TY - JOUR
T1 - Characterization of Ginkgo biloba leaf flavonoids as neuroexocytosis regulators
AU - Ban, Choongjin
AU - Park, Joon Bum
AU - Cho, Sora
AU - Kim, Hye Rin
AU - Kim, Yong Joon
AU - Bae, Hyungjin
AU - Kim, Chinhan
AU - Kang, Hakhee
AU - Jang, Davin
AU - Shin, Yong Sub
AU - Kim, Dae Ok
AU - Kim, Hyunggun
AU - Kweon, Dae Hyuk
N1 - Publisher Copyright:
© 2020 by the authors.
PY - 2020/4/1
Y1 - 2020/4/1
N2 - Ginkgo biloba leaf (GBL) is known as a potential source of bioactive flavonoids, such as quercetin, arresting the neuronal soluble N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE)-zippering. Here, the GBL flavonoids were isolated in two different manners and then examined for their bioactivity, physicochemical stability, and biocompatibility. The majority of flavonoids in the non-hydrolyzed and acidolyzed isolates, termed non-hydrolyzed isolate (NI) and acidolyzed isolate (AI) hereafter, were rich in flavonol glycosides and aglycones, respectively. Glycosidic/aglyconic quercetin and kaempferol were abundant in both NI and AI, whereas a little of apigenin, luteolin, and isorhamnetin were found in AI. NI was more thermostable in all pH ranges than quercetin, kaempferol, and AI. NI and AI both inhibited neurotransmitter release from differentiated neuronal PC-12 cells. NI and AI showed 1/2–1/3 lower EC50/CC50 values than quercetin and kaempferol. The NI and AI exhibited no toxicity assessed by the tests on chorioallantoic membranes of hen’s eggs, removing toxicological concerns of irritation potential. Moreover, GBL isolates, particularly AI, showed antioxidant and anti-inflammatory activities in the use below the CC50 levels. Taken together, these results suggest that GBL isolates that are rich in antioxidant flavonoids are effective anti-neuroexocytotic agents with high stability and low toxicity.
AB - Ginkgo biloba leaf (GBL) is known as a potential source of bioactive flavonoids, such as quercetin, arresting the neuronal soluble N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE)-zippering. Here, the GBL flavonoids were isolated in two different manners and then examined for their bioactivity, physicochemical stability, and biocompatibility. The majority of flavonoids in the non-hydrolyzed and acidolyzed isolates, termed non-hydrolyzed isolate (NI) and acidolyzed isolate (AI) hereafter, were rich in flavonol glycosides and aglycones, respectively. Glycosidic/aglyconic quercetin and kaempferol were abundant in both NI and AI, whereas a little of apigenin, luteolin, and isorhamnetin were found in AI. NI was more thermostable in all pH ranges than quercetin, kaempferol, and AI. NI and AI both inhibited neurotransmitter release from differentiated neuronal PC-12 cells. NI and AI showed 1/2–1/3 lower EC50/CC50 values than quercetin and kaempferol. The NI and AI exhibited no toxicity assessed by the tests on chorioallantoic membranes of hen’s eggs, removing toxicological concerns of irritation potential. Moreover, GBL isolates, particularly AI, showed antioxidant and anti-inflammatory activities in the use below the CC50 levels. Taken together, these results suggest that GBL isolates that are rich in antioxidant flavonoids are effective anti-neuroexocytotic agents with high stability and low toxicity.
KW - Anti-inflammatory activity
KW - Antioxidant activity
KW - Bioactivity
KW - Biocompatibility
KW - Flavonoids
KW - Ginkgo biloba leaf isolate
KW - Neurotransmission inhibition
KW - Physicochemical stability
UR - http://www.scopus.com/inward/record.url?scp=85083561648&partnerID=8YFLogxK
U2 - 10.3390/molecules25081829
DO - 10.3390/molecules25081829
M3 - Article
C2 - 32316426
AN - SCOPUS:85083561648
SN - 1420-3049
VL - 25
JO - Molecules
JF - Molecules
IS - 8
M1 - 25081829
ER -