Mira Syahfriena Amir Rawa1, Zurina Hassan2, Vikneswaran Murugaiyah3, Toshihiko Nogawa4, Habibah A Wahab5. 1. School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia; Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan; USM-RIKEN Centre for Aging Science (URICAS), Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia. 2. Centre for Drug Research, Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia. 3. School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia. 4. Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan; USM-RIKEN Centre for Aging Science (URICAS), Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia. Electronic address: nogawat@riken.jp. 5. School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia; USM-RIKEN Centre for Aging Science (URICAS), Universiti Sains Malaysia, 11800, Minden, Penang, Malaysia. Electronic address: habibahw@usm.my.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Enhancement of cholinergic functions in the brain via acetylcholinesterase inhibition is one of the main therapeutic strategies to improve symptoms associated with Alzheimer's or related cognitive deficits. There is a pathophysiological correlation between Alzheimer's and Diabetes Mellitus, as well as inflammation and oxidative stress that may cause cognitive decline. AIM OF THE STUDY: The present study was intended to evaluate anti-cholinesterase potential of 177 Malaysian plant extracts from 148 species known to have related ethnomedicinal uses such as anti-inflammatory, anti-oxidant, anti-diabetic, epilepsy, headache, memory enhancement and anti-aging. MATERIALS AND METHODS: Anti-cholinesterase screening against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes was performed on the basis of in-vitro colorimetric 96-well microplate-based assay method. Potent active plant extracts were subjected to liquid-liquid extraction and acid-base fractionation for further analysis. RESULTS: Fifty-seven plant extracts exhibited potent anti-cholinesterase activities (50-100% inhibition) at 200 μg/ml. Majority of the active plants originated from Fabaceae family. Coccoloba uvifera (L.) L. stem extract manifested the lowest IC50 of 3.78 μg/ml for AChE and 5.94 μg/ml for BChE. A few native species including Tetracera indica (Christm. & Panz.) Merr., Cyrtostachys renda Blume and Ixora javanica (Blume) DC. showed cholinesterase inhibition despite limited local medical applications. Further anti-AChE evaluation (50 μg/ml) of 18 potent plant extracts harbored active polar components in butanol and water fractions, except Senna pendula (Willd.) H.S.Irwin & Barneby (leaves and stems), Acacia auriculiformis Benth. (leaves), Artocarpus altilis (Parkinson ex F.A.Zorn) Fosberg (leaves), and Macaranga tanarius (L.) Mull.Arg. (leaves) that showed inhibitory activity in less polar fractions. The acidic extraction of these four plant species improved their inhibition level against AChE. CONCLUSION: This study rendered a preliminary overview of anti-cholinesterase activity from diverse Malaysian botanical families in which provided the medical relevance toward these native plant species, especially ones with limited ethnobotanical record or practice.
ETHNOPHARMACOLOGICAL RELEVANCE: Enhancement of cholinergic functions in the brain via acetylcholinesterase inhibition is one of the main therapeutic strategies to improve symptoms associated with Alzheimer's or related cognitive deficits. There is a pathophysiological correlation between Alzheimer's and Diabetes Mellitus, as well as inflammation and oxidative stress that may cause cognitive decline. AIM OF THE STUDY: The present study was intended to evaluate anti-cholinesterase potential of 177 Malaysian plant extracts from 148 species known to have related ethnomedicinal uses such as anti-inflammatory, anti-oxidant, anti-diabetic, epilepsy, headache, memory enhancement and anti-aging. MATERIALS AND METHODS: Anti-cholinesterase screening against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes was performed on the basis of in-vitro colorimetric 96-well microplate-based assay method. Potent active plant extracts were subjected to liquid-liquid extraction and acid-base fractionation for further analysis. RESULTS: Fifty-seven plant extracts exhibited potent anti-cholinesterase activities (50-100% inhibition) at 200 μg/ml. Majority of the active plants originated from Fabaceae family. Coccoloba uvifera (L.) L. stem extract manifested the lowest IC50 of 3.78 μg/ml for AChE and 5.94 μg/ml for BChE. A few native species including Tetracera indica (Christm. & Panz.) Merr., Cyrtostachys renda Blume and Ixora javanica (Blume) DC. showed cholinesterase inhibition despite limited local medical applications. Further anti-AChE evaluation (50 μg/ml) of 18 potent plant extracts harbored active polar components in butanol and water fractions, except Senna pendula (Willd.) H.S.Irwin & Barneby (leaves and stems), Acacia auriculiformis Benth. (leaves), Artocarpus altilis (Parkinson ex F.A.Zorn) Fosberg (leaves), and Macaranga tanarius (L.) Mull.Arg. (leaves) that showed inhibitory activity in less polar fractions. The acidic extraction of these four plant species improved their inhibition level against AChE. CONCLUSION: This study rendered a preliminary overview of anti-cholinesterase activity from diverse Malaysian botanical families in which provided the medical relevance toward these native plant species, especially ones with limited ethnobotanical record or practice.
Authors: Mira Syahfriena Amir Rawa; Mohammad G Al-Thiabat; Toshihiko Nogawa; Yushi Futamura; Akiko Okano; Habibah A Wahab Journal: Pharmaceuticals (Basel) Date: 2022-07-21