The study aims at providing a new suitable way to promote artificial cultivation, solving the problem of resources increasingly endangered wild medicine, and protecting the wild resources of Tibetan medicine. The content of quercetin,kaempferol and isorhamnetin was determined by HPLC. The correlation between flavonoids components and ecological factors was analyzed using partial least-squares regression (PLSR). Based on Maxent model combining using ArcGIS software, suitable regionalization for H.rhamnoides subsp. sinensis was studied.The results showed that the difference of quercetin,kaempferol and isorhamnetin content in samples from different regions were obvious. The main factors effecting quercetin content accumulation were the altitude andthe average monthly precipitation in January and August. The main factors effecting kaempferol accumulation were the altitude andthe average monthly precipitation in the coldest quarter and December. The main factors effecting isorhamnetin accumulation were the average monthly precipitation in August, January and the coldest quarter.The regional distribution suitability index for H.rhamnoides subsp. sinensis was 0-0.708. The suitable area 590 500 km², accounting for 6.13% of the total area. The preferably suitable area was 552 500 km², accounting for 5.73% of the total area.The methods used in the study is simple and feasible, the result is reliable which provide a new approach for Tibetan medicine resources sustainable exploitation and utilization.
Molecular targeted cancer therapy is a promising strategy to overcome the lack of specificity of anticancer drug. While the binding of c(RGDfK) (cyclic Arginine-Glycine-Aspartic acid-Phenylalanine-Lysine) to αvβ3 over-expressed on tumor cell has been validated, the underlying interaction remains poorly understood. In this work, docking calculation was applied to investigate the interactions between c(RGDfK)/c(RGDfK)-PEG and αvβ3. The calculated results indicated that c(RGDfK) interacted with αvβ3 mainly by electrostatic interaction, stabilization interaction, and hydrophobic interaction. Conjugation of PEG chain to the c(RGDfK) weakened the binding affinity of c(RGDfK) to αvβ3. Accordingly, docetaxel(DTX)-loaded target micelles (c(RGDfK)-PEG-PLA/PEG-PLA/DTX) were designed, characterized and evaluated using HeLa cells. In vitro release studies demonstrated both target and non-target micelles displayed almost the same profiles, which best fit in Ritger-Peppas model. Cellular uptake and MTT studies revealed that the target micelles with the presence of c(RGDfK) were more efficiently taken up by HeLa cells and significantly improved the cytotoxicity compared to that of non-target micelles. Cell inhibition rate of target micelles was improved by 20% after 24h. Our findings suggest that target micelles may be a potential anticancer drug delivery system in the treatment of integrin αvβ3 over-expressed on tumor cell.
OBJECTIVE: To establish a method for determination of 10 ingredients such as gentiopicroside, sweroside, and mangiferin in India swertia, and settle the index components and their limits.METHOD: By Welch materials AQ-C18 column, determination was conducted by the gradient elution with methanol and 0.4% formic acid as mobile phase, with column temperature 30 degrees C, flow rate at 1.0 mL x min(-1), and 254 nm as the detection wavelength.
RESULT: The linear relatives of 10 ingredients were good. The method showed the high precision and good reproducibility, and recovery rates were between 97% and 103%. The ingredients of market com-modities varied greatly.
CONCLUSION: This method is simple, sensitive, reproducible, and applicable to the determination of the main ingredients in India Swertia. Sweroside and mango glycosides were suggested as the index components for determination in Jia Di (Swertia chirayita), and their content limits are not less than 0.1%, 0.3%, respectively.
Asymmetry of waking electroencephalography (EEG) alpha power in frontal regions has been correlated with waking emotional reactivity and the emotional content of dream reports. Little is known regarding alpha asymmetry during sleep. The present study was performed to compare alpha power and alpha power asymmetry in various brain regions across states of sleep and wakefulness. Waking and sleep EEG were recorded in a group of patients undergoing polysomnographic evaluation for possible sleep disorders. Alpha EEG asymmetry in frontal and temporal regions was significantly correlated in waking versus sleep, particularly during rapid eye movement (REM) sleep. These results suggest that patterns of frontal alpha asymmetry are stable across sleep and waking and may be related to emotional reactivity during dreaming. During sleep, alpha power was highest during slow-wave sleep and lowest during REM sleep. Implications of these data for understanding the functional significance of alpha power during waking and sleeping are considered.
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OBJECTIVE: To investigate the underlying mechanism of reduced myocardial ischemia-reperfusion (I/R) injury in rats using the traditional Tibetan medicine Sanweitanxiang powder (SWTX).METHODS: Rats were randomly divided into six groups (n = 10) as follows: (a) propranolol dinitrate control group, given propranolol dinitrate 0.02 g/kg for 10 days before I/R, (b) SWTX with a high dose group, given SWTX 1.5 g/kg for 10 days before I/R, (c) SWTX with a medium dose group, given SWTX 1.25 g/kg for 10 days before I/R, (d) sham group (Sham), in which the rat heart was exposed by pericardiotomy but without I/R, (e) SWTX with a low dose group, given SWTX 1.0 g/kg for 10 days before I/R, and (f) I/R injury group. Rats were intragastrically pretreated with propranolol dinitrate or SWTX. After that, the operation to cause ischemia and reperfusion was conducted. The histopathologic changes of rat hearts were observed by hematoxylin and eosin staining and transmission electron microscopy. Ca2+ homeostasis protein expression was determined by western blot.
RESULTS: After SWTX pretreatment, the development of ultrastructural pathological changes from IR injury was attenuated. A decrease in the expression of B-cell lymphoma 2 associated X protein, and an increase in the expression of B-cell lymphoma 2 were observed. An increased activation of extracellular signal regulated kinases were found. Compared with the sham group, the expression of sarcoplasmic reticulum calcium-ATPase, phospholamban, and calsequestrin were all up-regulated after pretreatment with SWTX.
CONCLUSION: The protective mechanism of SWTX pretreatment on myocardial I/R injury might be related to its effect on maintaining the balance of calcium homeostasis in rat heart.
OBJECTIVE: To investigate the underlying mechanism of reduced myocardial ischemia-reperfusion (I/R) injury in rats using the traditional Tibetan medicine Sanweitanxiang powder (SWTX). METHODS: Rats were randomly divided into six groups (n = 10) as follows: (a) propranolol dinitrate control group, given propranolol dinitrate 0.02 g/kg for 10 days before I/R, (b) SWTX with a high dose group, given SWTX 1.5 g/kg for 10 days before I/R, (c) SWTX with a medium dose group, given SWTX 1.25 g/kg for 10 days before I/R, (d) sham group (Sham), in which the rat heart was exposed by pericardiotomy but without I/R, (e) SWTX with a low dose group, given SWTX 1.0 g/kg for 10 days before I/R, and (f) I/R injury group. Rats were intragastrically pretreated with propranolol dinitrate or SWTX. After that, the operation to cause ischemia and reperfusion was conducted. The histopathologic changes of rat hearts were observed by hematoxylin and eosin staining and transmission electron microscopy. Ca2+ homeostasis protein expression was determined by western blot. RESULTS: After SWTX pretreatment, the development of ultrastructural pathological changes from IR injury was attenuated. A decrease in the expression of B-cell lymphoma 2 associated X protein, and an increase in the expression of B-cell lymphoma 2 were observed. An increased activation of extracellular signal regulated kinases were found. Compared with the sham group, the expression of sarcoplasmic reticulum calcium-ATPase, phospholamban, and calsequestrin were all up-regulated after pretreatment with SWTX. CONCLUSION: The protective mechanism of SWTX pretreatment on myocardial I/R injury might be related to its effect on maintaining the balance of calcium homeostasis in rat heart.
This study is aimed to explore the effect of nitrogen, phosphorus and potassium combined application on the active components of Rhodiola crenulata. R. crenulata was used as the research object, "3414" fertilization experiment were conducted with regular fertilization of NPK(N 60 kg·hm⁻², P₂O₅ 100 kg·hm⁻²,KCl 160 kg·hm⁻²) to study the effect of different rates of NPK fertilization on the total amount of 4 phenolic constituents of gallic acid, salidroside, tyrol and ethyl gallate through field test. The results show that the content of salidroside was higher in the treatment of N₁P₂K₁ and N₁P₂K₂, andthe total amount of four phenols was higher in the treatment of N₁P₂K₂ and N₂P₂K₂. The suitable level of nitrogen, phosphorus and potassium promoted the accumulation of the 4 kinds of phenols.The amount of fertilizer recommended by the three factor fertilizer effect equation,(N 0 kg·hm⁻²,P₂O₅ 150 kg·hm⁻²,KCl 31.71 kg·hm⁻²) obtained the highest content of salidroside, and it was 1.54%.（N 35.54 kg·hm⁻²,P₂O₅ 150 kg·hm⁻²,KCl 237.73 kg·hm⁻²）obtained the highest content of 4 kinds of phenolic compounds, and it was 1.93%. This study provides a reference for the standardization of artificial planting of endangered Tibetan medicine.
A typical indicator of sepsis is the development of progressive subcutaneous and body‑cavity edema, which is caused by the breakdown of endothelial barrier function, leading to a marked increase in vascular permeability. Microvascular leakage predisposes to microvascular thrombosis, breakdown of microcirculatory flow and organ failure, which are common events preceding mortality in patients with severe sepsis. Melilotus suaveolens (M. suaveolens) is a Traditional Tibetan Medicine. Previous pharmacological studies have demonstrated that an ethanolic extract of M. suaveolens has powerful anti‑inflammatory activity and leads to an improvement in capillary permeability. However, the mechanisms underlying its pharmacological activity remain elusive. The present study aimed to assess the impact of M. suaveolens extract tablets on pulmonary vascular permeability, and their effect on regulating lung inflammation and the expression of vascular endothelial growth factor (VEGF) in the lung tissue of rats with sepsis. A cecal ligation and puncture (CLP) sepsis model was established for both the control and treatment groups. ~2 h prior to surgery, 25 mg/kg of M. suaveolens extract tablet was administered to the treatment group. Polymerase chain reaction and western blot analyses were used to assess the expression of nuclear factor (NF)‑κB and VEGF in the lung tissue, and ELISA was applied to detect changes in serum tumor necrosis factor‑α as well as interleukins (IL) ‑1, ‑4, ‑6, and ‑10. The lung permeability, wet/dry weight ratio and lung pathology were determined. The results demonstrated that in the lung tissue of CLP‑rats with sepsis, M. suaveolens extract inhibited the expression of NF‑κB, reduced the inflammatory response and blocked the expression of VEGF, and thus significantly decreased lung microvascular permeability. The effects of M. Suaveolens extract may be of potential use in the treatment of CLP‑mediated lung microvascular permeability.
The separation of high-purity compounds from traditional Tibetan medicines plays an important role in investigating their bioactivity. Nevertheless, it is often quite difficult to isolate compounds with high purity because of the complexity of traditional Tibetan medicines. In this work, an offline two-dimensional reversed-phase preparative method was successfully developed for the separation of high-purity compounds from Oxytropis falcata. Based on the analysis results, an ODS C18 prep column was used for first-dimensional preparation, and 14.8 g of the crude sample was separated into five fractions with a recovery of 74.6%. Then, an XAqua C18 prep column was used to isolate high-purity compounds in the second-dimensional preparation because its separation selectivity is different with the ODS C18 stationary phase. As a result, eight compounds in the crude sample were isolated in more than 98% purity. This is the first report of trans-cinnamic acid (1) and trifolirhizin (2) from Oxytropis falcata. This method has the potential to be an efficient separation method of high-purity compounds from Oxytropis falcata and it shows great promise for the separation of high-purity compounds from complex samples.
With the rapid development of Tibetan medicine industry, the study on plateau medicinal plants' endangered status is not enough, measures to protect is weak and the plateau ecological environment' inherent vulnerability, resulted in the shortage of Tibetan medicinal resources and affect the sustainable development . According to the existing endangered information of Tibetan medicine resources, how to formulate feasible protection plan, is an urgent problem of the rational development and utilization of Tibetan medicine resources to be solved. To find out the endangered Tibetan medicines in Qinghai Tibet Plateau, the Grade division method of Chinese Rare and Endangered Plants was applied, the endangered species were sorted out, which divided into class one (threatened) eleven species, class two (rare) twenty-one species, and class three (fading) forty-two species,a total of seventy-four species.In addition to national protection list in "Chinese rare and endangered plants". It's proposed to increase the endangered Tibetan medicinal species. Finally, according to the endangered status of the resources,from the survey of endangered Tibetan medicinal species regularly, the germplasm repository establishment of endangered Tibetan medicine, in situ conservation, artificial cultivation research and renew the idea, reasonable development and utilization, a total of 5 aspects to discussed the protection strategy, to provide a scientific basis for the protection and sustainable utilization of Tibetan medicine resources in Qinghai-Tibet Plateau.
BACKGROUND: Our previous studies on Asterothamnus centrali-asiaticus Novopokr. (ACN) and Arenaria kansuensis Maxim. (AKM) had led to the isolation of some phytochemical constituents and evaluation of anticonvulsant effect based on their extracts. ACN and AKM have been widely used in traditional Tibetan herbs for neuropsychiatric diseases and cardiopulmonary disorders.PURPOSE: The purpose is to investigate structure-activity relationships of flavonoids isolated from ACN and AKM, for binding to the benzodiazepine site (BZ-S) of γ-aminobutyric acid type A (GABAA) receptor complex, and to search for anticonvulsant compounds without undesirable effects such as myorelaxation and sedation.
STUDY DESIGN AND METHODS: The affinities of these flavonoids for the BZ-S of GABAA receptors were determined by [3H]flunitrazepam binding to mouse cerebellum membranes in vitro. And the anticonvulsant, myorelaxant and sedative effects were determined by pentylenetetrazol (PTZ)-induced seizure and electrogenic seizure protection, rotarod test and locomotor activity test, respectively.
RESULTS: Fifteen and thirteen flavonoids were isolated from ACN and AKM, respectively. Structure-activity relationships analysis indicated that 6-and/or 8-OMe flavones exhibited the most potent binding affinity to GABAA receptors. Furthermore, 2',4',5,7-tetrahydroxy-5',6-dimethoxyflavone (DMF, IC50 value of 0.10 μM), a flavone isolated from ACN, presented high anticonvulsant activity against chemical-induced seizures and electrogenic seizures, without myorelaxation and sedation.
CONCLUSION: This study suggested that these flavones, especially DMF, are new BZ receptor ligands and prospective therapeutic candidates for seizures.
AIM: Fructus phyllanthi tannin fraction (PTF) from the traditional Tibetan medicine Fructus phyllanthi has been found to inhibit lung and liver carcinoma in mice. In this study we investigated the anticancer mechanisms of PTF in human lung squamous carcinoma cells in vitro.METHODS: Human lung squamous carcinoma cell line (NCI-H1703), human large-cell lung cancer cell line (NCI-H460), human lung adenocarcinoma cell line (A549) and human fibrosarcoma cell line (HT1080) were tested. Cell viability was detected with MTT assay. Cell migration and invasion were assessed using a wound healing assay and a transwell chemotaxis chambers assay, respectively. Cell apoptosis was analyzed with flow cytometric analysis. The levels of apoptosis-related and metastasis-related proteins were detected by Western blot and immunofluorescence.
RESULTS: PTF dose-dependently inhibited the viability of the 3 human lung cancer cells. The IC50 values of PTF in inhibition of NCI-H1703, NCI-H460, and A549 cells were 33, 203, and 94 mg/L, respectively. PTF (15, 30, and 60 mg/L) dose-dependently induced apoptosis of NCI-H1703 cells. Treatment of NCI-H1703 and HT1080 cells with PTF significantly inhibited cell migration, and reduced the number of invasive cells through Matrigel. Furthermore, PTF dose-dependently down-regulated the expression of phosphor-ERK1/2, MMP-2 and MMP-9, up-regulated the expression of phosphor-JNK, but had no significant effect on the expression of ERK1/2 or JNK.
CONCLUSION: PTF induces cell apoptosis and inhibits the migration and invasion of NCI-H1703 cells by decreasing MPPs expression through regulation of the MAPK pathway.
Background: Cancer centers have increasingly offered integrative medicine therapies in response to their patients' unmet needs. We evaluated the growth of integrative medicine in leading academic cancer centers in the United States as reflected by their public-facing websites. Methods: We performed a systematic review of 45 National Cancer Institute (NCI)-designated comprehensive cancer center websites. Two researchers independently evaluated whether the websites provided information regarding integrative medicine modalities and, if so, whether the services were provided in the same health system. They compared the proportion of cancer centers providing the information on each modality in 2016 with the data from the prior study in 2009. Results: The most common integrative medicine therapies mentioned on the 45 NCI-designated comprehensive cancer center websites were exercise (97.8%) and acupuncture and meditation (88.9% each), followed by yoga (86.7%), massage (84.4%), and music therapy (82.2%). The majority of the websites also provided information on nutrition (95.6%), dietary supplements (93.3%), and herbs (88.9%). The most common therapies offered in the health systems were acupuncture/massage (73.3% each), meditation/yoga (68.9% each), and consultations about nutrition (91.1%), dietary supplements (84.4%), and herbs (66.7%). Compared with 2009, there was a statistically significant increase in the number of websites mentioning acupuncture, dance therapy, healing touch, hypnosis, massage, meditation, Qigong, and yoga (all P < .05). Conclusions: Leading US cancer centers increasingly present integrative medicine content on their websites, and the majority of them provide these services to patients in the same health systems.
OBJECTIVE: To investigate the role of Tibetan medicine-Twenty Wei Chenxiang Pill interfering with serum ET-1 level, in order to confirm that ET-1 is involved to the pathogenesis of hypoxic pulmonary hypertension.METHODS: 165 Wistar rats were randomly divided into high altitude control group,Tibetan medicine-Twenty Wei Chenxiang Pill group and plain control group. The physiological signal acquisition system was used to record pulmonary arterial pressure, and RV/(LV + S) ratio were caculated. Serum HIF-1alpha and ET-1 protein levels were determined by the method of ELISA, and ETA protein levels in lung tissue were determined by Western Blot method.
RESULTS: Compared with the high altitude group,in the rats of Tibetan medicine-Twenty Wei Chenxiang Pill group,the pulmonary arterial pressure decreased significantly from the seventh day and the seventh day (P < 0.01), the RV/(LV + S) ratio and serum HIF-1alpha levels decreased significantly from the third day (P < 0.05 or P < 0.01), the serum ET-1 levels decreased significantly from the third day (P < 0.05 or P < 0.01), and the expression of ETA protein decreased significantly from the beginning (P < 0.01 or P < 0.001).
CONCLUSION: ET-1 is one of the important factors causing pulmonary artery pressure increasing and right ventricular wall thickening, which plays a role in hypoxic pulmonary artery only involved in the early period hypoxia, but not in the later period. Tibetan medicine--twenty Wei Chenxiang Pill can prevent the pulmonary artery hypertension and the right ventricular wall thickening in rats, and its mechanism may be related to the direct inhibition of ET-1 and protein levels of ETA or the indirect downregulation of ET-1 level and ETA through inhibition of HIF-la level.
Nitraria tangutorum Bor., having edible berries, is valued for reputed health benefits in Qinghai-Tibet plateau. The phytochemical research on the fruit juice of N. tangutorum led to the isolation of twenty-six compounds including five new compounds, tangutorids A-D (1, 2, 3a, and 3b), and (3E,5E)-7-O-β-glucosyl-4-(2-methoxy-2-oxoethyl)hepta-3,5-dienoic acid (15). The structures of these compounds were elucidated through comprehensive spectroscopic analyses. Tangutorids A-F were the first examples of glucose-derived β-carbolines from natural products. The biogenetic pathways of 1-8 were proposed to involve Pictet-Spengler reactions and described starting from the co-isolated tryptophan (10) and corresponding aldehydes. All isolates were evaluated for their antioxidant and α-glucosidase inhibitory activities. Compounds 21, 22, and 24 showed antioxidant activity with SC50 values ranging from 12.2±1.9 to 30.4±2.7μg/mL, and compound 1 showed strong α-glucosidase inhibitory effect with IC50 value of 63.3±4.6μg/mL.
Based on literature data, related specimens, commercial samples and field investigation, botanical origin of "bolingguazi" was clarified. Boling guazi was found to be used as a Tibetan medicine in China from 8th century, it was derived from Herpetospermum pedunculosum of cucurbitaceae, and main species of bolingguazi used in most areas of China were H. pednculosura, while seeds of Momordica charantia, Thladiantha setispina and M. cohinchinensis were also available in some areas of China.
OBJECTIVE: To study the material composition of Tibetan medicine "Brag-zhun", and to provide the basis for interpretation of its source and reference for the establishment of quality standards.METHODS: Pharmacognosy routine method was used in macroscopic and microscopic identifications, inductively coupled plasma spectrometry was carried out to determine 26 kinds of mineral elements,and X-ray diffraction analysis was used for the crystalline phase detection of Brag-zhun. The content of calcium,organic matter, humic acid and fulvic acid was determined according to GB/T 14610-2008, "technical specification for soil analysis" , GB/T 11957-2001 and capacity titration, respectively. Moisture, ash content, acid insoluble ash content and water soluble extract were determined with reference to the Chinese Pharmacopoeia (2010 edition).
RESULTS: Animal feces were commonly found in Brag-zhun, the main crystal phase was SiO2, 26 kinds of mineral elements content in total was about 3%, 13 batches of medicinal materials in organic matter content was 29.03%-71.79%. Humic acid content was 28.37%-58.51%; fulvic acid content was 19.69%-41.43%; moisture was 5.2% -11.7%; total ash content was 17.82%-64.39%; acid insoluble ash content was 2.10%-39.09%; and water soluble extract was 28.39%-57.40%.
CONCLUSION: The traditional record of Brag-zhun from molten juice is lack of scientific basis. The mineral elements in Brag-zhun exist in amorphous. Brag-zhun contains a lot of organic matter including humic acid and fulvic acid, and inorganic matter mainly comes from sediment. The organic matter in rock has gone through a long geological evolution.
<b>Resumen: </b> <i>Las Himalaya contienen la mayor masa de hielo fuera de las regiones polares y son la fuente de los 10 ríos principales de Asia. La rápida reducción en el volumen de los glaciares del Himalaya se debe al cambio climático. Los efectos en cascada de la elevación de la temperatura y la pérdida de hielo y nieve en la región afectan, por ejemplo, la disponibilidad de agua (cantidad, estacionalidad), la biodiversidad (especies endémicas, relaciones depredador-presa), cambios en los límites de ecosistemas (movimiento de línea de árboles, cambios en los ecosistemas de elevación alta) y cambios globales (cambios en los monzones, pérdida de carbono del suelo). El cambio climático también tendrá impactos ambientales y sociales que probablemente incrementarán la incertidumbre en las reservas de agua y producción agrícola para poblaciones humanas de Asia. Se requiere desarrollar un entendimiento común del cambio climático por medio de investigación regional y a escala local para que se puedan identificar e implementar estrategias de mitigación y adaptación. Los retos derivados del cambio climático en el Himalaya solo pueden ser abordados mediante mayor colaboración regional en investigación científica y definición de políticas.</i>
<bold>Background: </bold>Tong Luo Hua Shi (TLHS) is a new formulation of the traditional Tibetan medicine Wu-wei-gan-lu that has been used for the treatment of rheumatoid arthritis (RA) for hundreds of years in China. This study aimed to evaluate the efficacy and safety of TLHS in patients with RA.<bold>Methods: </bold>This was a randomized, double-blind, placebo-controlled, dose-finding study performed in patients with active RA from five medical centers. Patients received three doses (4.8, 3.6, or 2.4 g/day po) of TLHS or placebo (tid po) for 8 weeks. Blood sampling, physical examination, and assessment of the American College of Rheumatology (ACR) 20 % improvement (ACR20) criteria were performed before and every 2 weeks after starting treatment. The primary endpoint was the ACR20. The secondary endpoints included safety.<bold>Results: </bold>A total of 240 participants were screened and 236 patients were randomized (n = 59/group); 20 dropped out. After 8 weeks, ACR20 improvements in the TLHS 4.8 g and 3.6 g groups were significantly higher than in the placebo group (P < 0.01 and P < 0.05, respectively). ACR50 improvement in the TLHS 4.8 g group was significantly higher compared with the placebo group (P < 0.01). Symptoms of RA were significantly relieved in the TLHS groups. In the TLHS groups, insomnia (n = 1), gastroenteric reactions (n = 2), arrhythmia (n = 1), and minor hepatic lesion (n = 1) were reported; in the placebo group, hepatic dysfunction (n = 1) was reported (P = 0.878).<bold>Conclusions: </bold>TLHS improved the symptoms of patients with RA according to the ACR20. Moreover, TLHS was safe.<bold>Trial Registration: </bold>Chinese Clinical Trial Registry: ChiCTR-TRC-12003871 . Registered on 1 January 2012. [ABSTRACT FROM AUTHOR]
OBJECTIVE: Positron emission tomography was used to investigate the neural substrates of normal human emotional and their dependence on the types of emotional stimulus.
METHOD: Twelve healthy female subjects underwent 12 measurements of regional brain activity following the intravenous bolus administration of [15O]H2O as they alternated between emotion-generating and control film and recall tasks. Automated image analysis techniques were used to characterize and compare the increases in regional brain activity associated with the emotional response to complex visual (film) and cognitive (recall) stimuli.
RESULTS: Film- and recall-generated emotion were each associated with significantly increased activity in the vicinity of the medial prefrontal cortex and thalamus, suggesting that these regions participate in aspects of emotion that do not depend on the nature of the emotional stimulus. Film-generated emotion was associated with significantly greater increases in activity bilaterally in the occipitotemporparietal cortex, lateral cerebellum, hypothalamus, and a region that includes the anterior temporal cortex, amygdala, and hippocampal formation, suggesting that these regions participate in the emotional response to certain exteroceptive sensory stimuli. Recall-generated sadness was associated with significantly greater increases in activity in the vicinity of the anterior insular cortex, suggesting that this region participates in the emotional response to potentially distressing cognitive or interoceptive sensory stimuli.
CONCLUSIONS: While this study should be considered preliminary, it identified brain regions that participate in externally and internally generated human emotion.
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A new diarylheptanoid, (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptan-3-one-5-O-β-D-6-Oacetylglucoside (<i>1</i>), together with two known diarylheptanoids, (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptan-3-one-5-O-β-D-glucopyranoside (<i>2</i>) and hirsutanonol (<i>3</i>), were isolated from Saxifraga tangutica. The structures of <i>1-3</i> were elucidated using 1D and 2D NMR spectral data, including high-resolution mass spectra (HR-ESI-MS). It was found that the new compound was acetyl-substituted (5S)-1,7-bis-(3,4-dihydroxyphenyl)-5-hydroxyheptan-3-one-5-O-β-D-glucopyranoside.
Traditional Tibetan medicine provides an abundant source of knowledge on human ailments and their treatment. As such, it is necessary to explore their active single compounds used to treat these ailments to discover lead compounds with good pharmacologic properties. In this present work, animal medicine, Osteon Myospalacem Baileyi extracts have been separated using a two-dimensional preparative chromatographic method to obtain single compounds with high purity as part of the following pharmacological research. Five high-purity cyclic dipeptides from chromatography work were studied for their dihydroorotate dehydrogenase inhibitory activity on recombinant human dihydroorotate dehydrogenase enzyme and compound Fr. 1-4 was found to contain satisfying inhibition activity. The molecular modeling study suggests that the active compound Fr. 1-4 may have a teriflunomide-like binding mode. Then, the energy decomposition study suggests that the hydrogen bond between Fr. 1-4 and Arg136 can improve the binding mode to indirectly increase the van der Waals binding energy. All the results above together come to the conclusion that the 2, 5-diketopiperazine structure group can interact with the polar residues well in the active pocket using electrostatic power. If some proper hydrophobic groups can be added to the sides of the 2, 5-diketopiperazine group, it is believed that better 2, 5-diketopiperazine dihydroorotate dehydrogenase inhibitors will be found in the future.
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