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Lithocaldehydes A (1) and B (2), a pair of novel diastereoisomers possessing an unprecedented 6/6/5/5/6 highly-fused ring system forming an earring-like skeleton, were isolated from the deep sea-derived fungus Phomopsis lithocarpus FS508. The structures of 1 and 2 were fully characterized and established through extensive spectroscopic interpretations and ECD calculations. Moreover, compounds 1 and 2 were shown to be promising antibiotics, exhibiting potent antifungal activities that are comparable to those of the positive control nystatin.

Phomeroids A (1) and B (2), two novel meroterpenoids representing two types of skeletons, together with one known homologous analogue (3) were isolated from the deep-sea-derived fungus Phomopsis tersa FS441. Phomeroid A is the first example of tropolonic sesquiterpenes consisting of a highly fused 6/6/11/6/5/5 ring system, while phomeroid B is the first example of meroterpenoids featuring an unusual 7/6/11/6-5 spiral core skeleton. All of them showed considerable cytotoxicity against the tested cell lines, and their biosynthetic pathways were also discussed.

Trichothecene toxins cause serious hazard towards human health and economical crops. However, there are no sufficient molecular strategies to reduce the hazard of trichothecene toxins. Thus it is urgent to exploit novel approaches to control the hazard of trichothecenes. In this study, four trichothecene toxin-resistance genes including mfs1, GNAT1, TRP1 and tri12 in Paramyrothecium roridum were excavated based on genome sequencing results, and then expressed in toxin-sensitive Saccharomyces cerevisiae BJ5464, the toxin resistance genes pdr5, pdr10 and pdr15 of which were firstly knocked out simultaneously by the introduction of TAA stop codon employing CRISPR/Cas9 system. Therefore, three novel hazardous toxin-resistance genes mfs1, GNAT1, TRP1 in P. roridum were firstly excavated by the co-incubation of DON toxin and toxin resistant genes-containing BJ5464 strains. The in vitro function and properties of novel toxin-resistance genes coding proteins including GNAT1, MFS1 and TRP1 were identified by heterologous expression and cellular location analysis as well as in vitro biochemical reaction. The excavation of novel trichothecene toxin-resistance genes provide novel molecular clues for controlling the harm of trichothecenes, meanwhile, this study will also pave a new way for the yield improvement of trichothecenes by heterologous expression to facilitate the development of trichothecenes as anti-tumor lead compounds.

Lithocarols A-F (1–6) possessing novel highly-oxygenated isobenzofuran core, together with a related known compound isoprenylisobenzofuran A (7) were isolated from the marine-derived fungus Phomopsis lithocarpus FS508. Among them, lithocarols A-E (1–5) represent the first examples of poly-ketal derivatives in tenellone family. The structures for all these compounds were fully elucidated by spectroscopic analysis, X-ray diffraction, and electronic circular dichroism calculations. Their cytotoxic assay disclosed that compounds 1–4 displayed moderate growth inhibitory effect against four human tumor cell lines with the IC50 values ranging from 10.5 to 38.7 μM.

Lithocarpinols A (1) and B (2), a pair of tenellone diastereoisomers with novel fused skeleton were isolated from the deep-sea derived fungus Phomopsis lithocarpus FS508. Their structures were elucidated by comprehensive spectroscopic analyses, X-ray diffraction and quantum molecular calculation. Their plausible biogenetic pathway featured an intriguing carbonyl-ene cyclization. Lithocarpinol A exhibited moderate inhibitory effect against HepG-2 and A549 tumor cell lines with IC50 values of 9.4 μmol/L and 10.9 μmol/L, respectively.

The culture broth of Cerrena sp. A593, which was isolated from Pogostemon cablin, showed potent cytotoxicity against several human tumor cell lines. The following chemical study resulted in the iso...

Four novel benzophenone derivatives, cytosporins A-D (1-4), hemiterpene-conjugated phenolics with an unprecedented benzo[b][1,5]dioxocane skeleton, were isolated from Cytospora rhizophorae A761. The structures of the new compounds were fully characterized on the basis of extensive spectroscopic analysis. The deduced structure represents the first example of natural meroterpenoids which bear a benzo[b][1,5]dioxocane framework embodying hemiterpene and benzophenone moieties. Moreover, compounds 1-4 were evaluated for in vitro antimicrobial activity.

A pair of novel enantiomeric benzophenone-hemiterpene adducts, (+)-cytorhizophin A (1a) and (−)-cytorhizophin A (1b) as well as cytorhizophin B (2), all of them featuring an unprecedented 6/7/6/7 tetracyclic fused ring system, together with their biosynthetically related precursor cytorhizophin C (3) were isolated from Cytospora rhizophorae A761. Their structures were fully characterized on the basis of extensive spectroscopic analysis, with the absolute configurations of 1 determined by X-ray diffraction and electronic circular dichroism (ECD) calculations. Moreover, compounds 1–3 were evaluated for in vitro antimicrobial activity.

One new cerapicane cerrenin A (1), and two new isohirsutane sesquiterpenoids cerrenins B and C (2 and 3), were isolated from the broth extract of Cerrena sp. A593. Cerrenin A featured a rare cage-like bicyclo[3.2.1]octane skeleton, and cerrenin B represented the rearranged triquinane-type sesquiterpenoid. Their structures were extensively elucidated by NMR spectroscopic analysis with the absolute configuration determined by X-ray crystallography and ECD calculations. The anti-cancer activity for all the compounds were evaluated, and their plausible biosynthetic relationships involving fascinating carbon skeleton rearrangements were also suggested.

Two new polyketide metabolites, the 12-membered macrolides 4-hydroxy-12-methyloxacyclododecane-2,5,6-trione (1) and 12-methyloxacyclododecane-2,5,6-trione (2), were isolated from the endophytic fungal strain Cladosprium colocasiae A801 of the plant Callistemon viminalis, together with five known derivatives. Their structures were fully characterized by means of detailed spectroscopic analysis for new structures, and in comparison with published data for known compounds. The antibacterial, cytotoxic, and α-glucosidase inhibitory activities of the new compounds 1 and 2 were evaluated.

Sesquiterpene synthases are key enzymes for biosynthesis of sesquiterpene compounds and are important for agarwood formation in Aquilaria sinensis.The As-sesTPS gene encoding a novel sesquiterpene synthase was expressed in Escherichia coli strain BL21 (DE3) as an inclusion body and purified by Ni affinity chromatography. The molecular weight of the protein was lower than the theoretical value. Amino acid sequencing results indicated that the 27.2kDa-recombinant protein was a truncated sesquiterpene synthase from chemically induced A. sinensis. After refolding, the truncated As-SesTPS protein catalyzed the conversion of farnesyl pyrophosphate (FPP) to nerolidol which is a characteristic component of agarwood. The optimal reaction pH for the As-SesTPS protein was 8.0, and the optimal temperature was 30°C. The values of Km and Vmax of As-SesTPS protein towards FPP were 0.0548mM, 42.83μmol/mg.min, respectively. The results of qPCR and iTRAQ demonstrated the much higher expression level of As-SesTPS gene in agarwood than that in whitewood. This study provides a foundation for elucidating the mechanism of agarwood formation in A. sinensis and the potential of the novel gene for improving the quality of artificial agarwood.

Lithocarpins A–D (1–4), the first examples of highly oxygenated tenellone-macrolide conjugated dimers, were isolated from the deep-sea derived fungus Phomopsis lithocarpus FS508. Their structures were elucidated by extensive spectroscopic analyses and X-ray diffraction techniques. Their plausible biogenetic pathways suggested a very intriguing and unusual [4 + 2] cycloaddition with an isobenzofuran as an electron-donating diene. Lithocarpins C and D exhibited a moderate inhibitory effect against three tumor cell lines with IC50 values ranging from 17.0 to 21.6 μM.

Objective To study the characteristic 2-(2-phenylethyl)chromone components of endophytic fungal strain of Aquilaria sinensis by solid culture. Methods The compounds were isolated by various chromatographic methods such as silica gel, reverse-phase silica gel, Sephadex-LH20 column chromatography as well as crystallization. Results Seven 2-(2-phenylethyl)chromone analogues were isolated from the solid culture of Botryosphaeria rhodina A13. Their structures were established by spectral data as well as physicochemical properties, and identified as 6-hydroxy-7-methoxy-2-(2-phenylethyl)chromone ( 1 ), 6,7-dimethoxy-2-(2-phenylethyl) chromone ( 2 ), (5 S ,6 R ,7 S ,8 R )-2-(2-phenylethyl)-5,6,7,8-tetrahydrchromone ( 3 ), 6-hydroxy-2-(2-phenylethyl)chromone ( 4 ), 4′-hydroxy-2-(2-phenylethyl)chromone ( 5 ), 6-methoxy-2-phenethyl-4 H -chromen-4-one ( 6 ), and 6-methoxy-2-(4′-methoxy-phenethyl)-4 H -chromen-4-one ( 7 ). Conclusion All of the compounds are isolated for the first time from the genus Botryosphaeria. This research opens up a new vista to produce the characteristic components of agarwood by endophytic fungi.

Epothilones are a kind of macrolides with strong cytotoxicity toward cancer cells and relatively lower side effects compared with taxol. Epothilone B derivate ixabepilone has been used for the clinical treatment of advanced breast cancer. However, the low yield of epothilones and the difficulty in the genetic manipulation of Sorangium cellulosum limited their wider application. Transcription activator-like effectors-Trancriptional factor (TALE-TF)-VP64 and clustered regularly interspaced short palindromic repeats (CRISPR)/dCas9-VP64 have been demonstrated as effective systems for the transcriptional improvement. In this study, a promoter for the epothilone biosynthesis cluster was obtained and the function has been verified. The TALE-TF-VP64 and CRISPR/dcas9-VP64 target P3 promoter were electroporated into S. cellulosum strain So ce M4, and the transcriptional levels of epothilone biosynthesis-related genes were significantly upregulated. The yield of epothilone B was improved by 2.89- and 1.53-fold by the introduction of recombinant TALE-TF-VP64-P3 and dCas9-VP64-P3 elements into So ce M4, respectively. The epothilone D yield was also improved by 1.12- and 2.18-fold in recombinant dCas9-So ce M4 and TALE-VP64 strains, respectively. The transcriptional regulation mechanism of TALE-TF-VP64 and the competition mechanism with endogenous transcriptional factor were investigated by electrophoretic mobility shift assay (EMSA) and chromatin immunoprecipitation (ChIP), demonstrating the combination of the P3 promoter and TALE-TF element and the competition between TALE-TF and endogenous transcriptional protein. This is the first report on the transcriptional regulation of the epothilone biosynthetic gene cluster in S. cellulosum using the TALE-TF and dCas9-VP64 systems, and the regulatory mechanism of the TALE-TF system for epothilone biosynthesis in S. cellulosum was also firstly revealed, thus shedding light on the metabolic engineering of S. cellulosum to improve epothilone yields substantially and promoting the application of epothilones in the biomedical industry.

Five new chromone-derived polyketides phaseolorins A-F (1&ndash, 5), together with nine known compounds, were isolated from the deep-sea derived fungus Diaporthe phaseolorum FS431. The structures of new compounds were determined by analysis of their NMR and high-resolution electrospray ionization mass spectroscopy (HRESIMS) spectroscopic data. The absolute configurations were confirmed by chemical transformations, extensively experimental electron capture detection (ECD) calculations, or X-ray crystallography. Among them, compound 2 represented the first example for a new family of chromone derivative possessing an unprecedented recombined five-member &gamma, lactone ring. Moreover, the new compounds (1&ndash, 5) were evaluated for in vitro cytotoxic activities against a panel of human cancer cell lines.

The culture broth of

The culture broth of Cerrena sp. A593, which was isolated from Pogostemon cablin, showed potent cytotoxicity against several human tumor cell lines. The following chemical study resulted in the isolation of two new triquinane-type sesquiterpenoids, named cerrenins D (1) and E (2), along with two known compounds plerocybellone A (3) and chloriolin B (4). Their structures were fully assigned with the aid of extensive spectroscopic analysis (1H and 13C NMR, HSQC, HMBC, 1H-1H COSY, HRESIMS, and IR) and data from the literature. Moreover, cytotoxic activity in vitro of compounds 1–4 were evaluated against SF-268, MCF-7, NCI-H460, and HepG-2 tumor cell lines. The new compound 1 exhibited weak growth inhibitory activity against all the four tumor cell lines with IC50 values of 41.01, 14.43, 29.67, 44.32 μM.

Glutamate-specific endopeptidase from Bacillus licheniformis (GSE-BL) is a serine protease with strong specificity toward Glu residue. The relatively complicated purification procedure for producing soluble active GSE-BL limits its wide application in biocatalysis and organic synthesis. In this study, recombinant gse-bl gene with full-length sequence was firstly expressed in the bacterium B. licheniformis (GSE-BL-B) and the yeast Pichia pastoris (GSE-BL-P) in a soluble and enzymatically active form. Pure GSE-BL-B and GSE-BL-P were obtained with yields of 62.5 mg/L and 78.4 mg/L, respectively, after one-step His 6 tag chromatography. Mature GSE-BL-B and GSE-BL-P, with similar enzymatic properties as matured GSE-BL expressed in Escherichia coli (GSE-BL-E), were obtained with yields of 50.8 mg/L and 63.2 mg/L after different durations of trypsin treatment. PNGase treatment and the corresponding enzymatic assay were conducted to validate the glycolysation of GSE-BL-P. The optimal reaction pH and temperature, as well as the kinetic analysis of GSE-BL-B and GSE-BL-P were investigated. The GSE-BLs expressed in B . licheniformis and P. pastoris are potential alternative for the production of enzymatically active GSE-BL with the advantages of much simpler and more cost-effective procedure. Thus, GSE-BLs can be widely applied in peptide synthesis, peptide recovery and sequence analysis.

With the extended applications of hexagonal silicon carbide (h-SiC) in the various fields, particularly in the application of the electronic devices, more and more attentions have been focused on the micro structures as well as their physical properties of h-SiC surface. In this study, we have performed the first principal calculations to compare the formation energies of four typical defects (Vc, Vsi, CI and SiI) on the 4H-SiC (0001) surface as well as in the interior layers. Due to the surface reconstruction and the reduced lattice constrain, the optimized structures of the defects on/near the 4H-SiC (0001) surface are quite different from the ones in the deeper layers. The distinguished formation energies as function of chemical potential indicate that we may control the defects concentrations in different layers by tuning the environmental conditions. This theoretical work provides a significant understanding to the formation mechanism of the point defects on the 4H-SiC surface, and paves a way to the modification of the SiC surface via electron irradiation or ion implantation with micro-defects introduced.

Eutypellol A (1), the first norsesquiterpenoid of sequicarene family, as well as eutypellol B (2), a rare 7-methyl oxidized 2-carene derivative, and one new natural product 2-(2-hydroxy-4-methylcyclohex-3-enyl)propanoic acid (3), along with eight known terpenoids, were isolated from the marine sediment-derived fungus Eutypella scoparia FS46 collected from the South China Sea. Their structures were established on the basis of extensive spectroscopic analysis. Compounds 1–3 were evaluated for their antibacterial activities against Staphylococcus aureus and cytotoxic activities against MCF-7, NCI-H460, and SF-268 tumor cell lines.

Chemical examination of the liquid culture of Endomelanconiopsis endophytica A326 isolated from the Chinese folk medicine Ficus hirta resulted in the isolation of two new xyloketals named xyloketals K and L (1–2) and three known analogs (3–5) including a new natural product (5). Their structures were determined on the basis of extensive spectroscopic analysis. All compounds were evaluated for their cytotoxic activities against the SF-268, MCF-7, NCI-H460, and HepG-2 tumor cell lines. Nonetheless, no significant activity was observed.

A pair of new azaphilone epimers, perangustols A-B (1-2), and two new natural products (3-4), together with two known metabolites (5-6) were isolated from the culture of the marine sediment-derived fungus Cladosporium perangustum FS62. The structures of these compounds were established on the basis of extensive spectroscopic analysis. The isolated compounds (1-6) were evaluated for their cytotoxic activities against the SF-268, MCF-7, NCI-H460, and HepG-2 tumor cell lines. Nonetheless, no significant activity was observed.

Two new pimarane-type diterpenes, scopararanes H-I (1–2), along with five known ones (3–7) were isolated from the culture broth of a marine sediment-derived fungus Eutypella sp. FS46, which was obtained from the South China Sea. Their structures were established by extensive spectroscopic analysis. All of them were evaluated for their cytotoxic activities against MCF-7, NCI-H460 and SF-268 tumour cell lines. Scopararane I (2) showed moderate inhibitory activities.

Chemical investigation of the liquid culture of the endophytic fungus Bipolaris sorokiniana A606, which was isolated from the medicinal plant Pogostemon cablin resulted in the isolation of four new cytotoxic compounds, named isocochlioquinones D-E (1-2) and cochlioquinones G-H (3-4), along with five known cochlioquinone analogues (5-9). Their structures were determined on the basis of extensive spectroscopic analysis. Isocochlioquinone D (1) possessed a rare benzothiazin-3-one moiety and cochlioquinone G (3) was the first example of cochlioquinones bearing an indole-4,7-dione fragment. All of the isolates (1-9) were evaluated for their cytotoxic activities against MCF-7, NCI-H460, SF-268 and HepG-2 tumor cell lines by the sulforhodamine B (SRB) assay. Compounds 4 and 6-9, featuring a cochlioquinone core, exhibited potent cytotoxicities in vitro against the four tumor cell lines, and a preliminary structure-activity relationship of these compounds was also discussed.

A new cytotoxic roridin-type trichothecene macrolide named epiroridin acid (1) and two known compounds epiroridin E (2) and mytoxin B (3) were isolated from the liquid culture of Myrothecium roridum A553, which was isolated from the medicinal plant Pogostemon cablin. The structure of the new macrolide (1) was elucidated by extensive spectroscopic measurements (UV, IR, MS, and 1D and 2D NMR) analyses. All isolated compounds (1-3) were evaluated for their cytotoxic activities against SF-268, MCF-7, NCI-H460, and HepG-2 tumor cell lines. The new compound (1) exhibited well cytotoxicity against the four selected tumor cell lines.

Three new thiodiketopiperazines, geospallins A–C (1–3), together with nine known analogues (4–12), were isolated from the culture of the deep-sea sediment-derived fungus Geosmithia pallida FS140. Among them, geospallins A and B (1 and 2) represent rare examples of thiodiketopiperazines featuring an S-methyl group at C-10 and a tertiary hydroxyl group at C-11. Their structures were determined by high-resolution electrospray mass spectrometry (HRESIMS), spectroscopic analyses, and electronic circular dichroism (ECD) calculations. Their angiotensin-converting enzyme (ACE) inhibitory activity was reported, and geospallins A–C (1–3) showed inhibitory activity with IC50 values of 29–35 µM.

Three new diterpenes koninginols A-C (1–3) and two new sesquiterpenoids 11-hydroxy-15-drimeneoic acid (4), koninginol D (5), together with twelve known compounds (6–17) were isolated from the endophytic fungus Trichoderma koningiopsis A729 derived from Morinda officinalis. Their structures were fully assigned with the aid of extensive spectroscopic analysis and reported data from the previous literatures. Koninginols A and B were disclosed as intriguing diterpene alkaloids, whereas the koninginol C was disclosed as one of the two examples of harziandione diterpene. All the isolates were evaluated for their antitumor activity, and compounds 1–2, 4–6, 11–13, 16–17 were evaluated for their antibacterial activity, wherein the new compounds 1 and 2 exhibited significant antibacterial activity against Bacillus subtilis with MIC values of 10 and 2 μg/mL, respectively.

Wheat yield is greatly reduced because of the occurrence of leaf spot diseases. Bipolaris sorokiniana is the main pathogenic fungus in leaf spot disease. In this study, B. sorokiniana from wheat leaf (W-B. sorokiniana) showed much stronger pathogenicity toward wheat than endophytic B. sorokiniana from Pogostemon cablin (P-B. sorokiniana). The transcriptomes and metabolomics of the two B. sorokiniana strains and transcriptomes of B. sorokiniana-infected wheat leaves were comparatively analyzed. In addition, the expression levels of unigenes related to pathogenicity, toxicity, and cell wall degradation were predicted and validated by quantitative reverse transcription polymerase chain reaction (qRT-PCR) analysis. Results indicated that pathogenicity-related genes, especially the gene encoding loss-of-pathogenicity B (LopB) protein, cell wall-degrading enzymes (particularly glycosyl hydrolase-related genes), and killer and Ptr necrosis toxin-producing related unigenes in the W-B. sorokiniana played important roles in the pathogenicity of W-B. sorokiniana toward wheat. The down-regulation of cell wall protein, photosystem peptide, and rubisco protein suggested impairment of the phytosynthetic system and cell wall of B. sorokiniana-infected wheat. The up-regulation of hydrolase inhibitor, NAC (including NAM, ATAF1 and CUC2) transcriptional factor, and peroxidase in infected wheat tissues suggests their important roles in the defensive response of wheat to W-B. sorokiniana. This is the first report providing a comparison of the transcriptome and metabolome between the pathogenic and endophytic B. sorokiniana strains, thus providing a molecular clue for the pathogenic mechanism of W-B. sorokiniana toward wheat and wheat&rsquo, s defensive response mechanism to W-B. sorokiniana. Our study could offer molecular clues for controlling the hazard of leaf spot and root rot diseases in wheat, thus improving wheat yield in the future.

Gliotoxin, produced by fungi, is an epipolythiodioxopiperazine (ETP) toxin with bioactivities such as anti-liver fibrosis, antitumor, antifungus, antivirus, antioxidation, and immunoregulation. Recently, cytotoxic gliotoxins were isolated from a deep-sea-derived fungus, Dichotomomyces cejpii. However, the biosynthetic pathway for gliotoxins in D. cejpii remains unclear. In this study, the transcriptome of D. cejpii was sequenced using an Illumina Hiseq 2000. A total of 19,125 unigenes for D. cejpii were obtained from 9.73 GB of clean reads. Ten genes related to gliotoxin biosynthesis were annotated. The expression levels of gliotoxin-related genes were detected through quantitative real-time polymerase chain reaction (qRT-PCR). The GliG gene, encoding a glutathione S-transferase (DC-GST), GliI, encoding an aminotransferase (DC-AI), and GliO, encoding an aldehyde reductase (DC-AR), were cloned and expressed, purified, and characterized. The results suggested the important roles of DC-GST, DC-AT, and DC-AR in the biosynthesis of gliotoxins. Our study on the genes related to gliotoxin biosynthesis establishes a molecular foundation for the wider application of gliotoxins from D. cejpii in the biomedical industry in the future.

Two new polyketide metabolites, the 12-membered macrolides 4-hydroxy-12-methyloxacyclododecane-2,5,6-trione (

Two new polyketide metabolites, the 12-membered macrolides 4-hydroxy-12-methyloxacyclododecane-2,5,6-trione (1) and 12-methyloxacyclododecane-2,5,6-trione (2), were isolated from the endophytic fungal strain Cladosprium colocasiae A801 of the plant Callistemon viminalis, together with five known derivatives. Their structures were fully characterized by means of detailed spectroscopic analysis for new structures, and in comparison with published data for known compounds. The antibacterial, cytotoxic, and α-glucosidase inhibitory activities of the new compounds 1 and 2 were evaluated.

Two new cyclohexene derivatives colletotricones A and B (1 and 2) and a new thiazole derivative colletotricole A (5), along with six known natural metabolites were isolated from the extract of Colletotrichum gloeosporioides A12, an endophytic fungus derived from Aquilaria sinensis. Among them, the colletotricones A and B possess a cyclohexenone skeleton, whereas the colletotricole A is a thiazole derivative. Their structures were fully assigned with the aid of extensive spectroscopic analysis and data from the literature. Moreover, cytotoxic activity in vitro of compounds 1 and 3–9 were evaluated against MCF-7, NCI-H460, HepG-2 and SF-268 tumour cell lines. The new compound 1 exhibited growth inhibitory activity against all the four tumour cell lines with IC50 values ranging from 15.7 to 46.8 μM.

The chemical investigation of the mycelia of endophytic fungus Daldinia eschscholtzii A630, which was isolated from the medicinal plant Pogostemon cablin, resulted in the isolation of two new compounds, named eschscholin A (1), 3-ene-2-methyl-2H-1-benzopyran-5-ol (2), and one new natural product 3,5-dihydroxy-2-methyl-4H-chromen-4-one (3), along with seven known compounds. Their structures were fully characterized by means of detailed spectroscopic analysis, and in comparison with published data for known compounds. All of the isolated compounds (1-10) were evaluated for their antibacterial activities.

Two new compounds isobenzofuranone A (1) and indandione B (2), together with eleven known compounds (3–13) were isolated from liquid cultures of an endophytic fungus Alternaria sp., which was obtained from the medicinal plant Morinda officinalis. Among them, the indandione (2) showed a rarely occurring indanone skeleton in natural products. Their structures were elucidated mainly on the basis of extensive spectroscopic data analysis. All of the compounds were evaluated with cytotoxic and α-glucosidase inhibitory activity assays. Compounds 11 and 12 showed significant inhibitory activities against four tumor cell lines; MCF-7, HepG-2, NCI-H460 and SF-268, with IC50 values in the range of 1.91–9.67 μM, and compounds 4, 5, 9, 10, 12 and 13 showed excellent inhibitory activities against α-glucosidase with IC50 values in the range of 12.05–166.13 μM.

In this study,the content of ethanol extraction of agarwood were performed following the method of Chinese Pharmacopoeia(ChP 2015 edition). The chromatographic fingerprints were established by GC-MS. Similarity Evaluation System for Chromatographic Fingerprint of traditional Chinese medicine（TCM）(version 2012) was employed to calculate the similarity of each chromatogram of agarwood. The ratios of sum peak area in the range of 170-270 min and 0-100 min of individual chromatogram were calculated using square peaks to normalization. AMDIS and RI were employed to identify the common and different peaks. Correlation coefficient P(corr) combined with Variable important in projection(VIP) value was employed to screen the different representative components based on OPLS-DA analysis. Grey related degree and TOPSIS were used to evaluate the quality of artificial agarwoods. The results showed that more than 10.0% of the ethanol extract content was found in 15 batches of artificial agarwoods among the total 18. The similarity of 18 batches artificial agarwoods was 0.439-0.779. The peak area ratios of two intervals were in the range of 0.307-13.254. The 9 common components and 8 different components were identified. Meanwhile, 2% salicylic acid is the best inducer based on grey related degree and TOPSIS. Grey related degree and TOPSIS can be used to evaluate the quality of artificial agarwoods rapidly. These results provide a reference data to evaluate the qualityof artificial agarwood.