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. 2022 Nov 3;22(1):275–308. doi: 10.1007/s11101-022-09845-w

Table 3.

Biological activities of isoflavonoids isolated from Millettia species

Biological activity Compound name Assay/Model Effect (MIC, IC50) Reference
Anti-inflammatory activity Scandenone RAW264.7 Macrophages Inhibition of NO-production (IC50: 8.5 µM) Raksat et al. (2019)
6,8-Diprenyorobol RAW264.7 Macrophages Inhibition of NO-production (IC50: 14.3 µM) Raksat et al. (2019)
Brandisianin A RAW264.7 Macrophages Inhibition of NO-production (IC50: 35.7 µM) Tang et al. (2016)
Griffoninaone D PLA2 and TPA-induced mouse ear Edema (Female Wistar rat) Inhibition of swelling (0.25 mg/ear, 5 mg/kg) Yankep et al. (2003)
(3S)-vestitol RAW264.7 Macrophages Inhibition of NO-production (IC50: 16.0 µM) Dat et al. (2019)
6-Deoxyclitoriacetal Male Sprague–Dawley rats inhibited the ear edema formation (1 mg/ear) Pancharoen et al. (2008)
α-Toxicarol Male Sprague–Dawley rats inhibited the ear edema formation (1 mg/ear) Pancharoen et al. (2008)
cis-3'',4''-Dihydro-3'',4''-Dihydroxylonchocarpusone RAW264.7 macrophages Dose dependent inhibition of NO-production Tu et al. (2020)
Milletenol A RAW264.7 macrophages Dose dependent inhibition of NO-production Tu et al. (2020)
Anticancer activity Griffonianone C MCF-7 cells Upregulation of mRNA expression of Ki-67 (10–8 M) and CD1 (10–7 M) Wanda et al. (2006)
Usararotenoid A MDB-MB-231 cancer Cells Cytotoxic (IC50: 87.3 µM) Deyou et al. (2015)
Millettosin MDB-MB-231 cancer Cells Cytotoxic to (IC50: 61.7 µM) Deyou et al. (2015)
12a-Epimillettosin MDB-MB-231 cancer Cells Cytotoxic (IC50: 100.7 µM) Deyou et al. (2015)
Usararotenoid C MDB-MB-231 cancer Cells Cytotoxic (IC50: 25.7 µM) Deyou et al. (2015)
4'-O-geranylisoliquiritigenin MDB-MB-231 cancer Cells Cytotoxic (IC50: 125.5 µM) Deyou et al. (2015)
Brandisianin B HeLa cancer Cells Cytotoxic (IC50: 9.7 µM) Kikuchi et al. (2007)
Brandisianin C HeLa cancer Cells Cytotoxic (IC50: 19.1 µM) Kikuchi et al. (2007)
Brandisianin E HeLa cancer Cells Cytotoxic (IC50: 21.7 µM) Kikuchi et al. (2007)
Barbigerone HepG2, C26, LL2 B16 cancer cell lines Induction of aptosis (HepG2 (IC50: 0.61 µM), C26 (IC50: 7.81 µM), LL2 (IC50: 0.36 µM), and B16 (IC50: 5.47 µM) Ye et al. (2012a, b)
Deguelin HepG2, C26, LL2, B16 cancer cell lines Induction of aptosis (HepG2 (IC50: 1.55 µM), C26 (IC50: 8.93 µM), LL2 (IC50: 0.51 µM), and B16 (IC50: 0.20 µM) Ye et al. (2012a, b)
3-Homo13-oxa-6a,12a-dehydrodeguelin HepG2, C26, LL2, B16 cancer cell lines Induction of aptosis (HepG2 (IC50: 17.48 µM), C26 (IC50: 10.10 µM), LL2 (IC50: 3.33 µM), and B16 (IC50: 10.15 µM) Ye et al. (2012a, b)
Tephrosin HepG2, C26, LL2, B16 cancer cell lines Induction of aptosis (HepG2 (IC50: 1.41 µM), C26 (IC50: 6.49 µM), LL2 (IC50: 0.56 µM), and B16 (IC500: 15.95 µM) Ye et al. (2012a, b)
6a,12a-dehydrodeguelin HepG2, C26, LL2, B16 cancer cell lines Induction of aptosis (HepG2 (IC50: 2.93 µM), C26 (IC50: 7.55 µM), LL2 (IC50: 1.35 µM), and B16 (IC50: 8.85 µM) Ye et al. (2012a, b)
Maximaisoflavone B MDA-MB-231 breast cancer cells Cytotoxic (IC50: 153.5 µM) Marco et al. (2017)
7,2′-Dimethoxy-4′,5′-dimethylenedioxy isoflavone MDA-MB-231 breast cancer cells Cytotoxic (IC50: 174.1 µM) Marco et al. (2017)
Durmillone A549 cancer cell line Cytotoxic (IC50: 6.6 ± 1.2 mM) Buyinza et al. (2021)
Jamaicin A549 cancer cell line Cytotoxic (IC50: 11.4 ± 5.0 mM) Buyinza et al. (2021)
Antibacterial activity Millexatin A Bacterial strains Growth inhibition: S. aureus, S. epidermidis and B. subtilis (2 µg/mL); S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
Millexatin F Bacterial strains Growth inhibition: S. aureus, S. epidermidis, and B. subtilis (2 µg/mL); S. typhyimurium and Ps. aeruginosa (128 2 µg/mL) Raksat et al. (2018)
Auriculatin Bacterial strains Growth inhibition: S. aureus, S. epidermidis, and B. subtilis (2 µg/mL); S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
3'-Methylorobol Bacterial strains Growth inhibition: S. aureus (32 µg/mL), S. epidermidis and B. subtilis (64 µg/mL); S. typhyimurium and Ps. Aeruginosa (128 µg/mL) Raksat et al. (2018)
Scandenone Bacterial strains Growth inhibition: S. aureus and B. subtilis (2 µg/mL); S. epidermidis (4 µg/mL); S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
Auriculasin Bacterial strains Growth inhibition: S. aureus and S. epidermidis (4 µg/mL); B. subtilis (8 µg/mL); S. typhyimurium and Ps. Aeruginosa (128 µg/mL) Raksat et al. (2018)
2'-Deoxyauriculasin Bacterial strains Growth inhibition: S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
Isoauroculatin Bacterial strains Growth inhibition: S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
Sumarol Bacterial strains Growth inhibition: S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
Maackiain Bacterial strains Growth inhibition: S. typhyimurium and Ps. aeruginosa (128 µg/mL) Raksat et al. (2018)
Millexatin I Bacterial strains Growth inhibition: M. luteus (64), S. mutans (128 µg/mL), S. epidermidis (128 µg/mL), S. cereus (64 µg/mL), S. aureus (64 µg/mL); S. typhimurium (128 µg/mL), S. flexneri (128 µg/mL) Raksat et al. (2019)
Millexatin J Bacterial strains Growth inhibition: M. luteus (32 µg/mL), S. mutans (128 µg/mL), S. epidermidis (128 µg/mL), S. typhimurium (128 µg/mL), E. coli (128 µg/mL) Raksat et al. (2019)
Millexatin K Bacterial strains Growth inhibition: M. luteus (64 µg/mL), S. mutans (128 µg/mL), S. epidermidis (128 µg/mL), S. cereus (32 µg/mL), S. aureus (32 µg/mL); S. typhimurium (128 µg/mL) Raksat et al. (2019)
Millexatin L Bacterial strains Growth inhibition: M. luteus (64 µg/mL), S. mutans (128 µg/mL), S. epidermidis (128 µg/mL), S. cereus (32 µg/mL), S. aureus (32 µg/mL); S. typhimurium (128 µg/mL) Raksat et al. (2019)
Millexatin M Bacterial strains Growth inhibition: S. epidermidis (128 µg/mL), S. cereus (128 µg/mL), S. aureus (128 µg/mL); S. typhimurium (128 µg/mL), S. flexneri (128 µg/mL) Raksat et al. (2019)
Millexatin B Bacterial strains Growth inhibition: S. epidermidis (128 µg/mL), S. aureus (128 µg/mL); S. typhimurium (128 µg/mL), Raksat et al. (2019)
Millexatin D Bacterial strains Growth inhibition: M. luteus (32 µg/mL), S. mutans (128 µg/mL), S. epidermidis (128 µg/mL), S. cereus (8 µg/mL), S. Aureus (8 µg/mL); S. typhimurium (128 µg/mL), S. aeuruginosa (128 µg/mL), E. coli (128 µg/mL) Raksat et al. (2019)
Millipurone Bacterial strains Growth inhibition: M. luteus (2 µg/mL), S. mutans (16 µg/mL), S. epidermidis (4 µg/mL), S. cereus (32 µg/mL), S. aureus (4 µg/mL); S. typhimurium (128 µg/mL), S. aeuruginosa (128 µg/mL), E. coli (128 µg/mL), S. flexneri (128 µg/mL) Raksat et al. (2019)
5,7,3',4'-tetrahydroxy-6,8-diprenylisoflavone (6,8-Diprenyorobol) Bacterial strains Growth inhibition: M. luteus (16 µg/mL), S. mutans (16 µg/mL), S. epidermidis (128 µg/mL), S. cereus (16 µg/mL), S. aureus (32 µg/mL); S. typhimurium (128 µg/mL), S. aeuruginosa (128 µg/mL), E. coli (128 µg/mL), S. flexneri (128 µg/mL) Raksat et al. (2019)
5-Hydroxy-7-methoxy-4'-O-(3-methylbut-2-enyl)isoflavone Bacterial strains Growth inhibition: S. aureus (32 µg/mL); S. epidermidis (128 µg/mL), S. typhimurium (128 µg/mL) Raksat et al. (2019)
7,4'-di-O-prenylgenistein Bacterial strains S. aureus (32 µg/mL); S. epidermidis (128 µg/mL), S. typhimurium (128 µg/mL); S. flexneri (128 µg/mL) Raksat et al. (2019)
Estrogenic activity Millewanin G 17 β-estradiol induced yeast Inhibition of β-galactosidase activity (IC50: 29 µM) Ito et al. (2006)
Millewanin H 17 β-estradiol induced yeast Inhibition of β-galactosidase activity IC50: 18 µM) Ito et al. (2006)
Furowanin B 17 β-estradiol induced yeast Inhibition of β-galactosidase activity (IC50: 13 µM) Ito et al. (2006)
4'-methoxy-7-O-[(E)-3-methyl-7-hydroxymethyl-2,6-octadienyl]isoflavone Yeast strain; MVLN cells; Ishikawa cells Induction of estradiol activity (S. sereviseae) (10–8 M); Induction of luciferase activity (10–6 M); AlkP induction (10−6 M) Wanda et al. (2006)
3',4'-dihydroxy-7-O -[(E)-3,7-dimethyl-2,6-octadienyl]isoflavone M Yeast strain; MVLN cells; Ishikawa cells Induction of estradiol activity (10–8 M); Induction of luciferase activity (10−5 M); AlkP induction (10−5 M) Wanda et al. (2006)
4'-O-geranylisoliquiritigenin Yeast strain; MVLN cells; Ishikawa cells Induction of estradiol activity (10–8 M); Induction of luciferase activity (10−6 M); AlkP induction (10−6 M) Wanda et al. (2006)
7-O-geranylformononetin Yeast strain; MVLN cells; Ishikawa cells Induction of estradiol activity (10–8 M); Induction of luciferase activity (10−6 M); AlkP induction (10−7 M) Wanda et al. (2006)
Griffonianone C Wanda et al. (2007)
Anti-Alzheimer ‘s Deguelin In vitro assay Inhibition of AChE activity (IC50: 126.70 µM) Tu et al. (2019)
Tephrosin In vitro assay Inhibition of AChE activity (IC50: 127.18 µM) Tu et al. (2019)
Barbigerone In vitro assay Inhibition of AChE (IC50: 121.60 µM) and BChE (IC50: 21.77 µM) activities Tu et al. (2019)
4',5-dimethoxy-6,6-dimethylpyrano isoflavone In vitro assay Inhibition of AChE (IC50: 131.17 µM) and BChE (IC50: 2.34 µM) activities Tu et al. (2019)
Larvaecidal activity Deguelin Aedes aegypti larvae Potent (IC50: 1.6 µg/mL) Yenesew et al. (2003a)
Tephrosin Aedes aegypti larvae Potent (IC50: 1.4 µg/mL) Yenesew et al. (2003a)
Anticoagulative activities Genistein Male New Zealand white rabbits Dose-dependent antithrobin activity Liao et al. (2013)
Daidzein Male New Zealand white rabbits Dose-dependent antithrobin activity Liao et al. (2013)
5,7,2',4'-tetrahydroxyisolfavone Male New Zealand white rabbits Dose-dependent antithrobin activity Liao et al. (2013)
Antioxidant activity Robustigenin, Viridiflorin, 12a-hydroxy-a -toxicarol TLC-spot DPPH-Assay Radical scavenging activity Pancharoen et al. (2008)
Antiplasmodial activity calopogonium isoflavone B; 3D7 and the Dd2 strains of Plasmodium falciparum 70–90% inhibition (40 µM) Marco et al. (2017)
Isoerythrin A-4′-(3-methylbut-2-enyl) ether 70–90% inhibition (40 µM) Marco et al. (2017)