Bisabolanoic acid A, a new polychiral sesquiterpene with AChE inhibitory activity from a mangrove-derived fungus Colletotrichum sp.

A new polychiral bisabolane sesquiterpene, bisabolanoic acid A (1), was isolated from the mangrove-derived fungus Colletotrichum sp. SCSIO KcB3-2. Its planar structure was identified on the basis of spectroscopic data analysis (HRESIMS, 1D, and 2D NMR), and the absolute configurations of three chiral carbons were determined by experimental and calculated electronic circular dichroism (ECD) and optical rotatory dispersion (ORD), together with Mo2(OAc)4-induced ECD methods. Bisabolanoic acid A (1) showed moderate inhibitory activity against acetylcholinesterase (AChE) with IC50 value of 2.2 µM, and the in silico molecular docking was also performed.

Citrinin and α-pyrone derivatives with pancreatic lipase inhibitory activities from Penicillium sp. SCSIO 41302.

One new citrinin monomer derivative (1), and two new natural products α-pyrone analogues (2a and 2b), were isolated from the sponge derived fungus Penicillium sp. SCSIO 41302. Their structures were determined by extensive spectroscopic analysis, chiral-phase HPLC analysis, modified Mosher's method, ECD calculations, and X-ray single-crystal diffraction. Bioactivity screening showed that compounds 2b and 8 exhibited obvious inhibitory activities against pancreatic lipase and acetyl cholinesterase with IC50 values of 48.5 and 4.8 µM, respectively, which indicated that different chiral center between enantiomers (2a and 2b) might result in different biological activities (IC50 value against PL for 2a >100 µg/ml).

HPLC-DAD-Guided Isolation of Diversified Chaetoglobosins from the Coral-Associated Fungus Chaetomium globosum C2F17.

Cytochalasans have continuously aroused considerable attention among the chemistry and pharmacology communities due to their structural complexities and pharmacological significances. Sixteen structurally diverse chaetoglobosins, 10-(indol-3-yl)-[13]cytochalasans, including a new one, 6-O-methyl-chaetoglobosin Q (1), were isolated from the coral-associated fungus Chaetomium globosum C2F17. Their structures were accomplished by extensive spectroscopic analysis combined with single-crystal X-ray crystallography and ECD calculations. Meanwhile, the structures and absolute configurations of the previously reported compounds 6, 12, and 13 were confirmed by single-crystal X-ray analysis for the first time. Chaetoglobosins E (6) and Fex (11) showed significant cytotoxicity against a panel of cancer cell lines, K562, A549, Huh7, H1975, MCF-7, U937, BGC823, HL60, Hela, and MOLT-4, with the IC50 values ranging from 1.4 µM to 9.2 µM.

Nanolamellar Tantalum Interfaces in the Osteoblast Adhesion.

The design of topographically patterned surfaces is considered to be a preferable approach for influencing cellular behavior in a controllable manner, in particular to improve the osteogenic ability of bone regeneration. In this study, we fabricated nanolamellar tantalum (Ta) surfaces with lamellar wall thicknesses of 40 and 70 nm. The cells attached to nanolamellar Ta surfaces exhibited higher protein adsorption and expression of ß1 integrin, as compared to the nonstructured bulk Ta, which facilitated the initial cell attachment and spreading. We thus, as expected, observed significantly enhanced osteoblast adhesion, growth, and alkaline phosphatase activity on nanolamellar Ta surfaces. However, the beneficial effects of nanolamellar structures on osteogenesis became weaker as the lamellar wall thickness increased. The interaction between cells and Ta surfaces was examined through adhesion forces using atomic force microscopy. Our findings indicated that the Ta surface with a lamellar wall thickness of 40 nm exhibited the strongest stimulatory effect. The observed strongest adhesion force between the cell-attached tip and the Ta surface with a 40 nm thick lamellar wall encouraged the much stronger binding of cells with the surface and thus well-attached, -stretched, and -grown cells. We attributed this to the increase in the available contact area of cells with the thinner nanolamellar Ta surface. The increased contact area allowed the enhancement of the cell surface interaction strength and, thus, improved osteoblast adhesion. This study suggests that the thin nanolamellar topography shows immense potential in improving the clinical performance of dental and orthopedic implants.

Indioceanicola profundi gen. nov., sp. nov., isolated from Indian Ocean sediment.

A novel basophilic bacterial strain, designated as SCSIO 08040T, was recovered from a deep-sea sediment sample collected from the Indian Ocean. The strain was Gram-stain-negative, vibrioid or spiral, light pink, 0.6-1.0 µm wide and 1.0-2.5 µm long. Growth occurred at 20-45 °C, pH 7-11 and <5 % (w/v) NaCl, with optimum growth at 28-37 °C, pH 7 and 0-3 % (w/v) NaCl. Catalase-, oxidase and urease-positive, nitrate reduction-negative. Analysis of 16S rRNA gene sequencing revealed that strain SCSIO 08040T had the highest similarity of 95.3 % to Rhodocista pekingensis 3-pT. Phylogenetic analysis based on nearly complete 16S rRNA gene sequences showed that the novel isolate formed a distinct phylogenetic lineage in the family Rhodospirillaceae. The whole-cell hydrolysate contained meso-diaminopimelic acid, galactose, mannose and xylose. The total cellular fatty acid profile was dominated by C18:1ω7c and C19:0cycloω8c. Q-10 was the predominant ubiquinone. The major phospholipids were diphosphatidylglycerol, phosphatidylcholine and phosphatidylethanolamine. The DNA G+C content of strain SCSIO 08040T was 66.82 mol%. Based on these polyphasic data, a new genus, Indioceanicola gen. nov., is proposed in the family Rhodospirillaceae with the type species Indioceanicola profundi sp. nov. and the type strain SCSIO 08040T (=DSM 105146T=CGMCC 1.15812T).

Overexpression of Long Non-Coding RNA ZXF2 Promotes Lung Adenocarcinoma Progression Through c-Myc Pathway.

OBJECTIVE: To investigate the expression of long non-coding RNA ZXF2 in lung adenocarcinoma tissues and its effect on cell proliferation, migration and invasion. METHODS: Forty pairs of cancerous and adjacent non-cancerous lung adenocarcinoma specimens were collected for the studies. Quantitative real-time PCR was used to analyze the expression of ZXF2 in tumor tissues and adjacent normal tissues. The expression of ZXF2 was correlated with patients' clinico-pathological data. Molecular pathway controlled by ZXF2 was explored by using small interfering RNA (siRNA) technology. CCK-8 cell proliferation assay, flow cytometry analysis and transwell assays were used to evaluate cell proliferation, migration and invasion. RESULTS: The expression of ZXF2 was 2 fold or higher in 27 out of 40 (67.5%) cases of lung adenocarcinoma specimens than that in non-cancerous tissues (P<0.05). The relative expression level of ZXF2 was positively correlated with tumor lymph node metastasis (χ(2)=8.485, P<0.05) and poor prognosis of the patients (p=0.0217). In order to explore the molecular mechanisms of ZXF2 mediated tumor progression, ZXF2 expression was inhibited by siRNA in A549 cells, a highly aggressive and metastatic lung adenocarcinoma cell line. We found that siRNA-ZXF2 treatment inhibited cell proliferation (P<0.01) leading to cell cycle arrest (P<0.01). The cell migration and invasion were suppressed by siRNA-ZXF2 treatment (P<0.01). Further biochemical studies revealed that the knockdown of ZXF2 led to down regulation of c-Myc signaling. CONCLUSION: ZXF2 was overexpressed in lung adenocarcinoma tissues and the high expression of ZXF was closely related to tumor progression through c-Myc related pathway. Given the fact that both ZXF2 and c-Myc are located in the same chromosome 8q24.2 loci, the potential interaction between ZXF2 and c-Myc might be a novel target for treatment of lung adenocarcinoma.

Asteltoxins with Antiviral Activities from the Marine Sponge-Derived Fungus Aspergillus sp. SCSIO XWS02F40.

Two new asteltoxins named asteltoxin E (2) and F (3), and a new chromone (4), together with four known compounds were isolated from a marine sponge-derived fungus, Aspergillus sp. SCSIO XWS02F40. The structures of the compounds (1-7) were determined by the extensive 1D- and 2D-NMR spectra, and HRESIMS spectrometry. All the compounds were tested for their antiviral (H1N1 and H3N2) activity. Compounds 2 and 3 showed significant activity against H3N2 with the prominent IC50 values of 6.2 ± 0.08 and 8.9 ± 0.3 µM, respectively. In addition, compound 2 also exhibited inhibitory activity against H1N1 with an IC50 value of 3.5 ± 1.3 µM.

Preoperative prognostic nutritional index predicts postoperative delirium in aged patients after surgery: A matched cohort study.

OBJECTIVE: Prognostic nutritional index (PNI) is an indicator to evaluate the nutritional immune status of patients. This study aimed to assess whether preoperative PNI could predict the occurrence of postoperative POD in aged patients undergoing non-neurosurgery and non-cardiac surgery. METHOD: The aged patients undergoing non-neurosurgery and non-cardiac surgery between January 2014 and August 2019 were included in the retrospective cohort study. The correlation between POD and PNI was investigated by univariate and multivariable logistic regression analysis, propensity score matching (PSM), inverse probability of treatment weighting (IPTW), and subgroup analysis. RESULTS: In the cohort (n = 29,814), the cutoff value of PNI was 46.01 determined by the receiver operating characteristic (ROC) curve. In univariate and three multivariable regression analysis, the ORs of PNI ≤ 46.01 was 2.573(95% CI:2.261-2.929, P < 0.001),1.802 (95% CI:1.567-2.071, P < 0.001),1.463(95% CI:1.246-1.718, P < 0.001),1.370(95% CI:1.165-1.611, P < 0.001). In the PSM model and IPTW model, the ORs of PNI ≤ 46.01 were 1.424(95% CI:1.172-1.734, P < 0.001) and 1.356(95% CI:1.223-1.505, P < 0.001). CONCLUSION: The PNI was found to have a predictive value for POD in patients undergoing non-neurosurgery and non-cardiac surgery. Improving preoperative nutritional status may be beneficial in preventing POD for aged patients.

Sesterterpenoids.

This review, with 166 references, covers the literature published on sesterterpenoids together with their relevant biological activities, source organisms and country of origin. The first total syntheses that have led to the revision of structures or stereochemistry have been included.

A glyoxylate-containing benzene derivative and butenolides from a marine algicolous fungus Aspergillus sp. SCSIO 41304.

A new glyoxylate-containing benzene derivative, methyl 2-(4-hydroxy-3-(3'-methyl-2'-butenyl)phenyl)-2-oxoacetate (1), together with ten known compounds (2-11), were isolated from the marine algicolous fungus, Aspergillus sp. SCSIO 41304. Their planar structures and absolute configurations were elucidated by detailed NMR, MS spectroscopic analysis and comparing with literature data. Compound 1 was isolated as a new fungal secondary metabolite, possessing a methyl glyoxylate moiety R-CO-CO-OCH3, which is rare in natural sources. All the isolated compounds (1-11) were tested for their antibacterial and enzyme inhibitory activities against acetylcholinesterase (AChE) and pancreatic lipase (PL). Among these compounds, aspulvinone H (4) showed moderate inhibition against AChE and PL with IC50 values of 25.95 and 47.06 µM, respectively. Further molecular docking simulation exhibited that compound 4 could well bind to the catalytic pockets of the AChE and PL.

Isolation, characterization, and bioactivity evaluation of 3-((6-methylpyrazin-2-yl)methyl)-1H-indole, a new alkaloid from a deep-sea-derived actinomycete Serinicoccus profundi sp. nov.

One new alkaloid, 3-((6-methylpyrazin-2-yl)methyl)-1H-indole (1) was obtained from the deep-sea actinomycete Serinicoccus profundi sp. nov., along with five known compounds (2-6). Their structures were determined on the basis of detailed analysis of the 1D and 2D NMR as well as MS data. The new indole alkaloid displayed weak antimicrobial activity against Staphylococcus aureus ATCC 25923 with an MIC value of 96 µg/mL. It showed no cytotoxicity on a normal human liver cell line (BEL7402) and a human liver tumor cell line (HL-7702).

Quadrilateral plate fractures of the acetabulum: Classification, approach, implant therapy and related research progress.

The quadrilateral plate (QP) is an essential structure of the inner wall of the acetabulum, an important weight-bearing joint of the human body, which is often involved in acetabular fractures. The operative exposure, reduction and fixation of QP fractures have always been the difficulties in orthopedics due to the special morphological structure and anatomical features of the QP. Fortunately, there have been many effective methods and instruments developed for QP exposure, reduction and fixation by virtue of the combined efforts of numerous orthopedists. At the same time, each method presents with its own advantages and disadvantages, resulting in different prognoses. It is necessary to have a thorough understanding of the anatomy, radiology and fixation techniques of the QP in terms of patient prognosis optimization. In this paper, the anatomical features, definition and classification of QP, operative approach selection, implant internal fixation methods and efficacy were reviewed.

Effects of delayed repair of peripheral nerve injury on the spatial distribution of motor endplates in target muscle.

Motor endplates (MEPs) are important sites of information exchange between motor neurons and skeletal muscle, and are distributed in an organized pattern of lamellae in the muscle. Delayed repair of peripheral nerve injury typically results in unsatisfactory functional recovery because of MEP degeneration. In this study, the mouse tibial nerve was transected and repaired with a biodegradable chitin conduit, immediately following or 1 or 3 months after the injury. Fluorescent α-bungarotoxin was injected to label MEPs. Tissue optical clearing combined with light-sheet microscopy revealed that MEPs were distributed in an organized pattern of lamellae in skeletal muscle after delayed repair for 1 and 3 months. However, the total number of MEPs, the number of MEPs per lamellar cluster, and the maturation of single MEPs in gastrocnemius muscle gradually decreased with increasing denervation time. These findings suggest that delayed repair can restore the spatial distribution of MEPs, but it has an adverse effect on the homogeneity of MEPs in the lamellar clusters and the total number of MEPs in the target muscle. The study procedures were approved by the Animal Ethics Committee of the Peking University People's Hospital (approval No. 2019PHC015) on April 8, 2019.

Bullectomy used to treat a patient with pulmonary vesicles related to COVID-19: A case report.

BACKGROUND: The corona virus disease 2019 (COVID-19) has been a pandemic for more than one year and estimated to affect the whole world in the near future. CASE SUMMARY: Here we reported that one COVID-19 patient with vesicles was treated by bullectomy. The patient's perioperative laboratory tests were analyzed. The pathological findings of bullectomy were described and compared with those of common bulla cases. CONCLUSION: This patient with vesicles underwent bullectomy and had a poor prognosis. He showed diffuse alveolar damage and extensive necrosis in bullectomy specimen. We hope our report will be of interest for clinicians who will treat COVID-19 patients in the future.

[Sterols of marine bryozoan Bugula neritina from the South China Sea].

OBJECTIVE: To study the sterol constituents of Bugula neritina from the South China Sea. METHODS: The alcohol extract of Bugula neritina was purified by silica gel column and Sephadex LH-20 column chromatography, and structures of the isolated compounds were identified by spectroscopic analysis and comparison with those of literatures. RESULTS: Ten sterols were isolated and identified from the petroleum ether fraction of alcohol extract of B. neritina L.:Cholest-4-en-3-one(I); cholesterol(II);3beta,5alpha,9alpha-trihydroxy-(22E,24R)-ergosta-7,22-dien-6-one(III); 24-methyl-5alpha-cholesta-7,22-diene-3beta,5,6beta-triol(IV); 3beta-Hydroxy-7-methoxy-Cholesta-5-en(V);5alpha, 8alpha-epidioxy-(22E,24R)-ergosta-6, 22-dien-3beta-ol(VI); 3beta-hydroxycholest-5-en-7-one (VII); and 6beta-hydroxy-cholest-4-en-3-one(VIII); Cholesta-5-ene-3beta,7beta-diol(IX); Cholesta-5,22(E)-dien-3beta,7alpha-diol(X). CONCLUSION: Compounds IV-X were isolated from Bugula neritina for the first time.

Characterization and Secretory Expression of a Thermostable Tannase from Aureobasidium melanogenum T9: Potential Candidate for Food and Agricultural Industries.

Being a key industrial enzyme, tannase is extensively applied in various fields. Despite the characterizations of a large number of tannases, there are hardly a few tannases with exceptional thermostability. In this detailed study, a tannase-encoding gene named tanA was identified from Aureobasidium melanogenum T9 and heterologously expressed in Yarrowia lipolytica host of food grade. The purified tannase TanA with a molecular weight of above 63.0 kDa displayed a specific activity of 941.4 U/mg. Moreover, TanA showed optimum activity at 60°C and pH 6.0. Interestingly, TanA exhibited up to 61.3% activity after incubation for 12 h at 55°C, signifying its thermophilic property and distinguished thermostability. Additionally, TanA was a multifunctional tannase with high specific activities to catalyze the degradation of various gallic acid esters. Therefore, this study presents a novel tannase, TanA, with remarkable properties, posing as a potential candidate for food and agricultural processing.

Sesquiterpenoids and meroterpenoids from a mangrove derived fungus Diaporthe sp. SCSIO 41011.

One new sesquiterpenoid, 1-methoxypestabacillin B (1), along with one known sesquiterpenoid (2) and six known chrodrimanin-type meroterpenoids (3‒8) were obtained from the solid cultures of a mangrove endophytic fungus Diaporthe sp. SCSIO 41011. Their structures including the absolute configuration at C-6 of compound 1, were determined by extensive spectroscopic analyses and ECD calculations. Meanwhile, the X-ray crystal structures and absolute configurations of two previously reported chrodrimanins E (3) and H (6), are described for the first time. All the compounds were examined for HIV latency-reversal and anti-influenza A virus activities.

Three-Dimensional Distribution of Bone-Resorption Lesions in Osteonecrosis of the Femoral Head Based on the Three-Pillar Classification.

OBJECTIVE: To investigate three-dimensional distribution of bone-resorptive lesions based on the three-pillar classification and its effect on the disease progression of osteonecrosis of the femoral head (ONFH). METHODS: A total of 194 femoral head CT images from 117 patients diagnosed with ARCO stage II and III ONFH were retrospectively reviewed from April 2014 to February 2019. Three-dimensional structures of the femoral head and the bone-resorptive lesions were reconstructed. Using the three-pillar classification and coronal plane of the femoral head, we divided each femoral head into six regions to observe the location characteristics of bone-resorption lesions, and explore the destruction of different areas of the femoral head by the bone-resorptive lesions. Then the hips were divided into two groups based on whether they contained bone-resorption lesions and compared the difference of stage II and stage III between the two groups. RESULTS: The regional distribution revealed 39 (27.27%), 55 (38.46%), six (4.20%), 23 (16.08%), 17 (11.89%) and three (2.10%) bone-resorptive lesions in regions I, II, III, IV, V and VI respectively. The lateral pillar, AL (I + IV), contained 44.76% of the lesions, central pillar, C (II + V), 48.95%, and medial pillar, M (III + VI), 6.29%. Moreover, there were 81.82% bone-resorption lesions in anterolateral pillar, AL (I + II + IV), and 18.18% in posteromedial pillar, PM (III + V + VI). In all ONFH hips, the lateral pillar of 81(88.04%) femoral heads were affected, the central pillar of 84 (91.30%) femoral heads were affected, and the medical pillar of 29 (31.52%) femoral heads were affected. The ratio of ARCO stage III in the group with bone-resorption lesions was significantly higher than that of the group without bone-resorption lesions (76.09% vs 30.39%, P < 0.001). CONCLUSIONS: This study demonstrated that the bone-resorption lesions are mainly distributed in the lateral and central pillar of the femoral head, and the two pillars of the femoral head are usually involved by bone-resorption lesions. Furthermore, the ratio of ARCO stage III in the group with bone-resorption lesions was significantly higher than that of the group without bone-resorption lesions, suggesting that the bone-resorption lesions might accelerate the progression of ONFH.

Pyrrolyl 4-quinolone alkaloids from the mangrove endophytic fungus Penicillium steckii SCSIO 41025: Chiral resolution, configurational assignment, and enzyme inhibitory activities.

Six undescribed 4-quinolone alkaloids, including four racemic mixtures, (±)-oxypenicinolines A-D, and two related ones, penicinolines F and G, together with seven known analogues, were isolated from the mangrove-derived fungus Penicillium steckii SCSIO 41025 (Trichocomaceae). The racemates were separated by HPLC using chiral columns. Their structures including absolute configurations were elucidated by extensive spectroscopic analysis, electronic circular dichroism (ECD) experiments, and single-crystal X-ray diffraction analysis. Structurally, (±)-oxypenicinolines A-D shared with an unusual 6/6/5/5 tetracyclic system incorporating a rare tetrahydro-pyrrolyl moiety. A plausible biosynthetic pathway for pyrrolyl 4-quinolone alkaloids is proposed. (±)-oxypenicinoline A and quinolactacide displayed α-glucosidase inhibitory activity with the IC50 values of 317.8 and 365.9 µΜ, respectively, which were more potent than that of acarbose (461.0 µM). Additionally, penicinoline and penicinoline E showed weak inhibitions toward acetylcholinesterase (AChE).