TY - JOUR
T1 - Flavonoids from the genus euphorbia
T2 - Isolation, structure, pharmacological activities and structure–activity relationships
AU - Magozwi, Douglas Kemboi
AU - Dinala, Mmabatho
AU - Mokwana, Nthabiseng
AU - Siwe-Noundou, Xavier
AU - Krause, Rui W.M.
AU - Sonopo, Molahlehi
AU - McGaw, Lyndy J.
AU - Augustyn, Wilma A.
AU - Tembu, Vuyelwa Jacqueline
N1 - Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2021/5
Y1 - 2021/5
N2 - Plants of the genus Euphorbia are widely distributed across temperate, tropical and sub-tropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohy-drate attached at either C-3 or C-7, and were designated as D-glucose, L-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.
AB - Plants of the genus Euphorbia are widely distributed across temperate, tropical and sub-tropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohy-drate attached at either C-3 or C-7, and were designated as D-glucose, L-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.
KW - Euphorbia
KW - Flavonoids
KW - Pharmacological activities
KW - Structure–activity relationship
UR - http://www.scopus.com/inward/record.url?scp=85105971636&partnerID=8YFLogxK
U2 - 10.3390/ph14050428
DO - 10.3390/ph14050428
M3 - Review article
AN - SCOPUS:85105971636
SN - 1424-8247
VL - 14
JO - Pharmaceuticals
JF - Pharmaceuticals
IS - 5
M1 - 428
ER -