Evaluating the efficacy and safety of perianal injection of liposomal ropivacaine HR18034 for postoperative analgesia following hemorrhoidectomy: A multicenter, randomized, double-blind, controlled phase II clinical trial.

STUDY OBJECTIVE: HR18034, composed of the ropivacaine encapsulated in multi-lamellar, concentric circular structure liposomes as the major component and a small amount of free ropivacaine, has performed well in animal experiments and phase I clinical trials. This trial was to investigate the efficacy, safety, pharmacokinetic profile and the minimum effective dose of HR18034 for postoperative analgesia after hemorrhoidectomy compared with ropivacaine. DESIGN: A multicenter, randomized, double-blind trial. SETTING: 19 medical centers in China. PATIENTS: 85 patients undergoing hemorrhoidectomy between October 2022 to November 2022. INTERVENTIONS: Patients were randomly divided into HR 18034 190 mg group, 285 mg group, 380 mg group and ropivacaine 75 mg group, receiving single local anesthetic perianal injection for postoperative analgesia. MEASUREMENTS: The primary outcome was the area under the resting state NRS score -time curve within 72 h after injection. The second outcomes included the proportion of patients without pain, the proportion of patients not requiring rescue analgesia, cumulative morphine consumption for rescue analgesia, etc. Safety was evaluated by adverse events incidence and plasma ropivacaine concentrations were measured to explore the pharmacokinetic characteristics of HR18034. MAIN RESULTS: The areas under the NRS score (at rest and moving states)-time curve were significantly lower in HR 18034 380 mg group than ropivacaine 75 mg at 24 h, 48 h, and 72 h after administration. However, this superiority was not observed in HR18034 190 mg group and 285 mg group. There was no difference in cumulative morphine consumption for rescue analgesia between HR 18034 groups and ropivacaine group. CONCLUSIONS: HR 18034 380 mg showed superior analgesic efficacy and equivalent safety compared to ropivacaine 75 mg after hemorrhoidectomy, thus preliminarily determined as minimum effective dose.

Phenylethanoid glycosides from Michelia champaca leaves.

Chemical investigation on the leaves of Michelia champaca L. (Magnoliaceae) led to the isolation of five previously undescribed phenylethanoid glycosides (PhGs), 4-O-ß-d-glucopyranosyl-acteoside (1), 4‴-O-(6-O-E-caffeoyl)-ß-d-glucopyranosyl-acteoside (2), 4‴-O-(6-O-E-caffeoyl)-ß-d-glucopyranosyl-isoacteoside (3), 6""-O-E-feruloyl-echinacoside (4), and 6""-O-p-E-coumaroyl-echinacoside (5), together with eighteen known PhGs. Their structures were determined by spectroscopic and chemical methods. All the known PhGs except acteoside (8) were not previously reported in the genus. Twenty-one PhGs exhibited more potent DPPH radical scavenging activity and FRAP than l-ascorbic acid (l-AA), and twenty-two PhGs showed better ABTS radical cation scavenging activity than l-AA. In addition, twelve PhGs displayed more potent cellular reactive oxygen species scavenging activity than curcumin. The results revealed that the leaves of M. champaca are a rich source of phenylethanoid glycosides and antioxidants.

Quasi-static testing of UHPC cupped socket piers-footing connection and its seismic fragility analysis under near-fault ground motions.

Assembly construction is extensively employed in bridge construction due to its ability to accelerate construction and improve quality. To speed the recovery of bridges after major earthquakes, this study proposes an assembled connection for precast piers and footings based on assembly construction. The precast piers are connected to the footings using ultra-high-performance concrete (UHPC) post-cast cupped sockets. Two specimens are tested with a 1:4 scale, namely, the cast-in-place (CIP) specimen and, the UHPC cupped socket pier specimen. Finite element models (FEM) of a continuous girder bridge with cupped socket connections are developed and verified by experimental results. The seismic fragility analysis is conducted to investigate the difference between the cupped socket connection and the CIP connection. The experimental results showed that the plastic hinge was formed on the precast piers and there was little damage to the UHPC sockets. The results of FEA indicate that UHPC cupped socket piers have slightly higher seismic fragility than the seismic fragility of cast-in-place piers. Then, some methods were proposed to reduce the seismic fragility of UHPC cupped socket piers, and their availability was confirmed by comparing them with the seismic fragility of CIP piers. Finally, an example bridge with this connection is introduced to illustrate replacing prefabricated piers after an earthquake.

Efficacy and safety of ciprofol for sedation in outpatient gynecological procedures: a phase III multicenter randomized trial.

Objective: Ciprofol (also known as cipepofol and HSK3486), is a compound similar to propofol in chemical structure and hypnotic effect. Herein we evaluated the efficacy and safety of ciprofol for sedation in outpatient gynecological procedures. Methods: This phase III multicenter randomized trial with a non-inferiority design was conducted in nine tertiary hospitals. We enrolled 135 women aged 18-65 years who were scheduled for ambulatory gynecological procedures. Patients were randomly assigned to receive either ciprofol (0.4 mg/kg for induction and 0.2 mg/kg for maintenance) or propofol (2.0 mg/kg for induction and 1.0 mg/kg for maintenance) sedation in a 2:1 ratio. Patients and investigators for data collection and outcome assessment were blinded to study group assignments. The primary outcome was the success rate of sedation, defined as completion of procedure without remedial anesthetics. The non-inferiority margin was set at -8%. Secondary outcomes included time to successful induction, time to full awake, time to meet discharge criteria, and satisfaction with sedation assessed by patients and doctors. We also monitored occurrence of adverse events and injection pain. Results: A total of 135 patients were enrolled; 134 patients (90 patients received ciprofol sedation and 44 patients propofol sedation) were included in final intention-to-treat analysis. The success rates were both 100% in the two groups (rate difference, 0.0%; 95% CI, -4.1 to 8.0%), i.e., ciprofol was non-inferior to propofol. When compared with propofol sedation, patients given ciprofol required more time to reach successful induction (median difference [MD], 2 s; 95% CI, 1 to 7; p < 0.001), and required more time to reach full awake (MD, 2.3 min; 95% CI, 1.4 to 3.1; p < 0.001) and discharge criteria (MD, 2.3 min; 95% CI, 1.5 to 3.2; p < 0.001). Fewer patients in the ciprofol group were dissatisfied with sedation (relative risk, 0.21; 95% CI, 0.06 to 0.77; p = 0.024). Patients given ciprofol sedation had lower incidences of treat-emergent adverse events (34.4% [31/90] vs. 79.5% [35/44]; p < 0.001) and injection pain (6.7% [6/90] vs. 61.4% [27/44]; p < 0.001). Conclusion: Ciprofol for sedation in ambulatory gynecological procedures was non-inferior to propofol, with less adverse events and injection pain. Clinical trial registration: ClinicalTrials.gov, identifier NCT04958746.

Flavonoid glycosides from the leaves of Michelia champaca.

Michelia champaca L. (Magnoliaceae) was cultivated in large scale for flowers as cosmetic raw materials, whereas the value of its leaves remains to be discovered. Our chemical study on the leaves yielded four new flavonol diglycosides, champaflavosides A-D (1-4), together with twenty-three known flavonoid glycosides (5-27). Their structures were determined by spectroscopic and chemical methods. Compounds 5-21 and 23-27 were not previously reported from the genus Michelia, and kaempferol 3-O-rutinoside (22) was obtained from this species for the first time. All the compounds were evaluated for antioxidant activity by four in vitro assays. Compounds 3-12 and 20 showed more potent 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity than l-ascorbic acid (l-AA). Compounds 2-23, 25, and 27 exhibited 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical cation scavenging activity superior to l-AA. The ferric reducing antioxidant powers (FRAP) of compounds 2-13, 17, and 19 were higher than l-AA. Further, eighteen compounds demonstrated cellular reactive oxygen species (ROS) scavenging activity, of which champaflavoside D (4), rhamnetin 3-O-neohesperidoside (8), quercetin 3-O-(6-O-E-p-coumaroyl)-neohesperidoside (9), and liquiritin (27) were more potent than curcumin. The results revealed that the renewable leaves of M. champaca are a rich source of flavonoids and antioxidants.

Chemical constituents from leaves of Jatropha curcas.

Objective: To investigate the chemical constituents from the leaves of Jatropha curcas and evaluate their inhibition on lipopolysaccharide (LPS)-activated BV-2 microglia cells. Methods: The n-BuOH extract of the leaves of J. curcas was isolated by macroporous adsorption resin, silica gel, ODS, column chromatography and semi-preparative HPLC. The structures of the compounds were identified by MS, NMR, ECD, and other spectroscopic methods. In addition, anti-neuroinflammatory effects of isolated compounds were evaluated by measuring the production of nitric oxide (NO) in over-activated BV-2 cells. Results: Seventeen compounds, including (7R,8S)-crataegifin A-4-O-ß-D-glucopyranoside (1), (8R,8'R)-arctigenin (2), arctigenin-4'-O-ß-D-glucopyranoside (3), (-)-syringaresinol (4), syringaresinol-4'-O-ß-D-glucopyranoside (5), (-)-pinoresinol (6), pinoresinol-4'-O-ß-D-glucopyranoside (7), buddlenol D (8), (2R,3R)-dihydroquercetin (9), (2S,3S)-epicatechin (10), (2R,3S)-catechin (11), isovitexin (12), naringenin-7-O-ß-D-glucopyranoside (13), chamaejasmin (14), neochamaejasmin B (15), isoneochamaejasmin A (16), and tomentin-5-O-ß-D-glucopyranoside (17) were isolated and identified. Compounds 2, 4 and 8 significantly inhibited the release of NO in BV-2 microglia activated by LPS, with IC50 values of 18.34, 29.33 and 26.30 µmol/L, respectively. Conclusion: Compound 1 is a novel compound, and compounds 2, 3, 8, 14-17 are isolated from Jatropha genus for the first time. In addition, the lignans significantly inhibited NO release and the inhibitory activity was decreased after glycosylation.

Adiponectin Attenuates Splenectomy-Induced Cognitive Deficits by Neuroinflammation and Oxidative Stress via TLR4/MyD88/NF-κb Signaling Pathway in Aged Rats.

Perioperative neurocognitive disorder (PND) is a common adverse event after surgical trauma in elderly patients. The pathogenesis of PND is still unclear. Adiponectin (APN) is a plasma protein secreted by adipose tissue. We have reported that a decreased APN expression is associated with PND patients. APN may be a promising therapeutic agent for PND. However, the neuroprotective mechanism of APN in PND is still unclear. In this study, 18 month old male Sprague-Dawley rats were assigned to six groups: the sham, sham + APN (intragastric (i.g.) administration of 10 µg/kg/day for 20 days before splenectomy), PND (splenectomy), PND + APN, PND + TAK-242 (intraperitoneal (i.p.) administration of 3 mg/kg TAK-242), and PND + APN + lipopolysaccharide (LPS) (i.p. administration of 2 mg/kg LPS). We first found that APN gastric infusion significantly improved learning and cognitive function in the Morris water maze (MWM) test after surgical trauma. Further experiments indicated that APN could inhibit the Toll-like receptor 4 (TLR4)/myeloid differentiation factor 88 (MyD88)/nuclear factor kappa B (NF-κb) p65 pathway to decrease the degree of oxidative damage (malondialdehyde (MDA) and superoxide dismutase (SOD)), microglia-mediated neuroinflammation (ionized calcium binding adapter molecule 1 (IBA1), caspase-1, tumor necrosis factor (TNF)-α, interleukin-1ß (IL-1ß), and interleukin-6 (IL-6)), and apoptosis (p53, Bcl2, Bax, and caspase 3) in hippocampus. By using LPS-specific agonist and TAK-242-specific inhibitor, the involvement of TLR4 engagement was confirmed. APN intragastric administration exerts a neuroprotective effect against cognitive deficits induced by peripheral trauma, and the possible mechanisms include the inhibition of neuroinflammation, oxidative stress, and apoptosis, mediated by the suppression of the TLR4/MyD88/NF-κb signaling pathway. We propose that oral APN may be a promising candidate for PND treatment.

Preliminary Study of an Adjustable, Wearable, Noninvasive Vest Providing Chest Compression to Assist with Breathing.

Respiratory muscle paralysis caused by acute cervical spinal cord injury usually leads to pulmonary ventilation dysfunction and even death from respiratory failure. In addition to invasive treatments such as mechanical ventilation, the utilization of noninvasive respiratory support equipment plays an important role in long-term assisted breathing. In this study, we describes a wearable, noninvasive vest with adjustable pressure that enables assisted breathing and with an automatic alarm, and we aims to explore its safety and effectiveness on healthy adult participants. The vest monitors the human heart rate and the blood oxygen index data in real time, the alarm is automatically activated when the data is abnormal. Eight healthy participants had no obvious discomfort during the test while wearing the vest. Lung volumes, antero-posterior diameters, and left-right diameters at the second, fourth, and sixth ribs levels were acquired before and after inflation of the vest airbag, the data acquired by the imaging analysis using chest computed tomography showed significant differences before and after the inflation (p < 0.05). Thus, The vest designed for this study can achieve uniform and effective compression of the thorax, significantly changed the size of the thorax and lungs. It is expected to be applied as noninvasive support for patients with respiratory dysfunction.

Distinct Urinary Metabolic Biomarkers of Human Colorectal Cancer.

Colorectal cancer (CRC) is one of the most commonly diagnosed cancers with high mortality rate due to its poor diagnosis in the early stage. Here, we report a urinary metabolomic study on a cohort of CRC patients (n =67) and healthy controls (n =21) using ultraperformance liquid chromatography triple quadrupole mass spectrometry. Pathway analysis showed that a series of pathways that belong to amino acid metabolism, carbohydrate metabolism, and lipid metabolism were dysregulated, for instance the glycine, serine and threonine metabolism, alanine, aspartate and glutamate metabolism, glyoxylate and dicarboxylate metabolism, glycolysis, and TCA cycle. A total of 48 differential metabolites were identified in CRC compared to controls. A panel of 12 biomarkers composed of chenodeoxycholic acid, vanillic acid, adenosine monophosphate, glycolic acid, histidine, azelaic acid, hydroxypropionic acid, glycine, 3,4-dihydroxymandelic acid, 4-hydroxybenzoic acid, oxoglutaric acid, and homocitrulline were identified by Random Forest (RF), Support Vector Machine (SVM), and Boruta analysis classification model and validated by Gradient Boosting (GB), Logistic Regression (LR), and Random Forest diagnostic model, which were able to discriminate CRC subjects from healthy controls. These urinary metabolic biomarkers provided a novel and promising molecular approach for the early diagnosis of CRC.

Star fruit extract and C-glycosylated flavonoid components have potential to prevent air pollutant-induced skin inflammation and premature aging.

Air pollution adversely affects skin, leading to skin inflammation and premature skin aging. Plant derived antioxidant compounds have been considered to be promising in discovery of effective agents for the protection of skin from the damage by air pollutants. Our previous studies demonstrated that Averrhoa carambola fruit (known as star fruit) is rich in flavonoid C-glycosides with unique structures and potent antioxidant activity. Thus, the star fruit extract (SFE) and main flavonoid C-glycoside components, carambolasides I, J, and P (1-3), carambolaflavone B (4), and isovitexin 2″-O-α-L-rhamnoside (5), were investigated for the activity against air pollutant stress in human epidermis. As a result, SFE and compounds 1-5 exhibited significant inhibitory activity against protein carbonylation in oxidative-stressed stratum corneum with the best activity being shown by compound 3. SFE and compounds 2-5 were also active against engine exhaust-induced protein carbonylation in stratum corneum. When further evaluated, SFE and compound 3 significantly inhibited gene expression of the key inflammation mediators IL-1α and COX-2 in PM-stressed keratinocytes. The results indicated that SFE and the flavonoid C-glycosides are potentially effective against air pollutant-induced skin inflammation and premature aging.

Understanding the Cognitive Immersion of Hospitality Architecture in Culture and Nature: Cultural Psychology and Neuroscience Views.

Hotel architectural design plays a critical role in the hospitality experiences of consumers, and it is important to consider that people may have different aesthetic cognitions toward the sensory properties of nature (i.e., the architecture of the hotel), such as its color and texture, as well as the landscape. While neuroaesthetics has emerged as a nascent field in hospitality research, few studies have investigated how nature reflects aesthetic experiences in the human brain. Moreover, the neuroaesthetic interpretation of architecture through the aesthetic triad is a novel interdisciplinary field. A field survey conducted at Amanfayun, a hotel in Hangzhou, China, in support of our propositions proves that sensory-motor, knowledge-meaning, and emotion valuation systems play key roles in appreciating architectural aesthetics. This study demonstrates that the evaluation of fluency, complexity, and naturalistic patterns of an architectural masterpiece is achieved through the sensory-motor systems. Our results also prove that familiarity, expectations, context, and cultural background directly affect the aesthetic knowledge of an individual and the meaning of architecture. Moreover, the interaction of sensory-motor and knowledge elements is uniformly moderated by the emotion valuation systems, resulting in a balanced appreciation of aesthetic architecture. Finally, the study reveals the central roles of culture and nature in cognitive rejuvenation.

Anti-neuroinflammatory effects in vitro and in vivo, and chemical profile of Jatropha curcas L.

The ethyl acetate extract of the stems of Jatropha curcas (ESJ) exerted prominent anti-neuroinflammatory effect through inhibiting microglial overactivation, and reducing mRNA expression of inflammatory factors, including nitric oxide (NO), inducible nitric oxide synthase, and interleukin-1ß in the cortex and the formation of NOD-like receptor family pyrin domain containing 3 (NLRP3) inflammasomes in C57BL/6 mice. Phytochemical research afforded twenty-three major constituents, including five undescribed components (diterpenes 1-3, 7 and a triterpene 18) and a new natural product [a diterpene, (3S,5S,10R)-3-hydroxy-12-methoxy-13-methylpodopcarpa-8,11,13-trien-7-one (8)], by comprehensive analysis of spectroscopic data. Bioassay showed that ESJ (IC50: 6.49 µg/mL), diterpenes 1, 5, 12, 14, 15, 17, triterpenes 18, 19, preussomerin 22, and lactone 23 (IC50 values from 0.10 to 49.05 µM) inhibited NO production more strongly than the positive control in lipopolysaccharide-stimulated BV-2 cells. HPLC experiment further substantiated that 1, 5, 12, 14-15, 17-19, 22-23 are the characteristic constituents of ESJ, suggesting they might possess the potential for the treatment of neuroinflammation.

MicroRNA-100 inhibits breast cancer cell proliferation, invasion and migration by targeting FOXA1.

MicroRNAs (miRNAs/miRs) are highly conserved single-stranded small non-coding RNAs, which are involved in the physiological and pathological processes of breast cancer, and affect the prognosis of patients with breast cancer. The present study used the Gene Expression Omnibus (GEO)2R tool to detect miR-100 expression in breast cancer tissues obtained from GEO breast cancer-related datasets. Bioinformatics analysis revealed that miR-100 expression was downregulated in different stages, grades and lymph node metastasis stages of breast cancer, and patients with high miR-100 expression had a more favorable prognosis. Based on these analyses, Cell Counting Kit-8, wound healing and Transwell assays were performed, and the results demonstrated that overexpression of miR-100 inhibited the proliferation, migration and invasion of breast cancer cells. To verify the tumor-suppressive effect of miR-100 in breast cancer, the LinkedOmics and PITA databases were used to assess the association between miR-100 and forkhead box A1 (FOXA1). The results demonstrated that miR-100 had binding sites within the FOXA1 gene, and FOXA1 expression was negatively associated with miR-100 expression in breast cancer tissues. Similarly, a negative association was observed between miR-100 and FOXA1 expression, using the StarBase V3.0 database. The association between miR-100 and FOXA1 was further verified via reverse transcription-quantitative PCR and western blot analyses, and the dual-luciferase reporter assay. The results demonstrated that miR-100 targeted the 3'-untranslated region of FOXA1 in breast cancer cells. Furthermore, rescue experiments were performed to confirm whether miR-100 exerts its antitumor effects by regulating FOXA1. The results demonstrated that overexpression of FOXA1 promoted the proliferation, migration and invasion of breast cancer cells; thus, the antitumor effects of miR-100 in breast cancer were reversed following overexpression of FOXA1. Taken together, the results of the present study suggest that miR-100 inhibits the proliferation, migration and invasion of breast cancer cells by targeting FOXA1 expression. These results may provide a novel insight and an experimental basis for identifying effective therapeutic targets of high specificity for breast cancer.

Circular RNA Circ_0003221 Promotes Cervical Cancer Progression by Regulating miR-758-3p/CPEB4 Axis.

BACKGROUND: Circular RNAs (circRNAs) play crucial roles in the development and progression of various cancers, including cervical cancer. However, the role and regulatory mechanism of circ_0003221 in cervical cancer are still unclear. METHODS: The expression of circ_0003221, microRNA-758-3p (miR-758-3p), cytoplasmic polyadenylation element-binding protein 4 (CPEB4) was detected by quantitative real-time PCR (qRT-PCR). Cell Counting Kit-8 (CCK-8), colony formation, and 5-Ethynyl-2'-deoxyuridine (Edu) assays were utilized to determine cell proliferation. Cell cycle distribution was analyzed by flow cytometry. Cell migration and invasion were detected by transwell assay. All protein levels were detected by Western blot assay. The interaction between miR-758-3p and circ_0003221 or CPEB4 was confirmed by dual-luciferase reporter, RNA immunoprecipitation (RIP) and RNA pull-down assays. Mice xenograft model of cervical cancer was established to verify the function of circ_0003221 in vivo. RESULTS: Circ_0003221 was upregulated in cervical cancer tissues and cells. Knockdown of circ_0003221 suppressed cell proliferation, migration, invasion, and EMT and induced cell cycle arrest in cervical cancer cells. MiR-758-3p was a direct target of circ_0003221, and miR-758-3p inhibition reversed the effects of circ_0003221 knockdown in cervical cancer cells. Moreover, CPEB4 was identified as a direct target of miR-758-3p, and miR-758-3p exerted its anti-cancer role by targeting CPEB4. Furthermore, circ_0003221 acted as a sponge of miR-758-3p to upregulate CPEB4 expression. In addition, circ_0003221 silence also suppressed tumor growth and EMT in vivo. CONCLUSION: Circ_0003221 knockdown inhibited cervical cancer progression via modulating miR-758-3p/CPEB4 axis, which might suggest a new insight into the pathogenesis of cervical cancer.

Multidisciplinary team therapy for left giant adrenocortical carcinoma: A case report.

BACKGROUND: Adrenocortical carcinoma (ACC) is a rare malignant epithelial tumor originating from adrenocortical cells that carries a very poor prognosis. Metastatic or inoperable diseases are often considered incurable, and treatment remains a challenge. Especially for advanced cases such as ACC complicated with renal venous cancer thrombus, there are few cumulative cases in the literature. CASE SUMMARY: The patient in this case was a 39-year-old middle-aged male who was admitted to the hospital for more than half a month due to dizziness and chest tightness. Computed tomography (CT) findings after admission revealed a left retroperitoneal malignant space-occupying lesion, but the origin of the formation of the left renal vein cancer thrombus remained to be determined. It was speculated that it originated from the left adrenal gland, perhaps a retroperitoneal source, and left adrenal mass + left nephrectomy + left renal vein tumor thrombus removal + angioplasty were performed under general anesthesia. Postoperative pathology results indicated a diagnosis of ACC. Postoperative steroid therapy was administered. At 3 mo after surgery, abdominal CT reexamination revealed multiple enlarged retroperitoneal lymph nodes and multiple low-density shadows in the liver, and palliative radiotherapy and mitotane were administered, considering the possibility of metastasis. The patient is currently being followed up. CONCLUSION: ACC is a highly malignant tumor. Even if the tumor is removed surgically, there is still the possibility of recurrence. Postoperative mitotane and adjuvant chemoradiotherapy have certain benefits for patients, but they cannot fully offset the poor prognosis of this disease.

Impact of edaravone on serum CXC chemokine ligand-13 levels and perioperative neurocognitive disorders in elderly patients with hip replacement.

BACKGROUND: Perioperative neurocognitive disorders (PND) are a series of severe complications in the perioperative and anesthetic periods with a decline in memory, execution ability, and information processing speed as the primary clinical manifestation. This study aimed to evaluate the impact of edaravone (EDA) on PND and peripheral blood C-X-C motif chemokine ligand 13 (CXCL13) levels in elderly patients with hip replacement. METHODS: A total of 160 elderly patients undergoing hip arthroplasty in Affiliated Dongguan People's Hospital of Southern Medical University (from March 2016 to March 2018) were randomly and double-blindly categorized into an EDA group and a control group (CON). Group EDA was administered intravenously EDA 30 min before surgery, and group CON was administered intravenously saline. The cognitive function of the two groups was evaluated 1-day before the operation and at 1 and 12 months after surgery, and the incidence of post-operative delirium was tested on days 1, 3, and 7 after surgery using the Chinese version of the confusion assessment method. Serum CXCL13 and interleukin (IL)-6 concentrations were measured before anesthesia, during surgery (30 min after skin incision), and on days 1, 3, and 7 after surgery. The continuous variables in accordance with normal distribution were tested using the Student's t test, the continuous variables without normal distribution using the Mann-Whitney U test, and categorical variables by the χ2 test or Fisher exact test. RESULTS: The incidence of post-operative delirium within 7 days after surgery was significantly higher in group CON than that in group EDA (31.3% vs. 15.0%, t = -5.6, P < 0.001). The modified telephone interview for cognitive status and activities of daily life scores were significantly higher in the group EDA than those in the group CON at 1 month (39.63 ±â€Š4.35 vs. 33.63 ±â€Š5.81, t = -2.13, P < 0.05 and 74.3 ±â€Š12.6 vs. 61.2 ±â€Š13.1, t = -1.69, P < 0.05) and 12 months (40.13 ±â€Š5.93 vs. 34.13 ±â€Š5.36, t = -3.37, P < 0.05 and 79.6 ±â€Š11.7 vs. 65.6 ±â€Š16.6, t = -2.08, P < 0.05) after surgery; and the incidence of neurocognitive dysfunction was significantly lower in the group EDA than that in the group CON (P < 0.05). Serum CXCL13 and IL-6 concentrations were significantly lower in the group EDA than those in the group CON during and after surgery (P < 0.05). CONCLUSION: EDA can significantly reduce the serum concentrations of CXCL13 and IL-6 and improve the PND of patients.

Dihydrochalcone C-glycosides from Averrhoa carambola leaves.

Ten undescribed dihydrochalcone C-glycosides, carambolasides R1‒R3, S1, S2, T1‒T3, 3-hydroxycarambolaside T1, and 3-hydroxycarambolaside P were isolated along with carambolasides I and P from the leaves of Averrhoa carambola L. (Oxalidaceae). Their structures were determined by spectroscopic and chemical methods. Among them, carambolasides P, T1, T2, and I with contents of 22.78, 14.39, 4.93, and 1.87 mg g-1 dry wt., respectively, were shown to be abundant in the leaves by HPLC analysis. All the compounds showed more potent ABTS radical cation scavenging activity than l-ascorbic acid. 3-Hydroxycarambolaside T1 and 3-hydroxycarambolaside P also demonstrated moderate DPPH radical scavenging activity. Further, carambolaside R3, 3-hydroxycarambolaside T1, and 3-hydroxycarambolaside P exhibited weak in vitro porcine pancreatic lipase inhibitory activity.

Flavan-3-ols and 2-diglycosyloxybenzoates from the leaves of Averrhoa carambola.

Averrhoa carambola L. (Oxalidaceae) was widely cultivated for fruits (star fruit), whereas the value of leaves remains to be discovered. Our study on the leaves yielded five flavan-3-ols (1-5) and two 2-diglycosyloxybenzoates. Their structures were determined by spectroscopic and chemical methods. Epicatechin-(5,6-bc)-4ß-(p-hydroxyphenyl)-dihydro-2(3H)-pyranone (1) and benzyl 2-ß-d-apiofuranosyl-(1 â†’ 6)-ß-d-glucopyranosyloxybenzoate (6) were new structures. 6-(S-2-Pyrrolidinone-5-yl)epicatechin (4) and 6-(R-2-pyrrolidinone-5-yl)epicatechin (5) were obtained as monomeric diastereomer for the first time and their absolute configurations were determined by electronic circular dichroism (ECD) computation. Epicatechin-(7,8-bc)-4α-(p-hydroxyphenyl)-dihydro-2(3H)-pyranone (2), epicatechin-(7,8-bc)-4ß-(p-hydroxyphenyl)-dihydro-2(3H)-pyranone (3), and methyl 2-ß-d-apiofuranosyl-(1 â†’ 6)-ß-d-glucopyranosyloxybenzoate (7) were not previously reported from the genus Averrhoa. Compounds 1-5 showed more potent 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities and ferric reducing antioxidant power (FRAP) than l-ascorbic acid. Meanwhile 1 and 3 exhibited lipase and α-glucosidase inhibitory activities, respectively. The results clarified the structures of flavan-3-ols and 2-diglycosyloxybenzoates in the leaves and their antioxidant, lipase, and α-glucosidase inhibitory activities.

A Review of Biologically Active Natural Products from a Desert Plant Cistanche tubulosa.

An Orobanchaceae plant Cistanche tubulosa (SCHENK) WIGHT (Kanka-nikujuyou in Japanese), which is one of the authorized plant resources as Cistanches Herba in both Japanese and Chinese Pharmacopoeias, is a perennial parasitic plant growing on roots of sand-fixing plants. The stems of C. tubulosa have traditionally been used for treatment of impotence, sterility, lumbago, and body weakness as well as a promoting agent of blood circulation. In recent years, Cistanches Herba has also been widely used as a health food supplement in Japan, China, and Southeast Asian countries. Here we review our recent studies on chemical constituents from the stems of C. tubulosa as well as their bioactivities such as vasorelaxtant, hepatoprotective, and glucose tolerance improving effects.

Carotenoid-Derived Flavor Precursors from Averrhoa carambola Fresh Fruit.

The fruit of Averrhoa carambola L. (Oxalidaceae), commonly known as star fruit or carambola, is popular in tropical and subtropical regions. Carotenoid-derived components, mainly C13- and C15-norisoprenoids, contribute greatly to the flavor of star fruit. Previously reported norisoprenoids were tentatively identified by GC-MS analysis after enzymatic hydrolysis. To gain accurate information about glycosidically bound flavor precursors in star fruit, a phytochemical study was conducted, which led to the isolation of 16 carotenoid derivatives-One new C13-norisoprenoid glucoside, (5R,6S,7E,9R)-5,6,9-trihydroxy-7-megastigmene 9-O-ß-d-glucoside (1); one new C15-norisoprenoid, (6S,7E,10S)-Δ9,15-10-hydroxyabscisic alcohol (11); and 14 known ones, of which 12 were in glucoside form. The structures of the two new compounds were elucidated on the basis of extensive spectroscopic data analysis and chemical reaction. Compound 11 was a rare C15-norisoprenoid with a double bond between C-9 and C-15, and its possible biogenetic pathway was proposed. The known compounds were identified by comparison of their mass and nuclear magnetic resonance (NMR) data with those reported in the literature. The structure identification of one new (1) and seven known (3⁻7, 9, and 10) C13-norisoprenoid glucosides from the genus Averrhoa for the first time enriches the knowledge of carotenoid-derived flavor precursors in star fruit.