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Keywords = Neurolaena lobata

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17 pages, 1975 KiB  
Article
In Vitro Inhibitory Activities against α-Glucosidase, α-Amylase, and Pancreatic Lipase of Medicinal Plants Commonly Used in Chocó (Colombia) for Type 2 Diabetes and Obesity Treatment
by Kevin P. Lévuok-Mena, Oscar J. Patiño-Ladino and Juliet A. Prieto-Rodríguez
Sci. Pharm. 2023, 91(4), 49; https://doi.org/10.3390/scipharm91040049 - 18 Oct 2023
Cited by 6 | Viewed by 4055
Abstract
Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants [...] Read more.
Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants on pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) were assessed, and the most promising species were selected to isolate and identify bioactive components. Artocarpus altilis, Momordica balsamina, Bauhinia picta, Neurolaena lobata, and Vismia macrophylla emerged as key species based on their traditional usage among the Chocó population. Notably, the extract derived from Vismia macrophylla demonstrated the most encouraging outcomes as a digestive enzyme inhibitor, exhibiting IC50 values of 0.99 ± 0.21 μg/mL, 5.61 ± 0.82 mg/mL, and 28.91 ± 2.10 μg/mL for AG, AA, and PL, respectively. Further chemical analysis led to the isolation of three bioactive compounds: 5′-demethoxycadensin G 1, para-hydroxybenzoic acid methyl ester 2, and para-hydroxybenzoic acid butyl ester 3. Compound 1 displayed the highest activity against AG (IC50 = 164.30 ± 0.11 μM), while compounds 2 (IC50 = 28.50 ± 4.07 μM) and 3 (IC50 = 10.15 ± 3.42 μM) exhibited potent inhibitory effects on PL. Molecular docking and enzymatic kinetics studies indicate that these bioactive compounds primarily act as mixed inhibitors of AG and non-competitive inhibitors of PL. These findings underscore the potential of V. macrophylla and its compounds as effective inhibitors of digestive enzymes associated with obesity and type 2 diabetes. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
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19 pages, 3473 KiB  
Article
Isolation and NMR Scaling Factors for the Structure Determination of Lobatolide H, a Flexible Sesquiterpene from Neurolaena lobata 
by Tibor Kovács, Ildikó Lajter, Norbert Kúsz, Zsuzsanna Schelz, Noémi Bózsity-Faragó, Anikó Borbás, István Zupkó, Georg Krupitza, Richard Frisch, Judit Hohmann, Andrea Vasas and Attila Mándi
Int. J. Mol. Sci. 2023, 24(6), 5841; https://doi.org/10.3390/ijms24065841 - 19 Mar 2023
Cited by 3 | Viewed by 2879
Abstract
A new flexible germacranolide (1, lobatolide H) was isolated from the aerial parts of Neurolaena lobata. The structure elucidation was performed by classical NMR experiments and DFT NMR calculations. Altogether, 80 theoretical level combinations with existing 13C NMR scaling [...] Read more.
A new flexible germacranolide (1, lobatolide H) was isolated from the aerial parts of Neurolaena lobata. The structure elucidation was performed by classical NMR experiments and DFT NMR calculations. Altogether, 80 theoretical level combinations with existing 13C NMR scaling factors were tested, and the best performing ones were applied on 1. 1H and 13C NMR scaling factors were also developed for two combinations utilizing known exomethylene containing derivatives, and the results were complemented by homonuclear coupling constant (JHH) and TDDFT-ECD calculations to elucidate the stereochemistry of 1. Lobatolide H possessed remarkable antiproliferative activity against human cervical tumor cell lines with different HPV status (SiHa and C33A), induced cell cycle disturbance and exhibited a substantial antimigratory effect in SiHa cells. Full article
(This article belongs to the Collection Feature Papers in Bioactives and Nutraceuticals)
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25 pages, 6623 KiB  
Article
Isolation, Structure Determination of Sesquiterpenes from Neurolaena lobata and Their Antiproliferative, Cell Cycle Arrest-Inducing and Anti-Invasive Properties against Human Cervical Tumor Cells
by Andrea Vasas, Ildikó Lajter, Norbert Kúsz, Sándor Balázs Király, Tibor Kovács, Tibor Kurtán, Noémi Bózsity, Nikolett Nagy, Zsuzsanna Schelz, István Zupkó, Georg Krupitza, Richard Frisch, Attila Mándi and Judit Hohmann
Pharmaceutics 2021, 13(12), 2088; https://doi.org/10.3390/pharmaceutics13122088 - 5 Dec 2021
Cited by 5 | Viewed by 3323
Abstract
Seven new germacranolides (13, 58), among them a heterodimer (7), and known germacranolide (4), eudesmane (9) and isodaucane (10) sesquiterpenes were isolated from the aerial parts of Neurolaena [...] Read more.
Seven new germacranolides (13, 58), among them a heterodimer (7), and known germacranolide (4), eudesmane (9) and isodaucane (10) sesquiterpenes were isolated from the aerial parts of Neurolaena lobata. Their structures were determined by using a combination of different spectroscopic methods, including HR-ESIMS and 1D and 2D NMR techniques supported by DFT-NMR calculations. The enantiomeric purity of the new compounds was investigated by chiral HPLC analysis, while their absolute configurations were determined by TDDFT-ECD and OR calculations. Due to the conformationally flexible macrocycles and difficulties in assigning the relative configuration, 13C and 1H NMR chemical shift and ECD and OR calculations were performed on several stereoisomers of two derivatives. The isolated compounds (110) were shown to have noteworthy antiproliferative activities against three human cervical tumor cell line with different HPV status (HeLa, SiHa and C33A). Additionally, lobatolide C (6) exhibited substantial antiproliferative properties, antimigratory effect, and it induced cell cycle disturbance in SiHa cells. Full article
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