Skip to main content
. 2021 Jan 19;13(1):124. doi: 10.3390/pharmaceutics13010124

Table 3.

Characterization of the identified phytochemicals in terms of origin and main enzymatic targets (substrates, inhibitors, and inducers).

Bioactive Plant Sources ALOX5 AMPK BSEP COX CYP GLP-1 HMGCoAR MAO NMDA ABC PLA2G2A SLC UGT Reference
BCRP MRP PgP PEPT; OCT; OAT, MATE, OATP
11-Angeloylsenkyunolide F * A. sinensis 3A42D6 [246]
Apigenin * M. chamomilla
M. officinalis
P. emblica
S. costus
1A2
2C9
2C19
3A4
21A6
21A8
21A9
22A8
22A11
22A4
1A1 [200,247,248,249,250,251,252,253]
α-Asarone A. calamus
A. gramineus
2 1A1
3A4
2B6
2C8
2C9
2C19
2D6
2E1
A
B
Ant [254,255,256,257,258,259,260]
β-Asarone A. calamus
A. gramineus
R. acori
2 3A4 A
B
[255,259,261]
Asiatic acid * C. asiatica 3A4
2D6
2C9
S [262,263,264,265]
Assoanine N. assoanus
Atractylenolide III * A. japonica
A. lancea
2B7 [266]
Avenanthramide A * A. sativa 2 [267,268]
Avenanthramide B * A. sativa 2 [268]
Avenanthramide C * A. sativa 2 [268,269]
Bacoside A * and B * B. monnieri 1A2
3A4
2C9
2C19
[270]
N-Acetyl Benzylamine * L. meyenii
N-Benzylhexadecanamide * L. meyenii
Berberine * C. chinensis
C. japonica
1A2
3A4S↓
2C9
2D6
↓↑S 21A8S [271,272,273,274,275,276,277]
Biapigenin * H. perforatum 1A2
3A4
2C9
2D6
A Ant S [124,200,278,279]
Bilobalide * G. biloba 1A1
1A2
3A4
2B6
2C9
2E1
6A2
22A6
22A8
[218,280,281,282]
Biochanin A * T. pratense 2 3A4 B ↓S 21A6
21A8
[245,248,283,284,285,286,287]
Buxakashmiramine B. papillosa
Buxamine B B. hyrcana
Caffeic acid * C. pluricaulis
F. vulgare
M. chamomilla
M. officinalis
R. officinalis
V. angustifolium
1,2 1A1
3A4
2C9
2C19
2D6
[288,289,290,291]
Caffein * C. arabica
I. paraguariensis
P. cupana
T. cacao
C. sinensis
1A2
3A4
[292,293]
β-Carbolines (Harmine) * L. meyenii
M. pruriens
P. harmala
1A1
1A2
2C9
2C19
2D6
2E1
A
B
2↑S [124,126,294,295,296]
9-Methyl-9B-Carboline * P. harmala 3A4
2D6S↓
A
B
0 [127,296,297]
Casticin * V. agnus-castus 3A4
2C9
[298]
Catalpol * R. glutinosa 3A4↑↓
2C9↑↓
2E1
[292,299,300,301]
Catechin * C. rotundus
L. bicolor
M. chamomilla
T. cacao
1A2
3A4
2C9
47A1
47A2
22A1
22A2
21A3
21A6
[302,303]
Chebulagic acid * T. chebula
P. emblica
2 [304,305]
Chlorogenic acid * F. vulgare
H. perforatum
I. paraguariensis
M. chamomilla
M. lucida
R. officinalis
2 1A2
3A4o
2E1
B 22A6
22A8
[306,307,308,309,310,311]
1,8-Cineole (eucalyptol) * F. vulgare
S. lavandulaefolia
R. officinalis
3A4S S [312]
Cinnamaldehyde * C. wilsonii 2 1A2
2E1
BS Ant [75,313,314,315,316,317]
Coniferyl ferulate * A. sinensis 3A4
2D6
[246,318]
Convolamine * C. pluricaulis
Conypododiol A. adscendens
Coptisine C. chinensis 1A2
3A4
2C9
2D6
A
B
S↑ 22A1S↓
22A2S↓
[272,273,274,319,320]
p-Coumaric acid * B. rufescens
M. lucida
2 [321,322]
Corilagin * T. chebula
P. emblica
2 2B4 [323]
Crocetin * C. sativus Ant 1
2
S [324,325,326]
Crocin * C. sativus 1
2
3A4
3A5
3A7
2B6
A
B
1
2
[327,328,329]
Curcumin * C. longa 1A2
3A4
2B6
2C9
2D6
↑↓ 1
2
21A6
21A8
1A1
1A6
1A9
[247,330,331,332,333,334,335,336,337,338,339]
Cyanidin-3-O-β-arabinose * V. angustifolium 1A2
3A4
[340]
Cyanidin-3-O-β-galactoside * V. angustifolium 1A2
3A4
2C9
S 0 [341,342]
Cyanidin-3-O-β-glucoside * E. amoenum
V. angustifolium
V. uliginosum L.
2 3A4
2C9↓
S 21A9 [341,343,344,345]
Cyclomicrophylline A B. papillosa
Cycloprotobuxine-C B. papillosa
Cyclovirobuxeine-A B. papillosa
Cynatroside A C. atratum
Cynatroside B C. atratum
Daidzein * L. bicolor
M. lucida
P. lobata
1A1S
1A2S
3A4
↓S 1 1A1S
1A9S
[245,285,346,347,348,349]
Decursin * A. gigas 1A1
1A2
2 [247,350]
Decursinol angelate * A. gigas 1A1
1A2
3A4S
2C19S
S [350,351,352]
Delphinidin * V. uliginosum L. 3A4
2B6
2C9
21A8 [341,344,353]
Delphinidin-3-O-β-galactoside * V. angustifolium
Diosgenin * D. polystachya
D. oppositifolia
T. foenum-graecum
2 3A4 S [354,355,356]
Ellagic acid * T. chebula
P. emblica
1A1↑↓
2B6
2E1
S 22A6
22A11
[357,358,359,360,361,362]
Ent-kaurane * C. tonkinensis 2 [363,364,365]
Epicatechin gallate (ECG) * C. sinensis 1A1
1A2
3A4
21A6S↓
21A8
[366,367,368,369]
Epigallocatechin-3-gallate (EGCG) * C. sinensis 1A1
1A2
3A4
3A5
2B6
2C8
2C9
2C19
2D6
2E1
S↓ 21A6
21A8S↓
21A9
22A1
22A2
47A1
47A2
[248,302,303,345,367,370,371,372,373,374,375,376]
Epinorgalantamine N. confusus
G. woronowii
Eugenol * C. wilsonii
R. acori
R. officinalis
2 1A1
2E1S
0 A 0↓ 1A1 [77,247,377,378,379,380,381,382,383]
Ferulic acid * A. sinensis
B. rufescens
1A1
1A2↑S
3A4↑S
2B6↑S
2C8↑S
2C9↑S
2C19↑S
2D6↑S
B Ant 1A1S
2B7S
[246,384,385,386,387]
Forskolin * C. forskohlii 2 3A4S↑
2C
2B6
s↓ [388,389,390,391,392,393,394,395,396,397]
Galantamine * G. nivalis
G. woronowii
L. radiata
N. confusus
P. illyricum
3A4S 0
2D6S
1A1S [398,399,400,401,402]
11-Hydroxy Galantamine * N. poeticus
Gallic acid * M. pruriens
P. emblica
T. chebula
2 3A4
2D6
A 21A8 2B7 [403,404,405,406,407,408,409]
Genistein * L. bicolor
M. lucida
M. pruriens
2 1A1
1A2↓S
3A4
2C8
2C9
2D6
A
B
↓S 1
2↓S
21A6↓S [218,285,369,374,409,410,411,412,413,414,415]
Gingerol * A. melegueta
Z. officinale Rosc.
3A4
2C9
2C19
[416,417]
Ginkgolide A * G. biloba 2 3A4
2C9
6A2
22A6
22A8
[218,281,418,419,420]
Ginkgolide B * G. biloba 3A4
2C9
6A2
22A6
22A8
[218,281,418]
Ginsenoside Rb * P. ginseng 1A1
1A2
3A4
2C9
21A8S [421,422,423]
Ginsenoside Rc * P. ginseng 3A4
2C9
21A8S [421,423]
Ginsenoside Rd * P. ginseng 3A4
2C9
2C19
2D6
21A8S [421,423]
Ginsenoside Rg * P. ginseng 1A1
1A2
3A4
2C9
2D6
S 21A8S [421,422,423]
1,2,3,4,6-Penta-O-galloyl-β-d-glucose * T. chebula 2 [424,425]
Glycyrrhetinic acid * G. glabra 21A9 [426]
Glycyrrhizin * G. glabra S 3A4
2D6
↑↓ 21A8 [247,257,427,428,429]
Haloxysterol A *, B *, C *, D * H. recurvum 2 [430]
Harpagide * S. buergeriana 3A40 [431]
8-O-E-p-Methoxy Cinnamoyl Harpagide S. buergeriana
E-Harpagoside * S. buergeriana 1↓0
2↓0
3A40 [431,432,433,434]
Huperzine A * H. serrata 1A2
3A4↑0
S [435,436,437]
Hyperforin * H. perforatum 1
20
2D6↓0
2C9
3A4
3A5
1A2
2C19
A0 Ant 2 ↑↓ 21A6
21A8
21A9
1A1↑↑ [98,124,202,278,438,439,440,441,442,443,444,445,446,447,448,449]
Hypericin * H. perforatum 2D6↓0
2C9
3A4
1A2
2C19
A↓0
B↓0
Ant 1 21A9↓S
1A6 [102,124,278,336,442,443,444,447,450,451,452,453,454,455]
Hyperoside * B. rufescens
C. japonica
H. perforatum
P. pterocarpum
2D6
2C9
S [289,456]
Isoliquiritigenin * G. uralensis 1A2
3A4
2C9
2C19
[457]
Isorhamnetin * G. biloba
R. nigrum
1A2
3A4
2 S↑↓ 21A8 [200,247,249,458,459]
Isosarcodine S. saligna 2 [430]
p-Kaempferol * A. melegueta
C. pluricaulis
C. japonica
C. rotundus
H. perforatum
I. paraguariensis
1A2
3A4
2C9
2C19
Ant ↓S 21A8
21A9
22A4
22A8
1A1 [200,218,250,251,374,460,461,462,463]
Kaempferol-3-glucoside * C. ternatea
C. pluricaulis
21A6
21A8
[345,463]
11α-Hydroxy-O-methylleucotamine P. illyricum
N-3-methoxybenzyl-linoleamide (macamide) * L. meyenii
Levodopa * M. pruriens Ant S [464,465]
Luteolin * L. bicolor
M. chamomilla
M. officinalis
P. emblica
R. officinalis
2 1A2
3A4
3A50
2B6
2C8
2C9
2C19
2D6
2E1
A
B
1A1↓S
1A9
2B7
[276,466,467,468,469,470,471,472]
Lycorine G. woronowii
P. illyricum
3A40 0 [342,473]
Malvidin 3-galactoside * V. angustifolium 3A4
2C9
↓S 21A6 [341,353,474]
Malvidin 3-glucoside * V. angustifolium
V. uliginosum L.
3A4
2C9
21A6 [341,353,474]
Malvidin-3-O-β-arabinose * V. angustifolium - [475]
Mangiferin * M. indica 1A1
1A2
3A4
2C8
2B6
2D6
1A1
1A9
2B7
[198,476,477]
Methylliberine * C. arabica
Mucunadine * M. pruriens
Mucunine * M. pruriens
Myricetin * M. peregrina
R. nigrum
1A2
3A4
2D6
1 ↓S 21A6 [218,247,248,276,478]
Naringenin L. bicolor
M. lucida
2 1A2↓0
3A4
2B60
2C9
2C19
2D60
2E10
A
B
22A6
21A6
21A8
21A9
1A1
1A3
1A6
1A9
2B4
2B7
[200,218,247,253,479,480,481,482,483,484,485,486,487,488]
Naringin * M. lucida 2 3A4↓↑
1A2
A 21A9 [200,253,338,483,487,489,490,491,492,493]
N,N-dimethyl buxapapine B. papillosa
Nobiletin * C. reticulata 2 1A1↓↑
1A2↓↑
3A4
A
B
1 21A8
21A9
[208,247,337,487,494,495,496,497]
Oleanolic acid * M. lucida
R. officinalis
2 1A2
3A4
A - 1 0 [276,498,499,500,501,502,503]
α-Onocerin * L. clavatum
p-Synephrine * C. aurantium 1A20
3A4
2D60
2E10
AS
BS
[79,504,505,506]
Paeonol * P. lactiflora 2 1A2S A
B
S [507,508,509,510,511]
Palmatine C. chinensis
C. speciosa
2 1A1
1A2S
3A4
2D6S
A [274,512,513,514,515]
Peonidin-3-O-β-arabinose * V. angustifolium
d-Pinitol B. rufescens
15-Methyl Pinusolidic acid * P. orientalis A [133]
Phyllanthin * P. emblica 1A20
3A4
2C90
2D60
2E10
20 [516,517]
Phytol M. lucida 2 [518,519,520]
α-Pinene * R. officinalis
S. lavandulaefolia
2 2B6 Ant [521,522,523]
Piperine * P. nigrum 1A2
3A4
2C9
2E1
22A2 1A1 [524,525,526]
Polygalaxanthone III * P. tenuifolia 2E1 [527]
Protocatechuic acid * A. oxyphylla
G. biloba
M. officinalis
R. officinalis
V. vinifera
1A1
1A2
2C9
2E1
[245,528]
Prurienidine * M. pruriens
Prurienine * M. pruriens
Puerarin * P. lobata 2 1A1
1A2
3A4
2B6
2C9
2D6
2E1
1A1 [529,530,531,532,533,534,535,536,537]
Quercetin * A. melegueta
C. sativus
C. rotundus
H. perforatum
I. paraguariensis
L. meyenii
M. lucida
P. emblica
R. nigrum
S. costus
V. uliginosum L.
1A1
1A2
3A4
2C8
2C9
2C19
2D6
A Ant ↑S 1
2
↓S 21A6
21A8
21A9
22A6
1A1
1A6
[24,200,218,247,289,338,374,462,487,488,538,539,540,541,542]
Quercetin-3-O-β-d-glucuronide P. pterocarpum 2 3A4 2 21A8
21A9
1A1 [539,543]
Resveratrol * V. vinifera 1A1↓S
1A2
3A4
2C9
2C19
2D6
A ↑S 2S 21A8S [218,298,338,544,545,546,547,548,549,550,551]
Rosarin * R. rosea 1A2
3A4
2C9
2D6
A0
B0
[552,553]
Rosavin * R. rosea 1A2
3A4
2C9
2D6
A0
B0
[552,553]
Rosin * R. rosea 1A2
3A4
2C9
2D6
A0
B0
[552,553]
Rosmarinic acid * M. officinalis
M. spicata
R. officinalis
3A4
2C9
2C19
2D6
2E1
1A1 [416,554,555]
Rutin * H. perforatum
L. bicolor
M. chamomilla
M. flexuosa
M. lucida
M. peregrina
V. uliginosum L.
2 1A1
3A4
B 21A6
21A8
21A9↓↑
[24,248,253,345,426,556,557,558,559,560,561,562,563]
Safranal * C. sativus 2B6 [247,328,564]
Salidroside * R. rosea 1
2
1A2
3A4
2B6
2C9
A
B
1 [565,566,567,568,569,570]
Salvianolic acid * M. spicata
S. miltiorrhiza
2 1A2
3A4
21A8S [571,572,573,574]
Sanguinine E. grandiflora
P. illyricum
3A40 [399]
Sarcocine S. saligna 15A1S
15A2S
[575]
Sarcodine S. saligna 2 [430]
Sarcorine S. saligna
Sarsalignenone S. saligna 2 [430]
Sarsasapogenin * A. racemosus A
B
21A6S [369,576]
Schisandrin B * S. chinensis 3A4
3A5
2B6
2E1S
21A6 [577,578,579,580,581]
Shatavarin IV * A. adscendens
A. racemosus
A
B
[582]
Shogaol * A. melegueta
Z. officinale Rosc.
1
2
1A2
2C9
2C19
1A1S
1A3S
2B7S
[583,584,585,586]
Sitoindosides VII-X * W. somnifera
β-Sitosterol * A. lancea
C. pluricaulis
M. peregrina
M. pruriens
2 3A40
3A50
2C190
0 [587,588,589,590,591,592]
Spirofornabuxine B. hyrcana
Stigmasterol * A. lancea 3A4
3A5
[590,593]
Syringin * E. senticosus - - - 2 2C9
2E1
S [93,594]
Tannic acid * T. chebula 2 1A2
3A4
2B6
1
2
21A6S↓ [333,369,595,596,597,598]
Tanshinone I * S. miltiorrhiza 1A1
1A2↑↓
2C9
2E1
S↓ 1A1o
1A30
1A90
2B70
[24,599,600,601,602]
Tanshinone IIA * S. miltiorrhiza 2 1A1
1A2↑↓
3A4↑↓
2C9
2E1
1A1o
1A30
1A90
2B70
[24,599,600,601,603]
Tanshinone IIB * S.miltiorrhiza
Tenuifolin * P.tenuifolia 2 [604]
Tenuifoliside B * P. tenuifolia
Tenuifoliside C * P. tenuifolia 2E1 [527]
Theacrine * C. arabica
T. grandiflorum
Theobromine * T. cacao 1A2S
3A40
2C90
2C190
2D60
0 [218,605]
Timosaponin AIII * A. asphodeloides 2 [606]
Trigonelline * T. foenum-graecum 1A2
3A40
2B60
2C80
2C190
2D6
2E10
[607,608]
Ursolic acid * R. officinalis 2 1A2
3A4↓S
2C8
2C9↓S
2C19
2D6
A 10 21A6
21A8
21A9
22A8
[276,409,501,609,610,611,612,613]
Vaganine S. saligna
(+)-α-Viniferin * C. chamiague 3A4S S [218]
Vinpocetine * V. minor 3A4S [614]
Withaferin A * W. somnifera 1A1 [615]
Withanolide A * W. somnifera 1A1 [615]
Withanolide B * W. somnifera 1A1 [615]
Z-Ligustilide * A. sinensis 1A1
3A4
2D6
[246,616]

*—Phytochemicals found in food supplements; —target inhibition; —target induction; s—bioactive is substrate of the target; Ant—Bioactive is a target antagonist; 0—No effect; (-)—Not reported; ABC—ATP-binding cassette; ALOX5—Arachidonate 5-lipoxygenase; AMPK—AMP-activated protein kinase; BCRP—Breast cancer resistance protein; BSEP—Bile salt export pump (ABCB11); COX—Cyclooxygenase; CYP—Cytochrome P450; GLP-1—Glucagon-like peptide-1; HMGCoAR—3-hydroxy-3-methyl-glutaril-CoA reductase; MAO—Monoamine Oxidase; MATE—Multi-antimicrobial extrusion protein; MRP—Multidrug resistance-associated protein; NMDA—N-methyl-d-aspartate; OAT—Organic anion transporter; OATP—Organic-anion-transporting polypeptide; OCT—Organic cation transport; P-gP—Glycoprotein P; UGT—Uridine diphosphate-glucuronosyltransferase; PLA2G2A—Phospholipase A2 Group IIA; SLC—Solute Carriers (15A/PEPT; 22A1-3/OCT1-3; 22A4/OCTN1; 22A6,8,11/OAT1,3,4; 47A/MATE; 21A3/OATP1A2; 21A6,8/OATP1B1,3; 21A9/OATP2B1; 21A14/OATP1C1); PEPT—Peptide transporter; association of two symbols (↑↓ or ↓0 or ↑0) for the same target, refers to conflicting information reported in literature.