Exploring the Enzymatic-Based Biological Activities of Kratom Leaves Extracts on Alpha-Amylase, Alpha-Glucosidase, Angiotensin-Converting Enzyme, and Cholinesterases

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Weerachai Pipatrattanaseree
Chanisara Intareeya
Sayan Koonnoot
Sakwichai Ontong
Thitiporn Thaptimthong
Sadudee Rattanajarasroj
Siriwan Chaisomboonpan
Attawadee Sae Yoon

Abstract

Introduction and objective: Kratom leaves (Mitragyna speciosa Korth) have been an integral part of traditional Thai medicine and local folk medicine for a long time. In Thailand, it has recently been legalized for use as a medicinal plant or traditional Thai medicine. Consequently, kratom has gained popularity as a medicinal plant based on people's beliefs. This study aimed to investigate the enzymatic-based biological activities of kratom extracts, specifically their anti-diabetic, anti-hypertensive, and anti-Alzheimer's disease properties, in order to provide scientific information for further development of kratom for medical use.


Methods: The kratom extracts used in this study were 95%, 70%, and 50% ethanolic extracts obtained from maceration, as well as an aqueous extract obtained from decoction method. All extracts were evaluated for inhibitory activities on alpha-glucosidase and alpha-amylase for anti-diabetes while its effect on angiotensin-I converting enzyme was examined for anti-hypertension. For the anti-Alzheimer's disease property, the inhibitory effects on acetylcholinesterase and butyrylcholinesterase were investigated.


Results: The study found that kratom extracts exhibited inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and alpha-glucosidase enzyme. The 95% ethanolic extract exhibited the highest activity on butyrylcholinesterase and acetylcholinesterase, with the half inhibitory concentration (IC50) values of 64.40 ± 16.74 µg/mL and 127.99 ± 6.15 µg/mL, respectively. The 70% and 50% ethanolic extracts demonstrated comparable effects on alpha-glucosidase enzyme, with IC50 values of 382.64 ± 16.18 µg/mL and 409.43 ± 19.14 µg/mL, respectively. However, all extracts were inactive on angiotensin-I converting enzyme and alpha-amylase enzyme. The content of mitragynine in the 95%, 70%, 50% ethanolic extracts and the aqueous extracts were 54.00 ± 1.17, 35.14 ± 0.64, 25.05 ± 0.05, and 18.08 ± 0.30 mg/g, respectively.


Discussion: Kratom extracts showed the most potential as butyrylcholinesterase and acetylcholinesterase inhibitors, and exhibited moderate activity in inhibiting alpha-glucosidase. The 95% ethanolic extract exhibited the highest mitragynine content, which was correlated with its ability to inhibit acetylcholinesterase and butyrylcholinesterase enzymes. This study was limited to explore only the in vitro enzymatic-based assays which require additional in vitro and in vivo assay models to conclude the possibility of using kratom as a medicine for patients or as dietary supplement.


Conclusion and recommendation: The findings of this study suggested the inhibitory effects of kratom extracts on acetylcholinesterase, butyrylcholinesterase and alpha-glucosidase. Moreover, further in vitro and in vivo assay models as well as clinical trials are necessary to confirm its potential for development as a traditional medicine, or dietary supplement.

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References

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