Anti-nociceptive effect of patchouli alcohol: Involving attenuation of cyclooxygenase 2 and modulation of mu-opioid receptor / 中国结合医学杂志

OBJECTIVE@#To explore the anti-nociceptive effect of patchouli alcohol (PA), the essential oil isolated from Pogostemon cablin (Blanco) Bent, and determine the mechanism in molecular levels.@*METHODS@#The acetic acid-induced writhing test and formalin-induced plantar injection test in mice were employed to confirm the effect in vivo. Intracellular calcium ion was imaged to verify PA on mu-opioid receptor (MOR). Cyclooxygenase 2 (COX2) and MOR of mouse brain were expressed for determination of PA's target. Cellular experiments were carried out to find out COX2 and MOR expression induced by PA.@*RESULTS@#PA significantly reduced latency period of visceral pain and writhing induced by acetic acid saline solution (P<0.01) and allodynia after intra-plantar formalin (P<0.01) in mice. PA also up-regulated COX2 mRNA and protein (P<0.05) with a down-regulation of MOR (P<0.05) both in in vivo and in vitro experiments, which devote to the analgesic effect of PA. A decrease in the intracellular calcium level (P<0.05) induced by PA may play an important role in its anti-nociceptive effect. PA showed the characters of enhancing the MOR expression and reducing the intracellular calcium ion similar to opioid effect.@*CONCLUSIONS@#Both COX2 and MOR are involved in the mechanism of PA's anti-nociceptive effect, and the up-regulation of the receptor expression and the inhibition of intracellular calcium are a new perspective to PA's effect on MOR.

Mechanism underlying berberine's effects on HSP70/TNFα under heat stress: Correlation with the TATA boxes / 中国天然药物

Heat stress can stimulate an increase in body temperature, which is correlated with increased expression of heat shock protein 70 (HSP70) and tumor necrosis factor α (TNFα). The exact mechanism underlying the HSP70 and TNFα induction is unclear. Berberine (BBR) can significantly inhibit the temperature rise caused by heat stress, but the mechanism responsible for the BBR effect on HSP70 and TNFα signaling has not been investigated. The aim of the present study was to explore the relationship between the expression of HSP70 and TNFα and the effects of BBR under heat conditions, using in vivo and in vitro models. The expression levels of HSP70 and TNFα were determined using RT-PCR and Western blotting analyses. The results showed that the levels of HSP70 and TNFα were up-regulated under heat conditions (40 °C). HSP70 acted as a chaperone to maintain TNFα homeostasis with rising the temperature, but knockdown of HSP70 could not down-regulate the level of TNFα. Furthermore, TNFα could not influence the expression of HSP70 under normal and heat conditions. BBR targeted both HSP70 and TNFα by suppressing their gene transcription, thereby decreasing body temperature under heat conditions. In conclusion, BBR has a potential to be developed as a therapeutic strategy for suppressing the thermal effects in hot environments.

Pomegranate leaf attenuates lipid absorption in the small intestine in hyperlipidemic mice by inhibiting lipase activity / 中国天然药物

Pomegranate leaf (PGL) has a definite role in regulating lipid metabolism. However, pharmacokinetic results show the main active ingredient, ellagic acid, in PGL has lower oral bioavailability, suggesting that the lipid-lowering effect of PGL may act through inhibiting lipid absorption in the small intestine. Our results demonstrated that pomegranate leaf and its main active ingredients (i.e., ellagic acid, gallic acid, pyrogallic acid and tannic acid) were capable of inhibiting pancreatic lipase activity in vitro. In computational molecular docking, the four ingredients had good affinity for pancreatic lipase. Acute lipid overload experiments showed that a large dosage of PGL significantly reduced serum total cholesterol (TG) and triglycerides (TC) levels in addition to inhibiting intestinal lipase activity, which demonstrated that PGL could inhibit lipase activity and reduce the absorption of lipids. We also found that PGL could reverse the reduced tight-junction protein expression due to intestinal lipid overload, promote Occludin and Claudin4 expression in the small intestine, and enhance the intestinal mucosal barrier. In conclusion, we demonstrated that PGL can inhibit lipid absorption and reduce blood TG and TC by targeting pancreatic lipase, promoting tight-junction protein expression and thereby preventing intestinal mucosa damage from an overload of lipids in the intestine.

Reproductive toxicity of brazilein in ICR mice / 中国天然药物

Brazilein is an active small molecular compound extracted from Caesalpinia sappan L. with favorable pharmacological properties on immune system, cardiovascular system, and nervous system. C. sappan has been used as a traditional medicine in China for hundreds of years for various diseases. However, the general reproductive toxicity of brazilein is still unknown. The purpose of the present study was to thoroughly evaluate the general reproductive toxicity of brazilein in ICR mice to support the future drug development and modernization of this potent traditional Chinese medicine. The results showed that, although no apparent toxicity on the reproducibility of the male was observed, brazilein might cause considerable risks to the fetuses and females as indicated by the ratios of dead fetuses and reabsorptions. In conclusion, our results from the present study provided some useful insights about the safety profile of brazilein, suggesting that brazilein should be used with caution in pregnant women.

Brazilein inhibits neuronal inflammation induced by cerebral ischemia and oxygen-glucose deprivation through targeting NOD2 expression / 中国天然药物

Brazilein is reported to have immunosuppressive effect on cardiovascular and cerebral-vascular diseases. The essential roles of innate immunity in cerebral ischemia are increasingly identified, but no studies concerning the influence of brazilein on the innate immunity receptors have been reported. The present study was designed to investigate the regulation of NOD2 (Nucleotide-binding oligomerization domain-containing protein 2) by brazilein for its protection of neuron in cerebral ischemia in vivo and oxygen-glucose deprivation in vitro. The results showed that brazilein could reverse the elevated expression of NOD2 and TNFα (tumor necrosis factor alpha) elicited by cerebral ischemia and reperfusion. This reduction could also be detected in normal mice and C17.2 cells, indicating that this suppressive effect of brazilein was correlated with NOD2. The results from GFP reporter plasmid assay suggested brazilein inhibited NOD2 gene transcription. In conclusion, brazilein could attenuate NOD2 and TNFα expression in cerebral ischemia and NOD2 may be one possible target of brazilein for its immune suppressive effect in neuro-inflammation.

Effects of Angelica dahurica on obesity and fatty liver in mice / 中国天然药物

Angelica dahurica (A. dahurica) is a traditional Chinese medicinal plant being used in clinical practice. The present study demonstrated that A. dahurica could reduce white-fat weight in high-fat-diet hyperlipidemic mice, decrease total cholesterol and triglyceride concentrations in the livers of both high-fat-diet and Triton WR1339 induced hyperlipidemic mice, and enhance the total hepatic lipase activities of them. These findings were further supported by the results derived from the experiments with HepG2 cells in vitro. In addition, the proteins related to lipids metabolism were investigated using LC-MS/MS, indicating that genes of lipid metabolism and lipid transport were regulated by A. dhurica. The results from LC-MS/MS were further conformed by Western blot and real time PCR assays. A. dahurica could down-regulate the expression of catalase (CAT) and sterol carrier protein2 (SCP2) and up-regulate the expression of lipid metabolism related genes-lipase member C (LIPC) and peroxisome proliferator-activated receptor gamma (PPARγ). In the Triton WR1339 mouse liver and HepG2 cells in vitro, A. dahurica was able to increase the expression of LIPC and PPARγ, confirming the results from in vivo experiments. Imperatorin showed the same activity as A. dahurica, suggesting it was one of the major active ingredients of the herb. In conclusion, our work represented a first investigation demonstrating that A. dahurica was able to regulate lipid metabolism and could be developed as a novel approach to fighting against fatty liver and obesity.

Understanding differences between Rheum palmatum and R. franzenbachii from perspective of chemistry, efficacy and toxicity / 中国中药杂志

Rheum franzenbachii (called Tudahuang in local) has some similarities with R. palmatum (rhubarb) collected by "China Pharmacopoeia" and is often used as a substitute of rhubarb. Can Tudahuang simply replace rhubarb in the application or whether is there difference between Tudahuang and rhubarb, and what is the difference it is important to verify the difference and understand its proper application in the field of clinical practice. In this paper, we discussed the differences of the two herbs from the views of chemistry, efficacy and toxicity based on the author's previous research work as well as literatures, by using the major role of the rhubarb "diarrhea" as the basic point. The analysis result showed that the role of diarrhea Tudahuang was much weaker than that of rhubarb. The reason lies in the difference between the contents of combined anthraquinones component. While acute toxicity in mice of Tudahuang is stronger than that of rhubarb. Thus, Tudahuang should not simply replace rhubarb in practice.

Transmembrane transport behavior of in vitro HepG2 cells of ananas and its effect on lipids and glucose distribution / 中国中药杂志

Pineapple (Ananas comosus) leaves contain mainly phenolic components with antioxidant and hypolipidemic effects. One of the principle components is p-coumaric acid. In this study, the transport behavior of p-coumaric acid, was observed after the administration of pineapple leaf phenols in vitro. Simultaneously, the effect of the phenols on glucose, total cholesterol and triglycerides transportation and metabolism in HepG2 cells was also observed. The results showed that the phenols had good transport characteristics. 5 min after the administration, p-coumaric acid of the phenols could be detected, and the content of p-coumaric acid reached the peak concentration after 60 min of the administration. p-coumaric acid of phenols have time-and dose-dependent manner. While promoting glucose transporter (GLUT4) and low density lipoprotein receptor (LDLR) expression, the phenols decreased intracellular lipid content. This reduction of intracellular lipid content was highly correlated with the promotion of lipoprotein lipase (LPL) and hepatic triglyceride lipase (HTGL) expression, while the reduction of intracellular glucose levels was correlated with glycogen synthesis in the cells.

Euphorbia kansui roots induced-diarrhea in mice correlates with inflammatory response / 中国天然药物

AIM@#Euphorbia kansui (E. KS) is a traditional medicine used in China for thousands of years with the effect of propulsion in the gastrointestines. However, there is no reported study of E. KS on gastrointestinal motility until now. The aim of this work is to study the effect of E. KS on the propulsion of gastrointestines, and to elucidate the possible mechanism of action.@*METHODS@#E.KS was prepared as a 30% ethanol extract and used for the experiment of small and large intestines of mice by oral administration with three different dosages (1.2, 0.6 and 0.3 g·kg(-1)). The feces were observed in vivo. The morphology was carried out to detect if there are any changes in the intestines after the extract of E. KS administration. The assays of mRNA and protein expression were employed to observe IL-1β, TNFα and caspase 3.@*RESULTS@#It was shown that the extract of E.KS promoted diarrhea in mouse feces after administration, inhibited the contraction of smooth muscle of mouse small intestine and caused the inflammatory exudation on the mucosa of the intestines, enhanced the expression of both mRNA and the protein levels of IL-1β and TNFα in the small or large intestines.@*CONCLUSION@#The results showed that the extract of E. KS acted on the intestinal smooth muscle with propulsion of feces involving the irritation of the intestines with acute inflammatory reactions.

Effect of baicalin on pattern recognition receptor TLR2/4-NOD2 and its significance of druggability / 中国中药杂志

Activation pattern recognition receptors can cause the startup of downstream signaling pathways, the expression of inflammatory factors, and finally immunological inflammatory reaction. Either exogenous pathogenic microorganisms or endogenous tissue components can activate these pattern recognition receptors as ligands at varying degrees, and then cause the immunological inflammatory reaction. Therefore, it is of great significance to inhibit relevant receptors, as well as the immunological inflammatory reaction, in order to avoid tissue injury during the course of disease. Baicalin is able to specifically inhibit the expression of TLR2/4-NOD2, inhibit the expression of inflammatory factors IL-1beta, IL-6 and TNF-alpha, and thereby reducing the injury of the tissue cells during the course of disease. This effect is non-specific with tissues, which is of great theoretical and practical significance in druggability. In addition, the drug metabolism and toxicity of baicalin are also discussed for its druggability in this article.

Role of baicalin in regulating Toll-like receptor 2/4 after ischemic neuronal injury / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Baicalin has a significant anti-inflammation effect and is widely used in the clinical treatment of stroke. Most of the studies of Toll-like receptor 2/4 (TLR2/4) during cerebral ischemia had defined their specific expressions in microglia in hippocampus tissue. To explore the targets of baicalin in stroke, we detected the expressions of TLR2/4 in vitro/vivo.</p><p><b>METHODS</b>By constructing a cerebral ischemia-reperfusion model in vivo and glucose oxygen deprivation model, we successfully induced neuron damage, then added baicalin and detected expressions of TLR2/4, nuclear factor-kB (NF-kB), tumor necrosis factor-alpha (TNFα), and interleukin-1β (IL-1β) in mRNA level and protein level.</p><p><b>RESULTS</b>We found distinct upregulations of TLR2/4 and TNFα in both mRNA level and protein level in PC12 cells and primary neurons. Moreover, TLR2/4 and TNFα expressions were significantly higher in mice hippocampus treated with cerebral ischemia-reperfusion. Baicalin could downregulate the expressions of TLR2/4 and TNFα in the damaged cells and mice hippocampus effectively.</p><p><b>CONCLUSIONS</b>Neurons could respond to the damage and activate the related signal pathway directly. TLR2/4 responsed to the damage and sent the signal to downstream factor TNFα through activating NF-kB. Baicalin could inhibit the inflammatory reaction in neuron damage and TLR might be its targets, which explained why baicalin could widely be used in the clinical treatment of stroke.</p>

New cerebroside from leaves of pineapple / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the leaves of pineapple.</p><p><b>METHOD</b>Chromatographic methods were used to isolate compounds from the leaves of pineapple and spectral methods were used to identify the structures of the isolated compounds.</p><p><b>RESULT</b>Compound 1 was isolated from the leaves of pineapple. It was identified as 1-O-beta-D-glucopyranosyl-(2S, 3R, 4E, 11E)-2-[(2(R)-hydroxydocosanoyl) amido]-4, 11-hexadecanediene-1, 3-diol.</p><p><b>CONCLUSION</b>Compound 1 was a new compound.</p>

Studies on phenolic constituents from leaves of pineapple (Ananas comosus) / 中国中药杂志

<p><b>OBJECTIVE</b>To study the phenolic constituents of the leaves of pineapple.</p><p><b>METHOD</b>Chromatographic methods were used to isolate compounds from the leaves of pineapple and spectroscopic methods were used to identify the structures of the isolated compounds.</p><p><b>RESULT</b>7 compounds, ananasate (1), 1-O-caffeoylglycerol (2), 1-O-p-coumaroylglycerol (3), caffeic acid (4), p-coumaric acid (5), beta-sitosterol (6) and daucosterol (7), were isolated from the leaves of pineapple.</p><p><b>CONCLUSION</b>1 was a new compound, and others were obtained from this plant for the first time.</p>

Analysis of the volatile components of YL2000 decoction by GC-MS / 中国中药杂志

<p><b>OBJECTIVE</b>To analyze the volatile components of YL2000 decoction, which contain four herbs: rhizome and root of the Notopterygium incisum, the root of the Angelica pubescens f. biserrata, Scutellaria baicalensis and Coptis chinensis and investigate the changes of volatile constituents from those four herbs before and after compatibility of the herbal medicines.</p><p><b>METHOD</b>The volatile components of YL2000 decoction were extracted by water-steam distillation, separated and identified by GC-MS. The relative percent content of each volatile component was quantified by area normalization method. The volatile components of YL2000 decoction were compared with the composition of the volatile oil from individual herb respectively.</p><p><b>RESULT</b>39 of the 146 separated constituents in volatile oil of YL2000 decoction, accounting for 85.66%, were identified and quantified. After compatibility of the herbal medicines, most volatile oil components reported by high proportion in individual herb were not detected, in the mean time, some components in volatile oil of YL2000 decoction have never been reported before in those of all four herbs.</p><p><b>CONCLUSION</b>The changes of volatile oil from those four herbs before and after compatibility of the herbal medicines indicate that solubilization, chemical reactions and evaporation of some volatile components during decocting may induce changes of several components.</p>

Studies on chemical constituents from flowers of Apocynum venetum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the flowers of Apocynum venetum.</p><p><b>METHOD</b>Chromatographic methods were used to isolate compounds from the flowers of A. venetum and spectral methods were used to identify the structures of the isolated compounds.</p><p><b>RESULT</b>Seven compounds, kaempferol (I), quercetin (II), quercetin-3-O-beta-D-glucoside (III), kaempferol-3-O-beta-D-glucoside (IV), vanillic acid (V), baimaside (VI), daucosterol (III), were isolated from the flowers of A. venetum.</p><p><b>CONCLUSION</b>Compound I, V, VI, VII were obtained from this plant for the first time.</p>

Chemical constituents from the rhizoma of Arundina graminifolia / 中国中药杂志

<p><b>OBJECTIVE</b>To isolate and elucidate the chemical constituents from the tuber of Arundina graminifolia.</p><p><b>METHOD</b>The compounds were extracted by 95% alcohol and isolated by column chromatography on silica gel, SephedaxLH-20 and ODS. The structures were determined by UV, IR, NMR and MS spectral analysis.</p><p><b>RESULT</b>Five compounds were isolated, and their structures were identified as (2E)-, 2-propenoic acid, 3-(4-hydroxy-3-methoxyphenyl)-decosyl ester (I), p-hydroxybenzyl alcohol (II), triacontanol (III) and p-hydroxybenzylethyl ether (IV), 3-hydroxy-5-methoxybibenzyl (V), respectively.</p><p><b>CONCLUSION</b>All compounds were isolated from the genus of Arundina for the first time.</p>