Reynosin and santamarine: two sesquiterpene lactones fromAmbrosia confertiflorawith bactericidal activity against clinical strains ofMycobacterium tuberculosis

Abstract

Materials and methods:The dichloromethanic extract of aerial parts of A. confertiflora was separated using chromatography columns. Mycobactericidal activity of the isolated compounds was evaluated using the Alamar Blue bioassay (128-16 lg/mL, 7 days). Cytotoxicity was tested against normal cell line L929 using the MTT ([3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium]) assay (100-3.125 lg/mL, 48 h). , 104-2010, 63-2009, 366-2009 and 430-2010 Mtb strains, respectively. Santamarine had MBCs of 128 lg/mL against the H3Rv and 104-2010 Mtb strains and MICs of 128 lg/mL against the H37Rv, 366-2009 and 104-2010 Mtb strains. We also isolated 1,10-epoxyparthenolide but only showed mycobacteriostatic activity (MIC 128 lg/mL) against the Mtb strain. Compounds were tested against the L929 cell line and the calculated selectivity index was <1. Discussion and conclusions: This is the first report of the mycobactericidal activity of these compounds against clinical Mtb strains. It is also the first report of the isolation of 1,10-epoxyparthenolide from A. confertiflora. The anti-mycobacterial activity of A. confertiflora was attributed to the SQLs identified.ARTICLE HISTORY

Santamarine Inhibits NF-κB Activation and Induces Mitochondrial Apoptosis in A549 Lung Adenocarcinoma Cells via Oxidative Stress

“…STM is a sesquiterpene lactone compound present in various plant species such as Inula helenium , Inula japonica [ 12 ], Magnolia grandiflora L. [ 13 ], Ambrosia confertiflora [ 14 ], and Saussurea lappa [ 15 ]. It has been reported to exhibit mycobactericidal effects [ 14 ]. It has also been shown to inhibit the growth of human gynecologic cancer cells [ 12 ].…”

SANTAMARINE: Mechanistic studies on multiple diseases

“…The effects of STM on Mtb were investigated in six clinical strains. Available data showed that STM had minimal bactericidal concentration (MBCs) of 128 µg/ml against H3Rv and 104‐2010 Mtb strains and minimal inhibitory concentration (MICs) of 128µg/ml against H37Rv, 366‐2009, and 104‐2010 Mtb strains (Coronado‐Aceves et al, ) (Figure and Table ).…”

“…STM could be isolated from the fruits, flowers, and leaves of Laurus nobilis L (Barla, Topçu, Öksüz, Tümen, & Kingston, ; Fang et al, ), flowers of Tanacetum vulgare ssp. Siculum (Rosselli et al, ) , rhizomes of Costus speciosus (Al‐Attas, El‐Shaer, Mohamed, Ibrahim, & Esmat, ), aerial parts of Ambrosia confertiflora (Coronado‐Aceves et al, ), roots of I. helenium (Li et al, ), and roots of Saussurea lappa (Choi et al, ) (Figure ). Various studies reported the effects of STM, including anticancer (Ma, Chong, Li, Cheung, & Tattersall, ; Mehmood, Maryam, Tian, Khan, & Ma, ; Wu, Zhu, Yan, Khan, & Yu, ), anti‐inflammatory (Matsuda et al, ), antibacterial (Sun, Syu, Don, Lu, & Lee, ), and anti‐ethanol activities (Matsuda, Shimoda, Uemura, & Yoshikawa, ).…”

Acyl Derivatives of Eudesmanolides To Boost their Bioactivity: An Explanation of Behavior in the Cell Membrane Using a Molecular Dynamics Approach

“…Reynosin (2) and santamarine (3; Figure 1) have shown strong bactericidal activity against Mycobacterium tuberculosis, with a minimal inhibitory concentration of 64 μg/mL. [2] In addition, reynosin also suppresses ROS production and reduces COX-2 levels via the NF-KB pathway. [3,4] In vivo studies have recently been carried out on this eudesmanolide, with hepatoprotective effects observed in mouse liver upon exposure to thioacetamide in order to generate apoptosis.…”