1.Bioactivity-guided discovery of antiviral templichalasins A‒C from the endophytic fungus Aspergillus templicola.
Teng CAI ; Jingzu SUN ; Wenxuan CHEN ; Qiang HE ; Baosong CHEN ; Yulong HE ; Peng ZHANG ; Yanhong WEI ; Hongwei LIU ; Xiaofeng CAI
Chinese Journal of Natural Medicines (English Ed.) 2025;23(6):754-761
The bioactivity-guided isolation of potentially active natural products has been widely utilized in pharmaceutical discovery. In this study, by screening fungal extracts against coxsackievirus B3 (CVB3), three new aspochalasins, templichalasins A‒C (1‒3), along with six known aspochalasins (4‒9) were isolated from an active extract derived from the endophytic fungus Aspergillus templicola LHWf045. Compound 1 features a unique 5/6/5/7/5 pentacyclic ring system, while compounds 2 and 3 possess unusual 5/6/6/7 tetracyclic skeletons. Their structures were characterized through extensive spectroscopic analyses, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. Additionally, we demonstrated that compound 4 can be readily converted into compounds 1‒3 under mild acidic conditions and proposed a plausible mechanism for this conversion. Bioactivity evaluation of compounds 1‒9 against CVB3 revealed the inhibitory effects of all compounds against the virus. Notably, compound 9 exhibited superior antiviral activity, surpassing the commercial drug ribavirin in selectivity index (SI) value.
Antiviral Agents/isolation & purification*
;
Aspergillus/chemistry*
;
Molecular Structure
;
Enterovirus B, Human/drug effects*
;
Endophytes/chemistry*
;
Cytochalasins/isolation & purification*
;
Drug Discovery
;
Humans
2.Antimicrobial activities of endophytic fungi residing in Aloe vera against diabetic wound pathogens
Md Abu Taher ; Tong Woei Yenn ; Leong Chean Ring ; Suzana Wahidin ; Mohd Azizan Mohd Noor ; Syarifah Ab Rashid ; Tan Wen-Nee
Malaysian Journal of Microbiology 2020;16(6):519-529
Aims:
Endophytic fungi are organisms that colonize living plant tissues without causing significant symptoms of
diseases. They are known as the repository of bioactive compounds. This study was aimed to isolate endophytic fungi
associated with Aloe vera and to assess their antimicrobial activity against the diabetic wound pathogens that result to
lower limb amputations.
Methodology and results:
In this study, 84 endophytic fungi were isolated from A. vera by using 5% sodium
hypochlorite and 70% ethanol as surface sterilants. On preliminary antimicrobial screening by agar plug assay, 12
(14.3%) isolates showed significant antagonistic activity on the test microorganisms. Two of the endophytes were
identified as Aspergillus flavus and Colletotrichum gloeosporioides through morphological and molecular techniques.
The fungal cultures fermented in shake flask were extracted subsequently with hexane, dichloromethane, ethyl acetate,
and n-butanol. Ethyl acetate and dichloromethane extracts of A. flavus and C. gloeosporioides inhibited all test bacteria.
The compounds in the extracts were seemed to be semi-polar in nature. On broth microdilution assay, minimal inhibitory
and minimal lethality concentration of ethyl acetate extracts of the fungi were found in the range of 0.63−2.50 and
1.25−5.00 mg/mL, respectively.
Conclusion, significance and impact of study
This study reveals that A. vera harbours a wide diversity of endophytic
fungi. A. flavus and C. gloeosporioides showing broad spectrum antimicrobial activity on wound pathogens may be
potential sources of bioactive compounds. Further investigations should be conducted to isolate and identify the
antimicrobial compound produced by these fungal isolates.
Endophytes--isolation &
;
purification
;
Aloe
3.Isolation,screening and identification of endophytic fungi and detection of its antifungal effects against Alternaria panax.
Chun-Yuan ZHOU ; Xiang-Min PIAO ; Mei-Xia YAN ; Ying-Ping WANG
China Journal of Chinese Materia Medica 2019;44(2):274-277
To obtain biocontrol fungus for Alternaria panax,the antifungal effects of one strain of endophytic fungi isolated from leaves of healthy ginseng were screened and evaluated by using dual-culture method,and the taxonomic assignment of the screened strain was identified based on the morphological characters and ITS sequence analysis. The results of dual-culture showed that one of the endophytes marked as FS-01 had good antifungal effects and the inhibitory rates of FS-01 strain to A. panax was( 60. 21±0. 12) %.The hyphae junction of the both strains,A. panax dissolved,broke and winded,while the hyphae of FS-01 strain remained normal. The inhibitory rates of non-sterilized FS-01 strain fermentation liqud was( 13. 94±0. 21) %. Strain FS-01 identified as Chaetomium globosum.
Alternaria
;
pathogenicity
;
Antibiosis
;
Chaetomium
;
classification
;
isolation & purification
;
Endophytes
;
isolation & purification
;
Fungicides, Industrial
;
Panax
;
microbiology
;
Plant Diseases
;
prevention & control
4.Isolation and identification of endophytic fungi from Chelidonium majus and their antifungal activity.
Ting HUANG ; Wei XIE ; Xiao-Dong LIU ; Kai-Xun TANG ; Rui YANG
China Journal of Chinese Materia Medica 2019;44(3):460-464
In order to find new source of antifungal agents, eleven cultivable endophytic fungi were isolated from the roots,stems and leaves of Chelidonium majus by traditional method. Seven of them were identified as Colletotrichum(L1, L2, L3, S1, S3, S4, S5), and three of them were identified as Fusarium(R1,R2,R3) by morphological features and molecular biological technology. The antifungal activity test showed that all the tested fungi displayed some inhibitory activity against five common plant pathogens(C. gloeosporioides, Curvularia lunata, Pyricularia oryza, Alternaria alternate and A. brassicae), and their inhibition rate of some test items were over 60%. Among them, R1, S2, S3 and S4 were more potent than others. This study enriches the understanding of endophytes from Ch. majus and provides a basis for the study of new microbial fungicides.
Alternaria
;
pathogenicity
;
Antibiosis
;
Ascomycota
;
pathogenicity
;
Chelidonium
;
microbiology
;
Colletotrichum
;
chemistry
;
isolation & purification
;
Endophytes
;
chemistry
;
isolation & purification
;
Fusarium
;
chemistry
;
isolation & purification
5.Isolation and identification of endophytic fungi from Huperzia serrata and their metabolites' inhibitory activities against acetylcholinesterase and anti-inflammatory activities.
Bo-Wen QI ; Ting MO ; Xin ZHANG ; Ya-Ru YAN ; Xi-Ping XU ; Hong-Yun YANG ; Xiao-Hui WANG ; Jun LI ; She-Po SHI ; Xiao LIU
China Journal of Chinese Materia Medica 2019;44(15):3213-3220
A total of 27 endophytic fungal strains were isolated from Huperzia serrata,which were richly distributed in the stems and leaves while less distributed in roots. The 27 strains were identified by Internal Transcribed Spacer( ITS) r DNA molecular method and one of the strains belongs to Basidiomycota phylum,and other 26 stains belong to 26 species,9 general,6 families,5 orders,3 classes of Ascomycota Phylum. The dominant strains were Colletotrichum genus,belonging to Glomerellaceae family,Glomerellales order,Sordariomycetes class,Ascomycota Phylum,with the percentage of 48. 15%. The inhibitory activities of the crude extracts of 27 endophytic fungal strains against acetylcholinesterase( ACh E) and nitric oxide( NO) production were evaluated by Ellman's method and Griess method,respectively. Crude extracts of four fungi exhibited inhibitory activities against ACh E with an IC50 value of 42. 5-62. 4 mg·L~(-1),and some fungi's crude extracts were found to inhibit nitric oxide( NO) production in lipopolysaccharide( LPS)-activated RAW264. 7 macrophage cells with an IC50 value of 2. 2-51. 3 mg·L~(-1),which indicated that these fungi had potential anti-inflammatory activities.The chemical composition of the Et OAc extract of endophytic fungus HS21 was also analyzed by LCMS-IT-TOF. Seventeen compounds including six polyketides,four diphenyl ether derivatives and seven meroterpenoids were putatively identified.
Acetylcholinesterase
;
Animals
;
Anti-Inflammatory Agents
;
isolation & purification
;
pharmacology
;
Ascomycota
;
chemistry
;
classification
;
isolation & purification
;
Cholinesterase Inhibitors
;
isolation & purification
;
metabolism
;
Endophytes
;
classification
;
isolation & purification
;
Huperzia
;
microbiology
;
Mice
;
RAW 264.7 Cells
6.A new phenolic compound from endophytic fungus Aspergillus fumigatus of Euphorbia royleana.
Yan-Jun CHEN ; Yan-Qi SUN ; Rui-Qi ZHANG ; Li-Jun ZHU ; Yi-Jian CHEN ; Li-Juan YANG ; Min ZHOU ; Miao DONG ; Yan-Qing YE
China Journal of Chinese Materia Medica 2019;44(24):5429-5432
This research was carried out to study the secondary metabolites of endophytic fungus Aspergillosis fumigatus from Euphorbia royleana. The endophytic fungus A. fumigatus was fermented by solid fermentation,and purified by various chromatographic methods after extraction. The structures of the compounds were identified by1 H-NMR,13 C-NMR and HSQC,HMBC spectra and physicchemical properties. Three compounds were isolated and their structures were identified as 3-( 3,4-dihydroxybenzoyl)-5-( 3,4-dihydroxyphenyl)-6-methyl-5,6-dihydro-2 H-pyran-2-one( 1),hydroxysydonic acid( 2) and 11-hydroxysydonic acid( 3). Compound 1 is a new compound.
Aspergillus fumigatus/chemistry*
;
Endophytes/chemistry*
;
Euphorbia/microbiology*
;
Fermentation
;
Phenols/isolation & purification*
7.Identification of endophytic bacteria BZJN1 and research on biological control of root rot of Atractylodes macrocephala.
Jing-Mao YOU ; Kun XIONG ; Sen MU ; Jie GUO ; Xiao-Liang GUO ; Yuan-Yuan DUAN ; Juan LI ; Fan CAO ; Zong-Cheng ZOU ; Hai TAN
China Journal of Chinese Materia Medica 2018;43(3):478-483
In this study, an endophytic bacteria strain BZJN1 was isolated from Atractylodes macrocephala, and identified as Bacillus subtilis by physiological and biochemical tests and molecular identification. Strain BZJN1 could inhibit the growth of mycelia of Ceratobasidium sp. significantly, and the inhibition rate was more than 70%. The mycelium growth deformity with bulge as spherical and partially exhaustible in apex or central with microscopic observation. The inhibitory rates under 3% and 6% concentrations of the cell free fermentation were 22.7% and 38.7% expectively. The field test proved that the control efficacy of treatment of 1×10⁸ cfu·mL⁻¹ is 75.27% and 72.37% after 10 and 20 days. All the treatments of strain BZJN1 was able to promote the growth of A. macrocephala, the treatment of 1×10⁸ cfu·mL⁻¹ could able to increase the yield to 14.1%.
Atractylodes
;
microbiology
;
Bacillus subtilis
;
physiology
;
Basidiomycota
;
pathogenicity
;
Biological Control Agents
;
Endophytes
;
classification
;
isolation & purification
;
Plant Diseases
;
microbiology
;
prevention & control
8.Study on secondary metabolites of endophytic fungi Penicillium dangeardii.
Hai-ning LV ; Guang-zhi DING ; Yun-bao LIU ; Jing QU
China Journal of Chinese Materia Medica 2015;40(9):1759-1761
Endophytic fungi Penicillium dangeardii, isolated from Lysidice rhodostegia Hance root, was fermented and the secondary metabolites were studied. By means of Sephadex LH-20 column chromatography, ODS column chromatography and PHPLC over the fermented culture, 5 compounds were isolated. By using ESI-MS and NMR, the structures of the compounds were determined as N-[9-(β- D-ribofuranosyl)-9H-purin-6-yl]-L-aspartic acid (1), 3-caffeoylquinic acid (2), 4-caffeoylquinic acid (3), and 5-caffeoylquinic acid (4), 3-hydroxy-benzoic acid-4-O-β-D-glucopyranoside (5).
Biological Factors
;
chemistry
;
isolation & purification
;
metabolism
;
Endophytes
;
chemistry
;
metabolism
;
Fabaceae
;
microbiology
;
Fermentation
;
Molecular Structure
;
Penicillium
;
chemistry
;
metabolism
;
Secondary Metabolism
9.A new lactone derivative from plant endophytic fungus Periconia sp. F-31.
De-wu ZHANG ; Ji-mei LIU ; Ri-dao CHEN ; Min ZHANG ; Li-yan YU ; Jun WU ; Jun-gui DAI
China Journal of Chinese Materia Medica 2015;40(12):2349-2351
To investigate the secondary metabolites of endophytic fungi Pericinia sp. F-31. Column chromatography on silica gel, Sephadex LH-20 and semi-preparative HPLC were used to separate and purify the compounds. Two compounds were isolated from the fermentation broth of Periconia sp. Their structures were identified as 5-(1-hydroxyhexyl) -6-methyl-2H-pyran-2-one (1) and 2-(3-hydroxy-4-methylphenyl) -propanoic acid (2). Compound 1 was a new lactone compound, compound 2 was new natural product, and the NMR data of compound 2 was reported for the first time.
Annona
;
microbiology
;
Ascomycota
;
chemistry
;
genetics
;
isolation & purification
;
metabolism
;
Drugs, Chinese Herbal
;
chemistry
;
isolation & purification
;
metabolism
;
Endophytes
;
chemistry
;
genetics
;
isolation & purification
;
metabolism
;
Lactones
;
chemistry
;
isolation & purification
;
metabolism
;
Mass Spectrometry
;
Molecular Structure
10.A new indole derivative from endophyte Myrothecium roridum IFB-E091 in Artemisia annua.
Li SHEN ; Ling-yu LI ; Xiao-jun ZHANG ; Ming LI ; Yong-chun SONG
Acta Pharmaceutica Sinica 2015;50(10):1305-1308
Three compounds were isolated from solid culture of endophyte Myrothecium roridum IFB-E091 in Artemisia annua. Their structures were determined as (S)-(-)-N-[2-(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide (1), N-(4-hydroxyphenethyl)acetamide (2) and asperfumoid (3), in which compound 1 was a new indole derivative. In cytotoxicity assay, the compound 1 had no obvious inhibition activity in human hepatoma cell line SMMC-7721 and human cervical carcinoma cell line HeLa.
Artemisia annua
;
microbiology
;
Cell Line, Tumor
;
drug effects
;
Endophytes
;
chemistry
;
Humans
;
Hypocreales
;
chemistry
;
Indoles
;
chemistry
;
isolation & purification


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