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. 2021 Feb 25;11(3):350. doi: 10.3390/biom11030350

Table 1.

Some Sesquiterpenoids that haveanticholinesterase inhibitory activity.

Name of Plant Part Used (Family) Solvent/Method Used for Extraction Extract/Volatile oil/Phytoconstituents Acetyl-Cholinesterase Inhibitory/Anti-Alzheimer Potential Ref.
Lycopodiastrum casuarinoides Whole plants
(Lycopodiaceae)
EtOH (75%) 7, 9 -diene -1,4 -epoxy-2 -hydroxy -10 -carboxylic acid [13] Potential inhibitory effects against AChE and BuChE with an IC50 = 9 ± 1 μM and 9 ± 1 μM respectively [98]
Lycium europaeum Linn. Roots
and leaves
(Solanaceae)
Ethanol Ethanolic fraction Ethanolic fraction of leaves (at 15 mg/kg) exhibited effect on learning and memory of experimental animals with IC50 = 76 ± 2 mg/mL [99]
Aquilaria or Gyrinops Roots and resinous heartwood
(Thymelaeaceae)
95% EtOH 2-oxoguaia-1(10),3,5,7(11), 8-pentaen-12,8-olide (14)
(Sesquiterpenoids)
4β,7α-H-eremophil-9(10)-ene-12,13-diol (15)
(Eremophilane- sesquiterpenoid)
4β,5α,7α,8α-H-3β-hydroxy-1(10)-ene-8,12-epoxy-guaia-12-one (16)
(−)Gweicurculactone (17)
(Guaiane-sesquiterpenoid)
The isolated compounds showed the AChE inhibitory activity at 50 μg/mL ((IC50)
IC50 (14) = 226 μM
IC50 (15) = 140 μM
IC50 (16) = 141 μM
IC50 (17) = 202 μM
Tacrine ( + ve control) =
65 ± 1 μg/mL
[100]
Valeriana jatamansi Jones Roots and rhizomes (Valerianaceae) EtOH (95%) Valeriananoids D (18)
Valeriananoids E (19)
At the conc. of 50 μM showed AChE inhibition potential activity [101]
Aquilaria sinensis (Lour.) (Thymelaeaceae) EtOH (95%) 3-oxo-7-hydroxyl holosericin A (20)
1,5;8,12-diepoxy-guaia-12-one (21)
8αβ)-octahydro-7-[1-(hydroxymethyl (22)
7α H- ethenyl]-1,8α-dimethyl naphthalen-4α(2H)-o (23)
Neopetasane (24)
Moderate inhibitory activities against Acetylcholinesterase (AChE) at 50 µg/mL,
IC50 (20) = 75 μM
IC50 (21) = 53 μM
IC50 (22) = 71 μM
IC50 (23) = 87 μM
IC50 (24) = 324 μM
[102]
Rhodomyrtus tomentosa leaves and stems
(Myrtaceae)
Petroleum ether (PE) extract (Triketone-sesquiterpene meroterpenoids) AChE inhibition rate is 81% at 500 μg/mL) [103]
Nelumbo nucifera Seeds (Nelumbonaceae) essential oil (EO), crude extract, and subsequent fractions Essential oil mainly comprised of oxygenated mono and sesquiterpenes The ethyl acetate fraction and EO caused significant inhibition of acetyl-cholinesterase and butyryl-cholinesterase with IC50 = 70 ± 1, 64 ± 1 and 75 ± 0.3, 58 ± 0.2, respectively in a dose-dependent manner.
EO was found to be non-competitive inhibitor of AChE.
[104]
Asteriscus maritimus (Linn.) Less Different parts of the plant (Asteraceae) Hydrodistillation Oxygenated sesquiterpenes of Essential oil Among the essential oils obtained from flowers, leaves, and stems, the flower oil was found to exhibit the highest anti-acetylcholinesterase activity (IC50 = 95 µg/mL) [105]
Myrciaria floribunda (H. West ex Willd.) Essential oil of fruit peel
(Myrtaceae)
Hydrodistillation
method
Essential oil with different sesquiterpenes Essential oil exhibited the AChE inhibitory potential with IC50 = (0.08 μg/mL and 23 μg/mL).
Neostigmine (as the standard used) had an IC50 of 23 μg/mL and 6 μg/mL).
[97]
Nigrospora oryzae and
Irpex lacteus
(Fungus on plant )
Culture Acetone Tremulanesesquiterpenes AChE inhibitory potential concentration of 50 μM. [106]
Curry Leaf Murraya koenigii
(Rutaceae)
Hexane and methanol Essential oil Inhibitory activities of active compounds of curry leaves against β-secretase were found and hence reported to be helpful in
preventing dementia (AD).
methanolic extract (70%) also showed weak inhibitory activity at 500 μg/mL against AChE
[107]
Teucrium persicum Boiss Aerial parts (Labiatae) Methanol (85%) Guaiasistanol (25)
(Guaianesesquiterpenoid)
Moderate inhibition of AChE (28%) by the isolated compound. [108]
Daphne holosericea (Diels) Hamaya Dry stems
(Thymelaeaceae)
Extracted with EtOH (95%) under reflux three times Holosericin B (26)
(Guaiane Sesquiterpenoids)
The isolated compound showed a moderateAChE Inhibitory Activity with 31% inhibition. [109]
Aquilaria sinensis (Lour.) Gilg Heartwood (Thymelaeaceae) Refluxed with Ethanol (95%) Extract EtOAc extract showed weak AChE inhibitory activity [110]
Homalomena sagittifolia Rhizomes
(Araceae)
Macerated with aqueous methanol 1α,4β,7β- eudesmanetriol (27)
1β, 4β, 7β-eudesmanetriol (28)
(Sesquiterpenoids)
Inhibition of acetylcholinesterase with IC50 (I) = 26 ± 4; (II) = 250 ± 8 μM [111]
Valeriana officinalis Roots
(Caprifoliaceae)
EtOH (95%) Spatulenol (29)
(Sesquiterpenoids)
AChE was inhibited at 100 mM (49%) [112]
Marsupella alpine
(Chinese liverwort)
Whole plants
(Gymnomitriaceae)
95% EtOH (95%) Marsupellin A (30)
Marsupellin B (31)
(ent-Longipinane-Type Sesquiterpenoids)
A bioautographic TLC assayforAChE inhibition was performed and compound showed moderate inhibition at 5 μM (28% and 26% respectively). [113]
Santalum album Heartwood
(Santalaceae)
Steam distillation α-santalol (32),
Sandalwood oil (rich in sesquiterpenoid alcohols)
the major constituent of the oil
TLC-bioautographic and colorimetric methods are used. Essential oil is found to be a potent inhibitor of tyrosinase IC50 = 171 µg/mL) and cholinesterase IC50 = 5–58 µg/mL.
For α-santalol, AChE Inhibition Zone (mm2) and BChE Inhibition Zone (mm2) were reported as 326 ± 19 and 425 ± 27 respectively.
[114]
Hedychium gardnerianum Sheppard ex Ker-Gawl Leaf essential oil (Zingiberaceae) Hydrodistillation Sesquiterpene hydrocarbons (47.8 to 52.7%) and oxygenated sesquiterpenes (15.2 to 16.3%) are main constituents of oil Microplate Assay was performed and the strongest inhibition against AChE was displayed by the sample collected from Furnas (FU) at IC50 = 1 mg/mL. [115]