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1.
Food Chem ; 450: 139339, 2024 Aug 30.
Article in English | MEDLINE | ID: mdl-38657343

ABSTRACT

Oxidative stress is prevalent in Type 2 Diabetes Mellitus (T2DM) and has been associated with high meat consumption. Carob Fruit Extract (CFE) contains phenolic compounds, making it a suitable functional ingredient. Current study aims to evaluate the effect of CFE-enriched meat (CFE-meat) consumption on the antioxidant status of proximal and distal colon, and its relationship with fecal phenolic compounds in late-stage T2DM rats. Three groups of eight rats were studied: 1) D, fed control-meat; 2) ED, fed CFE-meat since the beginning of the study; 3) DE, fed CFE-meat after confirming T2DM. CFE-meat consumption reduces colonic oxidative stress mainly in the proximal section and helps to ameliorate glutathione metabolism and antioxidant score. Difference between ED and DE groups were associated with colon homeostasis and T2DM progression suggesting greater fermentation but lower absorption in the DE group. CFE appears as a promising tool to improve the antioxidant status observed in late-stage T2DM.


Subject(s)
Antioxidants , Colon , Diabetes Mellitus, Type 2 , Fruit , Oxidative Stress , Phenols , Plant Extracts , Animals , Rats , Antioxidants/chemistry , Antioxidants/metabolism , Antioxidants/administration & dosage , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Plant Extracts/pharmacology , Fruit/chemistry , Colon/metabolism , Colon/drug effects , Phenols/chemistry , Phenols/administration & dosage , Male , Diabetes Mellitus, Type 2/metabolism , Diabetes Mellitus, Type 2/drug therapy , Oxidative Stress/drug effects , Meat/analysis , Humans , Rats, Wistar , Plant Gums/chemistry , Plant Gums/administration & dosage , Galactans , Mannans
2.
RSC Med Chem ; 14(7): 1377-1388, 2023 Jul 20.
Article in English | MEDLINE | ID: mdl-37484563

ABSTRACT

Modulation of PPAR-α by natural ligands is a novel strategy for the development of anticancer therapies. A series of 16 compounds based on the structure of 3-(pyridin-3-yl)-5-(thiophen-3-yl)-1,2,4-oxadiazole (natural compound) with antitumour potential were designed and synthesised. The cytotoxicity and PPAR agonist activity of these synthetic 1,2,4-oxadiazoles were evaluated in the A-498 and DU 145 tumour cell lines. Preliminary biological evaluation showed that most of these synthetic 1,2,4-oxadiazoles are less cytotoxic (sulforhodamine B assay) than the positive control WY-14643. Regarding the PPAR-α modulation, compound 16 was the most active, with EC50 = 0.23-0.83 µM (PPAR-α). Additionally, compound 16 had a similar activity to the natural compound (EC50 = 0.18-0.77 µM) and was less toxic in the RPTEC and WPMY-1 cell lines (non-tumour cells) (CC50 = 81.66-92.67 µM) than the natural compound. Looking at the link between chemical structure and activity, our study demonstrates that changes to the natural 1,2,4-oxadiazole at the level of the thiophenyl residue can lead to new agonists of PPAR-α with promising anti-tumour activity.

3.
Mar Drugs ; 21(5)2023 Apr 29.
Article in English | MEDLINE | ID: mdl-37233478

ABSTRACT

Nocuolin A (1), an oxadiazine, was isolated from the cyanobacterium Nostoc sp. Its chemical structure was elucidated using NMR and mass spectroscopic data. From this compound, two new oxadiazines, 3-[(6R)-5,6-dihydro-4,6-dipentyl-2H-1,2,3-oxadiazin-2-yl]-3-oxopropyl acetate (2) and 4-{3-[(6R)-5,6-dihydro-4,6-dipentyl-2H-1,2,3-oxadiazin-2-yl]-3-oxopropoxy}-4-oxobutanoic acid (3), were synthesised. The chemical structures of these two compounds were elucidated by a combination of NMR and MS analysis. Compound 3 showed cytotoxicity against the ACHN (0.73 ± 0.10 µM) and Hepa-1c1c7 (0.91 ± 0.08 µM) tumour cell lines. Similarly, compound 3 significantly decreased cathepsin B activity in ACHN and Hepa-1c1c7 tumour cell lines at concentrations of 1.52 ± 0.13 nM and 1.76 ± 0.24 nM, respectively. In addition, compound 3 showed no in vivo toxicity in a murine model treated with a dose of 4 mg/kg body weight.


Subject(s)
Cathepsin B , Nostoc , Animals , Mice , Molecular Docking Simulation , Cell Line, Tumor , Molecular Structure
4.
Phytochemistry ; 201: 113259, 2022 Sep.
Article in English | MEDLINE | ID: mdl-35662550

ABSTRACT

Two unknown 1,2,4-oxadiazoles (3-(pyridin-3-yl)-5-(thiophen-3-yl)-1,2,4-oxadiazole and 5-(3-hydroxyphenyl)-3-(pyridin-3-yl)-1,2,4-oxadiazole) and one known 1,2,4-oxadiazole (5-(3-methoxyphenyl)-3-(pyridin-3-yl)-1,2,4-oxadiazole) were isolated from tubers of Neowerdermannia vorwerkii, collected from the San Juan Huancollo, Ingavi province, La Paz, Bolivia. The chemical structures of these compounds were elucidated through NMR and HRMS spectroscopic analyses. All compounds showed apoptotic capacity against the SK-HEP-1 and Caco-2 tumour cells. 5-(3-methoxyphenyl)-3-(pyridin-3-yl)-1,2,4-oxadiazole and 5-(3-hydroxyphenyl)-3-(pyridin-3-yl)-1,2, 4-oxadiazole showed slight apoptotic capacities, with an IC50 between 17.46 ± 0.75 to 15.91 ± 0.62 µM and 39.29 ± 0.98 to 34.81 ± 0.70 µM, respectively. 3-(pyridin-3-yl)-5-(thiophen-3-yl)-1,2,4-oxadiazole showed a higher apoptotic capacity with an IC50 in the range of 0.98 ± 0.11 to 0.76 ± 0.03 µM, similar to that of the positive control (Dimethylenastron).


Subject(s)
Neoplasms , Oxadiazoles , Caco-2 Cells , Colon , Humans , Liver , Magnetic Resonance Spectroscopy , Oxadiazoles/chemistry , Oxadiazoles/pharmacology , Structure-Activity Relationship
5.
J Ethnopharmacol ; 292: 115198, 2022 Jun 28.
Article in English | MEDLINE | ID: mdl-35314420

ABSTRACT

ETHNO-PHARMACOLOGICAL RELEVANCE: The tuber of Neowerdermannia vorwerkii commonly known as 'Achacana' is used as an infusion in Andean countries to treat various gastrointestinal ailments, kidney and liver diseases. AIM OF THE STUDY: This study determined the anti-inflammatory activity of the aqueous extract from Neowerdermannia vorwerkii and identified the compounds related to this activity. MATERIALS AND METHODS: A bio-guided isolation of the active compounds of Neowerdermannia vorwerkii was carried out, selecting the sub-extracts and fractions depending on their anti-inflammatory activity in the Hs 738.St/Int, Hs 746T and NCI-N87 cells. RESULTS: Three compounds were obtained and characterised by nuclear magnetic resonance and mass spectrometry. These compounds are (3-(pyridin-3-yl)-5-(tiophen-3-yl)-1,2,4-oxadiazole (1), 5-(3-methoxyphenyl)-3-(pyridin-3-yl)-1,2,4-oxadiazole (2) and 5-(3-hydroxyphenyl)-3-(pyridin-3-yl)-1,2,4-oxadiazole (3). Regarding their anti-inflammatory activity, the three compounds inhibited the production of cytokines (IL-1ß, IL-6 and TNF-α), however, compound 1 was the most active, with an IC50 of 0.87 µM in all cell lines. CONCLUSION: In the present study, the anti-inflammatory activity of the aqueous extract of Neowerdermannia vorwerkii was tested and analysed, following the isolation of three 1,2,4-oxadiazoles type compounds with similar pharmacological properties.


Subject(s)
Anti-Inflammatory Agents , Plant Extracts , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Cytokines/metabolism , Oxadiazoles , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Stomach
6.
J Ethnopharmacol ; 289: 115009, 2022 May 10.
Article in English | MEDLINE | ID: mdl-35077827

ABSTRACT

ETHNO-PHARMACOLOGICAL RELEVANCE: The bark of Semialarium mexicanum commonly known as 'Cancerina' is used as an infusion in Central America and Mexico to treat various wound infections, as well as skin and vaginal ulcers. AIM OF THE STUDY: This study aimed to determine the wound healing, anti-inflammatory and anti-melanogenic activities of the aqueous extract of Semialarium mexicanum and to identify the compounds related to these activities. MATERIALS AND METHODS: A bio-guided isolation of the active compounds of Semialarium mexicanum was carried out, selecting the sub-extracts and fractions depending on their wound healing, anti-inflammatory and anti-melanogenic activities in the RAW 264.7, NIH/3T3 and B16-F10 cells. RESULTS: Three compounds were obtained and characterised by nuclear magnetic resonance and mass spectrometry. These compounds are (3ß)-3-Hydroxy-urs-12-en-28-oic acid (1), (3ß)-Urs-12-ene-3,28-diol (2) and (2α, 19α)-2,19-Dihydroxy-3-oxo-urs-12-en-28-oic acid (3). Regarding the anti-inflammatory activity, the three compounds inhibited the production of NF-κB and NO, however, compound 3 was the most active with IC50 values of 8.15-8.19 µM and 8.94-9.14 µM, respectively, in all cell lines. The anti-melanogenic activity of these compounds was evaluated by the inhibition of tyrosinase and melanin in the B16-F10 cell line. The three compounds showed anti-melanogenic activity, however, compound 3 was the most active with an IC50 of 8.03 µM for the inhibition of tyrosinase production, and an IC50 of 8.53 µM for the inhibition of melanin production. Finally, concerning the wound healing activity, the three compounds presented proliferative activity in all the tested cell lines, however, compound 3 showed higher cell proliferation percentages than compounds 1 and 2 (88.89-89.60% compared to 64.92-65.71% and 71.53-71.99%, respectively). CONCLUSION: The wound healing, anti-inflammatory and anti-melanogenic activity of the aqueous extract of Semialarium mexicanum was tested and analysed in the present study, after having isolated three ursane-type triterpenes.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Celastraceae/chemistry , Triterpenes/pharmacology , Wound Healing/drug effects , Animals , Anti-Inflammatory Agents/isolation & purification , Cell Line, Tumor , Inhibitory Concentration 50 , Medicine, Traditional , Melanins/metabolism , Melanoma, Experimental/metabolism , Mice , NIH 3T3 Cells , Plant Extracts/chemistry , Plant Extracts/pharmacology , RAW 264.7 Cells , Triterpenes/chemistry , Triterpenes/isolation & purification
7.
Nat Prod Res ; 35(24): 6204-6209, 2021 Dec.
Article in English | MEDLINE | ID: mdl-33111583

ABSTRACT

Activity-guided fractionations from the freshwater cyanobacterium Nodularia harveyana led to the isolation of two monogalactosyldiacylglycerols (MGDG), two digalactosyldiacylglycerols (DGDG), two monoglucosyldiacylglycerols (MGlcDG) and 1-(O-hexose)-3,25-hexacosanediol (HG). Structures were elucidated by a combination of 1D and 2D NMR analysis, HRMS and GC-MS. The potential for inhibition against TNF-α and NF-κB production of these seven compounds was tested in THP-1 cells. All compounds showed activity, but compound 7 showed higher inhibitory activity of TNF-α and NF-κB, with IC50 of 4.88 ± 0.13 and 3.64 ± 0.45 µM, respectively.


Subject(s)
Anti-Inflammatory Agents , Cyanobacteria , Glycolipids/pharmacology , Nodularia , Anti-Inflammatory Agents/pharmacology , Cyanobacteria/chemistry , Humans , NF-kappa B , Nodularia/chemistry , THP-1 Cells
8.
Nat Prod Res ; 35(22): 4690-4693, 2021 Nov.
Article in English | MEDLINE | ID: mdl-31894701

ABSTRACT

Activity-guided fractionations of leaves and stems from Loranthus acutifolius led to the isolation of 2',4',6-trimethoxyflavone (1), 3',4',5-trihydroxy-6,7,8-trimethoxyflavone (2), 2'4'-dihydroxy-6'-methoxy-chalcone (3) and 4',5-dihydroxy-6,7,8-trimethoxyflavone (4). The potential for inhibition against melanin production and tyrosinase activity of these 4 compounds was tested in B16-F10 cells. 2',4',6-trimethoxyflavone, 3',4',5-trihydroxy-6,7,8-trimethoxyflavone, 2'4'-dihydroxy-6'-methoxy-chalcone and 4',5-dihydroxy-6,7,8-trimethoxyflavone showed an inhibitory activity of melanin production with IC50 of 3.6 ± 0.05 µM, 8.1 ± 0.05 µM, 1.6 ± 0.03 µM and 6.5 ± 0.05 µM, respectively. In addition, 2',4',6-trimethoxyflavone, 3',4',5-trihydroxy-6,7,8-trimethoxyflavone, 2'4'-dihydroxy-6'-methoxy-chalcone and 4',5-dihydroxy-6,7,8-trimethoxyflavone were able to inhibit tyrosinase activity with IC50 of 4.0 ± 0.03 µM, 11.3 ± 0.05 µM, 5.7 ± 0.02 µM and 8.6 ± 0.04 µM, respectively. This is the first time that these compounds are reported in the L. acutifolius species showing anti-melanogenic activities.


Subject(s)
Loranthaceae , Melanins , Flavonoids/pharmacology , Monophenol Monooxygenase , Plant Leaves
9.
Nat Prod Res ; 35(22): 4698-4702, 2021 Nov.
Article in English | MEDLINE | ID: mdl-31913056

ABSTRACT

Activity-guided fractionations of black tubers of Tropaeolum tuberosum led to the isolation of 3-[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl] benzonitrile (1) and [3,5-Bis (1,1-dimethylethyl)-4-hydroxyphenyl] ethenylidene] bis-phosphonic acid tetraethyl ester (2). Compounds 1 and 2 showed an antibacterial effect against almost all the strains assayed, especially compound 2, showing the same inhibition potential for Enterococcus faecalis and Salmonella enteritidis as the ampicillin (MIC = 1.5 µM) and a better potential than chloramphenicol which has a MIC of 3.5 µM. In addition, compounds 1 and 2 showed a relevant antifungal inhibition against Candida tropicalis with MICs of 100 µM and 50 µM, and against Saccharomyces kudriavzevii with MICs of 25 µM and 1.5 µM. This is in comparison to fluconazole which had MICs of 150 µM (against Candida tropicalis) and 3.5 µM (against Saccharomyces kudriavzevii). This is the first time that compounds 1 and 2 are reported as showing antimicrobial activities.


Subject(s)
Anti-Infective Agents , Tropaeolum , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Antifungal Agents/pharmacology , Microbial Sensitivity Tests , Saccharomyces
10.
J Ethnopharmacol ; 268: 113603, 2021 Mar 25.
Article in English | MEDLINE | ID: mdl-33242619

ABSTRACT

ETHNO-PHARMACOLOGICAL RELEVANCE: Species of the genus Tagetes are well known for their anti-inflammatory properties. Tagetes minuta "Huacatay" is an endemic species of South America that has been used in traditional medicine since ancient times as a remedy for stomach and intestinal discomfort. AIM OF THE STUDY: The aim of this study is to investigate the anti-inflammatory activity of the aqueous and hydroalcoholic extracts of the Huacatay, identifying the compounds responsible for this activity. MATERIALS AND METHODS: Anti-inflammatory activity of the compounds, fractions and extracts was evaluated in Hs 746T (stomach), HIEC-6 (intestine) and THP-1 (monocytes peripheral blood) cells by measuring their inhibitory capacity against the NF-κB production. RESULTS: Aqueous and hydroalcoholic extracts of Tagetes minuta displayed anti-inflammatory activity in vitro, the hydroalcoholic extract being the most active (IC50 between 59.72 and 66.42 µg/mL) in all cell lines. Bio-guided hydroalcoholic extract fractionation led to the isolation and characterisation of two pheophytins, pheophytin a (1) and 132-hydroxy pheophytin a (2). Both compounds inhibited the production of NF-κB with IC50 values in the low micromolar range, with an IC50 between 12.32 and 16.01 µM for compound 1 and 7.91-9.87 µM for compound 2. CONCLUSIONS: The two pheophytins isolated in this study inhibit the production of NF-κB, thus showing that the traditional anti-inflammatory use of Tagetes minuta can be proved through pharmacological assays. This contributes to understanding the anti-inflammatory activity of the Huacatay extracts and their use in the treatment of stomach and intestinal discomfort.


Subject(s)
Anti-Inflammatory Agents/therapeutic use , Inflammatory Bowel Diseases , NF-kappa B/antagonists & inhibitors , Pheophytins/therapeutic use , Plant Extracts/therapeutic use , Tagetes , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Cell Line , Dose-Response Relationship, Drug , Ethanol/isolation & purification , Ethanol/pharmacology , Ethanol/therapeutic use , Humans , Inflammatory Bowel Diseases/drug therapy , Inflammatory Bowel Diseases/metabolism , NF-kappa B/metabolism , Pheophytins/isolation & purification , Pheophytins/pharmacology , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Signal Transduction/drug effects , Signal Transduction/physiology , Water/pharmacology
11.
Planta Med ; 87(5): 383-394, 2021 Apr.
Article in English | MEDLINE | ID: mdl-33007786

ABSTRACT

Tropaeolum tuberosum, commonly known as Mashua, is an herbal remedy used in traditional Andean medicine for the relief of kidney and bladder pain, as well as contusions. This study aimed to evaluate the fractions and isolated compounds from T. tuberosum with analgesic activity mediated by the transient receptor potential vanilloid-1 receptor. A bioguided phytochemical analysis based on NMR/MS was performed to identify the compounds of the n-heptane fractions from samples of purple tubers of T. tuberosum. The transient receptor potential vanilloid-1 agonist and antagonist activity were assessed through the measurement of intracellular Ca2+ in HEK001 cells. The chemical structure determination led to the identification of two alkamides: N-(2-hydroxyethyl)-7Z,10Z,13Z,16Z-docosatetraenamide (1: ) and N-oleoyldopamine (2: ). Both compounds induced increased intracellular calcium flow with IC50 values of 3.2 nM and 7.9 nM, respectively, thus activating the transient receptor potential vanilloid-1 receptor. Our research is the first report to show that these two compounds isolated from T. tuberosum can act as agonists of the transient receptor potential vanilloid-1 receptor, providing scientific evidence for the traditional use of this species in pain relief.


Subject(s)
Keratinocytes , Plant Tubers , TRPV Cation Channels , Tropaeolum , Analgesics , Capsaicin , Humans , Ion Channels , Keratinocytes/drug effects
12.
Phytochemistry ; 180: 112529, 2020 Dec.
Article in English | MEDLINE | ID: mdl-33032099

ABSTRACT

Three carbamidocyclophanes, A, F and V, and carbamidocylindrofridin A were isolated from the cultured freshwater cyanobacterium Cylindrospermum stagnale, collected in the Canary Islands. The chemical structures of these compounds were elucidated through NMR, HRMS and ECD spectroscopy. The absolute configuration of carbamidocyclophane A was confirmed using X-ray-diffraction. All compounds showed apoptotic capacity against the SK-MEL-1, SK-MEL-28 and SK-MEL-31 tumour cells. Carbamidocylindrofridin A had the highest anti-tumour potential, with an IC50 of 1 ± 0.3 µM in the SK-MEL-1 cell line.


Subject(s)
Cyanobacteria , Cell Line, Tumor , Magnetic Resonance Spectroscopy , Spain
13.
Phytochemistry ; 177: 112435, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32562919

ABSTRACT

Two alkaloids were isolated and identified for the first time in the black tubers of Tropaeolum tuberosum, collected from the Titicani-Taca, Ingavi province in La Paz, Bolivia. Their structures were elucidated by extensive NMR and MS spectroscopic analyses. The isolated compounds were evaluated for their cytotoxicity and apoptotic capacity against four human cancer cell lines. 2-Benzyl-3-thioxohexahydropyrrolo[1,2-c]imidazole-1-one (1) showed slight cytotoxic activity against all the cancer cell lines which were tested, with IC50 values ranging from 27.45 ± 0.80 to 31.07 ± 0.87 µM. Moreover, N-(4-acetyl-5-methyl-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl) acetamide (2) showed significant anti-cancer potential, with IC50 values between 1.26 ± 0.57 µM and 1.37 ± 0.09 µM against all human cancer cell lines which were tested. Treatment of tumour cell lines with the compounds caused an increase in the apoptotic rate of these cells, observing that compound 2 presented an apoptotic effect which was double with respect to the control (Dimethylenastron).


Subject(s)
Alkaloids , Antineoplastic Agents, Phytogenic , Tropaeolum , Bolivia , Cell Line, Tumor , Humans
14.
RSC Med Chem ; 11(10): 1196-1209, 2020 Oct 01.
Article in English | MEDLINE | ID: mdl-33479624

ABSTRACT

Thirty-five macamide analogues were synthesised by modifying the initial molecular structure. The resulting structures were confirmed using NMR and MS. Cytotoxicity and the anti-inflammatory activity of these synthetic macamides were evaluated in the THP-1 cell line. Preliminary biological evaluation indicated that most of these synthetic macamides did not present cytotoxicity (MTT assay) in the tested cell line with respect to the control (actinomycin D). Regarding the anti-inflammatory activity, several analogues had a greater potential for inhibition of TNF-α than natural macamides. Synthetic macamide 4a was the most active (IC50 = 0.009 ± 0.001 µM) compared to the C87 (control). Through looking at the link between the chemical structure and the activity, our study proves that changes made to natural macamides at the level of the alkyl chain, the benzyl position, the amide bond, and the addition of two methyl groups to the aromatic ring (meta position) lead us to obtaining new macamides with greater anti-inflammatory activity.

15.
J Ethnopharmacol ; 247: 112152, 2020 Jan 30.
Article in English | MEDLINE | ID: mdl-31421183

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Tropaeolum tuberosum Ruíz & Pavón (Tropaeolaceae). Sim (commonly called Mashua) is an indigenous plant that has medicinal values for various ethnic groups of the regions of the Andes mountain range of South America, which use it for the treatment of diseases venereal, lung and skin; for the healing of internal and external wounds; and as an analgesic for kidney and bladder pain. AIM OF THE REVIEW: We critically summarised the current evidence on the botanic characterisation and distribution, ethnopharmacology, secondary metabolites, pharmacological activities, qualitative and quantitative analysis, and toxicology of T. tuberosum. MATERIALS AND METHODS: The relevant information on T. tuberosum was gathered from worldwide accepted scientific databases via electronic search (Google scholar, Elsevier, SciFinder, ScienceDirect, PubMed, SpringerLink, Web of Science, Scopus, Wiley Online, Mendeley, Scielo and Dialnet electronic databases). Information was also obtained from the literature and books as well as PhD and MSc dissertations. Plant names were validated by 'The Plant List' (www.theplantlist.org). RESULTS: T. tuberosum has diverse uses in local and popular medicine, specifically for relieving pain and infections in humans. Regarding its biological activities, polar extracts (aqueous, hydroalcoholic) and isolated compounds from the tubers have exhibited a wide range of in vitro and in vivo pharmacological effects, including antibacterial, antioxidant, anti-inflammatory activities. Quantitative analysis (e.g., NMR, HPLC, GC-MS) indicated the presence of a set of secondary metabolites, including hydroxybenzoic acids, tannins, flavanols, anthocyanins, glucosinolates, isothiocyanates, phytosterols, fatty acids and alkamides in the tubers of T. tuberosum. Likewise, glucosinolates have been identified in the seeds and isothiocyanates have been detected in leaves, flowers and seeds. CONCLUSIONS: T. tuberosum has been tested for various biological activities and the extracts (tubers in particular) demonstrated a promising potential as an antibacterial, antioxidant, anti-inflammatory and inhibitors of benign prostatic hyperplasia. A lack of alignment between the ethno-medicinal uses and existing biological screenings was observed, indicating the need to explore its potential for the treatment against respiratory affections, urinary affections and blood diseases. Likewise, it is necessary to analyse deeply the relationship that exists between the different tuber colours of T. tuberosum and its use for the treatment of certain diseases. Validation of clinical studies of the antibacterial, antioxidant/anti-inflammatory, anti-spermatogenic activities and as inhibitors of benign prostatic hyperplasia is required. Moreover, studies on the toxicity, bioavailability, and pharmacokinetics, in addition to clinical trials, are indispensable for assessing the safety and efficacy of the active metabolites or extracts obtained from T. tuberosum. Other areas that need investigation are the development of future applications based on their active metabolites, such as neurodegenerative diseases (Alzheimer's disease, Parkinson's disease, Huntington's disease). Finally, the work purposes to motivate other research groups to carry out a series of scientific studies that can fill the gaps that exist with respect to Mashua properties, and thus be able to change the focus of T. tuberosum (Mashua) that currently has in the consumer society.


Subject(s)
Anti-Bacterial Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Plant Extracts/pharmacology , Tropaeolum/chemistry , Anti-Bacterial Agents/therapeutic use , Anti-Inflammatory Agents/therapeutic use , Antioxidants/therapeutic use , Ethnopharmacology , Humans , Plant Extracts/therapeutic use , Plant Tubers/chemistry , South America
16.
Planta Med ; 85(17): 1304-1315, 2019 Nov.
Article in English | MEDLINE | ID: mdl-31234214

ABSTRACT

Natural products and their derivatives represent the most consistently successful source of drug leads. Terpenoids, a structurally diverse group, are secondary metabolites widely distributed in nature, endowed with a wide range of biological activities such as antibacterial, anti-inflammatory, antitumoral, or neuroprotective effects, which consolidate their therapeutic value. During the last decades, and taking into consideration the prevalence of aging-related diseases, research activity into the neuroprotective effects of these types of compounds has increased enormously. Several signaling pathways involved in neuroprotection are targets of their mechanism of action and mediate their pleiotropic protective activity in neuronal cell damage. In the present review, molecular basis of the neuroprotection exerted by terpenoids is presented, focusing on preclinical evidence of the therapeutic potential of diterpenoids and triterpenoids on neurodegenerative disorders. By acting on diverse mechanisms simultaneously, terpenoids have been emphasized as promising multitarget agents.


Subject(s)
Neuroprotective Agents/pharmacology , Terpenes/pharmacology , Animals , Drug Delivery Systems , Humans , Neurodegenerative Diseases/drug therapy
17.
J Emerg Med ; 53(6): 919-923, 2017 Dec.
Article in English | MEDLINE | ID: mdl-29079490

ABSTRACT

BACKGROUND: As the numbers of emergency department (ED) visits and inpatient admissions continue to increase, there is growing interest in alternatives to inpatient hospitalization. OBJECTIVE: Our aim was to investigate a novel approach to expediting discharges from the ED with multidisciplinary discharge services to prevent an avoidable admission into the hospital. METHODS: This pilot study was conducted at a large urban tertiary-care ED in 2016. All patients presenting to the ED with planned inpatient or observation admission were considered for discharge with enhanced discharge planning services. The patients selected, discharge diagnoses, and outcomes were analyzed by descriptive statistics. This study was approved by the study site's Institutional Review Board, including waiver of patient consent. RESULTS: During the pilot period, 57 out of 143 (40%) selected patients with planned admission were discharged with enhanced discharge planning services. Median ED length of stay was 17.2 h and mean patient age was 73 years old. Of these patients, 7 (12%) returned within 72 h and 4 (0.07%) were subsequently admitted to the hospital. CONCLUSIONS: In this pilot study, a novel approach to expediting discharges from the ED with multidisciplinary discharge services was feasible and resulted in fewer admissions to the hospital.


Subject(s)
Patient Discharge/standards , Time Factors , Academic Medical Centers/organization & administration , Adult , Aged , Emergency Service, Hospital/organization & administration , Female , Humans , Male , Middle Aged , Patient Discharge/trends , Pilot Projects , Program Development/methods , Retrospective Studies
18.
Acad Med ; 92(1): 92-100, 2017 01.
Article in English | MEDLINE | ID: mdl-27166864

ABSTRACT

PURPOSE: Patients with limited English proficiency (LEP) experience lower-quality health care and are at higher risk of experiencing adverse events than fluent English speakers. Despite some formal training for health professions students on caring for patients with LEP, the hidden curriculum may have a greater influence on learning. The authors designed this study to characterize the hidden curriculum that medical and nursing students experience regarding the care of patients with LEP. METHOD: In 2014, the authors invited students from one medical school and one nursing school, who had completed an interprofessional pilot curriculum on caring for patients with LEP 6 to 10 months earlier, to participate in semistructured interviews about their clinical training experiences with LEP patients. The authors independently coded the interview transcripts, compared them for agreement, and performed content analysis to identify major themes. RESULTS: Thirteen students (7 medical and 6 nursing students) participated. Four major themes emerged: role modeling, systems factors, learning environment, and organizational culture. All 13 students described negative role modeling experiences, and most described role modeling that the authors coded as "indifferent." Students felt that the current system and learning environment did not support or emphasize high-quality care for patients with LEP. CONCLUSIONS: The hidden curriculum that health professional students experience regarding the care of patients with LEP is influenced by systems limitations and a learning environment and organizational culture that value efficiency over effective communication. Role modeling seems strongly linked to these factors as supervisors struggle with these same challenges.


Subject(s)
Clinical Competence , Communication Barriers , Curriculum , Education, Medical/organization & administration , Education, Nursing/organization & administration , Emigrants and Immigrants , Language , Adult , Female , Humans , Male , Physician-Patient Relations , Students, Medical , Translating , United States
20.
J Pediatr Psychol ; 34(1): 4-13, 2009.
Article in English | MEDLINE | ID: mdl-18073235

ABSTRACT

OBJECTIVE: To examine posttraumatic stress symptoms (PTSS) in parents of children with cancer as a function of time since diagnosis, treatment status, and relapse history, and as compared to parents of healthy children. METHOD: Participants included parents of 199 children with cancer, comprising a cross-sectional sample of diagnoses and treatment phases, ranging from currently on therapy to long-term survivors, and 108 parents of healthy children obtained via acquaintance control methods. Parents completed a standardized self-report measure of PTSS. RESULTS: Within the cancer group, parental report of PTSS differed as a function of treatment status and time since diagnosis. Parents of children on active treatment endorsed similar levels of PTSS as control parents, whereas parents of children off treatment reported significantly lower levels of PTSS than did controls. Similarly, parents of long-term survivors reported significantly lower levels of PTSS than did controls, while parents of recently diagnosed children did not differ from controls on PTSS. In contrast, parents of children who had suffered a relapse reported significantly higher levels of PTSS, and were much more likely to be identified as a posttraumatic stress disorder (PTSD) case. CONCLUSIONS: As a group, parents of children with cancer did not demonstrate any evidence of increased PTSS relative to parents of healthy children. Time since diagnosis, child treatment status, and relapse history are significant determinants of parent PTSS. Only parents of children who experienced a relapse appear to be at increased risk of PTSD. The current results appear discrepant from the existing literature, and possible explanations for these discrepancies are examined.


Subject(s)
Neoplasms/psychology , Parents/psychology , Stress Disorders, Post-Traumatic/diagnosis , Adaptation, Psychological , Adolescent , Child , Disease Progression , Female , Humans , Male , Neoplasms/diagnosis , Neoplasms/therapy , Outpatient Clinics, Hospital , Personality Inventory , Risk Factors , Stress Disorders, Post-Traumatic/psychology , Survivors/psychology
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