Growth performance, nutrient digestibility, fecal microbial diversity and volatile fatty acid, and blood biochemical indices of suckling donkeys fed diets supplemented with multienzymes.

BACKGROUND: As the foal grows, the amount of breast milk produced by the donkey decreases. In such cases, early supplemental feeding is particularly important to meet the growth needs of the foal. Foals have an incompletely developed gastrointestinal tract with a homogenous microbiota and produce insufficient amounts of digestive enzymes, which limit their ability to digest and utilize forage. Improving the utilization of early supplemental feeds, promoting gastrointestinal tract development, and enriching microbial diversity are the hotspots of rapid growth research in dairy foals. Plant-based feeds usually contain non-starch polysaccharides (NSPs), including cellulose, xylan, mannan, and glucan, which hinder nutrient digestion and absorption. In addition, proteins and starch (both biomolecules) form a composite system mainly through non-covalent interactions. The proteins wrap around the surface of starch granules and act as a physical obstacle, thereby inhibiting water absorption and expansion of starch and decreasing the enzyme's catalytic effect on starch. Glyanase, ß-mannanase, ß-glucanase, cellulase, protease, and amylase added to cereal diets can alleviate the adverse effects of NSPs. The current study determined the effects of adding multienzymes (glyanase, ß-mannanase, ß-glucanase, cellulase, protease, and amylase) to the diet of 2-month-old suckling donkeys on their growth performance, apparent nutrient digestibility, fecal volatile fatty acid (VFA) and pH, fecal bacterial composition, and blood biochemical indices. RESULTS: On day 120 of the trial, fecal samples were collected from the rectum of donkeys for determining bacterial diversity, VFA content, and pH. Moreover, fresh fecal samples were collected from each donkey on days 110 and 115 to determine apparent digestibility. The multienzymes supplementations did not affect growth performance and apparent nutrient digestibility in the donkeys; however, they tended to increase total height gain (P = 0.0544). At the end of the study, the multienzymes supplementations increased (P < 0.05) the Observed species, ACE, Chao1, and Shannon indices by 10.56%, 10.47%, 10.49%, and 5.01%, respectively. The multienzymes supplementations also increased (P < 0.05) the abundance of Firmicutes, Oscillospiraceae, Lachnospiraceae, Christensenellaceae, Christensenellaceae_R-7_group, and Streptococcus in feces, whereas decreased (P = 0.0086) the abundance of Proteobacteria. CONCLUSIONS: Multienzymes supplementations added to a basal diet for suckling donkeys can increase fecal microbial diversity and abundance.

Phakellisins A-E, cyclopeptides from a marine sponge Phakellia sp. guided by LC-MS.

A chemical investigation of the marine sponge Phakellia sp. from the South China Sea yielded five new cyclopeptides, phakellisins A-E (1-5). Structures of these compounds were determined by comprehensive analysis of 1D/2D NMR, HRESIMS/MS spectroscopic data and the advanced Marfey's method. All compounds were evaluated for their cytotoxic activity. Compound 1 showed a strong inhibitory activity against WSU-DLCL-2 cells with an IC50 value of 5.25 ± 0.2 µM by induction of G0/G1 cell cycle arrest and apoptosis.

Drug resistance and influencing factors of biofilm bacteria in upper urinary calculi patients with double J stent indwelling.

OBJECTIVE: To analyze the distribution and drug resistance of biofilm bacteria infected with upper urinary calculi patients with double J stent indwelling, and to explore the influencing factors of Biofilm Bacteria Infections. METHODS: A total of 400 patients with upper urinary calculi who adopted double J stent inserting in our hospital from January 2019 to January 2022 were included. Urine and double J stent samples were collected, pathogen cultures were performed, and then drug sensitivity test analysis was carried out for isolates. Univariate and multivariate logistic regression analyzes were used to analyze the influencing factors of patients with double J stent associated biofilm bacteria infections. RESULTS: A total of 13 strains (3.2%) of biofilm bacteria were detected in urine samples and 168 strains (42%) in double J stent samples (P < 0.05), 95 strains (23.7%) of pathogenic bacteria were separated from urine samples and 117 strains (29.2%) from double J-stent samples (P > 0.05). Escherichia coli were the most common bacteria. There was significantly higher drug resistance observed in biofilm bacteria versus urine-cultured pathogens (P < 0.05). Advanced age, long-term catheterization, inadequate water intake, hypoproteinemia, abnormal renal function, and diabetes mellitus were independent risk factors for biofilm bacteria infection associated with double J stent(P < 0.05). CONCLUSION: Among the upper urinary calculi patients with double J stent indwelling, the positive rate and drug resistance of biofilm bacteria obtained from double J stent were significantly higher than that from urine. More attention should be paid to the factors that influence biofilm bacteria infections.

Transurethral en bloc resection of a bladder perivascular epithelioid cell tumor (PEComa): a case report.

BACKGROUND: Perivascular epithelioid cell tumor (PEComa) is a mesenchymal tumor with distinct histologic and immunologic features. PEComas that originate in the bladder are extremely rare clinically, with only 35 cases reported in the English literature thus far. Here, we report a case of bladder PEComa resection by transurethral en bloc resection of bladder tumor (ERBT). CASE PRESENTATION: A 66-year-old female with a history of poorly controlled type 2 diabetes with associated complications of frequent urinary tract infections presented to our hospital for a routine physical examination. Outpatient ultrasound examination revealed a strong echogenic mass of approximately 1.5 × 1.3 × 1.3 cm in size on the posterior wall of the bladder. The enhanced computed tomography and enhanced magnetic resonance imaging after admission both suggested a well-defined isolated nodular mass on the posterior wall of the bladder with significant enhancement on the enhanced scan. The tumor was successfully and completely resected by ERBT. Postoperative pathological examination and immunohistochemical results confirmed the mass was a bladder PEComa. No tumor recurrence was observed in the six-month postoperative follow-up. CONCLUSION: Bladder PEComa is an extremely rare mesenchymal tumor of the urinary system. When imaging and cystoscopy reveal a nodular mass with an abundant blood supply in the bladder, PEComa should be included in the differential diagnosis of bladder tumors. Surgical resection is currently the primary option for the treatment of bladder PEComa. For a solitary, pedunculated, narrow-based, small-sized bladder PEComa, resection of the tumor by ERBT was a safe and feasible approach in our patient and may be considered for similar cases in the future.

Prophylactic Effect of Simultaneous Placement of Mesh on Incidence of Parastomal Hernia After Miles' Surgical Resection of Colorectal Cancer: A Prospective Study.

INTRODUCTION: To assess the prophylactic effect of simultaneous placement of mesh and the incidence of parastomal hernia (PSH) after abdominoperineal resection of rectal cancer. METHODS: This study included real-world data of 56 surgically resected patients with colorectal cancer who were consecutively assigned to two groups: control (no mesh, n = 32) and experimental (received mesh, n = 24). An artificial patch was placed under the tunica vaginalis of rectus abdominis for patients in the experimental group, whereas those in the control group received routine sigmoidostomy. The median follow-up time was >20 mo. The difference in hazards function was analyzed by cox regression analysis. The Kaplan-Meir analysis was used to determine the survival curves. A P value of <0.05 was considered as significant. RESULTS: The postoperative incidence rate of PSH was lower in the experimental (41.7%) group than in the control group (71.9%; P = 0.045). The PSH postoperative time in the experimental group was significantly delayed compared to the control group (48 mo versus 10 mo; P < 0.001). The risk of progression from H1 to H2 was less in the experimental group compared to the control group (49.28% versus 60.86%; P = 0.14). CONCLUSIONS: Prophylactic mesh placement significantly prolonged postoperative time for the recurrence of PSH. The incidence of recurrence of H2 (severe PSH) requiring secondary surgical repair was also reduced.

Effects of different grains on bacterial diversity and enzyme activity associated with digestion of starch in the foal stomach.

BACKGROUND: Compared with the stomach of ruminant cattle, the stomach of horse is small and mainly for chemical digestion, but the microorganisms in the stomach play an important role in maintaining the homeostasis of the internal environment. Due to the complexity of the microbes in the stomach, little is known about the diversity and structure of bacteria in the equine stomach. Grains are the main energy source for plant-eating livestock and energy is derived through enzymatic hydrolysis of grains into glucose or their microbial fermentation into Volatile fatty acids (VFA). However, the mechanism through which these ingested grains are chemically digested as well as the effect of these grains on the stomach remains elusive. This study explored the effects of feeding different grains (corn, oats, and barley) on bacterial diversity, structure, and composition in the foal's stomach content. Furthermore, the effects of different grains on the vitality of starch digestion-related stomach enzymes were investigated. RESULTS: No significant differences were observed (P > 0.05) in the bacterial rarefaction curves of Operational Taxonomic Units (OTUs) and diversity of the stomach microbiota in all foals. This study also revealed the statistical differences for Firmicutes, Cyanobacteria, Actinobacteria, Fibrobacteres, Lactobacillaceae, Streptococcaceae, Unidentified_Clostridiales, Prevotellaceae, Lactobacillus, Streptococcus, Unidentified_Cyanobacteria, Unidentified_Clostridiales, Lactococcus, Sphingomonas, Lactobacillus_hayakitensis, Lactobacillus_equigenerosi, and Clostridium_perfringens. The linear discriminant analysis effect size analysis revealed 9 bacteria at each classification level. The functional analysis of species information by using FAPROTAX software was able to predict 35 functions, and the top 5 functions were chemoheterotrophy, fermentation, animal_parasites_or_symbionts, nitrate_reduction, and aerobic_chemoheterotrophy. The study also revealed statistical differences for pH, glucose concentration, ß-amylase, maltase, and amylase. CONCLUSIONS: The different grains had no significant effect on the microbial diversity of the stomach content of the foal. However, the relative bacterial abundances differed significantly in response to different diets. Particularly, oats fed to the foals significantly increased the relative abundance of Firmicutes, Lactobacillaceae, Lactobacillus, and Lactobacillus_hayakitensis. The grain had no significant effect on the pH of the stomach content, glucose concentration, and enzyme viability in the foal.

Eosinophilic cystitis complicated with cystitis glandularis: a case report.

BACKGROUND: Eosinophilic cystitis (EC) is a rare inflammatory disease characterized by the gathering and infiltration of numerous eosinophilia (EOS) in the bladder wall. Because of Few cases of EC have been reported globally, the epidemiology of EC is not well known. We report herein the details of one very scarce case of large tumor-like eosinophilic cystitis complicated with cystitis glandularis (CG) diagnosed by biopsy. CASE PRESENTATION: A 45-year-old Chinese man was referred to our hospital for the treatment of right lumbago and odynuria. Ultrasound examination indicated the low echo on the right portion wall and the neck of the bladder. Computed tomography showed a remarkable enhancing large mass that measured 5.0 cm × 2.3 cm located on the right portion of the bladder with undefined margin. For further treatment, diagnostic transurethral resection of the bladder was performed, the postoperative histopathological diagnosis was EC complicated with CG. After transurethral resection, antibiotics, glucocorticoids, and antihistamines were treated. The patient recovered uneventfully and was discharged on postoperative day 8 without evidence of recurrence followed-up for 6 months. CONCLUSION: Large tumor-like eosinophilic cystitis complicated with cystitis glandularis is rare, malignant tumors need to be ruled out. We deem that prompt biopsy led to the exact diagnosis, appropriate treatment led to better prognosis.

Effects of steam-flaked grains on foals' growth and faecal microbiota.

BACKGROUND: There is little objective information concerning the effect of steam-flaked grains on foal's growth performance and faecal microbiota. To determine the effects of steam-flaked grains on foal's growth performance and faecal microbiota, faecal samples were collection from 18 foals which had been fed either corn, oat or barley diets over the 60 days of the experiment. Body weight and conformation measurements were collected. Next-generation sequencing of the V3 + V4 region of the 16 S rRNA gene was used to assess the microbial composition of faeces. Alpha diversity, Venn graph, Relative abundance and beta diversity are presented. RESULTS: There was a significantly higher larger increase in the body weight of those foals fed barley compared to either corn or oats. There were also significant changes in the Alpha diversity of the gut microbiota. The Shannon and Simpson indices were significantly higher in the barley fed group than those fed corn or oats. The Chao1 index was significantly higher in the oat fed group than the corn or barley fed groups. There were significant changes in the relative abundance of bacteria in the microbiota in terms of phylum, family and genus. The histogram of LDA value distribution showed that the 12 statistically different biomarkers of the bacteria were present. Tax4Fun function annotation clustering heat map showed that functional information was detected from 26 species of bacteria in faecal samples from the foals. CONCLUSIONS: Differences by starch sources were found in overall growth of the foals and in the faecal microbiota if either supplementary corn, oat or barley was fed. Further studies are required to determine the potential impact of the changes in the microbiota on the health and development of foals fed cereal starch of different sources.

Psychometric properties of the Chinese version of the modified polycystic ovary syndrome health-related quality-of-life questionnaire.

BACKGROUND: The modified polycystic ovary syndrome health-related quality-of-life questionnaire (MPCOSQ) is a 30-item instrument measuring quality-of-life in English-speaking patients with polycystic ovary syndrome (PCOS). We aimed to: 1) cross-culturally adapt the MPCOSQ into Chinese, and 2) assess the validity and reliability of the Chinese version of the MPCOSQ (Chi-MPCOSQ). METHODS: The MPCOSQ was translated using the forward-backward method, and its validity and reliability were assessed among 283 Chinese patients with PCOS. Internal consistency reliability and test-retest reliability were assessed by Cronbach's α and intra-correlation coefficient (ICC), respectively. Construct validity was tested through exploratory factor analysis and confirmatory factor analysis. Discriminant validity was assessed by Mann-Whitney U test to compare the scores on the Chi-MPCOSQ between 283 women with PCOS and 93 women without PCOS. RESULTS: Exploratory factor analysis generated a 7-factor structure of the 30-item version of the Chi-MPCOSQ, which accounted for 77% of the overall variance. The Chi-MPCOSQ had high internal consistency (Cronbach's α = 0.88) and good test-retest reliability (ICC = 0.89). Compared to PCOS patients, women without PCOS had consistently lower scores for every dimension of the Chi-MPCOSQ, demonstrating its good discriminant validity. CONCLUSION: The Chi-MPCOSQ is a valid and reliable instrument for measuring quality-of-life among Chinese women with PCOS.

Two novel non-holostane type glycosides from the viscera of sea cucumber Apostichopus japonicus.

Two novel glycosides, apostichoposide A1 (1) and B1 (2), were isolated from the viscera of Chinese sea cucumbers (Apostichopus japonicus, Selenka) collected in the Bohai sea. Both the isolated glycosides were characterized by non-holostane type aglycones having 18(16)-lactone and 7(8)-double bond. Cytotoxic activities of the two compounds were evaluated against three human cancer cell lines. Compound 1 had adequate cytotoxic activity against MGC-803 and PC-3M cell lines. Our results indicated that glycosides present in A. japonicus viscera are an important high value resource for biotechnological applications.

Numerical Study on the Characteristics of Boger Type Viscoelastic Fluid Flow in a Micro Cross-Slot under Sinusoidal Stimulation.

The cross-slot geometry plays an important role in the study of nonlinear effects of viscoelastic fluids. The flow of viscoelastic fluid in a micro cross-slot with a high channel aspect ratio (AR, the ratio of channel depth to width) can be divided into three types, which are symmetric flow, steady-state asymmetric flow and time-dependent flow under the inlet condition with a constant velocity. However, the flow pattern of a viscoelastic fluid in the cross-slot when a stimulation is applied at inlets has been rarely reported. In this paper, the response of cross-slot flow under an external sinusoidal stimulation is studied by numerical simulations of a two-dimensional model representing the geometry with a maximum limit of AR. For the cases under constant inlet velocity conditions, three different flow patterns occur successively with the increase of Weissenberg number (Wi). For the cases under sinusoidal varying inlet velocity conditions, when the stimulation frequency is far away from the natural frequency of a viscoelastic fluid, the frequency spectrum of velocity fluctuation field shows the characteristics of a fundamental frequency and several harmonics. However, the harmonic frequency disappears when the stimulation frequency is close to the natural frequency of the viscoelastic fluid. Besides, the flow pattern shows spatial symmetry and changes with time. In conclusion, the external stimulation has an effect on the flow pattern of viscoelastic fluid in the 2D micro cross-slot channel, and a resonance occurs when the stimulation frequency is close to the natural frequency of the fluid.

Inhibition of PI3K/Akt/NF-κB signaling with leonurine for ameliorating the progression of osteoarthritis: In vitro and in vivo studies.

Osteoarthritis (OA) is characterized as the degeneration and destruction of articular cartilage. In recent decades, leonurine (LN), the main active component in medical and edible dual purpose plant Herba Leonuri, has been shown associated with potent anti-inflammatory effects in several diseases. In the current study, we examined the protective effects of LN in the inhibition of OA development as well as its underlying mechanism both in vitro and in vivo experiments. In vitro, interleukin-1 beta (IL-1ß) induced over-production of prostaglandin E2, nitric oxide, inducible nitric oxide synthase, cyclooxygenase-2, interleukin-6 and tumor necrosis factor alpha were all inhibited significantly by the pretreatment of LN at a dose-dependent manner (5, 10, and 20 µM). Moreover, the expression of thrombospondin motifs 5 (ADAMTS5) and metalloproteinase 13 (MMP13) was downregulated by LN. All these changes led to the IL-1ß induced degradation of extracellular matrix. Mechanistically, the LN suppressed IL-1ß induced activation of the PI3K/Akt/NF-κB signaling pathway cascades. Meanwhile, it was also demonstrated in our molecular docking studies that LN had strong binding abilities to PI3K. In addition, LN was observed exerting protective effects in a surgical induced model of OA. To sum up, this study indicated LN could be applied as a promising therapeutic agent in the treatment of OA.

The pH-dependent elastic properties of nanoscale DNA films and the resultant bending signals for microcantilever biosensors.

The diverse mechanical properties of nanoscale DNA films on solid substrates have a close correlation with complex detection signals of micro-/nano-devices. This paper is devoted to formulating several multiscale models to study the effect of pH-dependent ionic inhomogeneity on the graded elastic properties of nanoscale DNA films and the resultant bending deflections of microcantilever biosensors. First, a modified inverse Debye length is introduced to improve the classical Poisson-Boltzmann equation for the electrical potential of DNA films to consider the inhomogeneous effect of hydrogen ions. Second, the graded characteristics of the particle distribution are taken into consideration for an improvement in Parsegian's mesoscopic potential for both attraction-dominated and repulsion-dominated films. Third, by the improved interchain interaction potential and the thought experiment about the compression of a macroscopic continuum DNA bar, we investigate the diversity of the elastic properties of single-stranded DNA (ssDNA) films due to pH variations. The relevant theoretical predictions quantitatively or qualitatively agree well with the relevant DNA experiments on the electrical potential, film thickness, condensation force, elastic modulus, and microcantilever deflections. The competition between attraction and repulsion among the fixed charges and the free ions endows the DNA film with mechanical properties such as a remarkable size effect and a non-monotonic behavior, and a negative elastic modulus is first revealed in the attraction-dominated ssDNA film. There exists a transition between the pH-sensitive parameter interval and the pH-insensitive one for the bending signals of microcantilevers, which is predominated by the initial stress effect in the DNA film.

Two Novel Multi-Functional Peptides from Meat and Visceral Mass of Marine Snail Neptunea arthritica cumingii and Their Activities In Vitro and In Vivo.

Neptunea arthritica cumingii (Nac) is a marine snail with high nutritional and commercial value; however, little is known about its active peptides. In this study, two multi-functional peptides, YSQLENEFDR (Tyr-Ser-Gln-Leu-Glu-Asn-Glu-Phe-Asp-Arg) and YIAEDAER (Tyr-Ile-Ala-Glu-Asp-Ala-Glu-Arg), were isolated and purified from meat and visceral mass extracts of Nac using a multi-bioassay-guided method and were characterized by using liquid chromatography-tandem mass spectrometry. Both peptides showed high antioxidant, angiotensin-converting enzyme (ACE)-inhibitory, and anti-diabetic activities, with half-maximal effective concentrations values less than 1 mM. Antioxidant and ACE-inhibitory activities were significantly higher for YSQLENEFDR than for YIAEDAER. In a zebrafish model, the two peptides exhibited strong scavenging ability for reactive oxygen species and effectively protected skin cells against oxidative damage without toxicity. Molecular docking simulation further predicted the interactions of the two peptides and ACE. Stability analysis study indicated that the two synthetic peptides maintained their activities under thermal stress and simulated gastrointestinal digestion conditions. The low molecular weight, high proportion of hydrophobic and negatively-charged amino acids, and specific C-terminal and N-terminal amino acids may contribute to the observed bio-activities of these two peptides with potential application for the prevention of chronic noncommunicable diseases.

Structural and biological diversity of natural p-terphenyls.

p-Terphenyls consisting of a C-18 tricyclic or polycyclic C-18 aromatic skeleton, have diverse structures because of the variation of the middle ring and the connections between the rings, and to the main skeleton. p-Terphenyls have recently been found to exhibit various biological activities such as cytotoxic, α-glucosidase inhibitory, antioxidant, and antimicrobial activity. In this review, we briefly summarized the structural varieties, biosyntheses, and bioactivities of natural p-terphenyl derivatives referring to the recent 10 years' publications.

[Analysis of Flame Spectrum at the Initial Stage of 0 # Diesel Oil Combustion].

With small-scale oil pool experimental and spectral analysis method, the flame spectrum in initial stage of 0(#) diesel oil combustion was conducted a preliminary study for the first time, which was used to develop the technique of intelligent identification and suppression of fire extinguishing at the initial stage of diesel oil combustion. It educed the overall characteristics flame spectrum at the initial stage of 0(#) diesel oil combustion: in 200～380 nm wavelength of near-ultraviolet bands, the spectral intensity is the weakest, the spectral intensity does not change with wavelength, the number of characteristics spectral bands is minimum, the number of obvious characteristics spectral peaks is almost none; in 380～780 nm wavelength of visible bands, the spectral intensity is the strongest, the spectral intensity increases with wavelength, the number of characteristics spectral bands is maximum, the number of obvious characteristics spectral peaks is large; in 780～1 100 nm wavelength of near-infrared bands, the spectral intensity is relatively strong, the inflection point of spectral intensity appears in 780 nm, the appeared intensity decreases with wavelength, the number of characteristics spectral bands is relatively large, the number of obvious characteristics spectral peaks is at a certain number. It is educed through further analysis of the flame spectrum that: the primary intermediate radicals includes OH, CN, CH, C(2), H(2)O, etc; the primary characteristic spectral bands includes the OH racial bands of 3 064  System and Vibration-Rotation bands, the CN racial bands of Violet System and Red System, the CH racial bands of 4 315  System, the C2 racial bands of The Swan system and Phillips Near Infra-red System, the H(2)O molecular Vibration-Rotation bands, etc; the bands and time distribution of primary intermediate radicals and its main generation mechanism; the existence of potassium in this experimental batches of 0(#) diesel oil and the spectral peak of spectral lines in 766 and 769 nm is obvious; the peak of spectral intensity in 431, 512, 516, 547, 589, 766, 769, 891, 927 nm is obvious, and it suitable for the sign of flame identification at the initial stage of 0(#) diesel oil combustion.

p-Terphenyl Derivatives from the Endolichenic Fungus Floricola striata.

Ten new p-terphenyl derivatives, floricolins A-J (1-10), together with six known compounds (11-16), were isolated from the extract of the endolichenic fungus Floricola striata. Chemical structures of these compounds were elucidated using spectroscopic data (HRESIMS and NMR). Among them, 9 and 10 were enantiomeric mixtures, and their configurations were established by single-crystal X-ray diffraction analysis using Cu Kα radiation. Evaluation of the isolated compounds against Candida albicans revealed that the most active compound, 3 (MIC 8 µg/mL), exerted fungicidal action by destruction of the cell membrane.

Heptaketides from an Endolichenic Fungus Biatriospora sp. and Their Antifungal Activity.

Twelve new heptaketides, biatriosporins A-L (1-12), biatriosporin M (13) (a ramulosin derivative), and 19 known compounds (14-32) were isolated from the endolichenic fungus Biatriospora sp. (8331C). The structures of these compounds were determined by analyzing MS and NMR data. The absolute configurations of compounds 1, 2, 7, and 9 were determined by single-crystal X-ray diffraction analysis, whereas compound 10 was deduced with Mosher's method. Four of the compounds were active in an antifungal assay. The most potent compound, compound 4, also sensitized clinically derived azole-resistant Candida albicans strains to fluconazole (FLC). A mechanistic investigation revealed that 4 inhibited the function of efflux pumps and reduced the transcriptional expression of the efflux-pump-related genes CDR1 and CDR2.

Three new drimane-type sesquiterpenoids, chaetothyrins A-C, from an endolichenic fungus Chaetothyriales sp.

Three new drimane-type sesquiterpenoids chaetothyrins A-C (1-3), were isolated from an endolichenic fungus Chaetothyriales sp. (4341B). Their structures were determined by analysis of MS and NMR data as well as single-crystal X-ray diffraction analysis.

[Metabolic stability and metabolic enzyme phaenotypes of lanceolatin B in liver microsomes of different species by UPLC-MS/MS].

To investigate the metabolic stability and parameters in vitro of lanceolatin B in liver microsomes of rats, human, Beagle dogs, and monkeys, and to identify the phaenotypes of CYP enzymes of lanceolatin B by using the liver microsome incubation system in vitro. After incubated with different species of liver microsomes, lanceolatin B was quantified by UPLC-MS/MS method to evaluate its metabolic stability and metabolic kinetic parameters in vitro. Lanceolatin B was incubated with specific inhibitors of CYP450 isoforms (CYP2E1, 2C19, 1A2, 2D6, 2C9, 3A4, and 2A1) to determine the phaenotypes of metabolic enzymes. The results showed that lanceolatin B was metabolized in the liver microsomes of rats and monkeys but not in the human and Beagle dogs. Their in vitro half-life T1/2 and intrinsic clearance rate CLint in rat and monkey liver microsomes were 11.57,8.07 min, and 0.12,0.17 mL•min⁻¹â€¢mg⁻¹ without significant difference. The results of metabolic phenotyping indicated that CYP1A2 was mainly involved in the metabolism of lanceolatin B. There existed a difference in the metabolism of lanceolatin B in different types of liver microsomes. Several of CYP450 isoforms metabolized lanceolatin B together in liver microsomes of rats, in which CYP1A2 was the major enzyme mainly responsible for the metabolism of lanceolatin B.