Evaluation of in silico,in vitro α-amylase inhibition potential and antidiabetic activity of Pterospermum acerifolium bark

Context: Pterospermum acerifolium (L.) Willd (Sterculiaceae) has been traditionally used in the treatment of diabetes mellitus but no scientific data has been published supporting the claimed ethnomedical use.

Objective: The present study was designed to estimate the in silico, in vitro α-amylase inhibition potential and anti-diabetic activity of Pterospermum acerifolium bark.

Materials and methods: In silico studies were performed between human pancreatic α-amylase (HPA) and β-sitosterol by using autodock 4.2 software. In vitro α-amylase inhibition study was carried out with 50% ethanol extract of the bark (PABEE) and its various fractions. The active ethyl acetate fraction (PABEF) was sub-fractionated into three fractions (PABE1, PABE2 and PABE3). Two doses (15 and 30?mg/kg) based on acute toxicity studies, of the above fractions were subjected to antidiabetic screening in vivo by STZ-nicotinamide induced type II diabetic rats.

Results: In silico studies showed the potent inhibition of β-sitosterol on human pancreatic amylase (HPA) with an estimated inhibition constant (K_i) of 269.35?nmol and two hydrogen bond interactions. PABEF showed marked α-amylase inhibition (69.94%) compared to other fractions. Diabetic rats treated with PABE3 (30?mg/kg) reduced the levels of fasting blood glucose, HbA1c, ALT, AST, ALP, triglycerides, total cholesterol, TBARS significantly (p?p?Conclusion: The present study confirmed the antihyperglycemic activity along with its status on hepatic biomarkers, antihyperlipidemic and antioxidant properties of Pterospermum acerifolium bark.     

数据窗口与Excel的数据交换技术在医保报表统计程序中的应用

本文通过医保报表统计程序开发的实例介绍了利用API及OLE技术来实现PB数据窗口与EXCEL之间的数据通信技术，具有很强的实用价值。     

颅内电极脑电图监测对枕叶致痫灶的定位价值

目的：探讨颅内电极埋藏后视频脑电图（V-EEG）监测对枕叶致痫灶的定位价值。方法：对19例经无创方法难以定位致痫灶的药物难治性枕叶癫痫（OLE）病人,开顷埋置硬脑膜下条状、栅格状电极和深部电极,行V-EEG监测,记录发作间期及发作期脑电图（EEG）变化,确定发作起源区,再手术切除致痫灶。结果：16例埋置硬脑膜下电极,3例联合应用硬脑膜下电极和深部电极。颅内电极V-EEG监测36～192h（平均68h）,均记录到发作间期痫样放电及发作期EEG情况。行枕叶致痼灶切除术后,平均随访24个月,13例发作消失（EngelⅠ级）,4例偶发（EngelⅡ级）,2例发作减少75％以上（EngelⅢ级）。结论：在致痫灶定位困难的顽固性OLE中,开颅埋藏硬脑膜下电极、深部电极,行V-EEG监测,根据癫痫发作初始期异常放电的节律和范围,可精确定位致痫灶。     

Oleamide restores sleep in adult rats that were subjected to maternal separation

Maternal separation (MS) induces a series of changes in rats' behavior; among them a reduction in spontaneous sleep. One potentially impaired system is the endocannabinoid system (eCBs), since it contributes to generate sleep. To investigate if there are situations early in life that affect the eCBs, which would contribute to make rats vulnerable to suffering insomnia, we studied the rodent model of MS. Rats were separated from their mothers for 3 h-periods daily, from postnatal day (PND) 2 to PND 16. Once they gained 250 g of body weight (adult rats), they were implanted with electrodes to record the sleep-waking cycle (SWC). MS rats and non-MS (NMS) siblings were assigned to one of the following groups: vehicle, oleamide (OLE, an agonist of the cannabinoid receptor 1, CB1R), OLE + AM251 (an antagonist of the CB1R) and AM251 alone. Expression of the CBR1 receptor was also analyzed in the frontal cortex (FCx) and in the hippocampus (HIP) of both NMS and MS rats. Results indicated that MS induced a reduction in both non-rapid eye movement (NREM) and rapid eye movement (REM) sleep with the consequent increase in waking (W) as compared to NMS siblings. OLE normalized the SWC, and AM251 blocked such an effect. CB1R expression was reduced in the FCx and in the HIP of MS rats. Our results indicate that MS reduces sleep and CB1R expression and OLE improves sleep in adult rats.     

长程视频脑电图在枕叶癫痫诊断及手术定位中的应用

目的：探讨长程视频脑电（V-EEG）在枕叶癫痫（OLE）手术诊断及定位中的应用。方法：27例难治性癫痫经过带蝶骨电极的长程V—EEG监测,结合磁共振成像（MRI）、发作间期正电子发射计算机断层扫描（PET）及视力视野检测结果确定癫痫起源位置为枕叶,对该27例长程V-EEG监测结果进行回顾分析,总结OLE的长程VEEG特点。结果：癫痫起源位置的EEG定位,4例位于颞枕区、4例顶枕区、1例颞顶枕区,18例单纯枕区。OLE具有较高视觉先兆出现率,本组为21例（78％）。发作间期EEG可以具有以下特征：①正常,②慢a节律或广泛θ节律,③一侧枕区脑波被抑制,④一侧或者双侧枕区存在异常电活动,⑤病灶周围脑区存在异常电活动,⑥病灶一侧半球各导联均分布有异常电活动,⑦异常电活动主要为尖波及尖慢波。OLE发作期初期（起始）EEG具有以下特征：①一侧枕区优先优势异常放电,②一侧颞枕区优先优势异常放电,③一侧顶枕区优先优势异常放电,④半球优势异常放电,⑤无侧别优势。结论：OLE具有相应的EEG及临床发作特征,蝶骨电极长程V-EEG结合影像学以及视力视野检查结果能有效诊断OLE,为准确定位提供一定可靠依据,有效指导手术治疗。     

The role of the CB1 receptor in the regulation of sleep

During the 1990s, transmembranal proteins in the central nervous system (CNS) that recognize the principal compound of marijuana, the delta-9-tetrahydrocannabinol (Delta9-THC) were described. The receptors were classified as central or peripheral, CB1 and CB2, respectively. To this date, it has been documented the presence in the CNS of specific lipids that bind naturally to the CB1/CB2 receptors. The family of endogenous cannabinoids or endocannabinoids comprises oleamide, arachidonoylethanolamine, 2-arachidonylglycerol, virodhamine, noladin ether and N-arachidonyldopamine. Pharmacological experiments have shown that those compounds induce cannabimimetic effects. Endocannabinoids are fatty acid derivates that have a variety of biological actions, most notably via activation of the cannabinoid receptors. The endocannabinoids have an active role modulating diverse neurobiological functions, such as learning and memory, feeding, pain perception and sleep generation. Experimental evidence shows that the administration of Delta9-THC promotes sleep. The activation of the CB1 receptor leads to an induction of sleep, this effect is blocked via the selective antagonist. Since the system of the endogenous cannabinoids is present in several species, including humans, this leads to the speculation of the neurobiological role of the endocannabinoid system on diverse functions such as sleep modulation. This review discusses the evidence of the system of the endocannabinoids as well as their physiological role in diverse behaviours, including the modulation of sleep.     

Naturally derived anti-inflammatory compounds from Chinese medicinal plants

Ethnopharmacological relevance

Though inflammatory response is beneficial to body damage repair, if it is out of control, it can produce adverse effects on the body. Although purely western anti-inflammatory drugs, orthodox medicines, can control inflammation occurrence and development, it is not enough. The clinical efficacy of anti-inflammation therapies is unsatisfactory, thus the search for new anti-inflammation continues. Chinese Material Medica (CMM) remains a promising source of new therapeutic agents. CMM and herbal formulae from Traditional Chinese Medicine (TCM), unorthodox medicines, play an improtant anti-inflammatory role in multi-targets, multi-levels, and multi-ways in treating inflammation diseases in a long history in China, based on their multi-active ingredient characteristics. Due to these reasons, recently, CMM has been commercialized as an anti-inflammation agent which has become increasingly popular in the world health drug markets. Major research contributions in ethnopharmacology have generated vast amount of data associated with CMM in anti-inflammtion aspect. Therefore, a systematic introduction of CMM anti-inflammatory research progress is of great importance and necessity.

Aim of the study

This paper strives to describe the progress of CMM in the treatment of inflammatory diseases from different aspects, and provide the essential theoretical support and scientific evidence for the further development and utilization of CMM resources as a potential anti-inflammation drug through a variety of databases.

Material and methods

Literature survey was performed via electronic search (SciFinder^®, Pubmed^®, Google Scholar and Web of Science) on papers and patents and by systematic research in ethnopharmacological literature at various university libraries.

Results

This review mainly introduced the current research on the anti-inflammatory active ingredient, anti-inflammatory effects of CMM, their mechanism, anti-inflammatory drug development of CMM, and toxicological information.

Conclusion

CMM is used clinically to treat inflammation symptoms in TCM, and its effect is mediated by multiple targets through multiple active ingredients. Although scholars around the world have made studies on the anti-inflammatory studies of CMM from different pathways and aspects and have made substantial progress, further studies are warranted to delineate the inflammation actions in more cogency models, establish the toxicological profiles and quality standards, assess the potentials of CMM in clinical applications, and make more convenient preparations easy to administrate for patients. Development of the clinically anti-inflammatory drugs are also warranted.