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1.
Chem Biodivers ; 21(4): e202400319, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38423999

RESUMEN

A new oxidized heptene, 7-benzoyloxy-4-hydroxy-1-ethoxy-2E,4Z-heptadiene-1,6-dione, namely siamheptene A (1), together with eight known compounds (2-9), were isolated from the leaves of Uvaria siamensis. Their structures were elucidated by detailed analysis of spectroscopic (IR, 1D and 2D NMR) and mass spectrometric data. Compound 9 is reported for the first time from Uvaria genus. Siamheptene A was evaluated for cytotoxicity against HeLa (cervical cancer cells), A549 (lung cancer cells), and Vero cells using the MTT assay and screened for antibacterial activities. In addition, the isolated compounds (1-7, and 9) were investigated for their antioxidant (DPPH, FRAP and ABTS+ assays), anti-glycation, and anti-tyrosinase properties. Based on our results, compound 1 had mild cytotoxicity against Hela and A549 cancer cell lines, with IC50 ranging from 31.09 to 31.67 µg/mL. Compound 1 also showed antioxidant activities in all tasted assays. However, it showed no detectable activity (>128 µg/mL) against various bacterial strains, and it has no inhibitory effects on tyrosinase enzymes. Among of all tested compounds, chrysin (5), showcased highest anti-glycation and anti-tyrosinase activities. This comprehensive analysis provides highlighting the potential of 1 as a lead compound for further structural modification and development of cytotoxic or antioxidant agents.


Asunto(s)
Antineoplásicos , Uvaria , Animales , Chlorocebus aethiops , Humanos , Monofenol Monooxigenasa , Uvaria/química , Antioxidantes/farmacología , Antioxidantes/química , Células Vero , Antineoplásicos/farmacología , Extractos Vegetales/química
2.
J Nat Prod ; 87(2): 207-216, 2024 02 23.
Artículo en Inglés | MEDLINE | ID: mdl-38237151

RESUMEN

Four new adjacent bis-tetrahydrofuran acetogenins, bullacin C (7), uvarirufin (9), and uvariasolins III (12) and IV (13), along with 11 known acetogenins, were isolated from the stem of Uvaria rufa. Their structures were elucidated based on spectroscopic data analysis, including 1D and 2D NMR, HRESIMS, and MALDI-MS/MS of the lithium adducts. Absolute configurations were assigned using Mosher ester analysis and ECD measurements. Uvarirufin (9) possesses a unique C-39 skeleton among acetogenins. Most tested acetogenins exhibited cytotoxicity against human cancer cell lines (HCT 116, 22Rv1, MDA-MB-435, OVCAR3). Squamocin (8) and uvarirufin (9) were found to be the most potent, with an IC50 value of 1.2 µM for both in HCT 116 colon cancer cells. Additionally, a new application of Dragendorff's reagent is proposed herein for the TLC detection of acetogenins.


Asunto(s)
Antineoplásicos , Neoplasias Ováricas , Uvaria , Femenino , Humanos , Acetogeninas/farmacología , Acetogeninas/química , Apoptosis , Línea Celular Tumoral , Espectroscopía de Resonancia Magnética , Estructura Molecular , Espectrometría de Masas en Tándem , Uvaria/química
3.
Phytochemistry ; 216: 113884, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37813133

RESUMEN

Six undescribed compounds, uvarirufols D and E, (+)-uvarigranol B, (-)-uvarigranol E, 6-acetoxy-5-hydroxy-7-methoxyflavanone and cherrevenaphthalene D, along with twelve known compounds, including polyoxygenated cyclohexenes, flavonoids, and lignans, were isolated from the methanol extract of Uvaria rufa stems. Their structures were elucidated by spectroscopic analyses and the absolute configurations were determined using electronic circular dichroism. Several isolates were evaluated for cytotoxic, antitubercular and anti-inflammatory potentials. (-)-6-Acetylzeylenol showed moderate inhibitory activity against Mycobacterium tuberculosis, with MIC value of 47.10 µg/mL. Cherrevenaphthalene D exhibited weak antimycobacterial activity and potent inhibitory effect on lipopolysaccharide-induced nitric oxide (NO) production in RAW 264.7 cells (EC50 = 8.54 µM). 8-Hydroxy-5,7-dimethoxyflavanone displayed moderate level of NO inhibition (EC50 = 43.62 µM) with little cytotoxicity. The polyoxygenated cyclohexenes and lignans were inactive against HCT 116 and 22Rv1 cancer cells (IC50 > 100 µM).


Asunto(s)
Lignanos , Uvaria , Uvaria/química , Estructura Molecular , Ciclohexenos/farmacología , Ciclohexenos/química , Lignanos/farmacología
4.
J Ethnopharmacol ; 300: 115673, 2023 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-36096348

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Streptococcus mutans a key pathogen, produces biofilm, acids and extracellular polysaccharides in the oral cavity; which leads to the development of dental caries. Control of these pathogenic markers can prevent dental caries. Uvaria chamae P. Beauv. is a medicinal plant traditionally used for many ailments including oral infections. Root, leaves and bark extracts has proven antibacterial activity including activity against caries causing S. mutans. However, its effect on the virulence properties of S. mutans, responsible for the development of dental caries, has not been studied. AIM OF THE STUDY: This study investigated the phytochemical constituents, anti-S. mutans, anti-adherence and anti-acidogenic activity of U. chamae root extract. MATERIALS AND METHODS: Extracts were prepared and phytochemical analysis was performed. Minimum inhibitory concentrations (MIC) were determined, and MIC and sub-MIC concentrations of the best solvent were selected for their effect on the virulence factors of S. mutans. The results were analysed using one-way ANOVA and Wilcoxon Rank Sum Tests. RESULTS: The dichloromethane extract, with proanthocyanidin as a major chemical constituent, produced an MIC of 0.02 mg/ml. At 6 h, exposure to 0.005, 0.01, and 0.02 mg/ml extract significantly reduced S. mutans adherence by 39, 59, and 77% respectively (p < 0.05). Uvaria chamae also significantly inhibited acid production in S. mutans at 10, 12, 14 and 16 h (p < 0.05). At ½ MIC, the plant extract caused remarkable downregulation of the virulence genes responsible for the adherence, biofilm formation, extracellular polysaccharide synthesis and acid production. CONCLUSIONS: This suggests that U. chamae extract may potentially be used to inhibit the proliferation of S. mutans and silencing the expression of pathology-related genes, which will prevent the development of dental caries.


Asunto(s)
Caries Dental , Proantocianidinas , Uvaria , Ácidos , Antibacterianos/química , Antibacterianos/farmacología , Biopelículas , Caries Dental/prevención & control , Cloruro de Metileno/farmacología , Pruebas de Sensibilidad Microbiana , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Proantocianidinas/farmacología , Solventes/farmacología , Streptococcus mutans , Uvaria/química , Factores de Virulencia
5.
Ethiop J Health Sci ; 32(4): 817-822, 2022 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-35950076

RESUMEN

Background: The objective of this study was to evaluate the anti-inflammatory activities and phytochemical composition of the leaves extracts of Boscia coriacea Graells and Uvaria leptocladon Oliv. Methods: The powdered leaves of Boscia coriacea Graells and Uvaria leptocladon Oliv were extracted by maceration and soxhlet extraction methods. Anti-inflammatory activity of the leaves extracts of Boscia coriacea Graells and Uvaria leptocladon Oliv were evaluated using carrageenan-induced paw edema model. Standard methods were used for analysis of phytochemical composition of the leaves extracts of Boscia coriacea Graells and Uvaria leptocladon Oliv. Data analysis was done using one way analysis of variance. Results: U. leptocladon Oliv (200 mg/kg) and B. coriacea Graells (200 mg/kg) showed percent inhibition on mice paw edema of 86% and 75% after six hours of carrageenan injection, respectively. The ethanol fraction (100 mg/kg) of U. leptocladon Oliv showed the highest anti-inflammatory effect after six hours of carrageenan injection. The phytochemical analysis of the leaves extracts of B. coriacea and U. leptocladon revealed the presence of tannins, alkaloids, cardiac glycoside, flavonoids, phenols, quinones, and saponins. Conclusion: The crude leaves extracts of B. coriacea Graells and U. leptocladon Oliv contain phytochemicals with anti-inflammatory activities.


Asunto(s)
Uvaria , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Carragenina/efectos adversos , Carragenina/análisis , Edema/tratamiento farmacológico , Ratones , Fitoquímicos/análisis , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Uvaria/química
6.
Phytochemistry ; 202: 113298, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-35780925

RESUMEN

Dulcisenes C-E, undescribed polyoxygenated cyclohexenes and twenty-one known compounds were isolated from the dichloromethane extract of the leaves of Uvaria dulcis Dunal. The structures of these undescribed compounds were determined by spectroscopic data analyses, including 1D and 2D NMR, IR, and MS techniques; their absolute configurations were analyzed by NOESY and ECD spectra. Cytotoxicity of sixteen more abundant isolates was evaluated. Cherrevenone and 2',3'-dihydroxy-4',6'-dimethoxychalcone exhibited cytotoxic activity against some cancer cell lines with IC50 values in the range of 3.3-11.8 µM.


Asunto(s)
Antineoplásicos Fitogénicos , Antineoplásicos , Uvaria , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Ciclohexenos/química , Estructura Molecular , Hojas de la Planta/química , Uvaria/química
7.
Fitoterapia ; 158: 105170, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35288209

RESUMEN

Three new oxygenated cyclohexene derivatives, pandensenol D - F (1-3), two new flavanoids, pandensone A and B (4-5), and seven known compounds (6-12) were isolated from the methanol extract of the leaves of Uvaria pandensis Verdc. (Annonaceae). The structures were characterized by NMR spectroscopic and mass spectrometric analyses. The isolated metabolites were evaluated for their antibacterial activity against the Gram-positive bacteria Bacillus subtilis and Staphylococcus epidermidis, the Gram-negative bacteria Enterococcus raffinosus, Escherichia coli, Paraburkholderia caledonica, Pectobacterium carotovorum and Pseudomonas putida, and for cytotoxicity against the MCF-7 human breast cancer cell line. Out of the tested compounds, pandensenol D (1) and (6',7'-dihydro-8'α,9'ß-dihydroxy)-3-farnesylindole (12) showed weak activity, whereas (8'α,9'ß-dihydroxy)-3-farnesylindole (11) strong activity against B. subtilis. Four of the isolated compounds (1, 4, 11 and 12) showed moderate cytotoxicity against MCF-7 breast cancer cells (EC50 > 100 µM).


Asunto(s)
Uvaria , Antibacterianos/farmacología , Bacillus subtilis , Ciclohexenos , Flavonoides/análisis , Flavonoides/farmacología , Humanos , Estructura Molecular , Hojas de la Planta/química , Uvaria/química
8.
Nat Prod Res ; 36(23): 6039-6043, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-35176917

RESUMEN

A new C-benzylated flavone, uvariaruflavone (1), along with 13 known compounds (2-14) were isolated from the twig and leaf extracts of Uvaria rufa Blume. Their structures were established by extensive spectroscopic methods. Flavones (5-8) and cyclohexene (10) were isolated from U. rufa for the first time. Most of the isolated compounds were evaluated for their α-glucosidase and α-amylase inhibitory activities. Of these, uvariaruflavone (1) showed the highest α-glucosidase inhibitory activity with an IC50 value of 44.3 µM, while ferrudiol (12) displayed the highest α-amylase inhibitory activity with an IC50 value of 73.5 µM.


Asunto(s)
Uvaria , Uvaria/química , alfa-Glucosidasas , Inhibidores de Glicósido Hidrolasas/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , alfa-Amilasas
9.
J Nat Prod ; 84(12): 3080-3089, 2021 12 24.
Artículo en Inglés | MEDLINE | ID: mdl-34802242

RESUMEN

Five new cyclohexene derivatives, dipandensin A and B (1 and 2) and pandensenols A-C (3-5), and 16 known secondary metabolites (6-21) were isolated from the methanol-soluble extracts of the stem and root barks of Uvaria pandensis. The structures were characterized by NMR spectroscopic and mass spectrometric analyses, and that of 6-methoxyzeylenol (6) was further confirmed by single-crystal X-ray crystallography, which also established its absolute configuration. The isolated metabolites were evaluated for antibacterial activity against the Gram-positive bacteria Bacillus subtilis and Staphylococcus epidermidis and the Gram-negative bacteria Enterococcus raffinosus, Escherichia coli, Paraburkholderia caledonica, Pectobacterium carotovorum, and Pseudomonas putida, as well as for cytotoxicity against the MCF-7 human breast cancer cell line. A mixture of uvaretin (20) and isouvaretin (21) exhibited significant antibacterial activity against B. subtilis (EC50 8.7 µM) and S. epidermidis (IC50 7.9 µM). (8'α,9'ß-Dihydroxy)-3-farnesylindole (12) showed strong inhibitory activity (EC50 9.8 µM) against B. subtilis, comparable to the clinical reference ampicillin (EC50 17.9 µM). None of the compounds showed relevant cytotoxicity against the MCF-7 human breast cancer cell line.


Asunto(s)
Ciclohexenos/química , Oxígeno/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Tallos de la Planta/química , Uvaria/química , Cristalografía por Rayos X/métodos , Ciclohexenos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Células MCF-7 , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química
10.
BMC Complement Med Ther ; 21(1): 234, 2021 Sep 18.
Artículo en Inglés | MEDLINE | ID: mdl-34537049

RESUMEN

BACKGROUND: Uvaria chamae (UC) and Olax subscorpioidea (OS) roots are included in traditional anti-cancer remedies and some studies have identified their chemopreventive/chemotherapeutic potential. This study aimed to identify some cellular/molecular mechanisms underlying such potential and the associated chemical constituents. METHODS: Effect on the viability of cancer cells was assessed using the Alamar Blue assay; ability to modulate oxidative stress was assessed using the 2',7'-dichlorofluorescein diacetate (DCFDA) assay; potential to modulate Nuclear factor erythroid 2-related factor like-2 (Nrf2) activity was assessed in the AREc32 luciferase reporter cell line; and anti-inflammatory effect was assessed using lipopolysaccharide-induced nitric oxide release model in the RAW264.7 cells (Griess Assay). Chemical constituents were identified through liquid chromatography-mass spectrometry (LC-MS). RESULTS: Extracts up to 100 µg/ml were non-toxic or mildly toxic to HeLa, AREc32, PC3 and A549 cells (IC50 > 200 µg/ml). Each extract reduced basal and peroxide-induced levels of reactive oxygen species (ROS) in HeLa cells. OS and UC activated Nrf2, with UC producing nearly four-fold induction. Both extracts demonstrated anti-inflammatory effects. Chamanetin, isochamanetin, isouvaretin, uvaricin I and other compounds were found in U. chamae root extract. CONCLUSION: As Nrf-2 induction, antioxidant and anti-inflammatory activities are closely linked with chemoprevention and chemotherapy of cancers, the roles of these plants in traditional anti-cancer remedies are further highlighted, as is their potential as sources of drug leads.


Asunto(s)
Antineoplásicos/farmacología , Doxorrubicina/farmacología , Neoplasias/tratamiento farmacológico , Olacaceae/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Uvaria/química , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antineoplásicos/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Factores de Transcripción con Cremalleras de Leucina de Carácter Básico/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas/efectos de los fármacos , Doxorrubicina/uso terapéutico , Humanos , Extractos Vegetales/química , Raíces de Plantas/química , Plantas Medicinales/química , Streptomyces/química
11.
Bioorg Chem ; 116: 105333, 2021 11.
Artículo en Inglés | MEDLINE | ID: mdl-34537516

RESUMEN

Natural products--polyoxygenated cyclohexenes exhibited potent anti-tumor activity, such as zeylenone, which is a natural product isolated from Uvaria grandiflora Roxb. This article will attempt to establish a gram-scale synthesis method of (+)-zeylenone and explain the structure-activity relationship of this kind of compound. Total synthesis of (+)-zeylenone was completed in 13 steps with quinic acid as the starting material in 9.8% overall yield. The highlight of the route was the control of the three carbon's chirality by single step dihydroxylation. In addition, different kinds of derivatives were designed and synthesized. Cell Counting Kit-8 (CCK8) assay was used for evaluating antitumor activity against three human cancer cell lines. The structure--activity relationship suggested that compounds with both absolute configurations exhibited tumor-suppressive effects. Moreover, hydroxyls at the C-1/C-2 position were crucial to the activity, and the esterification of large groups at C-1 hydroxyl eliminated the activity. Hydroxyl at the C-3 position was also important as proper ester substituent could increase the potency.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Ciclohexanos/farmacología , Dioxanos/farmacología , Uvaria/química , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Ciclohexanos/química , Ciclohexanos/aislamiento & purificación , Dioxanos/química , Dioxanos/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Ratones , Estructura Molecular , Estereoisomerismo , Relación Estructura-Actividad , Células Tumorales Cultivadas
12.
J Ethnopharmacol ; 271: 113863, 2021 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-33485972

RESUMEN

ETHNOPHARAMCOLOGICAL RELEVANCE: The age-long folkloric use of Uvaria chamae roots in the management of nipple discharge that is not related to pregnancy, childbirth or nursing but as a result of excessive production of prolactin (hyperprolactinemia) is yet to be substantiated with scientific data. AIM OF THE STUDY: This study investigated the anti-hyperprolactinemic activities of aqueous extract of Uvaria chamae roots (AEUCR) and associated biochemical changes in chlorpromazine (CPZ)-induced hyperprolactinemic female Wistar rats. MATERIALS AND METHODS: A total of sixty female rats (207.40 ± 2.69 g) were assigned into 6 groups: A-F. Animals in Group A received 0.5 ml of distilled water only whilst the 7 days CPZ-treated female rats (to induce hyperprolactinemia) in groups B, C, D, E, and F also received distilled water, 2.5 mg/kg body weight of bromocriptine (reference drug), 0.71, 1.41 2.83 mg/kg body weight of AEUCR for 28 days. RESULTS: AEUCR contained a total of 15 (75%) amino acids with seven (46.67%) being essential amino acids and eight (53.33%) as non-essential amino acids. Administration of CPZ increased (p < 0.05) the levels of prolactin and testosterone, and reduced (p < 0.05) the levels of estradiol, progesterone, follicle stimulating hormone (FSH), luteinizing hormone (LH), dopamine, triiodothyronine (T3) and tetraiodothyroxine (T4). Chlorpromazine also increased the levels of serum urea, creatinine, total protein, albumin, globulin, bilirubin, alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) of the animals. In contrast, AEUCR significantly (p < 0.05) reduced the CPZ-induced increases in the levels of prolactin and testosterone, and increased the levels of CPZ-induced reduction in the progesterone, estradiol, FSH, LH, dopamine, T3 and T4. The AEUCR also reversed (p < 0.05) the CPZ-induced related increases in the levels of urea, creatinine, total protein, albumin, globulin, bilirubin, ALT, AST and ALP similar to the trends in the distilled water- and bromocriptine-treated controls. The CPZ-induced remarkable increase in the size of lactating alveolus and lactiferous duct distribution in the mammary gland were restored to normal tubule-alveolar female pattern mammary glands, composed of branching ducts and small alveoli budding off the ducts. CONCLUSION: The study concluded that aqueous extract of Uvaria chamae root exhibited anti-hyperprolactinemic activity by restoring prolactin and dopamine levels and tubule-alveolar female pattern in female rats. It also ameliorated CPZ-induced changes in the liver and kidney function indices. This study justifies the folkloric use of Uvaria chamae root in the management of abnormal discharge by the nipples that is unrelated to pregnancy, childbirth and nursing.


Asunto(s)
Hiperprolactinemia/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Raíces de Plantas/química , Uvaria/química , Animales , Clorpromazina/toxicidad , Estradiol/metabolismo , Femenino , Hormona Folículo Estimulante/metabolismo , Humanos , Hiperprolactinemia/inducido químicamente , Riñón/efectos de los fármacos , Hígado/efectos de los fármacos , Hormona Luteinizante/metabolismo , Glándulas Mamarias Humanas/efectos de los fármacos , Glándulas Mamarias Humanas/patología , Medicina Tradicional , Extractos Vegetales/farmacología , Progesterona/metabolismo , Prolactina/metabolismo , Ratas Wistar , Testosterona/metabolismo , Hormonas Tiroideas/metabolismo , Agua/química
13.
Nat Prod Res ; 35(1): 140-143, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31184502

RESUMEN

The present study focuses on the emitted and endogenous scent profiles of Uvaria hamiltonii flowers. Among the 34 compounds identified, sesquiterpenoids were found to dominate the floral volatiles composition. Profiles from endogenous scent volatiles showed higher number of compounds than the emitted ones. The anthocyanin pigment responsible for the flower colour was also explored. It was found that a single anthocyanin compound, cyanidin-3-O-glucoside, was principally responsible for petal colour. Total phenolic content was evaluated and antioxidant capacities were studied with the help of DPPH, FRAP and ABTS assays. The total phenolic content and the antioxidant capacity were higher in methanolic extract as compared to aqueous, petroleum ether and ethyl acetate extracts of U. hamiltonii flowers.


Asunto(s)
Antocianinas/metabolismo , Flores/fisiología , Uvaria/química , Uvaria/metabolismo , Compuestos Orgánicos Volátiles/metabolismo , Antocianinas/análisis , Antioxidantes/análisis , Antioxidantes/química , Flores/química , Odorantes/análisis , Fenoles/análisis , Pigmentación , Extractos Vegetales/química , Compuestos Orgánicos Volátiles/análisis
14.
Nat Prod Res ; 35(15): 2476-2481, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-31631698

RESUMEN

A new farnesylindole, (R)-3-(8'-hydroxyfarnesyl)-indole (1), as a scalemic mixture (33% ee) along with nine known compounds (2-10), including one farnesylindole, three flavanones, three flavone derivatives and two chalcone derivatives were isolated from the methanolic crude extract of the flowers from Anomianthus dulcis. All compounds were purified by appropriate chromatographic techniques and their structures elucidated by spectroscopic methods. Compounds 1, 2 and 8 showed moderate antiplasmodial activities against TM4/8.Two and K1CB1 strains of which compound 2 displayed the best activity with IC50 values of 27.9 ± 2.57 and 21.4 ± 1.68 µM, respectively. In addition, compound 1 also presented modest cytotoxicity against a KB cell line with an IC50 value of 22.3 ± 0.39 µM. None of these compounds showed cytotoxicity against Vero cells.


Asunto(s)
Antimaláricos , Indoles/farmacología , Extractos Vegetales , Uvaria/química , Animales , Antimaláricos/aislamiento & purificación , Antimaláricos/farmacología , Chlorocebus aethiops , Flores/química , Indoles/aislamiento & purificación , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Plasmodium falciparum , Células Vero
15.
Recent Pat Biotechnol ; 14(4): 295-311, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32885765

RESUMEN

BACKGROUND: Snakebite envenomation is a global priority ranked top among other neglected tropical diseases. There is a folkloric claim that Uvaria chamae is beneficial for the management of snakebite and wounds in African ethnobotanical surveys. Besides, there are many registered patents asserting the health benefits of U. chamae. OBJECTIVE: This study aimed to investigate U. chamae's potentials and identify candidates for the development of tools for the treatment and management of N. nigricollis envenomation. METHODS: Freshly collected U. chamae leaves were air-dried, powdered, and extracted in methanol. The median lethal dose of the extract was determined and further fractionated with n-hexane, n-butanol and ethyl acetate. Each fraction was tested for neutralizing effect against venom-induced haemolytic, fibrinolytic, hemorrhagic, and cytotoxic activities. RESULTS: U. chamae fractions significantly (p<0.05) neutralized the haemolytic activity of N. nigricollis venom in n-butanol; 31.40%, n-hexane; 33%, aqueous residue; 39.60% and ethyl acetate; 40.70% at the concentration of 100mg/ml of each fraction against 10mg/ml of the snake venom when compared to the positive control. The fibrinolytic activity of N. nigricollis venom was significantly (p<0.05) neutralized in n-hexane at 73.88%, n-butanol; 72.22% and aqueous residue; 72.22% by the fractions of U. chamae. In addition, haemorrhagic activity of N. nigricollis venom was significantly (p<0.05) neutralized by U. chamae fractions at the concentrations of 100mg/ml, 200mg/ml and 400mg/ml except for n-butanol and aqueous residues at 400 mg/ml. CONCLUSION: U. chamae leaves fractions possess a high level of protection against N. nigricollis venoms-induced lethality and thus validate the pharmacological rationale for its usage in the management of N. nigricollis envenomation.


Asunto(s)
Antivenenos/farmacología , Extractos Vegetales/farmacología , Mordeduras de Serpientes/fisiopatología , Uvaria/química , Animales , Antifibrinolíticos/farmacología , Bovinos , Femenino , Hemólisis/efectos de los fármacos , Hemorragia/metabolismo , Masculino , Naja , Patentes como Asunto , Hojas de la Planta/química , Sustancias Protectoras/farmacología , Ratas , Ratas Wistar , Venenos de Serpiente/sangre , Venenos de Serpiente/metabolismo
16.
Inflammopharmacology ; 28(5): 1195-1218, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32617790

RESUMEN

The therapeutic efficacy of the contemporary anti-inflammatory drugs are well established; however, prolonged use of such can often lead to serious and life-threatening side effects. Natural product-based anti-inflammatory compounds with superior efficacy and minimum toxicity can serve as possible therapeutic alternatives in this scenario. Genus Uvaria is a part of Annonaceae family, while the majority of its species are widely distributed in tropical rain forest regions of South East Asia. Uvaria species have been used extensively used as traditional medicine for treating all sorts of inflammatory diseases including catarrhal inflammation, rheumatism, acute allergic reactions, hemorrhoids, inflammatory liver disease and inflamed joints. Phytochemical analysis of Uvaria species has revealed flavones, flavonoids, tannins, saponins, polyoxygenated cyclohexene and phenolic compounds as major phyto-constituents. This review is an attempt to highlight the anti-inflammatory activity of Uvaria species by conducting a critical appraisal of the published literature. The ethnopharmacological relevance of Uvaria species in the light of toxicological studies is also discussed herein. An extensive and relevant literature on anti-inflammatory activity of Uvaria species was collected from available books, journals and electronic databases including PubMed, ScienceDirect, Scopus, Proquest and Ovid. Extracts and isolates of Uvaria species exhibited significant anti-inflammatory activity through various mechanisms of action. 6,7-di-O-Methyl-baicalein, flexuvarol B, chrysin, (-)-zeylenol, 6-hydroxy-5,7-dimethoxy-flavone, and pinocembrin were the most potent anti-inflammatory compounds with comparable IC50 with positive controls. Therefore, it is suggested that further research should be carried out to determine the pharmacokinetics, pharmacodynamics and toxicity of these therapeutically significant compounds, to convert the pre-clinical results into clinical data for drug development and design.


Asunto(s)
Inflamación/tratamiento farmacológico , Extractos Vegetales/farmacología , Uvaria/química , Animales , Antiinflamatorios/farmacología , Humanos , Medicina Tradicional/métodos , Fitoquímicos/farmacología , Fitoterapia/métodos
17.
BMC Vet Res ; 16(1): 49, 2020 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-32041607

RESUMEN

BACKGROUND: Uvaria chamae (Annonaceae), Phyllantus amarus (Phyllantaceae) and Lantana camara (Verbenaceae) are empirically alleged to be used as Beninese medicinal plants in the treatment of salmonellosis. This study aimed to produce scientific data on in vitro and in vivo efficacy of Uvaria chamae, Lantana camara and Phyllantus amarus on multiresistant Salmonella spp isolated in Benin. RESULTS: After performing in vitro tests on aqueous and ethanolic extracts of these plants, only the aqueous extract of Uvaria chamae (leaves) showed the best anti-Salmonella's activity and was used for this in vivo experiment. The induction of salmonellosis revealed 9 × 108 CFU/ml was the optimal concentration triggering and maintaining symptoms in chicks. This infective concentration was used for in vivo assessment. Twenty-four hours post inoculation, the symptoms of salmonellosis (wet cloaca, diarrhea stools and somnolence) were observed in infected groups. After 7 days of treatment, the reduction of bacterial load at 100 mg/L, 200 mg/L, 400 mg/L of the extract was respectively 85%, 52.38% and 98% for Uvaria chamae, Phyllantus amarus and Lantana camara in the chick's groups infected with Salmonella Typhimurium ATCC 14028. On the other hand, colistin completely cancelled the bacterial load (reduction rate of 100%). With the groups infected with Salmonella spp (virulent strain), the reduction rate of bacterial load at 100 mg/L, 200 mg/L, 400 mg/L of extract was 0%, 98.66%, and 99.33%. The extracts at 200 and 400 mg/L were more active than colistin, which reduced the bacterial load by 33.33%. The toxicity tests did not show any negative effect of Colistin and the Uvaria chamae's extract on the biochemical and hematological parameters of the chicks. CONCLUSION: The aqueous extract of Uvaria chamae is active in vitro and in vivo on multiresistant strains of Salmonella enterica. This plant is a good candidate for the development of an improved traditional medicine for the management of salmonellosis.


Asunto(s)
Lantana/química , Malpighiales/química , Extractos Vegetales/farmacología , Enfermedades de las Aves de Corral/tratamiento farmacológico , Salmonella/efectos de los fármacos , Uvaria/química , Animales , Benin , Pollos , Extractos Vegetales/química , Plantas Medicinales , Enfermedades de las Aves de Corral/microbiología , Salmonelosis Animal/tratamiento farmacológico , Salmonelosis Animal/microbiología
18.
Nat Prod Res ; 34(17): 2495-2499, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-30580591

RESUMEN

The phytochemical investigation of the leaf extracts of Uvaria hamiltonii (Annonaceae) led to the isolation and identification of ten compounds including a new seco-cyclohexene (1) together with nine known compounds (2-10). Their structures were elucidated by intensive analysis by spectroscopic methods and comparisons of their spectroscopic data with those of compounds reported in the literature. Compounds 2, 8, and 9 showed potent α-glucosidase inhibitory activity with the IC50 values ranging from 2.6-7.1 µM.


Asunto(s)
Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Extractos Vegetales/química , Uvaria/química , Annonaceae/química , Ciclohexenos/aislamiento & purificación , Ciclohexenos/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Estructura Molecular , Fitoquímicos/análisis , Fitoquímicos/farmacología , Hojas de la Planta/química , Análisis Espectral , alfa-Glucosidasas/efectos de los fármacos
19.
Nat Prod Res ; 34(6): 880-883, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30445869

RESUMEN

Uvaria chamae (Annonaceae), is an essential oil bearing plant; the root is acclaimed as an effective remedy for folkloric diabetic therapy. The root extracts were evaluated for composition, antiglycation, antioxidant, and cytotoxicity. Flavonoids, cardiac glycosides, and tannins were relatively high in the alcohol extract; benzyl benzoate (23.3%), dimethoxy-p-cymene (14.2%), τ-cadinol (12.1%), and methyl thymol (8.7%) predominated the constituents identified by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The ethanol extract demonstrated significant antiglycation activity (IC50, 1.12 mg/mL), and cytotoxicity to brine shrimp (LC50, 25.01 µg/mL). The extract (IC50, 8.0 µg/mL; absorbance 0.531, 100 µg/mL) also exhibited better antioxidant effects compared with the essential oil (IC50, 50.0 µg/mL; absorbance 0.292, 100 µg/mL) using 2,2-diphenyl-1-picrylhydrazyl radical and ferric reducing power assays respectively. U. chamae root possess antiglycation effect, and may also reduce oxidative stress in patients with diabetes; its antiglycation effect, oil composition, and cytotoxicity are reported for the first time.[Formula: see text].


Asunto(s)
Aceites Volátiles/química , Extractos Vegetales/química , Raíces de Plantas/química , Uvaria/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Cromatografía de Gases y Espectrometría de Masas , Humanos , Extractos Vegetales/farmacología , Polisacáridos/antagonistas & inhibidores , Terpenos
20.
Artículo en Inglés | MEDLINE | ID: mdl-31747375

RESUMEN

Garcinia kola (GK) stem bark, Uvaria chamae (UC) root, and Olax subscorpioidea (OS) root are components of various indigenous/traditional anticancer regimens. It is, therefore, possible that they might combat oxidative stress and impair cellular proliferation linked to carcinogenesis. In this study, we investigated the antioxidative, mito-depressive, and DNA-damaging activities of the three plant extracts in order to provide further mechanistic insights into their potential anticancer roles in documented cancer remedies that include them. Antioxidative properties were investigated in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging assays and an animal model of drug (cisplatin)-induced oxidative stress. The Allium cepa assay and the single cell gel electrophoresis (SCGE) assay were used to assess mito-depressive and DNA-damaging activities. GK and OS showed significantly higher antioxidant activities in the DPPH assay than ascorbic acid; OS had the lowest IC50 of the three plants in the NO assay, comparable to that of ascorbic acid. Pretreatment with the extracts produced an ameliorative and protective effect against the cisplatin-induced oxidative stress as shown by inhibition of lipid peroxidation and improved or restored reduced glutathione and superoxide dismutase levels. In the Allium test, the three extracts produced significant decreases in root growth and also significant cytotoxicity as evidenced by decreased mitotic index. Each of the extracts also showed significantly increased tail DNA (%) in the SCGE assay, indicating the significant DNA-damaging effect. Taken together, this study demonstrates the possible chemopreventive and chemotherapeutic potentials of the three study extracts, which may explain the roles of their source plants in traditional remedies in the therapy of cancers.


Asunto(s)
Antimitóticos/farmacología , Antioxidantes/farmacología , Daño del ADN/efectos de los fármacos , Garcinia kola/química , Neoplasias/tratamiento farmacológico , Tallos de la Planta/química , Uvaria/química , Animales , Compuestos de Bifenilo/farmacología , Glutatión/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Masculino , Ratones , Estrés Oxidativo/efectos de los fármacos , Corteza de la Planta/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Ratas , Ratas Sprague-Dawley
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