Antitubercular constituents from Premna odorata Blanco

Lirio, Stephen; Macabeo, Allan Patrick G.; Paragas, Erickson M.; Knorn, Matthias; Kohls, Paul; Franzblau, Scott G.; Wang, Yuehong; Aguinaldo, Ma. Alicia M.

doi:10.1016/j.jep.2014.04.015

Cited by 32 publications

(32 citation statements)

References 23 publications

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Section: Introductionmentioning

confidence: 99%

“…Premna odorata Blanco, Lamiaceae, popularly known as 'fragrant Premna' is a small tree native to temperate and tropical Asia, including the Philippines, and cultivated in different global locations (Lirio et al, 2014). In the Philippines, a decoction of the leaves was considered as diuretic, carminative, and febrifuge and used for vaginal irrigation, coughs, beriberi, abdominal pains, and dysentery (Lirio et al, 2014;Pinzon et al, 2011). The saturated linear fatty acid ester 1-heneicosyl formate was identified as the most potent antituberculosis ingredient of P. odorata leaves, with half maximal inhibitory concentration (IC 50 ) of 8 μg/mL (Lirio et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

“…In the Philippines, a decoction of the leaves was considered as diuretic, carminative, and febrifuge and used for vaginal irrigation, coughs, beriberi, abdominal pains, and dysentery (Lirio et al, 2014;Pinzon et al, 2011). The saturated linear fatty acid ester 1-heneicosyl formate was identified as the most potent antituberculosis ingredient of P. odorata leaves, with half maximal inhibitory concentration (IC 50 ) of 8 μg/mL (Lirio et al, 2014). Generally, P. odorata is considered among the top plant sources of acylated iridoid glycosides and rhamnopyranoses (Zhang et al, 2016;Cui, 2013;Otsuka et al, 1992;Otsuka et al, 1991;Otsuka et al, 1989).…”

Section: Introductionmentioning

confidence: 99%

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Acylated Iridoids and Rhamnopyranoses from Premna odorata (Lamiaceae) as Novel Mesenchymal–Epithelial Transition Factor Receptor Inhibitors for the Control of Breast Cancer

Elmaidomy

Mohyeldin

Ibrahim

et al. 2017

Phytotherapy Research

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Phytochemical investigation of Premna odorata Blanco, Lamiaceae, leaves afforded three new acylated iridoid glycosides 1–3, and two new acylated rhamnopyranoses 9 and 10, in addition to ten known compounds. The structures of the new compounds were confirmed using extensive 1D and 2D NMR analysis. Molecular modeling study suggested the potential of the acylated rhamnopyranoses to bind at the c-Met kinase domain. Cell free Z’-LYTE assay testing revealed the good c-Met phosphorylation inhibitory activity of 9, followed by 8, and 10, with IC50 values of 2.5, 6.9 and 12.7 µM, respectively. The MTT cell proliferation assay testing against the human c-Met-expressing highly invasive MDA-MB-23 suggested compound 9 as the most active with IC50 value of 13.3 µM. Testing of compound 9 against multiple phenotypic breast cancer cell lines including MCF-7, BT-474 cells, and MDA-MB-468 proved enhanced activity against the highly c-Met expressing triple-negative breast cancer cell lines. Acylated rhmnopyranoses are potential novel c-Met inhibitors appropriate for future optimizations to control c-Met-dependent breast malignancies.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Acylated Iridoids and Rhamnopyranoses from Premna odorata (Lamiaceae) as Novel Mesenchymal–Epithelial Transition Factor Receptor Inhibitors for the Control of Breast Cancer

Elmaidomy

Mohyeldin

Ibrahim

et al. 2017

Phytotherapy Research

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“…Researchers tested the extract, pure compounds and mixtures of these compounds. Pure substances displayed greater anti-mycobacterial potential than mixtures, which means that it is justified to use pure substances and not the whole plant or extract [9]. Another plant used in folk medicine to treat bronchitis in the Philippines is Pandanus tectorius, an evergreen tree which contains tirucallanetriterpene as the most active compound (MIC 64 µg/ml) [10].…”

Section: Extracts and Natural Substances Isolated From Plantsmentioning

confidence: 99%

Anti-tubercular substances produced by plants

Polak¹,

Kapka‐Skrzypczak²

2017

J Pre Clin Clin Res.

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Tuberculosis is one of the common causes of death worldwide, and according to the World Health Organization, in 2015, about 10.4 mln people globally is suffering from that disease. Despite great development in medicine and discovery of many antimycobacterial drugs, tuberculosis remains an unsolved problem. The populations of countries in Africa, Asia and South America have difficult access to hygiene, medical care and medicines, and they therefore resort to consulting traditional practitioners who mainly use drugs from natural sources which they prepare themselves. Plants are the biggest source of such medicines and are used as extracts, decoctions or powders, often without any evidence of their actual activity. Isolates from plants sometimes contain unknown substances or some second metabolites of microorganisms. In vitro studies have shown that some of these medicines have effective antimycobacterial properties, even against clinical, resistant strains. This is hopeful in the situation where more and more cases of tuberculosis prove to be resistant to standard drugs. Extracts of medicinal plants are often synergistic with synthetic drugs. Substances with insufficient MIC can be a basis for derivatives which have better properties. This thesis summarizes the current international knowledge of the use of plant substances used in the treatment of tuberculosis that could be potential new antituberculous drugs.

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“…These observations suggest that the protein-ligand interactions in the TBNAT-ZINC14690579 complex are mainly non-directional. For instance, one of the main elements involved in the interaction between TBNAT and ZINC14690579 derives from a cluster of non-polar residues located between Leu99-Ala100 and Ala103-Pro107 (Table 5 A potential anti-tuberculosis activity of ZINC14690579 can be extrapolated from evidence of inhibitory activity of the extract from Premna odorata Blanco (Lamiaceae), a medicinal plant traditionally used in Albay Province, in south-eastern Luzon, Philippines, against M. tuberculosis [44].…”

Section: Molecular Dynamics Simulations Of Tbnat-zinc14690579 Complexmentioning

confidence: 99%

<em>In Silico</em> Screening and Analysis of Potential Inhibitors of Arylamine N-Acetyltransferases (NATs) from the Traditional Chinese Medicine: A Study Using Free Available Tools

Azevedo¹,

Richardt²,

Oliveira³

et al. 2017

Preprint

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Arylamine N-acetyltransferases (NATs) are cytosolic enzymes, highly polymorphic, present in both eukaryotes and prokaryotes. These enzymes play an important role in the detoxification and activation of xenobiotics as well as in the synthesis of endogenous compounds. Specific NATs have been pointed out in the literature as possible therapeutic targets. In particular, the human NAT1, for the treatment of certain cancers, and the NAT from M. tuberculosis (TBNAT), for the treatment of tuberculosis. This paper describes an in silico approach to prospect and select potentially inhibitors of NAT1 and TBNAT from the Traditional Chinese Medicine (TCM) using free available tools. A library with ligands from TCM was previously screened in order to select only compounds with optimal pharmacological properties. The affinity of the selected ligands with respect to NAT enzymes was then evaluated by virtual screening (VS). Subsequently, the complexes with the best ligands were submitted to molecular dynamics (MD) simulations aiming to obtain better quality information on affinity and selectivity. The results for one specific ligand, ZINC14690579, indicated its potential for affinity and selectivity. ZINC14690579 structure may represent the discovery of a new scaffold for future development of NAT inhibitors.

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Antitubercular constituents from Premna odorata Blanco

Cited by 32 publications

References 23 publications

Acylated Iridoids and Rhamnopyranoses from Premna odorata (Lamiaceae) as Novel Mesenchymal–Epithelial Transition Factor Receptor Inhibitors for the Control of Breast Cancer

Acylated Iridoids and Rhamnopyranoses from Premna odorata (Lamiaceae) as Novel Mesenchymal–Epithelial Transition Factor Receptor Inhibitors for the Control of Breast Cancer

Anti-tubercular substances produced by plants

<em>In Silico</em> Screening and Analysis of Potential Inhibitors of Arylamine N-Acetyltransferases (NATs) from the Traditional Chinese Medicine: A Study Using Free Available Tools

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