Influence of Transverse Abdominis Plane Block on Intraoperative Diaphragmatic and Respiratory Functions in Patients Receiving Laparoscopic Colorectal Surgery.

Background: The positive roles of deep muscle relaxation in abdominal surgeries and transversus abdominis plane block (TAPB) in the postoperative analgesia. This study aimed to discuss the effects of TAPB on abdominal muscle relaxation, the intraoperative diaphragmatic, and the respiratory functions. Methods: The patients were randomly divided into the TAPB group who received single-shot TAPB bilaterally (n=30), and the control group who did not receive TAPB (n=30). Both groups keep the same steps for other procedures in the surgeries and anesthesia. Four time points for monitoring were defined: The moment when pneumoperitoneum pressure stabilized following endotracheal intubation and anesthetic induction (T0), appearance of the first incisure in the pressure-volume (P-V) loop (T1), appearance of the second incisure in the P-V loop (T2), and the moment with single stimulation (SS) =20% (T3). Primary observation parameters were SS1 measured by muscle relaxation monitoring at T1, and SS2 at T2. Secondary observation parameters included surgeon's satisfaction with surgical field and respiratory dynamics at the four time points. Results: The two groups were comparable in age, gender, BMI, ASA grade, and operation time. The TAPB group had a dramatic reduction in the total dose of intraoperative sufentanil (0.73±0.21 ug/kg) compared with the control group (0.87±0.18 ug/kg) (P=0.023); Other use of drug did not differ between the two groups. The two groups did not differ significantly in SS at either T1 (SS1) or T2 (SS2). In either group, surgeon's satisfaction with surgical field at T1 and T2 decreased dramatically compared with T0 and T3 (all P<0.05). At each time point, the respiratory dynamics and the surgeon's satisfaction with surgical field did not differ significantly between the two groups. Conclusion: TAPB reduced the use of intraoperative analgesics without altering the degree of abdominal relaxation, or affecting surgeon's satisfaction with surgical field in the patients receiving laparoscopic colorectal surgery.

Shelf-life extension of soy sauce by using chitosan oligosaccharides combined with tea polyphenols.

Chitosan oligosaccharides (COs) and tea polyphenols (TPs) have antioxidant and antibacterial activities. This study aims to explore the preservative effects of 0.1 % COs alone and combined with 0.08 % TPs on soy sauce during room-temperature storage. Soy sauce treated with 0.1 % COs alone and combined with 0.08 % TPs had lower total bacterial count, Escherichia coli count and pH, and higher amino acid nitrogen and overall likeness score than those of the control group during room-temperature storage. Treatment with 0.1 % COs combined with 0.08 % TPs extended the shelf life of soy sauce by at least 15 months compared with the control group. Results showed 0.1 % COs combined with 0.08 % TPs may be a feasible method to extend the shelf life of soy sauce during room-temperature storage.

Inhibitive effects of phytic acid combined with glutathione on the browning and oxidation of King Oyster mushroom (Pleurotus eryngii) slices during drying and storage.

Phytic acid and glutathione can inhibit polyphenoloxidase (PPO) activity and suppress browning. This study investigated the effects of phytic acid alone (Treatment-1) or combined with glutathione (Treatment-2) on inhibiting browning and oxidation resistance of King Oyster mushroom (Pleurotus eryngii) slices during drying and storage. In King Oyster mushroom slices, 0.08% phytic acid combined with 0.1% glutathione inhibited the PPO activity by 97.6%, suppressed browning by 78.09% after 6 h of drying at 60 °C and inhibited browning by 69.93% and oxidation by 78.75% after 12 months of storage at âˆ¼ 20 °C. Results indicated that using phytic acid combined with glutathione may inhibit browning and suppress the oxidation of King Oyster mushroom slices during drying and storage.

Effects of dexmedetomidine on dynamic lung compliance in general anesthesia with desflurane: A randomized controlled study.

Objective: The aim of this study was to evaluate the effect of dexmedetomidine on lung compliance in patients under general anesthesia with desflurane. Methods: This prospective, randomized, double-blind, controlled trial included 51 patients who received general anesthesia undergoing lower limb fracture surgery. Participants were assigned to either the experimental (loading dose of 0.25 µg/kg dexmedetomidine over 10 min, followed by a maintenance dose of 0.3 µg/kg/h until the end of the surgery) or control (0.9% saline) group. Anesthesia was maintained with desflurane, analgesics and muscle relaxants. The two groups were compared for hemodynamic parameters, dynamic lung compliance, oxygenation index, and postoperative complications. Results: While dynamic lung compliance showed no significant difference between the two groups at T1 (P = 0.321), it was significantly higher in the experimental group at all other time points (all P < 0.001). In the control group, Cdyn at T4, T5, T6, and T7 were lower than that at T1 (P = 0.032, 0.043, 0.032 and 0.018, respectively). There were no significant between-group differences in the mean arterial pressure and heart rate. Compared to the control group, the experimental group had a higher oxygenation index at T1 (P < 0.001), T2 (P < 0.001), T3 (P < 0.001), T4 (P = 0.02), and T5 (P = 0.016) and significantly lower peak airway pressure at all time points (all P < 0.001). Both groups had comparable postoperative outcomes. Conclusions: Dexmedetomidine infusion at a loading dose of 0.25 µg/kg and maintenance dose of 0.3 µg/kg/h improved dynamic lung compliance in patients receiving desflurane during general anesthesia.

Axial Compressive Behavior of Cross-Shaped CFST Stub Columns with Steel Bar Truss Stiffening.

Concrete-filled steel tube (CFST) columns have been widely used in residential buildings due to their high bearing capacity, good ductility, and reliable seismic performance. However, conventional circular, square, or rectangular CFST columns may protrude from the adjacent walls, resulting in inconvenience in terms of the arrangement of furniture in a room. In order to solve the problem, special-shaped CFST columns, such as cross-shaped, L-shaped, and T-shaped columns, have been suggested and adopted in engineering practice. These special-shaped CFST columns have limbs with the same width as the adjacent walls. However, compared with conventional CFST columns, the special-shaped steel tube provides weaker confinement to the infilled concrete under axial compressive load, especially at concave corners. The parting at concave corners is the key factor affecting the bearing capacity and ductility of the members. Therefore, a cross-shaped CFST column with steel bar truss stiffening is suggested. In this paper, 12 cross-shaped CFST stub columns were designed and tested under axial compression loading. The effects of steel bar truss node spacing and column-steel ratio on the failure mode, bearing capacity, and ductility were discussed in detail. The results indicate that the columns with steel bar truss stiffening can change the final deformation mode of the steel plate from single-wave buckling to multiple-wave buckling, and the failure modes of columns also subsequently change from single-section concrete crushing failure to multiple-section concrete crushing failure. The steel bar truss stiffening shows no obvious effect on the axial bearing capacity of the member but significantly improves the ductility. The columns with a steel bar truss node spacing of 140 mm can only increase the bearing capacity by 6.8% while nearly doubling the ductility coefficient from 2.31 to 4.40. The experimental results are compared with those of six design codes worldwide. The results show that the Eurocode 4 (2004) and the Chinese code CECS159-2018 can be safely used to predict the axial bearing capacity of cross-shaped CFST stub columns with steel bar truss stiffening.

The role of senescence genes in the treatment, prognosis, and tumor microenvironment of gastric cancer.

AIM: Gastric cancer (GC) has a high incidence and poor prognosis. Senescence genes are suggested to participate in immune cell infiltration, thus affecting the immunotherapy of GC. In this research, we established a senescence-related GC model to explore and verify the role of senescence genes in the prognosis, treatment, and tumor microenvironment (TME) of GC. METHODS: The TCGA GC (TCGA-STAD) dataset was used to screen key senescence genes from differentially expressed genes (DEGs). A prognostic risk model was trained utilizing the TCGA-STAD dataset and validated using an external GEO dataset. The CIBERSORT algorithm was run to explore the relationship between senescence genes and TME. The chemotherapy drug sensitivities in GC patients were calculated utilizing R package pRRophetic. RESULTS: A total of 37 senescence-related DEGs were obtained. Five key senescence-related genes were further screened to establish a senescence-related risk model based on Cox regression. The survival status of GC patients in the high-risk group was found to be worse than that in the low-risk group. According to the results of gene set enrichment analysis, the senescence-related risk was mainly associated with cytokine activity, immune mechanism, and related pathways. By analyzing the sensitivity of common chemotherapy drugs in GC patients, it was revealed that the sensitivities of high-risk patients to Dasatinib, Lapatinib, and Pazopanib were lower than those of low-risk patients. The CIBERSORT algorithm was executed to analyze the TME in the high-risk group, revealing elevated levels of CD8 T cells, Macrophages M2, and resting Mast cells. In addition, decreased levels of resting memory CD4 T cells , resting NK cells, activated Dendritic cells, and activated Mast cells were also observed. CONCLUSION: Senescence genes were related to the prognosis, response to chemotherapy drugs, and TME of GC. Our senescence-related risk model could forecast the survival of patients, their response to chemotherapy drugs, and the TME to a certain extent.

PADI1 and Its Co-Expressed Gene Signature Unveil Colorectal Cancer Prognosis and Immunotherapy Efficacy.

Peptidyl arginine deiminase 1 (PADI1) catalyzes protein citrullination and has a role in regulating immune responses. The tumor immune microenvironment has been reported to be important in colorectal cancer (CRC), which was correlated with the ability of CRC patients to benefit from immunotherapy. However, there is a lack of molecular markers for matching CRC immunotherapy. Previously, single-gene risk models have only considered the effect of individual genes on intrinsic tumor properties, ignoring the role of genes and their co-expressed genes as a whole. In this study, we analyzed the differential expression of PADI1 in colorectal cancer (CRC). We found that PADI1 was highly expressed in CRC. Subgroup survival analysis revealed a prognostic survival difference for PADI1 in CRC patients aged less than 65 years, male, T stage, N0, M0, and stage I-II (p < 0.05). In addition, we analyzed the functions and signaling pathways associated with PADI1 in CRC and found that it was highly enriched in several immune-related functions and pathways. Then, a set of PADI1 co-expressed genes (PCGs) risk-prognosis scores was developed with PADI1 as the core, which could accurately predict the prognosis of CRC (p < 0.05). PCGs risk score can be an independent prognostic factor for CRC. A new set of Norman plot models were developed for clinical characteristics with age, sex, and TNM stage, which can accurately predict CRC 1, 3, and 5 years survival, and calibration curves and decision curve analysis (DCA) validated the accuracy of the models. The risk score assessed the immune microenvironment of CRC and found that the immune score was higher in the low-risk group, and CD4+ T cells, helper T cells, and eosinophils were more infiltrated in the low-risk group (p < 0.05). Immunotherapy efficacy was better in the low-risk group (p < 0.05). The underlying mechanism may be that the high-risk group of PCGs was enriched in some pathways that promote immune escape and immune dysfunction. In conclusion, PCGs may better predict CRC prognosis and immunotherapeutic response.

Intelligent Algorithm-Based Echocardiography to Evaluate the Effect of Lung Protective Ventilation Strategy on Cardiac Function and Hemodynamics in Patients Undergoing Laparoscopic Surgery.

The aim of this study was to analyze the effect of optimal pulmonary compliance titration of PEEP regimen on cardiac function and hemodynamics in patients undergoing laparoscopic surgery. 120 patients undergoing elective laparoscopic radical resection of colorectal cancer were included as the study subjects and randomly divided into the experimental group (n = 60) and the control group (n = 60). The control group had a fixed positive end-expiratory pressure (PEEP) = 5 cmH2O. The experimental group had transesophageal ultrasound monitoring through on an improved noise reduction algorithm (ONLM) based on nonlocal mean filtering (NLM) according to optimal pulmonary compliance titration of PEEP. There was significant difference in cerebral oxygen saturation and blood glucose level at T4-T6 between the experimental group and the control group (P < 0.05); the signal-to-noise ratio (SNR), figure of merit (FOM), and structural similarity (SSIM) of ONLM algorithm were significantly higher than those of NLM algorithm and Bayes Shrink denoising algorithm, and the differences were statistically significant (P < 0.05); there was significant difference in stroke volume (SV) and cardiac output (CO) at T4-T6 between the experimental group and the control group (P < 0.05); there was significant difference in pH, partial pressure of carbon dioxide (PCO2), and PO2 at T4-T6 between the experimental group and the control group (P < 0.05); pH was higher, and PCO2 and PO2 were lower in the experimental group. The results showed that transesophageal ultrasound based on the ONLM algorithm can accurately assess cardiac function and hemodynamics in patients undergoing laparoscopic surgery. In addition, optimal pulmonary compliance titration of PEEP could better maintain arterial acid-base balance during perioperative period and increase cerebral oxygen saturation and CO, but this strategy had no significant effect on hemodynamics.

Long non­coding RNA PART1: dual role in cancer.

Increasing evidence has shown that long non-coding RNAs (lncRNAs), which are non-coding endogenous single-stranded RNAs, play an essential role in various physiological and pathological processes through transcriptional interference, post-transcriptional regulation, and epigenetic modification. Moreover, lncRNAs, as oncogenes or tumor suppressor genes, play an important role in the occurrence and development of human cancers. Prostate androgen-regulated transcript 1 (PART1) was initially identified as a carcinogenic lncRNA in prostate adenomas. The upregulated expression of PART1 plays a tumor-promoting role in liver, prostate, lung cancers, and other tumors. In contrast, the expression of PART1 is downregulated in esophageal squamous cell carcinoma, glioma, and other tumors, which may inhibit the tumor. PART1 plays a dual role in cancer and regulates cell proliferation, apoptosis, invasion, and metastasis through a variety of potential mechanisms. These findings suggest that PART1 is a promising tumor biomarker and therapeutic target. This article reviews the biological functions, related mechanisms, and potential clinical significance of PART1 in a variety of human cancers.

Nickel-Catalyzed Chemo- and Regioselective Benzylarylation of Unactivated Alkenes with o-Bromobenzyl Chlorides.

Chemo- and regioselectively nickel-catalyzed reductive benzylarylation of unactivated alkenes with o-bromobenzyl chlorides is disclosed herein, in which electrophiles participate through a single-component double-site approach. Moreover, its utility is underscored by the concise synthesis of bioactive Indane compounds and postreaction functionalizations leading to structurally diverse scaffolds. Preliminary mechanistic investigations suggest a radical chain reaction mechanism.

Over-expression of vitronectin correlates with impaired survival in gastric cancers.

ABSTRACT: Over-expression of vitronectin (VN) is associated with tumorigenesis. The present study aimed to evaluate the prognostic value of VN expression in gastric cancer.The least absolute shrinkage and selection operator analysis was performed to screen the hub gene from The Cancer Genome Atlas gastric cancer patients with complete follow-up data, and 347 patients were finally included. Moreover, 102 patients were enrolled from the Affiliated Fuzhou First Hospital of Fujian Medical University. VN expression in paired gastric cancer and adjacent gastric normal tissues was detected using immunohistochemistry, and the clinicopathological significance of VN expression was evaluated. The prognostic significance of VN expression in gastric cancer patients was evaluated using by Kaplan-Meier method and Cox regression analysis and confirmed using Oncomine.VN was the prognosis relative gene which screened by The Cancer Genome Atlas dataset. Moreover, we identified the VN expression in an external dataset by immunohistochemistry. The result demonstrated that VN expression was remarkedly elevated in gastric cancer tissues (P < .001). High VN expression correlated with higher pathological Tumor-Node-Metastasis stage, and poorer survival outcomes. Cox regression analysis showed that VN expression was independently predictive of overall survival (OS) and disease-free survival (P = .004, P < .001, respectively). A prognostic risk score for OS was built based on VN expression. A meta-analysis from Oncomine datasets revealed that significantly lower VN mRNA levels in gastric cancer correlated with poorer OS.VN expression could be a prognostic marker of gastric cancer.

The α-Subunit of the Chloroplast ATP Synthase of Tomato Reinforces Resistance to Gray Mold and Broad-Spectrum Resistance in Transgenic Tobacco.

Chloroplast ATP synthase (cpATPase) is responsible for ATP production during photosynthesis. Our previous studies showed that the cpATPase CF1 α subunit (AtpA) is a key protein involved in Clonostachys rosea-induced resistance to the fungus Botrytis cinerea in tomato. Here, we show that expression of the tomato atpA gene was upregulated by B. cinerea and Clonostachys rosea. The tomato atpA gene was then isolated, and transgenic tobacco lines were obtained. Compared with untransformed plants, atpA-overexpressing tobacco showed increased resistance to B. cinerea, characterized by reduced disease incidence, defense-associated hypersensitive response-like reactions, balanced reactive oxygen species, alleviated damage to the chloroplast ultrastructure of leaf cells, elevated levels of ATP content and cpATPase activity, and enhanced expression of genes related to carbon metabolism, photosynthesis, and defense. Incremental Ca2+ efflux and steady H+ efflux were observed in transgenic tobacco after inoculation with B. cinerea. In addition, overexpression of atpA conferred enhanced tolerance to salinity and resistance to the fungus Cladosporium fulvum. Thus, AtpA is a key regulator that links signaling to cellular redox homeostasis, ATP biosynthesis, and gene expression of resistance traits to modulate immunity to pathogen infection and provides broad-spectrum resistance in plants in the process.

Role of HAND2-AS1 in human tumors.

Long noncoding RNAs (lncRNAs) are molecules more than 200 nucleotides in length. They play roles in various cells, mainly regulating cell growth, differentiation, and apoptosis. They also participate in the pathogenesis of many diseases. In fact, several studies have shown that lncRNAs function as cancer or tumor suppressor genes and play important roles in the occurrence and development of cancer in humans. New evidence has shown that lncRNA heart and neural crest derivatives expressed 2-antisense RNA 1 (lncRNA HAND2-AS1) hinders the occurrence and development of various tumors. Overexpression of HAND2-AS1 was found to be significantly related to the clinical and pathological characteristics of cancer patients, as well as the regulation of cell proliferation, apoptosis, invasion, metastasis, and energy metabolism through several possible mechanisms. Therefore, HAND2-AS1 may be a promising tumor biomarker and therapeutic target. Here, we review the biological functions, mechanisms, and potential clinical significance of HAND2-AS1 in numerous human tumors.

TAPB and RSB protects cardiac diastolic function in elderly patients undergoing abdominopelvic surgery: a retrospective cohort study.

BACKGROUND: Diastolic dysfunction, an early manifestation and clinical symptom of heart failure with preserved ejection fraction, can be influenced by various anesthesia management strategies. Trans-esophageal echocardiography was used to undertake to assess left ventricular diastolic function during anesthesia maintenance using sevoflurane alone and sevoflurane combining with transversus abdominis plane block and rectus sheath block in elderly patients with diastolic dysfunction undergoing abdominopelvic surgery. METHODS: Thirty-eight patients were divided into two groups in this retrospective study, sevoflurane and sevoflurane combining with TAPB and RSB according to employing different anesthesia maintenance schemes. The parameters HR, MAP, CVP, E, A, E/A, e, a, e/a, and E/a were obtained immediately after anesthesia induction hemodynamics stability (HR1, MAP1, CVP1, E1, A1, E1/A1, e1, a1, e1/a1, and E1/a1) and 1 hour later (HR2, MAP2, CVP2, E2, A2, E2/A2, e2, a2, e2/a2, and E2/a2). RESULTS: Transmitral diastolic Doppler flow characteristics illustrated E/A significant decreases in the S group but increases in the ST group (p = 0.02 < 0.05) 1 hour after anesthesia induction hemodynamic stability. Tissue Doppler imaging characteristics showed a more significant increase e/a (P = 0.005 < 0.05) and decreases in a value (p = 0.009 < 0.05) in the ST group 1 hour after anesthesia induction hemodynamics stability. CONCLUSIONS: Maintaining anesthesia with sevoflurane combining with TAPB and RSB was more suitable for protecting cardiac diastolic function than sevoflurane alone in elderly patients with diastolic dysfunction undergoing open abdominal and pelvic surgery.

The role of long non-coding RNA MIAT in cancers.

Long non-coding RNAs (lncRNAs), a kind of non-coding single-strand RNAs, play an important role as carcinogenic genes or tumor suppressors in the development of human cancer. Myocardial infarction-associated transcript (MIAT) was first identified as a lncRNA in 2006 and originally isolated as a candidate gene for myocardial infarction. Later, it was reported that MIAT exhibits regulatory effects on the human cell cycle. Since its discovery, MIAT has also been identified as a carcinogenic regulator in many malignant tumors. High expression of MIAT is related to the clinicopathological characteristics of cancer patients. It can also regulate cell proliferation, invasion, metastasis, and anti-apoptosis through a variety of mechanisms. Therefore, MIAT is considered a potential biomarker and therapeutic target in cancer. In this review, we summarize the biological function, mechanism, and potential clinical significance of MIAT during tumorigenesis.

Olfactory Sensitivity Is Related to Erectile Function in Adult Males.

BACKGROUND: The olfactory system influences human social behavior, in particular the selection of a spouse. However, there is currently a lack of clinical research on the relationship between the olfactory system and erectile dysfunction (ED) in adult males. AIM: We explored the association between olfactory sensitivity and erectile function and its possible mechanisms. RESULTS: A total of 574 patients, adult males aged between 19 and 42 years, diagnosed with ED in the Department of Infertility and Sexual Medicine of the Third Affiliated Hospital of Sun Yat-sen University from 2015 to 2018 were analyzed retrospectively. Among them, 115 patients (20.03%) had rhinologic diseases (RDs). In addition, in 201 adult male patients who underwent nasal surgery in the ENT department from 2012 to 2016, including 29 (14.43%) with ED, nasal congestion, nasal discharge, and hyposmia were the most common complaints based on the numerical rating scale (NRS). Furthermore, a prospective study was performed in a total of 102 sequential outpatients (male adults) with RD only (n = 46), ED only (n = 42) and both RD and ED (n = 14) in 2019, together with 40 healthy (male adults) volunteers as controls. The results showed that ED patients with RD had severe nasal discomfort and decreased erectile function (P < 0.0001). The olfactory sensitivity of patients with ED was lower than that of the controls, and patients with both ED and RD had the worst olfactory sensitivity (P < 0.0001). Spearman correlation analyses showed that sense of smell was positively correlated with the International Index of Erectile Function-5 score (R = 0.507, P ≤ 0.0001) and the Erection Hardness Scale score (R = 0.341, P < 0.0001). Logistic regression analyses showed that having an olfactory disorder (OD), RD, age, and visual analog scale (VAS, over 5) score were risk factors for ED outcome, indicating that OD patients had a 16.479-fold increased risk for an ED outcome (P < 0.05). CONCLUSION: A significant correlation was detected between olfactory sensitivity and erectile function in adult males. In particularly, impairment of olfactory sensitivity is more common in patients with both ED and RD than in patients suffering from a single disease.

Role of SNHG16 in human cancer.

A growing body of evidence suggests that long non-coding RNAs (lncRNAs), a novel class of non-coding endogenous single-stranded RNA, play a key role in multiple physiological and pathological processes through transcriptional interference, post-transcriptional regulation, and epigenetic modification. Furthermore, many studies have shown that lncRNAs-as oncogenes or tumour suppressors-play an important role in the occurrence and development of human cancers. Small nucleolar RNA host gene 16 (SNHG16) was initially identified as an oncogenic lncRNA in neuroblastoma, and has since been identified as a carcinogenic regulator of various malignant tumours. Overexpression of SNHG16 is associated with clinical and pathological characteristics of cancer patients, and regulates cell proliferation, apoptosis, invasion and metastasis through a variety of potential mechanisms. Therefore, SNHG16 may be a promising biomarker and therapeutic target for cancers. In this review, we summarize the biological function, related mechanisms and potential clinical significance of SNHG16 in multiple human cancers.

Long non-coding RNA TP73-AS1 in cancers.

More and more evidence indicates that long non-coding RNAs (lncRNAs), as a kind of non-coding endogenous single-stranded RNA, play an essential role as oncogenes or tumour suppressors in the occurrence and development of human cancers. The tumour protein P73 antisense RNA 1 (TP73-AS1) was initially found to be down-regulated in oligodendroglioma and may act as a non-protein-encoding RNA. Since its discovery, TP73-AS1 has been identified as a carcinogenic regulator of many malignancies. At the same time, the high expression of TP73-AS1 is related to the clinicopathological features of patients with cancer. It also regulates cell proliferation, anti-apoptosis, invasion and metastasis through a variety of potential mechanisms, suggesting that it may be a promising biomarker and therapeutic target for cancer. In this review, we summarize the biological functions, mechanisms, and potential clinical implications of TP73-AS1 dysregulation in tumourigenesis and progression.

Optimization of Ultrasonic Flavonoid Extraction from Saussurea involucrate, and the Ability of Flavonoids to Block Melanin Deposition in Human Melanocytes.

(1) Background: Flavonoids are the primary medicinal ingredient of Saussurea involucrate, which have significant antioxidant capacity. Optimizing the extraction of Saussurea involucrate flavonoids (SIFs) and exploring the ability to block melanin deposition caused by reactive oxygen can greatly promote the development of S. involucrate whitening products. (2) Methods: Ultrasonic extraction process was optimized using the Box-Behnken design (BBD) and response surface methodology (RSM). Then, the effect of SIFs on antioxidant activity and anti-deposition of melanin, and genes related to the melanin synthesis are studied. (3) Results: The optimal extraction procedures are as follows: the extraction time, ethanol content, and solvent ratio (v/w) are 64 min, 54%, and 54:1, respectively. The reducing activity and scavenging rates of 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion, hydroxyl radical, and ABTS+ were promoted as more S. involucrate flavonoid extract was added. The SIFs extract induced a decrease in the melanin synthesis by inhibiting the human melanoma A375 cell tyrosinase activity. SIFs also depress expression of melanin synthesis related genes. (4) Conclusions: the highest SIFs content was obtained by using 54% ethanol and 54:1 solvent ratio (v/w) for 64 min. The extract of SIFs exhibited good ability of antioxidant and anti-deposition of melanin in human melanocytes.

Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors.

A series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors was developed during our previous work. In the present work, a new series of highly potent bisthiazole-based compounds were designed and synthesized. Among the prepared compounds, compound H13, which contains an α-(S)-methyl-substituted benzyl group, displays potent inhibitory activity toward human HDACs and several cancer cells lines. Compound H13 has a favorable PK profile and high tissue distribution specificity in the colon, as well as good efficacy in the AOM-DSS mouse model for colitis-associated colonic tumorigenesis.