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).

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.

Cytotoxic benzopyranone and xanthone derivatives from a coral symbiotic fungus Cladosporium halotolerans GXIMD 02502.

Coral-derived microorganisms have been historically proven to be prolific sources of bioactive secondary metabolites. Twelve benzopyranone and/or xanthone derivatives, including a new benzopyranone with an uncommon carboxyl group at C-8, coniochaetone K (1), were obtained from the Beibu Gulf-derived coral symbiotic fungus Cladosporium halotolerans GXIMD 02502. Their structures were determined by extensive spectroscopic data interpretation and comparison with literature values. The absolute configuration of 1 was accomplished by comparison of specific optical rotation as well as quantum chemical ECD calculations. The in vitro cytotoxicity of compounds 1-12 against two human prostatic cancer cell lines, C4-2B and 22RV1, were evaluated. And compounds 1, 3, 6-8, and 10-11 demonstrated significant cytotoxicity with inhibitions ranging from 55.8% to 82.1% at the concentration of 10 µM.

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.

[Open-wedge high tibial osteotomy and unicomartmental knee arthroplasty in treating medial compartment osteoarthritis of the knee: a Meta analysis].

OBJECTIVE: To systematic evaluate the outcome of open-wedge high tibial osteotomy(OWHTO) and unicomartmental knee arthroplasty (UKA) in treating medial compartment osteoarthritis of the knee. METHODS: According to the retrieval strategy made by the Cochrane collaboration, a computer-base research of Medline, Pubmed, EMbase, Cochrane Library, CBM, CNKI, and Wanfang databases was performed and search deadline was March 2018. Related Chinese and English orthopedic journals and conference papers were manually searched. Controlled studies of OWHTO and UKA in the treatment of medial knee osteoarthritis were included. The quality of included researches was evaluated, and the data of postoperative knee function, complications, total knee arthroplasty(TKA) revision rates, and postoperative pain were extracted. Meta analysis was performed using the RevMan 5.0 software. RESULTS: A total of 8 articles that met the criteria were included containing a total of 675 patients. Meta-analysis showed that there was no significant difference in postoperative HSS score, knee score, functional score, and Lysholm score between the OWHTO and UKA groups(P=0.32, P=0.87, P=0.22, P=0.53). The range of joint motion in the OWHTO group was better than that in the UKA group, and the difference was statistically significant(P=0.009). There was no significant difference in postoperative complications and the rates of revision to TKA between the two groups(P=0.81, P=0.23). There was no difference in postoperative knee pain between the two groups. CONCLUSIONS: In the treatment of medial compartmental osteoarthritis of the knee that meets the surgical indications, OWHTO had better postoperative joint mobility. The results were similar in postoperative knee score, postoperative complications, and postoperative TKA revision rates between OWHTO and UKA groups.

Peptides and polyketides isolated from the marine sponge-derived fungus Aspergillus terreus SCSIO 41008.

Two new isomeric modified tripeptides, aspergillamides C and D (compounds 1 and 2), together with fifteen known compounds (compounds 3-17), were obtained from the marine sponge-derived fungus Aspergillus terreus SCSIO 41008. The structures of the new compounds, including absolute configurations, were determined by extensive analyses of spectroscopic data (NMR, MS, UV, and IR) and comparisons between the calculated and experimental electronic circular dichroism (ECD) spectra. Butyrolactone I (compound 11) exhibited strong inhibitory effects against Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with the IC50 being 5.11 ± 0.53 µmol·L-1, and acted as a noncompetitive inhibitor based on kinetic analysis.