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Bioguided Isolation of Alternariol Derivatives fromFicus-derived Endophyte Alternaria alternata

By: Abdou, Randa.
Contributor(s): Attia, Gouda H.
Publisher: Karnataka Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(2), Apr-June.Description: 497-502p.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian journal of pharmaceutical education and researchSummary: Background: Endophytes are a rich source of bioactive natural products and suggested to contribute to the biological or defense activities of their host plants. Following our research on the discovery of bioactive metabolites from endophytes, Alternaria alternata was isolated from the leaves of Ficus carica L. fam Moraceae. Materials and Methods: Large scale cultivation of the endophytic strain was carried out and the obtained extract was subjected to preliminary screening of antifungal and cytotoxic activities. Results: Promising antifungal and cytotoxic activities were obtained for the extract. Bio-guided fractionation resulted in the isolation and identification of four alternariol derivatives (alternariol, alternariol-5-O-sulphate, alternariol-5-O-methyl ether, alternariol-5-O-methyl ether-4`-O-sulphate). The isolated compounds were tested for antifungal and cytotoxic effects. Results revealed highest antifungal activity for alternariol against A. terreus (MIC= 2.64 μg mL -1 ) and F. oxysporum (MIC= 36 μg mL -1 ) while alternariol-5-O-methyl ether exhibited the highest cytotoxicity against K-562 (CC50 = 3.72 μg mL-1 ) and HUVEC (CC50 = 2.06 μg mL-1 ) cell lines. Conclusion: All alternariol derivatives showed potent cytotoxic and antifungal activities against A. terreus suggesting the contribution of this endophyte in the known antimicrobial and anticancer activities of the host plant.
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Background: Endophytes are a rich source of bioactive natural products and suggested
to contribute to the biological or defense activities of their host plants. Following our
research on the discovery of bioactive metabolites from endophytes,
Alternaria alternata
was isolated from the leaves of
Ficus carica L. fam
Moraceae. Materials and Methods:
Large scale cultivation of the endophytic strain was carried out and the obtained extract
was subjected to preliminary screening of antifungal and cytotoxic activities. Results:
Promising antifungal and cytotoxic activities were obtained for the extract. Bio-guided
fractionation resulted in the isolation and identification of four alternariol derivatives
(alternariol, alternariol-5-O-sulphate, alternariol-5-O-methyl ether, alternariol-5-O-methyl
ether-4`-O-sulphate). The isolated compounds were tested for antifungal and cytotoxic
effects. Results revealed highest antifungal activity for alternariol against
A. terreus
(MIC= 2.64 μg mL -1
) and
F. oxysporum (MIC= 36 μg mL -1
) while alternariol-5-O-methyl
ether exhibited the highest cytotoxicity against K-562 (CC50
= 3.72 μg mL-1
) and HUVEC
(CC50
= 2.06 μg mL-1
) cell lines. Conclusion: All alternariol derivatives showed potent
cytotoxic and antifungal activities against
A. terreus suggesting the contribution of this
endophyte in the known antimicrobial and anticancer activities of the host plant.

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