Biological Activities of Extracts and Isolated Calotropin from Gomphocarpus purpurascens Leaves: A Computational and Experimental Study

Tsegu Kiros; Seid Mohammed; Aman Dekebo; Yadessa Melaku

Makale detayları

Biological Activities of Extracts and Isolated Calotropin from Gomphocarpus purpurascens Leaves: A Computational and Experimental Study

Yazarlar:

Tsegu Kiros | Seid Mohammed | Aman Dekebo | Yadessa Melaku

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Natural Products and Bioactive Compounds

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 4, pp.1377-1386

Belge Tipi:

Makale

Yayın Tarihi:

3/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001327158

pISSN:

2149-0120

Anahtar kelimeler:

Özet:

 Gomphocarpus purpurascens A.Richs. sub-family: Asclepiadaceae, family: Apocynaceae is an endemic plant in Ethiopia and Eritrea. The chromatographic fractionation of the chloroform:methanol 1:1 leaf extract resulted in the isolation of a cardenolide-type compound named calotropin. Its structure was confirmed based on the 1D-NMR 1H, 13C, and DEPT-135 spectral data along with reported work. This is the first report on the isolation of calotropin from the leaves of G. purpurascens. The n-hexane extract displayed better antibacterial activity against E. coli and P. aeruginosa 8.1  0.0 to 10.8  0.1 mm up to 12,500 μgmL concentration. Generally, all the extracts and the isolated compound, calotropin, showed better antibacterial activity against the P. aeruginosa strain than chloramphenicol 7.1  0.2 to 7.3  0.5 mm. The tested chloroform: methanol 1:1 extract indicated a weak antifungal activity against C. albicans compared to ketoconazole 10 µgdisc 17.67  2.52 mm. On the contrary, all the extracts were found to have a good DPPH radical scavenging activity IC50 values, 1.1-2.7 µgmL comparable to ascorbic acid 1.0 µgmL. The isolated calotropin exhibited a stronger binding capacity -10.3 kcalmol against the P. aeruginosa PqsA 5OE3 protein model than chloramphenicol -7.0 kcalmol. This compound was also found to violate Lipinskis rules of five with a molecular weight  500 gmol and showed immunotoxicity and cytotoxicity properties. Given that this is a preliminary report, further biochemical investigations would be needed on this G. purpurascens plant to identify additional phytoconstituents with superior efficacy.

 Gomphocarpus purpurascens A.Richs. sub-family: Asclepiadaceae, family: Apocynaceae is an endemic plant in Ethiopia and Eritrea. The chromatographic fractionation of the chloroform:methanol 1:1 leaf extract resulted in the isolation of a cardenolide-type compound named calotropin. Its structure was confirmed based on the 1D-NMR 1H, 13C, and DEPT-135 spectral data along with reported work. This is the first report on the isolation of calotropin from the leaves of G. purpurascens. The n-hexane extract displayed better antibacterial activity against E. coli and P. aeruginosa 8.1  0.0 to 10.8  0.1 mm up to 12,500 μgmL concentration. Generally, all the extracts and the isolated compound, calotropin, showed better antibacterial activity against the P. aeruginosa strain than chloramphenicol 7.1  0.2 to 7.3  0.5 mm. The tested chloroform: methanol 1:1 extract indicated a weak antifungal activity against C. albicans compared to ketoconazole 10 µgdisc 17.67  2.52 mm. On the contrary, all the extracts were found to have a good DPPH radical scavenging activity IC50 values, 1.1-2.7 µgmL comparable to ascorbic acid 1.0 µgmL. The isolated calotropin exhibited a stronger binding capacity -10.3 kcalmol against the P. aeruginosa PqsA 5OE3 protein model than chloramphenicol -7.0 kcalmol. This compound was also found to violate Lipinskis rules of five with a molecular weight  500 gmol and showed immunotoxicity and cytotoxicity properties. Given that this is a preliminary report, further biochemical investigations would be needed on this G. purpurascens plant to identify additional phytoconstituents with superior efficacy.

 Gomphocarpus purpurascens A.Richs. sub-family: Asclepiadaceae, family: Apocynaceae is an endemic plant in Ethiopia and Eritrea. The chromatographic fractionation of the chloroform:methanol 1:1 leaf extract resulted in the isolation of a cardenolide-type compound named calotropin. Its structure was confirmed based on the 1D-NMR 1H, 13C, and DEPT-135 spectral data along with reported work. This is the first report on the isolation of calotropin from the leaves of G. purpurascens. The n-hexane extract displayed better antibacterial activity against E. coli and P. aeruginosa 8.1  0.0 to 10.8  0.1 mm up to 12,500 μgmL concentration. Generally, all the extracts and the isolated compound, calotropin, showed better antibacterial activity against the P. aeruginosa strain than chloramphenicol 7.1  0.2 to 7.3  0.5 mm. The tested chloroform: methanol 1:1 extract indicated a weak antifungal activity against C. albicans compared to ketoconazole 10 µgdisc 17.67  2.52 mm. On the contrary, all the extracts were found to have a good DPPH radical scavenging activity IC50 values, 1.1-2.7 µgmL comparable to ascorbic acid 1.0 µgmL. The isolated calotropin exhibited a stronger binding capacity -10.3 kcalmol against the P. aeruginosa PqsA 5OE3 protein model than chloramphenicol -7.0 kcalmol. This compound was also found to violate Lipinskis rules of five with a molecular weight  500 gmol and showed immunotoxicity and cytotoxicity properties. Given that this is a preliminary report, further biochemical investigations would be needed on this G. purpurascens plant to identify additional phytoconstituents with superior efficacy.

 Gomphocarpus purpurascens A.Richs. sub-family: Asclepiadaceae, family: Apocynaceae is an endemic plant in Ethiopia and Eritrea. The chromatographic fractionation of the chloroform:methanol 1:1 leaf extract resulted in the isolation of a cardenolide-type compound named calotropin. Its structure was confirmed based on the 1D-NMR 1H, 13C, and DEPT-135 spectral data along with reported work. This is the first report on the isolation of calotropin from the leaves of G. purpurascens. The n-hexane extract displayed better antibacterial activity against E. coli and P. aeruginosa 8.1  0.0 to 10.8  0.1 mm up to 12,500 μgmL concentration. Generally, all the extracts and the isolated compound, calotropin, showed better antibacterial activity against the P. aeruginosa strain than chloramphenicol 7.1  0.2 to 7.3  0.5 mm. The tested chloroform: methanol 1:1 extract indicated a weak antifungal activity against C. albicans compared to ketoconazole 10 µgdisc 17.67  2.52 mm. On the contrary, all the extracts were found to have a good DPPH radical scavenging activity IC50 values, 1.1-2.7 µgmL comparable to ascorbic acid 1.0 µgmL. The isolated calotropin exhibited a stronger binding capacity -10.3 kcalmol against the P. aeruginosa PqsA 5OE3 protein model than chloramphenicol -7.0 kcalmol. This compound was also found to violate Lipinskis rules of five with a molecular weight  500 gmol and showed immunotoxicity and cytotoxicity properties. Given that this is a preliminary report, further biochemical investigations would be needed on this G. purpurascens plant to identify additional phytoconstituents with superior efficacy.

Makale detayları

Biological Activities of Extracts and Isolated Calotropin from Gomphocarpus purpurascens Leaves: A Computational and Experimental Study

Yazarlar:

Tsegu Kiros | Seid Mohammed | Aman Dekebo | Yadessa Melaku

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Natural Products and Bioactive Compounds

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 4, pp.1377-1386

Belge Tipi:

Makale

Yayın Tarihi:

3/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001327158

pISSN:

2149-0120

Gomphocarpus purpurascens

Asclepiadaceae

Apocynaceae

calotropin

biological activities

docking analysis

Sayı

Makale detayları

Biological Activities of Extracts and Isolated Calotropin from Gomphocarpus purpurascens Leaves: A Computational and Experimental Study

Yazarlar: Tsegu Kiros | Seid Mohammed | Aman Dekebo | Yadessa Melaku

Yayıncı: Turkish Chemical Society

Ana Başlıklar: Natural Products and Bioactive Compounds

Dergi: Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 4, pp.1377-1386

Belge Tipi: Makale

Yayın Tarihi: 3/2024

Belge Dili: İngilizce

Document ID (Org No.): 2001327158

pISSN: 2149-0120

Gomphocarpus purpurascens

Asclepiadaceae

Apocynaceae

calotropin

biological activities

docking analysis

Sayı

Yazarlar:

Tsegu Kiros | Seid Mohammed | Aman Dekebo | Yadessa Melaku

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Natural Products and Bioactive Compounds

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry Vol.11 Issue 4, pp.1377-1386

Belge Tipi:

Makale

Yayın Tarihi:

3/2024

Belge Dili:

İngilizce

Document ID (Org No.):

2001327158

pISSN:

2149-0120