Effects of moxibustion on intestinal barrier function and TLR4/NF-κB p65 signaling pathway in obese rats. / è‰¾ç¸å¯¹è‚¥èƒ–å¤§é¼ è‚ é“å±éšœåŠŸèƒ½åŠTLR4/NF-κB p65信号通路的影响.

OBJECTIVES: To observe the effects of moxibustion on intestinal barrier function and Toll-like receptor 4 (TLR4)/nuclear factor-κB p65 (NF-κB p65) signaling pathway in obese rats and explore the mechanism of moxibustion in the intervention of obesity. METHODS: Fifty-five Wistar rats of SPF grade were randomly divided into a normal group (10 rats) and a modeling group (45 rats). In the modeling group, the obesity model was established by feeding high-fat diet. Thirty successfully-modeled rats were randomized into a model group, a moxibustion group, and a placebo-control group, with 10 rats in each one. In the moxibustion group, moxibustion was applied at the site 3 cm to 5 cm far from the surface of "Zhongwan" (CV 12), with the temperature maintained at (46±1 ) ℃. In the placebo-control group, moxibustion was applied at the site 8 cm to 10 cm far from "Zhongwan" (CV 12), with the temperature maintained at (38±1) ℃. The intervention was delivered once daily for 8 weeks in the above two groups. The body mass and food intake of the rats were observed before and after intervention in each group. Using ELISA methool, the levels of serum triacylglycerol (TG), total cholesterol (TC) and lipopolysaccharide (LPS) were detected and the insulin resistance index (HOMA-IR) was calculated. HE staining was used to observe the morphology of colon tissue. The mRNA expression of zonula occludens-1 (ZO-1), Occludin, Claudin-1, TLR4 and NF-κB p65 in the colon tissue was detected by quantitative real-time PCR; and the protein expression of ZO-1, Occludin, Claudin-1, TLR4 and NF-κB p65 was detected by Western blot in the rats of each group. RESULTS: Compared with the normal group, the body mass, food intake, the level of HOMA-IR, and the serum levels of TC, TG and LPS were increased in the rats of the model group (P<0.01); those indexes in the moxibustion group were all reduced when compared with the model group and the placebo-control group respectively (P<0.01, P<0.05). Compared with the normal group, a large number of epithelial cells in the mucosa of colon tissue was damaged, shed, and the inflammatory cells were infiltrated obviously in the interstitium in the rats of the model group. When compared with the model group, in the moxibustion group, the damage of the colon tissue was recovered to various degrees and there were few infiltrated inflammatory cells in the interstitium, while, the epithelial injury of the colon tissue was slightly recovered and the infiltrated inflammatory cells in the interstitium were still seen in the placebo-control group. The mRNA and protein expressions of ZO-1, Occludin and Caudin-1 were decreased in the model group compared with those in the normal group (P<0.01). When compared with the model group and the placebo-control group, the mRNA and protein expressions of these indexes were increased in the moxibustion group (P<0.01, P<0.05). In the model group, the mRNA and protein expressions of TLR4 and NF-κB p65 were increased when compared with those in the normal group (P<0.01), and the mRNA and protein expressions of these indexes were reduced in the moxibustion group when compared with those in the model group and the placebo-control group (P<0.01). CONCLUSIONS: Moxibustion can reduce the body mass and food intake, regulate the blood lipid and improve insulin resistance in the rats of obesity. It may be related to alleviating inflammatory response through improving intestinal barrier function and modulating the intestinal TLR4/NF-κB p65 signaling pathway.

Efficacy of acupuncture therapy on cancer-related insomnia: a systematic review and network meta-analysis.

Objectives: Cancer-related insomnia (CRI) takes a toll on many cancer survivors, causing distressing symptoms and deteriorating the quality of life. Acupuncture therapy has been used for CRI already. However, it is still uncertain which acupuncture regime is best for CRI. The primary objective of this review is to conduct a comparative evaluation and ranking of the effectiveness of different acupuncture therapies for CRI. Methods: Randomized controlled trials (RCTs) that were published up to July 31, 2023, from 8 databases (PubMed, Embase, Cochrane library, Web of Science, China National Knowledge Infrastructure, Wanfang Database, VIP Database, and China Biology Medicine disc) were integrated in this study. Trials that met the inclusion criteria were evaluated the risk of bias. Pittsburgh sleep quality index (PSQI) was used to assess the efficacy of different acupuncture therapies as the primary outcome. Then, STATA 15, R, and OpenBUGS were applied to perform the network meta-analysis. PRISMA statements were followed in this network meta-analysis. Results: A total of 37 studies were included in this review, involving 16 interventions with 3,246 CRI participants. Auriculotherapy + moxibustion [surface under the cumulative ranking curve (SUCRA) 98.98%] and auriculotherapy (SUCRA 77.47%) came out top of the ranking, which were more effective than control, medicine, usual care and sham acupuncture. Conclusion: Auriculotherapy + moxibustion and auriculotherapy + acupuncture emerged as the top two acupuncture regimes for CRI and future studies should pay more attention to CRI. Clinical trial registration: https://clinicaltrials.gov/, identifier INPLASY202210095.

Los posibles mecanismos de pardeamiento del tejido adiposo blanco: una diana novedosa para el tratamiento de la obesidad.

Introduction: The increase of the obesity pandemic worldwide over the last several decades has generated a constant need for the scientific world to develop new possibilities to combat obesity. Since the discovery that brown adipose tissue (BAT) exists in adult humans, and BAT activation contributes to a negative energy balance, much more attention has been focused on the understanding of the molecular switches and their different regulatory mechanisms turning on energy expenditure. Recent insights have revealed that a range of stimuli including cold exposure, physical activity and diet, and critical transcription molecules such as PPARγ, PRDM16, PGC-1α and UCP1, aiming at the induction of BAT activation, could cause the browning of white adipose tissue, thereby dissipating energy and increasing heat production. An increasing number of studies that point to the white adipose tissue (WAT) browning strategies aiming at diet-induced and/or genetically determined obesity have been tested in mouse models as well as in human studies. The aim of this review is to summarize the transcriptional regulators as well as the various mediators that have been regarded as potential therapeutic targets in the process of WAT browning.

Introducción: La creciente prevalencia mundial de la obesidad en las últimas décadas ha hecho que la comunidad científica siga necesitando desarrollar nuevas posibilidades para luchar contra la obesidad. Desde que se descubrió que el tejido adiposo pardo (TAP) existe en los adultos y que la activación del TAP contribuye al equilibrio energético negativo, se ha prestado más atención a la comprensión de los interruptores moleculares y sus diferentes mecanismos de regulación del consumo de energía. Estudios recientes han demostrado que una serie de estímulos, incluyendo la exposición al frío, la actividad física y la dieta, y moléculas clave de transcripción como PPARγ, PRDM16, PGC-1α y UCP1, dirigidos a inducir la activación del TAP, podrían causar un pardeamiento del tejido adiposo blanco (TAB), disipando energía y aumentando la producción de calor. Se ha realizado un número cada vez mayor de estudios sobre estrategias de pardeamiento del TAB para la obesidad inducida por la dieta y/o genéticamente determinada. Desafortunadamente, el potencial terapéutico de estas estrategias de pérdida de peso mediante la inducción de la activación del TAP y el pardeamiento del TAB no se ha confirmado en seres humanos. El objetivo de esta revisión es resumir los reguladores de la transcripción y los mediadores que se consideran objetivos terapéuticos potenciales en el proceso de pardeamiento del TAB.

Effects of moxibustion on reproduction and metabolism of polycystic ovary syndrome: a protocol for meta-analysis and systematic review.

INTRODUCTION: Polycystic ovary syndrome (PCOS) is one of the most common endocrinopathy in women of reproductive age. Recently, moxibustion, as a complementary and alternative therapy, has been commonly used in assisted reproduction and improvement of metabolic abnormalities in patients with PCOS. Currently, intervention efficacy of the use of moxibustion in PCOS treatment still remains controversial due to lack of high-quality evidence. Consequently, this study protocol was designed to objectively review and evaluate the effectiveness and safety of moxibustion treatment for PCOS. METHODS AND ANALYSIS: Electronic searches will be carried out from inception to May 2021 in the online databases of The Cochrane Library, PubMed, EMBASE, Chinese Biomedical Literature, Chongqing VIP Chinese Science and Technology Periodical Database (VIP) and China National Knowledge Infrastructure. The Chinese Clinical Trial Registry Center and Clinical Trials will be used for searching ongoing trials. Randomised controlled trials and the first period in randomised cross-over trials involving any type of moxibustion for patients with PCOS will be included. Primary outcomes will be the ovulation rate, pregnancy rate and sex hormone levels, and secondary outcomes will be changes in clinical symptoms and metabolic indicators, total effective rate and the incidences of side effects and adverse events. Briefly, two reviewers will independently conduct study selection and data extraction, and the risk of bias will be assessed. Prior to the formal meta-analysis, the heterogeneity of included studies will be assessed. Review Manager Statistical Software (RevMan) V.5.3 will be used for data processing. Finally, the Grading of Recommendations Assessment, Development and Evaluation method will be applied to evaluate the quality of evidence. ETHICS AND DISSEMINATION: Ethical approval is not necessary since this study is designed as a systematic review. This study will be disseminated by a peer-review journal or conference presentation.

Effect of Electroacupuncture on Neurological Deficit and Activity of Clock and Bmal1 in Cerebral Ischemic Rats.

Acute focal cerebral ischemic stroke (IS) is a leading cause of morbidity and mortality worldwide. Acupuncture is an emerging alternative therapy that has been beneficial to acute brain ischemia. However, the underlying protective mechanism of its neuroprotective effect remains unclear. Human original circadian rhythm will be lost after IS, which seriously affects the quality of life and functional recovery of stroke patients. We hypothesize that acupuncture treats IS by regulating the balance of Clock and Bmal1. This study aims to explore the effect of acupuncture at acupoints GV20 and BL23 on neuroprotection and anti-apoptosis in middle cerebral artery occlusion (MCAO) rats and expression of apoptosis and circadian rhythm related proteins. Male Sprague-Dawley (SD) rats were randomly divided into five groups: normal group (Normal), sham model group (Sham MCAO), MCAO model group (MCAO), sham electroacupuncture group (Sham EA) and electroacupuncture group (EA). The MCAO model was prepared by electrocoagulation. The first acupuncture treatment was performed within 2 h after surgery, and then acupuncture therapy was performed on 1st day, 2nd day and 3rd day respectively. After their neurological examination at 72 h of ischemia, the rats from each group were sacrificed. Triphenyltetrazolium chloride (TTC) staining was used to evaluate the brain infarct size. Ultrastructural observation on cerebral ischemic cortex and serum inflammatory cytokines were evaluated. TUNEL staining was used to detect cell apoptosis of brain tissue. The expression levels of proteins Bax, bcl-2, caspase-3, Clock and Bmal1 in the cerebral ischemic region were detected by immunofluorescence staining. Here, we presented evidence that EA at GV20 and BL23 could significantly improve the neurological deficit score and infarct size, and alleviate the cell apoptosis of brain tissue. Moreover, acupuncture treatment upregulated the anti-apoptotic Bcl-2/Bax ratio and reversed the upregulation of caspase-3 following 72-h cerebral ischemia. In addition, the expression levels of circadian proteins Clock and Bmal1 were upregulated in EA group while compared with MCAO group. Our study demonstrated that acupuncture exerted neuroprotective effect against neuronal apoptosis after stroke and the mechanism might be related with regulation of circadian rhythm proteins Clock and Bmal1.

Kalshiolin A, new lignan from Kalimeris shimadai.

The Asian plant Kalimeris shimadai has been used as food and ethnologic medicine for over a thousand years. In this study, we isolated and identified one new lignan, kalshiolin A (1), and 12 known lignans (2-13). The structures were characterized by the comprehensive analyses of spectroscopic data (HR-ESI-MS, IR, 1D, and 2D-NMR) and the absolute configuration of 1 was determined from ECD calculations. The new compound 1 was also screened for cytotoxic activity but did not show significant potency (IC50 35.9-43.3 µM) against A549, MDA-MB-231, MCF7, KB, and KB-VIN cell lines.

Kalshinoids A-F, Anti-inflammatory Sesquiterpenes from Kalimeris shimadae.

In a study of the potential anti-inflammatory constituents from Kalimeris shimadae, six new sesquiterpenes, kalshinoids A-F (1-6), together with 21 known compounds (7-27), were isolated. The structures and absolute configurations of the new compounds were discerned from extensive spectroscopic analysis, and the absolute configurations of kalshinoids A, B, E, and F were established by ECD calculations. Furthermore, the identified compounds were tested for anti-inflammatory activity as assessed by inhibition of tumor necrosis factor-alpha (TNF-α) in THP-1 cells. Three sesquiterpenes [kalshinoid F, 4(15)-eudesmen-1ß,7,11-triol, and 4α,10α,11-trihydroxy-1ßH,5ßH-guai-7(8)-ene] reduced levels of TNF-α in lipopolysaccharide-stimulated THP-1 cells in a concentration-dependent manner and were more potent than dexamethasone. These natural sesquiterpenes merit further investigation as possible anti-inflammatory agents.

The feasibility of two anthropometric indices to identify metabolic syndrome, insulin resistance and inflammatory factors in obese and overweight adults.

OBJECTIVES: A body shape index (ABSI) and body roundness index (BRI) were reported to predict diabetes and hypertension in general population, but their validity was regularly questioned. The aim of this study was to evaluate whether ABSI and BRI are the best anthropometric indices to reflect metabolic syndrome (MetS), insulin resistance (IR), and inflammatory factors in obese and overweight Chinese adults. METHODS: Cross-sectional data on sociodemographic, lifestyle, anthropometric indices, clinical characteristics, and biochemical measurements were collected for 1442 Chinese obese and overweight adults. Logistic regression analysis examined the associations between anthropometric indices with incidences of MetS and IR in both sexes. Furthermore, the correlation between anthropometric indices and inflammatory factors was assessed. RESULTS: Multivariate regression analysis depicting BRI and waist circumference (WC) were associated significantly with MetS and IR. BRI had the highest odds ratios (ORs) for IR and WC had the highest ORs for MetS in all anthropometric indices. However, ABSI did not exhibit any association between the MetS and IR. The ABSI adjusted regression coefficients (ß values) were 0.403 for high-sensitivity C reactive protein, 0.077 for tumor necrosis factor-α, and 0.022 for interleukin-6. BRI and WC were also significantly associated with three inflammatory factors. Comparing the lowest with the highest quintile, BRI had the largest ORs for MetS (OR, 5.778; 95% confidence interval [CI], 2.954-11.303; P < 0.01) and IR (OR, 6.212; 95% CI, 2.912-13.250; P < 0.01). CONCLUSION: Only BRI and WC, not ABSI, can significantly determine the presence of MetS and IR. BRI showed the optimal capability to identify IR in obese and overweight population.

[Electroacupuncture Reduces Body Fat by Down-regulating IL-6 and Vimentin in Abdominal White Adipose Tissue of Diet-induced Obesity Rats].

OBJECTIVE: To investigate the effect of electroacupuncture (EA) on IL-6 and vimentin protein expression in white adipose tissue (WAT) of diet-induced obesity (DIO) rats, so as to reveal its mechanism underlying losing weight. METHODS: Thirty-four Wistar rats were randomly divided into normal (control, n＝10), model, sham-EA and EA groups (n＝8 in each of the latter 3 groups). The obesity model was established by feeding the rats with high fat diet. EA (2 Hz/15 Hz, 1 mA) was applied to bilate-ral "Zusanli "(ST 36) and "Tianshu "(ST 25) for 30 min, 5 times per week for a total of 8 weeks. For sham-EA group, two sham points (about 5 mm lateral to ST 36 and to ST 25) were only punctured with filiform needles but without electrical stimulation. Du-ring EA treatment, all rats were fed with normal fodder, and their body weight were measured once a week. Histopathologic changes (diameters of adipose cells) of abdominal WAT were observed under microscope after sectioning and H．E. staining, and the expression levels of IL-6 and vimentin in the WAT were detected by Western blot. RESULTS: Compared with the control group, the body weight, diameter of fat cells and the expression levels of IL-6 and vimentin in the WAT were significantly increased in the model group (P<0.05). Following EA, the body weight, diameter of fat cells and the expression levels of IL-6 and vimentin proteins were considerably down-regulated in the EA group (P<0.05), rather than in the sham-EA group relevant to the model group (P>0.05)．. CONCLUSION: EA intervention can effectively down-regulate the expression of IL-6 and vimentin in WAT of DIO rats, which may contribute to its action in reducing body fat by relieving chronic inflammation.

The WT1/MVP-Mediated Stabilization on mTOR/AKT Axis Enhances the Effects of Cisplatin in Non-small Cell Lung Cancer by a Reformulated Yu Ping Feng San Herbal Preparation.

Chemo-resistance is an obstacle in therapy of lung cancer. Alternative therapy of using herbal medicine has been proposed to resolve this obstacle. Yu Ping Feng San (YPFS), a common Chinese herbal medicinal mixture, has been reported to show anti-drug resistance on cisplatin (DDP), a common lung cancer drug. To optimize the anti-cancer function of YPFS, different Chinese herbal extracts having known function to overcome lung cancer were screened in combining with YPFS, as to increase the efficacy of DDP in drug resistance lung cancer cell, A549/DDP. Amongst these herbal extracts, Ginkgo Folium exhibited the most promoting sensitized effect. This revised herbal formula, named as YPFS+GF, promoted the DDP-induced toxicity by over 2-fold as compared to that of YPFS alone; this potentiation was confirmed by inducing cell apoptosis. The anti-drug resistance of YPFS, triggered by an increase of intracellular concentration of DDP, was accompanied by an increased expression and activity of WT1, which consequently decreased the transcript level of MVP. In addition, the MVP-mediated downstream effector mTOR2/AKT was disrupted after application of YPFS+GF in DDP-treated A549/DDP cell: this disruption was characterized by the decline of mTORC2 components, e.g., Rictor, p-mTOR, as well as the phosphorylation level of its downstream protein AKT. The disruption on mTORC2/AKT could be reversed by mTORC2 inducer insulin and promoted by mTORC2 inhibitor PP242. Thus, the anti-drug resistance of YPFS+GF in DDP-treated lung cancer cells might be mediated by the down regulation of WT1/MVP axis, as well as the downstream anti-apoptotic pathway of mTORC2/AKT signaling. Herbal medicine is one of the main adjuvant therapies in non-small cell lung cancer, and this novel herbal formula supports the prescription of traditional Chinese medicine in cancer treatment.

Flavonoids, a Potential New Insight of Leucaena leucocephala Foliage in Ruminant Health.

We investigated the constituents of Leucaena leucocephala foliage collected from Guangdong province in China and isolated 17 diverse flavonoids (1-17), including flavones (5-9, 11, and 12), flavonols (1, 10, and 16), flavanone 4, flavanonol 15, and flavonol glycosides (2, 3, 13, 14, and 17). Flavonoids quercetin (1), quercetin-3- O-α-rhamnopyranoside (2), and myricetin-3- O-α-rhamnopyranoside (17) were the major flavonoids components in L. leucocephala leaves, at a total concentration of about 2.5% of dry matter. pHRE-Luc inductive activity to mimic the activation of erythropoietin (EPO) gene, anti-inflammatory, antidiabetic, and antioxidant activities of isolated flavonoids (1-17) were evaluated. Flavonoids 7, 10, and 13 could strongly induce the transcriptional activity of pHRE-Luc, which indicated their potential to induce the expression of EPO. Flavonoids 7, 10, 13, and 17 displayed strong anti-inflammatory activity, relatively equal to the positive control dexamethasone. Flavonoids 1, 2, 3, 11, 12, 16, and 17 showed stronger antioxidant activities of DPPH radical scavenging capacity than ascorbic acid. Flavonoids 1, 2, and 10 showed weak cellular antioxidant activities against tert-butyl hydroperoxide (tBHP) induced ROS formation. Flavonoid rhamnoside 2 and arabinoside 3 undergone deglycosylation to the aglycone quercetin under anaerobic incubation with cattle rumen microorganisms. Furthermore, the potential health benefits for ruminant of flavonoids, which was rich in L. leucocephala foliage, was also discussed.

Limonoids and triterpenoid from fruit of Swietenia macrophylla.

Five new limonoids, swieteliacates A-E (1-5) and a tirucallane-type triterpenoid, swietesenin (6), together with four known compounds (7-10) were isolated from fruit of Swietenia macrophylla. Their structures were determined by spectroscopic analyses. The new compounds were tested in vitro for their cytotoxic effects against five human cancer cell lines. Compound 2 exhibited moderate cytotoxic activities against SW480 and HL-60 cancer cell lines with IC50 values of 30.6 and 32.9µM, respectively.

A new sesquiterpene from Kalimeris integrifolia.

A new sesquiterpene kalinturoside A (1), and 17 known compounds friedelan-3-ol (2), 24-ethyl-5a-cholesta-7, 22(E)-dien-3-one (3), friedelin (4), syringaresinol (5), α-spinasterol (6), ciwujiatone (7), syringic acid (8), scopoletin (9), apocynin (10), 1-(3-hydroxy-4, 5-dimethoxyphenyl)ethan-1-one (11), apigenin (12), 5-hydroxymethylfurfural (13), stigmasterol-3-O-ß-d-glucopy-ranoside (14), bidenoside C (15), citrusin (16), irioresinol A (17) and syringaresinol-4-O-ß-d-glucopyranoside (18) were isolated from the herbs of Kalimeris integrifolia. The structures of these compounds were elucidated using spectroscopic techniques such as NMR and MS. All of the compounds were isolated from this genus for the first time.

Ginkgetin induces autophagic cell death through p62/SQSTM1-mediated autolysosome formation and redox setting in non-small cell lung cancer.

Promoting cell death by autophagy could be a novel treatment for cancer. The major player in autophagy, p62, serves as a good therapeutic target. Ginkgetin, a biflavonoid from Ginkgo biloba leaves, exhibited promising anticancer activity in non-small cell lung cancer cell lines, with an IC50 lower than that of cisplatin. This anticancer effect of ginkgetin was illustrated in a xenograft nude mouse model. Ginkgetin induced autophagic cell death in A549 cells, and this effect was markedly reversed by chemical and genetic approaches. Ginkgetin showed potential binding affinity to p62. Upregulation of p62 through chemical and genetic means decreased cell death, lysosome acidification, and autophagosome formation, which consequently disrupted autolysosome formation. In addition, the decreased autophagy induced by p62 overexpression increased Nrf2/ARE activity and the oxygen consumption rate and decreased on formation of reactive oxygen species. These phenomena were exhibited in a reciprocal manner when p62 was knocked down. Thus, p62 may be a potential target in ginkgetin-induced autophagic cell death, and ginkgetin could be developed as a novel anticancer drug.

Comparative Study of Different Acorus Species in Potentiating Neuronal Differentiation in Cultured PC12 Cells.

Acori Tatarinowii Rhizoma (ATR), the rhizome of Acorus tatarinowii Schott, is a common traditional Chinese medicine being used clinically for mental disorder. However, other Acorus species herbs are all having the same Chinese name 'Chang Pu', making the confusion in herbal market. Acori Graminei Rhizoma (AGR) and Acori Calami Rhizoma (ACR) are common adulterants of ATR. Here, we aim to provide a comparative analysis between ATR, AGR, and ACR in potentiating neuronal differentiation. Volatile oil, derived from Acorus species, was applied onto cultured PC12 cells, and various parameters were determined: (i) transcriptional activation of neurofilament promoters was determined by the promoter-driven luciferase activity assay; (ii) the neurite outgrowth of PC12 cells was captured and measured; and (iii) the neurofilament expression and its underlying mechanism were analyzed by western blotting. The co-treatment of ATR, AGR, or ACR volatile oil with low concentration of nerve growth factor (NGF) could potentiate the NGF-induced neuronal differentiation in cultured PC12 cells. In addition, application of protein kinase A inhibitor H89 in cultures blocked the induction of neurofilament. Among these three Acorus species, ATR volatile oil showed the highest NGF-induced induction in neurite outgrowth and neurofilament expression, as compared with that of AGR and ACR. Copyright © 2017 John Wiley & Sons, Ltd.

New Acetylenic Acids and Derivatives from the Edible Mushroom Craterellus lutescens (Cantharellaceae).

Thirteen new acetylenic acids and their derivatives, craterellynes G-Q (1, 2, 4-10, 12, 13), 9-epi-craterellyne H (3), and 14-O-ethyl-craterellyne O (11), were isolated from the fruiting bodies of edible mushrooms Craterellus lutescens. The structures of these compounds were identified by various spectroscopic and chemical means. The stereoconfigurations of 1-13 were elucidated by the combination of acetonide formation, J-based configuration analysis, and modified Mosher's method. Craterellyne I exhibited cytotoxicities against human cancer strains and inhibition of nitric oxide (NO) production, as well as weak antimicrobial activity against Candida albicans.

Two new terpenoids from Kalimeris indica.

A new nor-sesquiterpene kalimeristone A (1), a new nor-triterpenoid kalimerislactone B (2) and eight known compounds 7-hydroxy-4'methoxyisoflavone (3), episyringaresinol (4), epipinoresinol (5), rhamnetin (6), vanillin (7), p-hydroxybenzaldehyde (8), syringic acid (9) and 3, 4-dihydroxybenzaldehyde (10) were isolated from the herbs of Kalimeris indica. The structures of these compounds were elucidated using spectroscopic techniques, such as NMR and MS. All of the compounds were isolated from this genus for the first time. The cytotoxicities against four cancer cell lines were evaluated in vitro, but were inactive.

Nuclear Factor kB and Inhibitor of kB: Acupuncture Protection Against Acute Focal Cerebral Ischemia in Rodents.

Context • Acute, focal, cerebral ischemic stroke is a leading cause of morbidity and mortality worldwide. Acupuncture is an emerging alternative therapy for treatment of acute brain ischemia. Nevertheless, the precise mechanism underlying the neuroprotective effects of acupuncture has not been elucidated. Nuclear factor κB (NF-κB) and nuclear factor of κ light polypeptide gene enhancer in B cell inhibitor alpha (IκB-α) are involved in cerebral inflammation. However, the involvement of NF-κB and IκB-α in the protective effects of acupuncture on ischemic tolerance remains unknown. Objective • The study evaluated the hypothesis that acupuncture can exert a neuroprotective action in a rat model of middle cerebral artery occlusion (MCAO). Design • The rats were randomly divided into a normal group (N), a sham model group (SM), an MCAO model group (M), a sham acupuncture group (SA), and an acupuncture group (A). Setting • All of processes of this study were conducted at Hubei University of Chinese Medicine (Hubei Shang, China). Animals • The animals were 100 Sprague-Dawley rats, aged 3 mo. Intervention • Craniotomy and electrocoagulation of the middle cerebral artery were conducted to generate acute, focal, cerebral ischemic models in 3 groups, excluding the N and SM groups. The SM group received a surgical fenestration similar to the M group, but the procedure did not include the coagulation of the exposed artery. In the A group, acupuncture was administered at the acupoints Baihui (GV-20) and Renzhong (GV-26). In the SA group, sham acupuncture was performed at a depth of 5 mm at a position close to the left side of the GV-20 and GV-26 points. The N, M, and SM groups received neither the acupuncture nor the sham acupuncture treatment. Outcome Measures • The study (1) evaluated neurological function using the modified neurological severity score; (2) examined the ultrastructure; (3) assessed the infarct volume; (4) determined levels of serum inflammatory cytokines; and (5) measured protein expression in the hippocampus 24 h after MCAO using a Western blot analysis. Results • Acupuncture significantly decreased infarct size and improved neurological function. The levels of the target protein NF-κB and of serum inflammatory cytokines significantly decreased in group A compared with those in groups M and SM. The IκB-α level was generally higher in group A than in groups M and SM. Conclusions • Acupuncture can significantly enhance the expression of IκB-α, which is the inhibitory protein of NF-κB, and it can inhibit the expression of various inflammatory cytokines induced by NF-κB, thereby alleviating acute, focal, cerebral ischemic injury.

Chemical Constituents and Their Bioactivities of Mushroom Phellinus rhabarbarinus.

Phellinus rhabarbarinus soaked in wine has folk usages by local residents of Ailao mountain of Yunnan province, China, which were to daub the wound to prevent infection and to drink to enhance immunity and treat other diseases such as cough, gastritis, and cancer. Systemic investigation on the chemical constituents of fruiting bodies of P. rhabarbarinus resulted in the isolation of 11 lanostane triterpenoids (1-10) including three new ones, namely, phellibarins A-C (1-3), together with five ergosterols (11-15). This is the first time reporting secondary metabolites of P. rhabarbarinus. Compounds 2, 3, 7, and 8 showed inhibitory activities against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages, whereas compounds 2-4, 6, 7, and 10 exhibited cytotoxicities against human cancer cell lines. The results of this assessment suggested that the lanostane triterpenoids in fruiting bodies of P. rhabarbarinus played key roles in its folk usages.

Leucocontextins A-R, lanostane-type triterpenoids from Ganoderma leucocontextum.

Eighteen new lanostane-type triterpenoids, namely leucocontextins A-R (1-18) were isolated from the fruiting bodies of Ganoderma leucocontextum. Their structures were established by 1D and 2D NMR data in conjunction with HRESIMS/HREIMS, X-ray single crystal diffraction analysis. Compound 18 exhibited weak cytotoxicity against K562 and MCF-7 cell lines with IC50 of 20-30 µM.