. 2021 Sep 3;26(17):5369. doi: 10.3390/molecules26175369

Table 1.

Bioactive compounds isolated from Polyalthia plants.

Category	Name of Compound	Pharmacological Activities Described in References	Concentration	In Vitro/ In Vivo Model
			IC₅₀/EC₅₀/
			Minimal Inhibitory Concentration (MIC)
Aporphine	(−)-Anonaine (1)	Cytotoxicity [14]	8.6–28.9 μM	AGS, DLD1, HA59T, and HepG2
	Bidebiline E (2)	Anti-bacterial [19]	6.25 μg/mL	Mycobacterium tuberculosis
	Bidebiline E (2)	Inhibition of wnt protein [73]	20.2 μM	SW480
Proaporphine	(+)-Stepharine (3)	Cytotoxicity [27]	9.4–9.9 μg/mL	MCF-7, MDA-MB-231
Oxoaporphine	Liriodenine (4)	Cytotoxicity [27,31,74]	4.46–10.28 μg/mL	MCF-7, MDA-MB-231
	Liriodenine (4)	Cytotoxicity [27,31,74]	0.57–2.33 μg/mL	KB, A549, HCT-8, P-388, and L-1210,
	Lanuginosine (oxoxylopine) (5)	Cytotoxicity [74]	1 μg/mL	Unavalible
	Oxostephanosine (6)	Cytotoxicity [74]	1 μg/mL	Unavalible
	Oxostephanine (7)	Cytotoxicity [39]	1.47–1.73 μg/mL [39]	SPC-A-1 and BEL-7402
	Lysicamine (8)	Cytotoxicity [27]	8.94–16.75 μg/mL	MCF-7, MDA-MB-231
Azafluorene	5-Hydroxy-6-methoxyonychine (isoursuline) (9)	Cytotoxicity [14]	21.7 μg/mL	HA59T
	6,8-Dihydroxy-7-methoxy-1-methyl-azafluorenone (10)	Cytotoxicity [75]	2.64–3.58 μg/mL	A549, GLC4, and adrinamycin-resistance GLC4
		Apoptosis [76]	20–55 μM	HL-60, U937, MOLT-4, MDA-MB-231, and HepG2
		anti-bacterial [75]	0.78 μg/mL	M. tuberculosis
	Polylongine (11)	Cytotoxicity [27]	9.94–10.41 μg/mL	MCF-7 and MDA-MB-231
Anthraquinones	Marcanine A (12)	Cytotoxicity [77]	1.53–11.78 μM	BEL-7402, K562, SPCA-1, and SGC-7409
Acetogenin	Debilisone B (13)	Anti-bacterial [78]	25 μg/mL	M. tuberculosis
	Debilisone C (14)	Anti-bacterial [78]	12.5 μg/mL	Same as above
	Debilisone E (15)	Anti-bacterial [78,79]	25 μg/mL	M. tuberculosis
		Anti-bacterial [78,79]	64 μg/mL	Morexella catarrhalis
		Cytotoxicity [79]	18.4–40.3 μg/mL	HepG2, A549, HCC-S102, HL-60, and P-388
Prenylated Benzopyran	Polycerasoidol (16)	Anti-inflammatory [28]	4.9 μΜ	Inhibition of mononuclear leukocyte adhesion to endothelium
	1-(2-furyl)pentacosa-16,18-diyne (17)	Anti-viral [80]	43.3 μg/mL	ΔTat/RevMC99 syncytium assay for human immunodeficiency virus (HIV)
	23-(2-furyl)tricosa-5,7-diynoic acid (18)	Anti-viral [80]	8.9 μg/mL	Same as above
2-substituted furans	19-(2-furyl)nonadeca-5,7-diynoic acid (19)	Anti-viral [22]	47 μg/mL	Anti-viral assay against herpes simplex type 1 (HSV-1)
	19-(2-furyl)nonadeca-5-ynoic acid (20)	Anti-viral [22]	19.4 μg/mL	Same as above
	21-(2-furyl)heneicosa-14,16-diyne-1-ol (21)	Cytotoxicity [22]	12.4 μg/mL	NCI-H187
8-Oxoprotoberberine	pendulamine A (22)	Anti-bacterial [18]	0.02 μg/mL	Gram-positive bacteria
			0.02 μg/mL	Corynebacterium hoffmanii and Micrococcus lysodicklycus
			0.2 μg/mL	Staphylococcus aureus
			2 μg/mL	Bacillus subtillis
			12.5 μg/mL	Streptococcus viridans
			20 μg/mL	S. pyogenes
			0.02 μg/mL	Gram-negative bacteria
			0.02 μg/mL	Salmonella typhi
			0.2 μg/mL	S. paratyphi A
			2 μg/mL	Klebsiella pneumoniae and Pseudomonas aeruginosa
	pendulamine B (23)	Anti-bacterial [18]	0.02 μg/mL	Gram-positive bacteria
			0.02 μg/mL	C. hoffmanii, S. viridans, and M. lysodicklycus
			0.2 μg/mL	S. aureus,
			2 μg/mL	S.s faecalis
			20 μg/mL	S. pyogenes
			0.2 μg/mL	Gram-negative bacteria
			0.2 μg/mL	S. paratyphi A and S. typhi
			2 μg/mL	K. pneumoniae
	(−)-8-oxo-2,9,10-Trihydroxy-3-methoxyberberine	Cytotoxicity [81]	24.1 μM	MCF-7
	(consanguine B) (24)	Cytotoxicity [81]	33.5 μM	HeLa
Tetrahydroprotoberberine	(−)-stepholidine (25)	Cytotoxicity [27]	16.56 μg/mL	MCF-7
Amides	N-trans-Feruloyltyramine (26)	Cytotoxicity [27]	21.17-25.54 μg/mL	MCF-7, MDA-MB-231, HepG2, Hep3B
Amides	N-trans-p-Coumaroyltyramine (27)	Cytotoxicity [27]	17.35 μg/mL	MCF-7
Sesquiterpenes	Polyalone A (28)	Cytotoxicity [82]	18.9–24.8 μΜ	HeLa, A549, MCF-7, and HL-60
	9-Ketocyclocolorenone (29)	Cytotoxicity [82]	20.5–26.2 μΜ	Same as above
	Blumenol A(30)	Cytotoxicity [82]	24.5–28.2 μΜ	Same as above
	(−)-Methyl dihydrophaseate (31)	Cytotoxicity [82]	22.6–27.1 μΜ	Same as above
	Bis-enone (32)	Cytotoxicity [82]	25.6–30.1 μΜ	Same as above
Diterpenoids	Longimide A (33)	Cytotoxicity [83]	4.12–10.13 μg/mL	KB, MCF-7, A549, and C33A
	Longimide A (33)	Cytotoxicity [83]	44.7 μg/mL	NIH3T3
	labd-13E-en-8-ol-15-oic acid (34)	Cytotoxicity [27]	15.4–18.33 μg/mL	HepG2 and Hep3B
	1-naphthaleneacetic-7-oxo-1,2,3,4,4a,7,8,8a-octahydro1,2,4a,5-tetramethyl acid (35)	Cytotoxicity [84]	50 μM	HL-60
Clerodane diterpenoids	16-Hydroxycleroda-3,13Z-dien-15,16-olide (36)	Cytotoxicity, apoptosis, anti-cancer [36,43]	Details are in Table 2	786-O, A498, HL-60, T24, C6, N18, Caco-2, K562, MCF-7, MDA-MB-231, GBM8401,
		Cytotoxicity, apoptosis, anti-cancer [36,43]	Details are in Table 2	SW620, MOLT-4, HepG2, Hep3B, and A549
		Anti-inflammatory [27,60,72]	3.05 ± 1.13 μg/mL	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils.
			1–10 μM	LPS-treated RAW264.7 cells
			1.6–6.4 mg/kg	irritable bowel disease in mouse model (ADM/DSS-induced colitis)
		Anti-bacterial [85]		Gram-negative bacteria
			125 μg/mL	S. typhi
			250 μg/mL	P. aeruginosa, K. ozaenae, and Proteus mirabilis
				Gram-positive bacteria
			7.8 μg/mL	S. aureus
			125 μg/mL	S. pyogenes
			500 μg/mL	C. hoffmanii
		Anti-fungal [85]	62.5 μg/mL	Aspergillus niger and Trichophyton metagrophyte
		Anti-fungal [85]	250 μg/mL	Candida albicans
	16-Hydroxy-cleroda-3,13(14)Z-dien-15,16-olide-2-one (37)	Anti-bacterial [85]		Gram-positive bacteria
		Anti-bacterial [85]	15.6 μg/mL	B. subtilis
		Anti-inflammatory [27]	62.5 μg/mL	C. diphtheriae, C. xerosis, and S. aureus
			500 μg/mL	C. hoffmanii, and S. pyogenes
			7.96 ± 1.78 μg/mL	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils
	16α-Hydroxycleroda-3,13Z-dien-15,16-olide (38)	Cytotoxicity [14,33,84,86,87,88],	0.5 μg/mL	P-388
			1.2 μg/mL	Mel2
			3.4–8.7 μg/mL	A431, BC1, Col2, HT, KB, drug-resistance KB, LNCaP, Lu1, and ZR75-1
			23.6–26.9 μM	AGS, HA59T
			21.28–34.89 μM	HT-29
			21.28–34.89 μM	A549, MCF-7, HL-60, SMMC-7721, and SW-480
		Anti-bacterial [20,48,49,89]		Gram-positive bacteria
			6.25 μg/mL	S. aureus, Sporothrix schenckii, and Arthrobacter citreus
			1.56 μg/mL	B. subtillis, B. polymyxa, and B. pumilus
			3.12 μg/mL	B. cereus, B. licheniformis, and Clostridium sp.
				Gram-negative bacteria
			0.78 μg/mL	E. coli, P. aeryginosa, and S. typhimurium
			1.56 μg/mL	K. aerogenes and Sarcina lutea
			3.12 μg/mL	P. putida and Nocardia sp.
		Anti-inflammatory [29]	9.46 ± 0.33 nM	COX1 inhibitory assay
			10.34 ± 0.26 nM	COX2 inhibitory assay
			14.38 ± 0.32 nM	5-LOX inhibitory assay
	16-Hydroxycleroda-4(18),13 -dien-15,16-olide (39)	Cytotoxicity [27]	1.97–10.43 μg/mL	MCF-7, MDA-MB-231, HepG2, and Hep3B
		Anti-inflammatory [29]	11.85 ± 0.19 nM	COX1 inhibitory assay
			8.49 ± 0.55 nM	COX2 inhibitory assay
			14.38 ± 0.32 nM	5-LOX inhibitory assay
	Kolavenic acid (40)	cytotoxicity [87]	1.39–3.34 μg/mL	A549, MCF-7, and HT-29
		Anti-bacterial [85]	31.25 μg/mL	B. subtilis and C. diphtheriae
		Anti-bacterial [85]	125 μg/mL	C. hoffmanii and C. xerosis
	16-Oxocleroda-3,13E-dien-15-oic acid (41)	Cytotoxicity [10]	3.1–3.7 μM	MCF-7 and A549
		anti-bacterial [85]		Gram-negative bacteria
			500 μg/mL	P. aeruginosa, S. typhi, K. ozaenae, K. aerogenes, E. coli, sarcina lutea, Nocardia sp., and P. mirabilis
				Gram-positive bacteria
			500 μg/mL	A. citreus, B. cereus, B. licheniformis, B. polymyxa, B. pumilus, B. subtilis, Clostridium sp. S. pyogenes, C. hoffmanii, and S. aureus
		Anti-fungal [85]	62.5 μg/mL	Trichonphyton mentagrophyte
			125 μg/mL	A. niger
			250 μg/mL	C. albicans
	16-Oxocleroda-3,13Z-dien-15-oic acid (polyalthialdoic acid) (42)	Cytotoxicity [87]	0.552–0.753 μg/mL	A549, MCF-7, and HT-29
	16-Oxocelroda-3,13(14)E-dien-15-oic acid methyl ester (43)	Anti-inflammatory [27]	0.6 ± 0.09 μg/mL	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils
	3β,16α-dihydroxycleroda-4(18),13(14)Z-dien-15,16-olide (44)	Cytotoxicity [33]	2.2–16μg/mL	P-388, BC1, Col2, LNCaP, Lu1, ZR75-1
		Cytotoxicity [33]	12–16 μg/mL	Mel2, A431, HT, and KB
		Cytotoxicity [90]	10.474–24.096 μg/mL	KB, C33A, PA1, MCF-7
		Cytotoxicity [90]	18.564 μg/mL	Vero
		anti-bacterial [85]		Gram-positive bacteria
			62.5 μg/mL	C. diphtheriae, C. xerosis, and S. pyogenes
			125 μg/mL	S. faecalis and C. hoffmanii
			250 μg/mL	S. saprophyticus
			500 μg/mL	B. subtilis
	(−)-3α,16α-dihydroxycleroda-4(18),13(14)Z-dien-15,16-olide (45)	Cytotoxicity [90]	13.415–29.778 μg/mL	KB, C33A, PA1, and MCF-7
		Cytotoxicity [90]	20.345 μg/mL	Vero
	Anti-inflammatory [29]	10.85 ± 0.17 nM	COX1 inhibitory assay
		12.82 ± 0.21 nM	COX2 inhibitory assay
		16.94 ± 0.56 nM	5-LOX inhibitory assay
4β,16α-dihydroxycleroda-13(14)Z-en-15,16-olide (46)	Cytotoxicity [33]	5.1–16 μM	A431. BC1, Col2, HT, LNCaP, Lu1, Mel2, P-388, ZR75-1
16β-Hydroxycleroda-3,13(14)Z-dien-15,16-olide (47)	Anti-oxidant [57]	23.5 μg/mL	DPPH assay
(4→2)-abeo-16(R&S)-2,13Z-clerodadien-15,16-olide-3-al (48)	Cytotoxicity [27]	2.36–11.89 μg/mL	MCF-7, MDA-MB-231, HepG2, and Hep3B
	Anti-bacterial [85]		Gram-positive bacteria
		31.25 μg/mL	B. subtilis
		125 μg/mL	C. hoffmanii, C. xerosis, S. saprophyticus, S. faecalis, and S. pyogenes
	Anti-inflammatory [27]	4.32 ± 0.59 μg/mL	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils
(4→2)-abeo-2,13-diformyl-cleroda-2,12E-dien-14-oic acid (49)	Cytotoxicity [91]	37.35–39.31 μM	HeLa, MCF-7, and A549
16,16-dimethoxy-cleroda-3,13Z-dien-15-oic acid (50)	Cytotoxicity [32]	22.43 μM	SMMC-7721
Polylauiester A (51)	Cytotoxicity [91]	33.21–35.65 μM	HeLa, MCF-7, and A549
Polylauiamide B (52)	Cytotoxicity [91]	28.09–29.25 μM	Same as above
Polylauiamide C (53)	Cytotoxicity [91]	25.01–30.30 μM	Same as above
Polylauiamide D (54)	Cytotoxicity [91]	26.73–28.88 μM	Same as above
solidagonal acid (55)	Cytotoxicity [27]	14.67–18.12 μg/mL	MCF-7 and MDA-MB-231
	Anti-bacterial [85]		Gram-positive bacteria
	Anti-bacterial [85]	31.25 μg/mL	B. subtilis, C. hoffmanii, and S. saprophyticus
ENT-kaur-16-en-19-oic acid (56)	Anti-viral [92]	13.7 μg/mL	Anti-syncytium assay against HIV
Triterpene	Suberosol (57)	Anti-viral [23]	3 μg/mL	Inhibition of HIV replication in H9 lymphocytes
		Cytotoxicity [93]	34.30 μg/mL	SPC-A-1
			15.02 μg/mL	SGC-7901
	24-Methylenecycloartane-3β, 16β, 23β-triol (longitriol) (58)	Cytotoxicity [83]	10.03–30.88 μg/mL	KB, MCF-7, A549, C33A
		Cytotoxicity [94]	19.3–23 μM	MDA-MB-231 and SF-268
		Cytotoxicity [94]	40.3 μM	MRC-5
		Apoptosis [94]	40 μM	NCI-H460
Triterpenoids	Friedelin (59)	Anti-bacterial [95]	5 μg/mL	E. coli and M. tetragenus
Triterpenoids	Stigmast-4-ene-6α-ol-3-one (60)	Anti-bacterial [95]	5 μg/mL	Same as above
Flavonoids	Quercetin (61)	Anti-oxidant [54]	1.56 μg/mL	Trolox equivalent antioxidant capacity (TEAC) assay
	Quercetin-3-O-β-glucopyranoside (62)	Anti-oxidant [54]	1.56 μg/mL	TEAC assay
	Rutin (63)	Anti-oxidant [54]	1.56 μg/mL	TEAC assay
Others	Crassalactones A (64)	Cytotoxicity [96]	0.18–1.9 μg/mL	P-388, KB, Col-2, BCA-1, Lu-1, and ASK
	Crassalactone B (65)	Cytotoxicity [96]	3.8 μg/mL	P-388
	Crassalactone D (66)	Cytotoxicity [96]	1.1–4 μg/mL	P-388, KB, Col-2, BCA-1, and ASK
	Aristolactam AII (67)	Cytotoxicity [96]	2.7 μg/mL	P-388
	(+)-Tricinnamate (68)	Cytotoxicity [96]	3.1 μg/mL	P-388
	(+)-Rumphiin (69)	Cytotoxicity [39]	63.2–187.6 μg/mL	SPC-A-1 and K562
	α-Spinasterol (70)	Cytotoxicity [97]	60.07 ± 7.10 nM/ml	Caco-2
	Dehydrogoniothalamin (71)	Anti-inflammatory [65]	11.6 ± 1.2 μM	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils
	Dehydrogoniothalamin (71)	Anti-inflammatory [65]	6.8 ± 0.9 μM	inhibition of elastase release by human neutrophils
	Goniothalamin (72)	Anti-inflammatory [65]	8.3 ± 1.4 μM	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils
	Goniothalamin (72)	Anti-inflammatory [65]	15.4 ± 1.1 μM	inhibition of elastase release by human neutrophils
	(−)-5-Hydroxy-goniothalamin (71)	Cytotoxicity [65]	7.9 μM	A549
		Anti-inflammatory [65]	8.1 ± 2.3 μM	Inhibition of fMLP/CB-induced superoxide anion production by human neutrophils
		Anti-inflammatory [65]	14.6 ± 0.7 μM	Inhibition of elastase release by human neutrophils
	Octadeca-9,11,13-triynoic acid (72)	Anti-bacterial [19]	6.25 μg/mL	M. tuberculosis
	Octadeca-9,11,13-triynoic acid (72)	Cytotoxicity [19]	13 μg/mL	BC1
	α-Humulene (73)	Anti-bacterial [19]	6.25 μg/mL	M. tuberculosis
	F2 peptide	Apoptosis [98]	30 μg/mL	A549 and HeLa

Index of cell lines. Lung cancer: A549, GLC4, NCI-H460, NCI-H187, Lu-1, and SPCA-1. Gastric cancer: AGS, SGC-7409, and SGC-7901. Liver cancer: HA59T, HepG, Hep3B, BEL-7402, HCC-S102, and SMMC-7721. Breast cancer: BC1, BCA-1, MCF-7, MDA-MB-231, and ZR75-1. Uterine and cervix cancer: C33A and HeLa. Skin cancer: Mel2 and A431. Blood cancer: HL-60, K562, MOLT-4, and U937. Lympoma: P-388 and HT. Head and neck cancer: KB. Urothelial cancer: 786-O, A498, and T24. Prostate cancer: LNCaP. Brain cancer: ASK, SF-268, GBM8401, C6, and N18. Colon cancer: Col-2, HT-29, SW-480, Caco-2, DLD1, and SW620. Normal immortalized cell lines: NIH3T3, RAW264.7, Vero, and MRC-5.