Abstract
Neolitsea acuminatissima (Lauraceae) is an endemic plant in Taiwan. One new carboline alkaloid, demethoxydaibucarboline A (1), two new eudesmanolide-type sesquiterpenes, methyl-neolitacumone A (2), neolitacumone E (3), and twelve known compounds (4–15) were isolated from the root of Neolitsea acuminatissima. Their structures were elucidated by spectroscopic analysis. Glucuronidation represents a major metabolism process of detoxification for carcinogens in the liver. However, intestinal bacterial β-Glucuronidase (βG) has been considered pivotal to colorectal carcinogenesis. To develop specific bacterial-βG inhibitors with no effect on human βG, methanolic extract of roots of N. acuminatissima was selected to evaluate their anti-βG activity. Among the isolates, demethoxydaibucarboline A (1) and quercetin (8) showed a strong bacterial βG inhibitory effect with an inhibition ratio of about 80%. Methylneolitacumone A (2) and epicatechin (10) exhibited a moderate or weak inhibitory effect and the enzyme activity was less than 45% and 74%, respectively. These four compounds specifically inhibit bacterial βG but not human βG. Thus, they are expected to be used for the purpose of reducing chemotherapy-induced diarrhea (CID). The results suggest that the constituents of N. acuminatissima have the potential to be used as CID relief candidates. However, further investigation is required to determine their mechanisms of action.
Highlights
The Neolitsea genus (Lauraceae) is an important component with approximately 85 species and includes evergreen shrubs and small trees in the tropical and subtropical region of Asia [1]
The methanolic extract of the root of Neolitsea acuminatissima (NARM) showed a strong inhibitory effect on E. coli βG (eβG) with an inhibition ratio of 68%, without affecting the activity of human βG. (The details are shown in the Supporting Information, Figure S1.) According to preliminary anti-eβG data, we proposed the existence of active constituents in N. acuminatissima, since the chemical constituents and biological activity of roots of this plant have seldom been investigated previously
The structure determination of three new compounds was described in the those paper
Summary
The Neolitsea genus (Lauraceae) is an important component with approximately 85 species and includes evergreen shrubs and small trees in the tropical and subtropical region of Asia [1]. Phytochemical studies of Neolitsea have revealed the presence of alkaloids, benzenoids, flavonoids, lignans, quinone, sesquiterpenes, steroids, terpenoids, and others [2,4,5,6,7,8,9,10]. This success has spurred the continuing search for more bioactive constituents of Formosan Neolitsea plants. Neolitsea acuminatissima (Hayata) Kanehira & Sasaki is an endemic species and evergreen small tree distributed in broad-leaved forests at high altitude throughout
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