scholarly journals Estimation of Costunolide and Dehydrocostus Lactone in Saussurea lappa and its Polyherbal Formulations followed by their Stability Studies Using HPLC-DAD

2015 ◽  
Vol 11 (41) ◽  
pp. 180 ◽  
Author(s):  
KSuresh Babu ◽  
PR Rao Vadaparthi ◽  
K Kumar ◽  
VankaUma Maheswara Sarma ◽  
QaziAltaf Hussain
Planta Medica ◽  
2017 ◽  
Vol 84 (05) ◽  
pp. 329-335 ◽  
Author(s):  
Siwattra Choodej ◽  
Khanitha Pudhom ◽  
Tohru Mitsunaga

We investigated the tumor necrosis factor-alpha (TNF-α) inhibitory activity of sesquiterpenes from Saussurea lappa root extracts. According to the hexane and EtOAc extracts showing significant activity with IC50 values of 0.5 and 1.0 µg/mL, respectively, chromatographic fractionation of the extracts was performed and led to the isolation of 10 sesquiterpenes (1–10). Costunolide (1), a major compound, and dehydrocostus lactone (4) exhibited high efficiency in decreasing TNF-α levels, with IC50 values of 2.05 and 2.06 µM, respectively. In addition, sesquiterpene analogues were synthesized to establish their structure-activity relationship (SAR) profile. Among the semi-synthetic analogues, compounds 6a and 16 showed the most potent activity with IC50 values of 1.84 and 1.97 µM, respectively. More importantly, compound 6a showed less toxicity than costunolide and 16. These results provided the first SAR profile of sesquiterpene lactones and indicated that the α-methylene-γ-lactone moiety plays a crucial role in TNF-α inhibition. Additionally, the epoxide derivative 6a might represent a lead compound for further anti-TNF-α therapies, owing to its potent activity and reduced toxicity.


2010 ◽  
Vol 5 (10) ◽  
pp. 1934578X1000501 ◽  
Author(s):  
Jin-ao Duan ◽  
Pengfei Hou ◽  
Yuping Tang ◽  
Pei Liu ◽  
Shulan Su ◽  
...  

Five sesquiterpenes, dehydrocostus lactone (1), santamarine (5), β-cyclocostunolide (6), 4α-hydroxy-4β-methyldihydrocostol (7) and 10α-hydroxyl-artemisinic acid (9), along with four other compounds, β-sitosterol (2), daucosterol (3), 5-hydroxy-methyl-furaldehyde (4), and trans-syingin (8), were isolated and identified from the roots of Saussurea lappa (Compositae). Based on previous reports and our study, sesquiterpene derivatives are common and characteristic constituents of the genus Saussurea. Among the nine compounds obtained, 9 is a new sesquiterpene. It is an artemisinic acid derivative, whose structural skeleton has not been reported for Saussurea species before, but artemisinic acid is a common compound in another Compositae species, Artemisia annua. Dehydrocostus lactone (1) is present in high-content and is a possible bioprecursor of 10α-hydroxyartemisinic acid (9).


2008 ◽  
Vol 46 (12) ◽  
pp. 3651-3658 ◽  
Author(s):  
Eun Ji Kim ◽  
Soon Sung Lim ◽  
So Young Park ◽  
Hyun-Kyung Shin ◽  
Jong-Sang Kim ◽  
...  

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2506 ◽  
Author(s):  
Jingkun Liu ◽  
Min Xie ◽  
Xiuzhuang Li ◽  
Hui Jin ◽  
Xiaoyan Yang ◽  
...  

Allelochemicals are the media of allelopathy and form the chemical bases of plant-environment interactions. To determine true allelochemicals and their autotoxic effects, seven compounds were isolated and identified from in-situ sampled rhizosphere soil of cultivated Saussurea lappa. Of these; costunolide (2), dehydrocostus lactone (3) and scopoletin (4) showed significant inhibition on seedling growth in a concentration-dependent manner. Detection and observation demonstrated that the antioxidase system was found to be affected by these chemicals, resulting in the accumulation of ROS and membrane damage. To investigate their release ways, the compounds were traced back and volumes quantified in rhizosphere soil and plant tissues. This work made clear the chemical bases and their physiological effects on the plants. These chemicals were found to be the secondary metabolites of the plants and included in the rhizosphere soil. The findings identified a potential pathway of plant-plant interactions, which provided theoretical basis to overcoming replanting problems. This research was also useful for exploring ecological effects of allelochemicals in green agriculture.


2010 ◽  
Vol 30 (4) ◽  
pp. 421-428 ◽  
Author(s):  
Kwang-Min Cho ◽  
Xue-Hua An ◽  
Jae-Kwan Chon ◽  
Hyo-Sun Kim ◽  
Jae-Chul Chun

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