TY - JOUR
T1 - Preclinical anti-inflammatory and antioxidant effects of Azanza garckeana in STZ-induced glycemic-impaired rats, and pharmacoinformatics of it major phytoconstituents
AU - Lawal, Bashir
AU - Sani, Saidu
AU - Onikanni, Amos S.
AU - Ibrahim, Yunusa O.
AU - Agboola, Abdulhakeem R.
AU - Lukman, Halimat Yusuf
AU - Olawale, Femi
AU - Jigam, Ali A.
AU - Batiha, Gaber El Saber
AU - Babalola, Shukurat B.
AU - Mostafa-Hedeab, Gomaa
AU - Lima, Clara Mariana Gonçalves
AU - Wu, Alexander T.H.
AU - Huang, Hsu Shan
AU - Conte-Junior, Carlos Adam
N1 - Funding Information:
The authors are thankful for the financial support provided by the Fundação de Amparo à Pesquisa do Estado do Rio de Janeiro (FAPERJ) Brazil — grant number [ E-26/200.891/2021 ], and the Conselho Nacional de Desenvolvimento Científicoe Tecnológico (CNPq) - grant number [ 313119/2020-1 ].
Publisher Copyright:
© 2022 The Authors
PY - 2022/8
Y1 - 2022/8
N2 - The quest for novel anti-diabetic medication from medicinal plants is very important since they contain bioactive phytochemicals that offer better activity and safety compared to conventional therapy. In the present study, in vitro, in vivo and in silico approaches were explored to evaluate the anti-inflammatory, antioxidants, and hypoglycemic activities of the crude methanol extract of Azanza garckeana pulp. Our in vitro analysis revealed that the extract contains total phenols (260.80 ± 2.23 mg/100 g) and total flavonoids (10.28 ± 1.29 mg/100 g) contents, and demonstrated dose-dependent in vitro antioxidants activities in; DPPH (IC50 =141.30 ± 1.64 µg/mL), FRAP (IC50 =155.07 ± 1.03 µg/mL), LPO (IC50 =184.96 ± 2.01 µg/mL), and ABTS (IC50 =162.56 ± 1.14 µg/mL) assays; anti-inflammatory activities in: membrane stabilization (IC50 =141.34 ± 0.46 µg/mL), protein denaturation (IC50 =203.61 ± 2.35 µg/mL) and proteinase activities (IC50=f 171.35 ± 1.56 µg/mL) assays; and hypoglycemic activities in: α- amylase (IC50 277.85 ± 2.51 µg/mL), and glucose uptake by yeast cells assays. In vivo analysis revealed that the extract exhibited dose-dependent anti-inflammatory, hypoglycemic activities and improved the weight gain in STZ-induced diabetic rats. In addition, the extract attenuated oxidative stress and increased the activities of SOD, catalase, GSH while depleting the level of LPO in STZ induced diabetic rats. Consequently, the liquid chromatography mass spectrometry (LC-MS) characterization of A. garckeana pulp, revealed the presence of 2-Hexadecen-1-ol,3,7,11,15-tetramethyl-,(2E,7 R,11 R)-, nonyl flavanone, testolactone and 6-(Benzyloxy)− 4,4-Dimethyl-2-Chromanone. These compounds were subjected to pharmacoinformatics analysis among which testolactone and 6-(Benzyloxy)− 4,4-Dimethyl-2-Chromanone demonstrated the best drug-likeness, pharmacokinetics, and also exhibited potential hypoglycemic and anti-inflammatory properties. Altogether, the present study provides preclinical evidence of the antioxidant, anti-inflammatory and antidiabetic activities of A. garckeana extract suggesting its potential applications for the development of alternative therapy for diabetes and its associated inflammatory condition.
AB - The quest for novel anti-diabetic medication from medicinal plants is very important since they contain bioactive phytochemicals that offer better activity and safety compared to conventional therapy. In the present study, in vitro, in vivo and in silico approaches were explored to evaluate the anti-inflammatory, antioxidants, and hypoglycemic activities of the crude methanol extract of Azanza garckeana pulp. Our in vitro analysis revealed that the extract contains total phenols (260.80 ± 2.23 mg/100 g) and total flavonoids (10.28 ± 1.29 mg/100 g) contents, and demonstrated dose-dependent in vitro antioxidants activities in; DPPH (IC50 =141.30 ± 1.64 µg/mL), FRAP (IC50 =155.07 ± 1.03 µg/mL), LPO (IC50 =184.96 ± 2.01 µg/mL), and ABTS (IC50 =162.56 ± 1.14 µg/mL) assays; anti-inflammatory activities in: membrane stabilization (IC50 =141.34 ± 0.46 µg/mL), protein denaturation (IC50 =203.61 ± 2.35 µg/mL) and proteinase activities (IC50=f 171.35 ± 1.56 µg/mL) assays; and hypoglycemic activities in: α- amylase (IC50 277.85 ± 2.51 µg/mL), and glucose uptake by yeast cells assays. In vivo analysis revealed that the extract exhibited dose-dependent anti-inflammatory, hypoglycemic activities and improved the weight gain in STZ-induced diabetic rats. In addition, the extract attenuated oxidative stress and increased the activities of SOD, catalase, GSH while depleting the level of LPO in STZ induced diabetic rats. Consequently, the liquid chromatography mass spectrometry (LC-MS) characterization of A. garckeana pulp, revealed the presence of 2-Hexadecen-1-ol,3,7,11,15-tetramethyl-,(2E,7 R,11 R)-, nonyl flavanone, testolactone and 6-(Benzyloxy)− 4,4-Dimethyl-2-Chromanone. These compounds were subjected to pharmacoinformatics analysis among which testolactone and 6-(Benzyloxy)− 4,4-Dimethyl-2-Chromanone demonstrated the best drug-likeness, pharmacokinetics, and also exhibited potential hypoglycemic and anti-inflammatory properties. Altogether, the present study provides preclinical evidence of the antioxidant, anti-inflammatory and antidiabetic activities of A. garckeana extract suggesting its potential applications for the development of alternative therapy for diabetes and its associated inflammatory condition.
KW - Anti-inflammatory
KW - Antidiabetic
KW - Antioxidant
KW - Azanza garckeana
KW - Diabetes mellitus
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U2 - 10.1016/j.biopha.2022.113196
DO - 10.1016/j.biopha.2022.113196
M3 - Article
C2 - 35667233
AN - SCOPUS:85132386748
SN - 0753-3322
VL - 152
JO - Biomedicine and Pharmacotherapy
JF - Biomedicine and Pharmacotherapy
M1 - 113196
ER -
