibited significant analgesic activities in neuropathic, inflammatory, visceral and formalin pain at the spinal level. It is noteworthy that CEMR-1 showed non-tolerance-forming analgesic properties, while CEMR-2 exhibited substantially reduced antinociceptive tolerance. Furthermore, both analogues displayed no or reduced side effects on conditioned place preference response, physical dependence, locomotor activity and gastrointestinal transit. CONCLUSIONS AND IMPLICATIONS: The present investigation demonstrated that CEMR-1 and CEMR-2 displayed potent and long-lasting antinociception with a favourable side effect profile at the spinal level. Therefore, CEMR-1 and CEMR-2 might serve as promising analgesic compounds with minimal opioid-like side effects.


Assuntos
Neuralgia , Dor Visceral , Humanos , Analgésicos Opioides/farmacologia , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Neuralgia/tratamento farmacológico , Dor Visceral/tratamento farmacológico , Receptores Opioides mu/agonistas , Formaldeído/uso terapêutico
18.
Eur J Pharmacol ; 978: 176775, 2024 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-38925288

RESUMO

The development of multitarget opioid drugs has emerged as an attractive approach for innovative pain management with reduced side effects. In the present study, a novel hybrid peptide BNT12 containing the opioid and neurotensin (NT)-like fragments was synthesized and pharmacologically characterized. In acute radiant heat paw withdrawal test, intracerebroventricular (i.c.v.) administration of BNT12 produced potent antinociception in mice. The central antinociceptive activity of BNT12 was mainly mediated by µ-, δ-opioid receptor, neurotensin receptor type 1 (NTSR1) and 2 (NTSR2), supporting a multifunctional agonism of BNT12 in the functional assays. BNT12 also exhibited significant antinociceptive effects in spared nerve injury (SNI)-neuropathic pain, complete Freund's adjuvant (CFA)-induced inflammatory pain, acetic acid-induced visceral and formalin-induced pain after i.c.v. administration. Furthermore, BNT12 exhibited substantial reduction of acute antinociceptive tolerance, shifted the dose-response curve to the right by only 1.3-fold. It is noteworthy that BNT12 showed insignificant chronic antinociceptive tolerance at the supraspinal level. In addition, BNT12 exhibited reduced or no opioid-like side effects on conditioned place preference (CPP) response, naloxone-precipitated withdrawal response, acute hyperlocomotion, motor coordination, gastrointestinal transit, and cardiovascular responses. The present investigation demonstrated that the novel hybrid peptide BNT12 might serve as a promising analgesic candidate with limited opioid-like side effects.


Assuntos
Neurotensina , Receptores de Neurotensina , Animais , Masculino , Camundongos , Neurotensina/análogos & derivados , Neurotensina/farmacologia , Neurotensina/química , Receptores de Neurotensina/metabolismo , Receptores de Neurotensina/agonistas , Analgésicos/farmacologia , Analgésicos/química , Analgésicos/administração & dosagem , Analgésicos Opioides/farmacologia , Analgésicos Opioides/administração & dosagem , Tolerância a Medicamentos , Dor/tratamento farmacológico
19.
Cell Prolif ; 57(4): e13564, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37853840

RESUMO

'Human neural stem cells' jointly drafted and agreed upon by experts from the Chinese Society for Stem Cell Research, is the first guideline for human neural stem cells (hNSCs) in China. This standard specifies the technical requirements, test methods, test regulations, instructions for use, labelling requirements, packaging requirements, storage requirements, transportation requirements and waste disposal requirements for hNSCs, which is applicable to the quality control for hNSCs. It was originally released by the China Society for Cell Biology on 30 August 2022. We hope that publication of the guideline will facilitate institutional establishment, acceptance and execution of proper protocols, and accelerate the international standardization of hNSCs for clinical development and therapeutic applications.


Assuntos
Células-Tronco Neurais , Transplante de Células-Tronco , Humanos , Diferenciação Celular , China
20.
Cell Prolif ; 57(4): e13563, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37881164

RESUMO

Human midbrain dopaminergic progenitors (mDAPs) are one of the most representative cell types in both basic research and clinical applications. However, there are still many challenges for the preparation and quality control of mDAPs, such as the lack of standards. Therefore, the establishment of critical quality attributes and technical specifications for mDAPs is largely needed. "Human midbrain dopaminergic progenitor" jointly drafted and agreed upon by experts from the Chinese Society for Stem Cell Research, is the first guideline for human mDAPs in China. This standard specifies the technical requirements, test methods, inspection rules, instructions for usage, labelling requirements, packaging requirements, storage requirements, transportation requirements and waste disposal requirements for human mDAPs, which is applicable to the quality control for human mDAPs. It was originally released by the China Society for Cell Biology on 30 August 2022. We hope that the publication of this guideline will facilitate the institutional establishment, acceptance and execution of proper protocols, and accelerate the international standardization of human mDAPs for clinical development and therapeutic applications.


Assuntos
Neurônios Dopaminérgicos , Mesencéfalo , Humanos , China , Neurônios Dopaminérgicos/metabolismo
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