Chemical composition and anticholinesterase activity of lagochilus inebrians D. Kh. Akramov,1

8-O-Acetylharpagide (6). C₁₇H₂₆O₁₁, white powder. IR spectrum (ÊBr, ν, cm^–1): 3434, 2917, 1711, 1652, 1375,
1238, 1076. ¹Í NMR spectrum (400 MHz, CD₃OD, δ, ppm, J/Hz): 6.38 (1H, d, J = 6.4, H-3), 6.07 (1H, d, J = 1.3, H-1), 4.91 (1H, dd, J = 6.4, 1.6, H-4), 4.59 (1H, d, J = 7.9, H-1′), 3.89 (1H, dd, J = 12.0, 1.7, H-6′a), 3.72 (1H, dd, J = 4.7, 1.4, H-6), 3.69 (1H, dd, J = 12.0, 5.4, H-6′b), 3.39 (1H, t, J = 8.9, H-3′), 3.31 (1H, m, H-5′), 3.30 (1H, m, H-4′) , 3.20 (1H, dd, J = 9.2, 8.0, H-2′), 2.86 (1H, br.s, H-9), 2.17 (1H, ddd, J = 15.1, 1.2, 1.2, H-7a), 2.01 (3H, s, COCH₃) , 1.95 (1H, dd, J = 15.1, 4.5, H-7b), 1.46 (3H, s, 8-CH₃). ¹³C NMR spectrum (100 MHz, CD₃OD, δ, ppm): 94.6 (C-1), 143.8 (C-3), 105.0 (C-4), 73.3 (C-5), 77.7 (C-6, 3′), 46.1 (C-7), 88.6 (C-8), 22.5 (CH₃-8), 55.6 (C-9), 99.9 (C-1′), 74.6 (C-2′), 71.7 (C-4′), 78.2 (C-5′), 62.9 (C-6′) , 22.2
(COCH₃), 173.3 (COCH₃).
Acetylcholinesterase inhibitors are used to increase acetylcholine in the brain in one method for treating Alzheimer’s disease. Several medicines used to treat Alzheimer’s disease are obtained from plants [14]. For example, galantamine was isolated from the plant Galanthus woronowii [15]. The anticholinesterase activity of the MeOH extract of L. inebrians and compounds isolated from it was studied because this plant is used in folk medicine as a sedative. The enzyme-inhibiting activity of the samples was checked using the method of Ellman et al. [16]. Galantamine was used as a standard. Screening results for 1 revealed higher [2.18 mg galantamine equivalent (GALAE)/g of sample] anticholinesterase activity than the MeOH extract (1.90 mg GALAE/g) and 5 (1.10 mg GALAE/g). Compound 4 had the lowest inhibitory activity (0.61 mg GALAE/g). Thus, 1 requires further studies for treating Alzheimer’s disease.
Asetilkolinesteraza inhibitörleri Altsgeymer kasalligini davolash uchun bir usulda miyada asetilkolinni ko'paytirish uchun ishlatiladi. Altsgeymer kasalligini davolash uchun ishlatiladigan bir qancha dorilar o'simliklardan olinadi [14]. Misol uchun, galantamin Galanthus woronowii o'simligidan ajratilgan [15]. L. inebrianlarning MeOH ekstrakti va undan ajratilgan birikmalarning antixolinesteraza faolligi oʻrganildi, chunki bu oʻsimlik xalq tabobatida tinchlantiruvchi vosita sifatida qoʻllaniladi. Namunalarning fermentni inhibe qiluvchi faolligi Ellman va boshqalar usuli yordamida tekshirildi. [16]. Galantamin standart sifatida ishlatilgan. 1 uchun skrining natijalari MeOH ekstrakti (1,90 mg GALAE/g) va 5 (1,10 mg GALAE/g) dan yuqori [2,18 mg galantamin ekvivalenti (GALAE)/g namuna] antikolinesteraza faolligini aniqladi. Murakkab 4 eng past inhibitiv faollikka ega (0,61 mg GALAE/g). Shunday qilib, 1 Altsgeymer kasalligini davolash uchun qo'shimcha tadqiqotlar talab qiladi.
ACKNOWLEDGMENT
The work was performed according to the scientific research plan of the Institute of the Chemistry of Plant Substances, AS, RUz, for basic research on the topic “Secondary Metabolites of Plants of Uzbekistan: Chemical Structure, Biological Activity and Development of Biotechnologies” (Grant VA-FA-F-7-009).