气相色谱法测定复方丁香吸入剂中有效成分的含量

以正十一醇为内标，用程序升温填充柱ＧＣ法同时测定复方丁香吸入剂中的丁香酚、冰片及薄荷醇的含量。本法采用ＦＩＤ为检测器，色谱柱为１０％ＰＥＧ－２０ＭＣｈｒｏｍｏｓｏｂＷＡＷ－ＤＭＣＳ８０～１００目。２ｍ×４ｍｍ（Ｉ．Ｄ．）不锈钢填充柱，柱室温度程序为１４０℃（６ｍｉｎ）３℃／ｍｉｎ→１７５℃（１０ｍｉｎ）。样品用乙酸乙酯超声振荡提取３０ｍｉｎ，过滤后便可进样分析。     

GC法测定丁蔻理中丸中丁香酚的含量

目的：采用气相色谱法测定丁蔻理中丸中丁香酚的含量。方法：气相色谱法，聚乙二醇(PEG)—20M柱，柱长2m，内径4mm；柱温180℃，进样器220℃，FID检测器；柱头压力：150kPa，内标物：桂皮醛。结果：所测丁香酚与其它组分具有良好的分离效果，线性范围为8.92～71．36μg／ml，平均回收率为99．9％，RSD为1．28％(n=5)。结论：本方法简便、快速，结果准确，可用于丁蔻理中丸中丁香酚的含量测定。     

LC/MSn鉴定丁香酚布洛芬酯在大鼠尿中的主要代谢产物

 目的研究鉴定丁香酚布洛芬酯在大鼠体内的代谢行为。方法选择健康Wistar大鼠3只单剂量20mg·kg^-1尾静脉给药丁香酚布洛芬酯后,收集0～12h尿样。将尿样经SPEC₁₈固相萃取柱纯化后,采用LC/MSn方法对尿中的待测的代谢产物进行选择离子监测(SIM)和多级全扫描质谱分析(MSn)。结果在尿中首次检测到丁香酚布洛芬酯的7种代谢产物,其中包括1种Ⅰ相代谢产物和6种Ⅱ相代谢产物。结论丁香酚布洛芬酯在大鼠体内主要先水解成丁香酚和布洛芬,经进一步代谢与葡萄糖醛酸结合。     

复方丁香洗剂中丁香酚和苦参碱的含量测定

目的建立紫外分光光度法及酸性染料比色法测定复方丁香洗剂中丁香酚和苦参碱的含量.方法丁香酚、苦参碱均可与氢氧化钠成盐而溶于碱,易于分离,前者于(296±2)nm波长处测定吸收度,后者与溴麝香草酚蓝络合后于(415±2)nm波长处测定吸收度.结果丁香酚平均回收率为98.30%,RSD为0.76%,在10.26～23.95 mg·L-1范围有良好的线性关系(r=0.999 8);苦参碱平均回收率为98.63%,RSD为0.83%,在3～10.5 mg·L-1范围线性关系良好(r=0.999 6).结论本方法准确,灵敏度好,可用于复方丁香洗剂或中药制剂中的丁香酚、苦参碱含量测定.     

Inhibition of Nav1.7 channels by methyl eugenol as a mechanism underlying its antinociceptive and anesthetic actions

Aim:

Methyl eugenol is a major active component extracted from the Chinese herb Asari Radix et Rhizoma, which has been used to treat toothache and other pain. Previous in vivo studies have shown that methyl eugenol has anesthetic and antinociceptive effects. The aim of this study was to determine the possible mechanism underlying its effect on nervous system disorders.

Methods:

The direct interaction of methyl eugenol with Na⁺ channels was explored and characterized using electrophysiological recordings from Na_v1.7-transfected CHO cells.

Results:

In whole-cell patch clamp mode, methyl eugenol tonically inhibited peripheral nerve Na_v1.7 currents in a concentration- and voltage-dependent manner, with an IC₅₀ of 295 μmol/L at a −100 mV holding potential. Functionally, methyl eugenol preferentially bound to Na_v1.7 channels in the inactivated and/or open state, with weaker binding to channels in the resting state. Thus, in the presence of methyl eugenol, Na_v1.7 channels exhibited reduced availability for activation in a steady-state inactivation protocol, strong use-dependent inhibition, enhanced binding kinetics, and slow recovery from inactivation compared to untreated channels. An estimation of the affinity of methyl eugenol for the resting and inactivated states of the channel also demonstrated that methyl eugenol preferentially binds to inactivated channels, with a 6.4 times greater affinity compared to channels in the resting state. The failure of inactivated channels to completely recover to control levels at higher concentrations of methyl eugenol implies that the drug may drive more drug-bound, fast-inactivated channels into drug-bound, slow-inactivated channels.

Conclusion:

Methyl eugenol is a potential candidate as an effective local anesthetic and analgesic. The antinociceptive and anesthetic effects of methyl eugenol result from the inhibitory action of methyl eugenol on peripheral Na⁺ channels.     

Antibacterial Effects of Cinnamon: From Farm to Food,Cosmetic and Pharmaceutical Industries

Herbs and spices have been used since ancient times, because of their antimicrobial properties increasing the safety and shelf life of food products by acting against foodborne pathogens and spoilage bacteria. Plants have historically been used in traditional medicine as sources of natural antimicrobial substances for the treatment of infectious disease. Therefore, much attention has been paid to medicinal plants as a source of alternative antimicrobial strategies. Moreover, due to the growing demand for preservative-free cosmetics, herbal extracts with antimicrobial activity have recently been used in the cosmetic industry to reduce the risk of allergies connected to the presence of methylparabens. Some species belonging to the genus Cinnamomum, commonly used as spices, contain many antibacterial compounds. This paper reviews the literature published over the last five years regarding the antibacterial effects of cinnamon. In addition, a brief summary of the history, traditional uses, phytochemical constituents, and clinical impact of cinnamon is provided.     

Eugenol and its association with levodopa in 6‐hydroxydopamine‐induced hemiparkinsonian rats: Behavioural and neurochemical alterations

Parkinson's disease is a neurodegenerative disorder that affects the central nervous system and is mainly characterized by the loss of dopaminergic neurons and pro‐oxidant mechanisms. Eugenol has been widely studied due to its anti‐inflammatory and antioxidant activities, making it a promising neuroprotective agent. This study aimed to investigate the effects of eugenol and its combined action with levodopa in the 6‐hydroxydopamine‐induced Parkinson's disease model. Wistar rats were subjected to intrastriatal injection of 6‐hydroxydopamine (21 μg) and then treated with eugenol (0.1, 1, or 10 mg/kg), levodopa (25 mg/kg) or their combination (eugenol 10 mg/kg + levodopa 12.5 mg/kg) orally for 14 days. On the 14th day, the animals were subjected to behavioural tests, and after euthanization and dissection of the brain areas, neurochemical analyses were performed. The results showed that eugenol reduced the oxidative stress and behavioural disturbances induced by 6‐hydroxydopamine. The eugenol and levodopa combination was more effective in some behavioural parameters and body‐weight gain in addition to promoting an increase in reduced glutathione levels compared to levodopa alone. Thus, the neuroprotective activity of eugenol was observed against motor and neurochemical disorders. Additionally, the eugenol and levodopa combination was promising when compared to conventional treatment.     

Antibacterial effects of 18 medicinal plants used by the Khyang tribe in Bangladesh

Context: The resistance of bacteria to antibiotics is raising serious concern globally. Asian medicinal plants could improve the current treatment strategies for bacterial infections. The antibacterial properties of medicinal plants used by the Khyang tribe in Bangladesh have not been investigated.

Objective: The present study examines the antibacterial properties of 18 medicinal plants used by the Khyang tribe in day-to-day practice against human pathogenic bacteria.

Materials and methods: Leaves, bark, fruits, seeds, roots and rhizomes from collected plants were successively extracted with hexane, ethyl acetate and ethanol. The corresponding 54 extracts were tested against six human pathogenic bacteria by broth microdilution assay. The antibacterial mode of actions of phytoconstituents and their synergistic effect with vancomycin and cefotaxime towards MRSA was determined by time-killing assay and synergistic interaction assay, respectively.

Results and discussion: Hexane extract of bark of Cinnamomum cassia (L.) J. Presl. (Lauraceae) inhibited the growth of MRSA, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Acinetobacter baumannii with MIC values below 100 µg/mL. From this plant, cinnamaldehyde evoked at 4?×?MIC in 1?h an irreversible decrease of MRSA count Log10 (CFU/mL) from 6 to 0, and was synergistic with vancomycin for MRSA with fractional inhibitory concentration index of 0.3.

Conclusions: Our study provides evidence that the medicinal plants in Bangladesh have high potential to improve the current treatment strategies for bacterial infection.     

布洛芬丁香酚酯微乳的镇痛作用及大鼠体内药动学研究

目的:研究布洛芬丁香酚酯微乳剂的镇痛作用及其在大鼠体内的药动学.方法:采用小鼠热板法考察布洛芬丁香酚酯微乳的镇痛作用.大鼠尾静脉给药后,分别于给药后5,10,25,40 min和1,1.5,2,3,4,5,7和9 h取血.采用高效液相色谱法测定血浆中布洛芬的浓度.结果:布洛芬丁香酚酯微乳可剂量依赖性延长小鼠热板痛阀时间,且效果等同于同剂量布洛芬.布洛芬丁香酚酯微乳及布洛芬溶液组静脉注射后的消除半衰期(t1/2)分别为(6.30±0.56)和(2.79±0.29)h,清除率(CL)分别为(94.93±12.09)和(112.17±7.00)mL·h-1·kg-1,稳态表观分布容积(Vss)分别为(543.62±64.68)和(243.12±6.87)mL·kg-1,两组存在显著性统计学差异(P＜0.05).结论:布洛芬丁香酚酯微乳与布洛芬溶液剂镇痛作用相当,静脉注射后消除时间较布洛芬明显延长.     

布洛芬丁香酚酯前体药物的合成及其水解动力学

目的合成布洛芬丁香酚酯并研究其在不同pH水溶液中及血浆、肝匀浆中的水解动力学。方法以布洛芬和丁香酚为原料,经过酯化反应合成了布洛芬前体药物布洛芬丁香酚酯,利用HPLC法测定不同pH值的缓冲溶液、血浆及肝均浆中药物水解动力学。经UV、IR、MS和NMR确证了目标化合物的结构。结果布洛芬丁香酚酯在pH为1.10~9.96时水解速率常数不受pH影响,pH为10.91~11.91时随pH值增加水解速率增大;在血浆及肝均浆中布洛芬丁香酚酯可迅速水解成布洛芬和丁香酚。结论布洛芬丁香酚酯是一个具有良好前景的非甾体抗炎前体药物。