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1.
AAPS PharmSciTech ; 25(5): 107, 2024 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-38730121

RESUMEN

Treatment therapies used to manage osteoporosis are associated with severe side effects. So worldwide herbs are widely studied to develop alternative safe & effective treatments. Cissus quadrangularis (CQ) has a significant role in bone health and fracture healing. It is documented that its extracts increase osteoblastic differentiation & mineralization. Currently, Cissus quadrangularis is available in the form of tablets in the market for oral delivery. But these conventional forms are associated with poor bioavailability. There is a need for a novel drug delivery system with improving oral bioavailability. Therefore, a Cissus quadrangularis-loaded self-emulsifying drug delivery system (CQ-SEDDS) was developed which disperses rapidly in the gastrointestinal fluids, yielding nano-emulsions containing a solubilized drug. This solubilized form of the drug can be easily absorbed through lymphatic pathways and bypass the hepatic first-pass effect. The emulsification efficiency, zeta potential, globule size, in-vitro dissolution, ex-vivo, in-vivo and bone marker studies were performed to assess the absorption and permeation potential of CQ incorporated in SEDDS. CQ-SEDDS with excipients Tween 80, Cremophor RH40, Transcutol HP & α-Tocopherol acetate had shown about 76% enhancement in the bioavailability of active constituents of CQ. This study provided the pre-clinical data of CQ-SEDDS using osteoporotic rat model studies.


Asunto(s)
Disponibilidad Biológica , Cissus , Sistemas de Liberación de Medicamentos , Emulsiones , Osteoporosis , Animales , Osteoporosis/tratamiento farmacológico , Ratas , Cissus/química , Sistemas de Liberación de Medicamentos/métodos , Femenino , Administración Oral , Excipientes/química , Solubilidad , Extractos Vegetales/farmacocinética , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Tamaño de la Partícula , Ratas Sprague-Dawley
2.
J Mater Sci Mater Med ; 34(7): 33, 2023 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-37466722

RESUMEN

Natural medicines plants are significant considerable attention as potential therapeutic agents for bone tissue engineering. Cissus quadrangularis L (CQ). is a potent therapeutic plant known for its own osteogenic properties. In this research work, a phytoconstituents-filled composite was produced by incorporating CQ extract with gelatin (Gel) and pectin (Pec) polymers collective through ß- tricalcium phosphate (ß-TCP) bioceramic via a green template method. The effect of CQ-filled composite morphology and chemical structural properties, in vitro cytotoxicity, cell proliferation, and differentiation was investigated. FTIR spectroscopic results indicated the prepared materials' structural confirmation. The CQ extract was the alcoholic -OH merge with the hydroxyl and -NH groups in the range of 3000 cm-1 to 3500 cm-1. Scanning electron microscopy images showed that the ß-TCP ceramic was perfectly embedded in Gel-Pec polymeric matrix, which is important for bone regeneration. In vitro cell culture results indicated that ß-TCP/Gel-Pec/CQ composite provided 92.0% of a favorable substrate for mesenchymal stem cell viability. The gene expression and RT-PCR studies represent the materials with good osteogenic expression, especially the ß-TCP/Gel-Pec/CQ composite is observed at 168.0% and 188.0% for RUNx2 and OCN, respectively. The result of the physicochemical characterizations and cell viability studies suggest that CQ-loaded ß-TCP/Gel-Pec composite can serve as a potential biomaterial for bone tissue repair and regeneration.


Asunto(s)
Cissus , Cissus/química , Polímeros/farmacología , Regeneración Ósea , Fosfatos de Calcio/química , Osteogénesis , Diferenciación Celular
3.
Cancer Treat Res Commun ; 36: 100732, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37379774

RESUMEN

Cissus quadrangularis plant from Vitaceae family, native in India. Many parts of this plant have medicinal values but most precious is stem of this plant. In past years number of studies reported their activities and secondary metabolites in Cissus quadrangularis plant and their pharmacological activities and uses in traditional medicine system. It is reported to possess excellent medicinal properties and potent fracture healing properties, antimicrobial, antiulcer, antioxidative, cholinergic activity and beneficial effect on cardiovascular diseases, possesses antiulcer and cytoprotective property in indomethacin-induced gastric mucosal injury. The aim of this study was to determine the qualitative phytochemical analysis, antimicrobial activity, cell viability and in vitro anticancer activity of a potential of Cissus quadrangularis stem extract against A549 human lung cancer cell line. The disc diffusion method was employed to determine the antimicrobial activity of Cissus quadrangularis stem extract and showed potential antibacterial and antifungal activity against various microorganisms. Results have shown that Stem methanolic extract induced a significant decrease of tumour cell viability. The cell viability assay clearly showed that the cells treated with Cissus quadrangularis methanolic extract has significantly reduced the lung cancer cell viability in a dose dependant manner. The stem methanolic extract was tested for the in vitro antiproliferative potential on A549 human lung cancer cell line using different concentrations, namely 1000, 62.5 and 7.8 µg/ml. We observed the IC50 dose at 65.2 µg/ml concentration. In cell culture A549 cells treated with Cissus quadrangularis stem methanolic extract in 24 h the cells growth is controlled.


Asunto(s)
Cissus , Neoplasias Pulmonares , Humanos , Cissus/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Línea Celular , Antibacterianos/uso terapéutico , Neoplasias Pulmonares/tratamiento farmacológico
4.
Chem Biodivers ; 20(1): e202200678, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-36480444

RESUMEN

Purification through repeated column chromatography over silica gel and Sephadex LH-20 of the ethanol extract of the stems of Cissus aralioides (Baker) Planch. resulted in the isolation of a new ceramide, aralioidamide A (1), along with five known compounds (2-6). Their structures were determined by the extensive analyses of their spectroscopic (1D and 2D NMR) and spectrometric data, and comparison with those reported in the literature. Aralioidamide A (1) displayed weak antibacterial activity (MIC=256 µg/mL) against Bacillus subtilis, Staphylococcus aureus and Shigella flexneri and was inactive (MIC>256 µg/mL) against the tested fungi.


Asunto(s)
Cissus , Vitaceae , Cissus/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Ceramidas/farmacología , Antibacterianos/química , Pruebas de Sensibilidad Microbiana
5.
BMC Oral Health ; 22(1): 377, 2022 09 05.
Artículo en Inglés | MEDLINE | ID: mdl-36064680

RESUMEN

BACKGROUND: Over the past years, polysaccharide-based scaffolds have emerged as the most promising material for tissue engineering. In the present study, carrageenan, an injectable scaffold has been used owing to its advantage and superior property. Cissus quadrangularis, a natural agent was incorporated into the carrageenan scaffold. Therefore, the present study aimed to assess the antioxidant activity and biocompatibility of this novel material. METHODS: The present in vitro study comprised of four study groups each constituting a sample of 15 with a total sample size of sixty (n = 60). The carrageenan hydrogel devoid of Cissus quadrangularis acted as the control group (Group-I). Based on the concentration of aqueous extract of Cissus quadrangularis (10% w/v, 20% w/v and 30% w/v) in carrageenan hydrogel, respective study groups namely II, III and IV were considered. Antioxidant activity was assessed using a 1,1-diphenyl-2-picrylhydrazyl radical scavenging assay, whereas the biocompatibility test was performed using a brine shrimp lethality assay. The microstructure and surface morphology of the hydrogel samples containing different concentrations of Cissus quadrangularis aqueous extract was investigated using SEM. One-way ANOVA with the post hoc tukey test was performed using SPSS software v22. RESULTS: A significant difference (P < 0.05) in the antioxidant activity was observed among the study groups. Group III reported the highest activity, whereas the control group showed the least antioxidant activity. Additionally, a significant (P < 0.01) drop in the antioxidant activity was observed in group IV when compared with group III. While assessing the biocompatibility, a significant (P < 0.001) dose-dependent increase in biocompatibility was observed with the increasing concentration of aqueous extract of Cissus quadrangularis. SEM analysis in group III showed even distribution throughout the hydrogel although the particles are close and densely arranged. Reduced antioxidant activity in group IV was probably due to clumping of the particles, thus reducing the active surface area. CONCLUSION: Keeping the limitations of in vitro study, it can be assumed that a carrageenan based injectable hydrogel scaffold incorporated with 20% w/v Cissus quadrangularis can provide a favourable micro-environment as it is biocompatible and possess better antioxidant property.


Asunto(s)
Cissus , Antioxidantes/farmacología , Carragenina , Cissus/química , Humanos , Hidrogeles , Extractos Vegetales/farmacología
6.
Biomarkers ; 27(8): 743-752, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-35896310

RESUMEN

BACKGROUND: Diabetic cardiomyopathy (DCM) is an age-related disease, and its progression is accompanied by hyperglycaemia, cardiac dysfunction, and myocardial structural and functional abnormalities. Cissus quadrangularis, a traditional medicinal plant, contains polyphenols, flavonoids, phytosterols, carbohydrates and ascorbic acid. It is used to treat osteoporosis, asthma, haemorrhoids and menstrual disorders.Objective: In the current research, we have investigated the effect of ethanolic extract of C. quadrangularis (EECQ) against a high-fat diet (HFD)/streptozotocin-induced DCM by estimating cardiac biomarkers, inflammatory markers and Reactive oxygen species (ROS) production. MATERIAL AND METHODS: Rats were fed with an HFD for 12 weeks, followed by single-shot low-dose streptozotocin (35 mg/kg; i.p.). The treatment was performed by EECQ (200 mg/kg/day, orally) for six weeks. RESULTS: The extract EECQ improves glucose, insulin tolerance tests and hypercholesteremia. DCM is characterized by cardiac dysfunction, cardiac biomarkers CKMB and LDH, which were attenuated by the EECQ treatment. The hypertrophic biomarker ANP, BNP expression and cardiomyocyte surface area were decreased by EECQ. Moreover, EECQ also alleviated the biomarkers Angiotensin II and renin level. EECQ also reduced oxidative stress, ROS production and cardiac inflammation. CONCLUSIONS: Thus, these findings suggested that EECQ could be used as a possible therapeutic regiment to treat DCM.


Cissus quadrangularis ameliorates hyperglycaemia, hyperinsulinemia and hyperlipidaemia.Cissus quadrangularis mitigates cardiac dysfunction.Cissus quadrangularis decreases RAAS activation, thereby down-regulates ANP, BNP expression.Cissus quadrangularis alleviates ROS propagated oxidative stress and apoptosis.


Asunto(s)
Cissus , Diabetes Mellitus , Cardiomiopatías Diabéticas , Ratas , Animales , Cissus/química , Estreptozocina/farmacología , Cardiomiopatías Diabéticas/tratamiento farmacológico , Especies Reactivas de Oxígeno , Sistema Renina-Angiotensina , Extractos Vegetales/farmacología , Extractos Vegetales/química , Estrés Oxidativo , Inflamación/tratamiento farmacológico , Etanol/farmacología , Diabetes Mellitus/tratamiento farmacológico
7.
Appl Biochem Biotechnol ; 194(1): 232-245, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34800282

RESUMEN

Cissus rotundifolia has been reported to possess various biological activities such as anti-diabetic, anti-fertility, anti-hyperlipidemic, anti-malarial, anti-osteoporotic, and anti-parasitic activities. Therefore in the present study, eleven selected constituents of Cissus rotundifolia which includes aconitic acid, astragalin, acteoside, aliospiroside A, beta amyrin, bergenin, formononetin, gallic acid, isovitexin, isoorientin, and isoquercitrin were studied on the docking behavior of human neutrophil elastase (HNE), matrix metalloproteinases (MMP 2 and MMP 9), and tyrosinase by using PatchDock method. Furthermore, molecular physicochemical, bioactivity score/drug-likeness, ADME (absorption, distribution, metabolism, and excretion), and toxicity analyses were also carried out using Molinspiration, Swiss ADME, and ProTox-II methods, respectively. The molecular physicochemical investigation showed that three ligands such as acteoside, aliospiroside A, and isoorientin have three violations for Lipinski's rule of five. Similarly, ADME analysis one ligand (formononetin) predicated to have high blood-brain barrier (BBB) permeability effect. The docking studies showed that isovitexin exhibited the highest atomic contact energy (-341.61 kcal/mol) for human neutrophil elastase (HNE), more over alliospiroside A has shown maximum atomic contact energy for both matrix metalloproteinases (MMP 2 [-618.00 kcal/mol] and MMP 9 [-634.73 kcal/mol]). Furthermore, isoquercitrin has exhibited the highest atomic contact energy (-145.70 kcal/mol) for tyrosinase. Thus, the present investigation outcome provides new knowledge in understanding eleven Cissus rotundifolia constituents as possible novel inhibitors against HNE, MMP 2, MMP 9, and tyrosinase.


Asunto(s)
Cissus/química , Inhibidores Enzimáticos/química , Elastasa de Leucocito , Metaloproteinasa 2 de la Matriz/química , Metaloproteinasa 9 de la Matriz/química , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa , Humanos , Elastasa de Leucocito/antagonistas & inhibidores , Elastasa de Leucocito/química , Monofenol Monooxigenasa/antagonistas & inhibidores , Monofenol Monooxigenasa/química
8.
Molecules ; 26(19)2021 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-34641616

RESUMEN

Several Cissus species have been used and reported to possess medicinal benefits. However, the anti-inflammatory mechanisms of Cissus subtetragona have not been described. In this study, we examined the potential anti-inflammatory effects of C. subtetragona ethanol extract (Cs-EE) in vitro and in vivo, and investigated its molecular mechanism as well as its flavonoid content. Lipopolysaccharide (LPS)-induced macrophage-like RAW264.7 cells and primary macrophages as well as LPS-induced acute lung injury (ALI) and HCl/EtOH-induced acute gastritis mouse models were utilized. Luciferase assays, immunoblotting analyses, overexpression strategies, and cellular thermal shift assay (CETSA) were performed to identify the molecular mechanisms and targets of Cs-EE. Cs-EE concentration-dependently reduced the secretion of NO and PGE2, inhibited the expression of inflammation-related cytokines in LPS-induced RAW264.7 cells, and decreased NF-κB- and AP-1-luciferase activity. Subsequently, we determined that Cs-EE decreased the phosphorylation events of NF-κB and AP-1 pathways. Cs-EE treatment also significantly ameliorated the inflammatory symptoms of HCl/EtOH-induced acute gastritis and LPS-induced ALI mouse models. Overexpression of HA-Src and HA-TAK1 along with CETSA experiments validated that inhibited inflammatory responses are the outcome of attenuation of Src and TAK1 activation. Taken together, these findings suggest that Cs-EE could be utilized as an anti-inflammatory remedy especially targeting against gastritis and acute lung injury by attenuating the activities of Src and TAK1.


Asunto(s)
Lesión Pulmonar Aguda/tratamiento farmacológico , Antiinflamatorios/administración & dosificación , Cissus/química , Etanol/efectos adversos , Gastritis/tratamiento farmacológico , Ácido Clorhídrico/efectos adversos , Lipopolisacáridos/efectos adversos , Macrófagos/citología , Polifenoles/administración & dosificación , Lesión Pulmonar Aguda/inducido químicamente , Lesión Pulmonar Aguda/genética , Administración Oral , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Citocinas/genética , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Gastritis/inducido químicamente , Gastritis/genética , Regulación de la Expresión Génica/efectos de los fármacos , Células HEK293 , Humanos , Quinasas Quinasa Quinasa PAM/genética , Quinasas Quinasa Quinasa PAM/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/inmunología , Masculino , Ratones , Extractos Vegetales/química , Polifenoles/química , Células RAW 264.7 , Transducción de Señal/efectos de los fármacos , Resultado del Tratamiento , Familia-src Quinasas/genética
9.
Curr Top Med Chem ; 21(26): 2409-2424, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34503406

RESUMEN

BACKGROUND: Cissus incisa is a Vitaceae with a pantropical distribution. In northern Mexico, its leaves have traditionally been used to treat skin infections, abscesses and tumors. Despite its medicinal uses, few studies have been reported. OBJECTIVE: The objective of this study is to summarize the phytochemical and biological studies carried out so far on the leaves of C. incisa, since this part of the plant is the one frequently used, and awaken scientific interest towards the plant. METHODS: Since C. incisa was an undocumented species, most of the information comes from reports of our research group. Databases, books, and websites were also consulted. The information collected was organized and presented in a synthesized way. Plant name was checked with the database "The Plant List". RESULTS: 171, 260, and 114 metabolites were identified by UHPLC-QFTOF-MS in the hexane, chloroform/ methanol, and aqueous extracts, respectively. Fatty acyls, sphingolipids, sterols, glycerolipids, prenol lipids, and terpenes are common metabolites found in these extracts. 2-(2´-hydroxydecanoyl amino)-1,3,4-hexadecanotriol-8-ene, 2,3-dihydroxypropyl tetracosanoate, ß-sitosterol, ß-sitosterol-D-glucopyranoside, α-amyrin-3-O-ß-D-glucopyranoside were also isolated and characterized. Extracts, phytocompounds and semi-synthetic derivatives showed antimicrobial activity against multi-drug resistant bacteria and various cancer cell lines. Results from Perturbation- Theory-Machine Learning-Information-Fusion model (PTMLIF), molecular docking, and vesicular contents assay identified potential targets on the cell membrane, suggesting an antibacterial mechanism of action for ceramides from C. incisa leaves. CONCLUSION: This review reports the efforts of the scientific community in authenticating species used in traditional medicine. Moreover, it gives a compendium of phytochemistry and the biological activities of the components from C. incisa leaves.


Asunto(s)
Cissus/química , Fotoquímica , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Antibacterianos , Humanos , Medicina Tradicional , Simulación del Acoplamiento Molecular
10.
J Biosci ; 462021.
Artículo en Inglés | MEDLINE | ID: mdl-34544907

RESUMEN

Contemporary demand calls for a high restorative index as an indispensable requirement for bone tissue engineering scaffolds, where therapeutic agents of natural origin function as a modulator for new bone formation become of utmost importance. The study presents a systematic investigation of the edible stem part of Cissus quadrangularis (CQ) as a natural resource of bioactive metabolites capable of invoking early biomineralization and osteogenesis in vitro. Phytochemical screening of CQ stem extracts (sequential solvent extraction: polarity hexane

Asunto(s)
Biomineralización/efectos de los fármacos , Cissus/química , Osteogénesis/efectos de los fármacos , Extractos Vegetales/farmacología , Tallos de la Planta/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Osteosarcoma , Extractos Vegetales/química , Ingeniería de Tejidos
11.
J Ethnopharmacol ; 279: 114355, 2021 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-34181958

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Cissus quadrangularis L. is a perennial herb of the Vitaceae family and is utilized comprehensively as a medicinal herb in most tropical regions by various names. This herb is documented to possess a wide-ranging ethnomedicinal uses in malaria, fever, epilepsy, gout, piles, skin diseases, colic, etc. AIM OF THE REVIEW: A organized summary of the botany, traditional uses, phytochemistry, pharmacology, toxicology, available marketed formulations and filed patents were presented to explore the future therapeutic potential and scientific potential of this herb. MATERIALS AND METHODS: For a review of the literature, various databases were searched, including PubMed, EMBASE, and Scopus etc. From, total 408 records of this herb, we have screened 155 articles consist of desired information and available as full text. Present manuscript is structured from comprehensive information on this herb from screened 155 records. Plant taxonomy was confirmed to the database "The Plant List". RESULTS: Phytochemical assessment as a whole indicated the presence of flavonoids, triterpenoids, alkaloids, saponins, iridoids, stilbenes, vitamins, steroids, and glycosides. A toxicity study revealed that its LD50 value is above 3000 mg/kg in animals indicating its safety. A variety of pharmacological studies of aerial parts of this herb by different extracts have demonstrated analgesic, anti-inflammatory, anticonvulsant, antimicrobial, anticancer, anti-osteoporotic activity and other bone-related disorders to justify its name as Hadjod. Still, the herb has been utilized in clinical practice and several patents were filed in India and US for its antiosteoporotic property. CONCLUSION: The studies on Cissus quadrangularis Linn. are extensive, but gaps still remain. The molecular mechanism, structure-activity relationship, potential synergistic and antagonistic effects of these components needs to be further elucidated. These findings suggest the need for further research on this herb for the management of several other chronic ailments.


Asunto(s)
Cissus/química , Medicina Tradicional/métodos , Extractos Vegetales/farmacología , Animales , Etnofarmacología , Humanos , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/química
12.
Molecules ; 26(8)2021 Apr 11.
Artículo en Inglés | MEDLINE | ID: mdl-33920405

RESUMEN

The bioassay-guided fractionation of a CHCl3-MeOH extract from the stems of Cissus trifoliata identified an active fraction against PC3 prostate cancer cells. The treatment for 24 h showed an 80% reduction in cell viability (p ≤ 0.05) by a WST-1 assay at a concentration of 100 µg/mL. The HPLC-QTOF-MS analysis of the fraction showed the presence of coumaric and isoferulic acids, apigenin, kaempferol, chrysoeriol, naringenin, ursolic and betulinic acids, hexadecadienoic and octadecadienoic fatty acids, and the stilbene resveratrol. The exposure of PC3 cells to resveratrol (IC25 = 23 µg/mL) for 24 h induced significant changes in 847 genes (Z-score ≥ ±2). The functional classification tool of the DAVID v6.8 platform indicates that the underlying molecular mechanisms against the proliferation of PC3 cells were associated (p ≤ 0.05) with the process of differentiation and metabolism. These findings provide experimental evidence suggesting the potential of C. trifoliata as a promising natural source of anticancer compounds.


Asunto(s)
Antineoplásicos Fitogénicos/química , Proliferación Celular/efectos de los fármacos , Cissus/química , Proteínas de Neoplasias/genética , Transcriptoma , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Apigenina/química , Apigenina/aislamiento & purificación , Apigenina/farmacología , Bioensayo , Supervivencia Celular/efectos de los fármacos , Flavanonas/química , Flavanonas/aislamiento & purificación , Flavanonas/farmacología , Flavonas/química , Flavonas/aislamiento & purificación , Flavonas/farmacología , Perfilación de la Expresión Génica , Humanos , Quempferoles/química , Quempferoles/aislamiento & purificación , Quempferoles/farmacología , Masculino , Análisis por Micromatrices , Proteínas de Neoplasias/clasificación , Proteínas de Neoplasias/metabolismo , Células PC-3 , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/aislamiento & purificación , Triterpenos Pentacíclicos/farmacología , Extractos Vegetales/química , Resveratrol/química , Resveratrol/aislamiento & purificación , Resveratrol/farmacología , Ácido Betulínico
13.
Bioorg Chem ; 109: 104745, 2021 04.
Artículo en Inglés | MEDLINE | ID: mdl-33640629

RESUMEN

The developing of antibacterial resistance is becoming in crisis. In this sense, natural products play a fundamental role in the discovery of antibacterial agents with diverse mechanisms of action. Phytochemical investigation of Cissus incisa leaves led to isolation and characterization of the ceramides mixture (1): (8E)-2-(tritriacont-9-enoyl amino)-1,3,4-octadecanetriol-8-ene (1-I); (8E)-2-(2',3'-dihydroxyoctacosanoyl amino)-1,3,4-octadecanetriol-8-ene (1-II); (8E)-2-(2'-hydroxyheptacosanoyl amino)-1,3,4-octadecanetriol-8-ene (1-III); and (8E)-2-(-2'-hydroxynonacosanoyl amino)-1,3,4-octadecanetriol-8-ene (1-IV). Until now, this is the first report of the ceramides (1-I), (1-II), and (1-IV). The structures were elucidated using NMR and mass spectrometry analyses. Antibacterial activity of ceramides (1) and acetylated derivates (2) was evaluated against nine multidrug-resistant bacteria by Microdilution method. (1) showed the best results against Gram-negatives, mainly against carbapenems-resistant Acinetobacter baumannii with MIC = 50 µg/mL. Structure-activity analysis and molecular docking revealed interactions between plant ceramides with membrane proteins, and enzymes associated with biological membranes of Gram-negative bacteria, through hydrogen bonding of functional groups. Vesicular contents release assay showed the capacity of (1) to disturb membrane permeability detected by an increase of fluorescence probe over time. The membrane disruption is not caused for ceramides lytic action on cell membranes, according in vitro hemolyticactivity results. Combining SAR analysis, bioinformatics and biophysical techniques, and also experimental tests, it was possible to explain the antibacterial action of these natural ceramides.


Asunto(s)
Acinetobacter baumannii/efectos de los fármacos , Antibacterianos/farmacología , Ceramidas/farmacología , Cissus/química , Simulación del Acoplamiento Molecular , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Ceramidas/química , Ceramidas/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Farmacorresistencia Bacteriana/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad
14.
Anticancer Agents Med Chem ; 21(18): 2536-2545, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33568037

RESUMEN

BACKGROUND: Cervical cancer is the second leading cause of cancer in women, which necessitates safe and potential therapeutic agents. OBJECTIVE: This study was designed to investigate the antiproliferative effect of ethanolic extract of Cissus quadrangularis L. (CQ) against human cervical adenocarcinoma HeLa cell line and in silico analysis of selected active agents against apoptosis executioner enzyme caspase-3. METHODS: Cell viability was analyzed in HeLa cells at different concentrations (25-300 µg/ml) of CQ extract. Reactive oxygen species (ROS) generation, cellular apoptosis, cell cycle analysis and caspases-3 activation were evaluated. In silico, structure-based virtual screening analysis was carried out using AutoDock Vina and iGEMDOCK. RESULTS: Cell viability of HeLa cells was reduced significantly (p < 0.05) in a dose-dependent manner, however, CQ extract showed non-toxic to normal kidney epithelial NRK-52E cells. CQ extract induced the intracellular ROS level, nuclear condensation and reduced the mitochondrial membrane potential (MMP) with the induction of annexin V-FITC positive cells. CQ extract arrested cells in G0/G1 and G2/M checkpoints and activated caspase-3 activity significantly in HeLa cells. The molecular docking study showed a strong binding affinity of CQ phytocomponents against the caspase-3 (PDB ID: 1GFW) protein of human apoptosis. PASS analyses of selected active components using Lipinski's Rule of five showed promising results. Further, drug-likeness and toxicity assessment using OSIRIS Data Warrior V5.2.1 software exhibited the feasibility of phytocomponents as drug candidates with no predicted toxicity. CONCLUSION: This study suggested that active constituents in CQ extract can be considered as potential chemotherapeutic candidates in the management of cervical cancer.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Cissus/química , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Neoplasias del Cuello Uterino/tratamiento farmacológico , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Células HeLa , Humanos , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células Tumorales Cultivadas , Neoplasias del Cuello Uterino/patología
15.
Sci Rep ; 11(1): 2008, 2021 01 21.
Artículo en Inglés | MEDLINE | ID: mdl-33479386

RESUMEN

Obesity is associated with the growth and expansion of adipocytes which could be decreased via several mechanisms. Cissus Quadrangularis (CQ) extract has been shown to reduce obesity in humans; however, its effect on human white adipocytes (hWA) has not been elucidated. This study aimed to investigate the effects of CQ on obesity, lipolysis, and browning of hWA. CQ treatment in obese humans significantly decreased waist circumference at week 4 and week 8 when compared with the baseline values (p < 0.05 all) and significantly decreased hip circumference at week 8 when compared with the baseline and week 4 values (p < 0.05 all). Serum leptin levels of the CQ-treated group were significantly higher at week 8 compared to baseline levels (p < 0.05). In hWA, glycerol release was reduced in the CQ-treated group when compared with the vehicle-treated group. In the browning experiment, pioglitazone, the PPAR-γ agonist, increased UCP1 mRNA when compared to vehicle (p < 0.01). Interestingly, 10, 100, and 1000 ng/ml CQ extract treatment on hWA significantly enhanced UCP1 expression in a dose-dependent manner when compared to pioglitazone treatment (p < 0.001 all). In conclusion, CQ decreased waist and hip circumferences in obese humans and enhanced UCP1 mRNA in hWA suggestive of its action via browning of hWA.


Asunto(s)
Cissus/química , Obesidad Abdominal/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Proteína Desacopladora 1/genética , Adipocitos Marrones/efectos de los fármacos , Adipocitos Blancos/efectos de los fármacos , Adulto , Femenino , Humanos , Leptina/genética , Lipólisis/efectos de los fármacos , Masculino , Obesidad Abdominal/patología , Extractos Vegetales/química , ARN Mensajero/genética
16.
J Nat Prod ; 83(11): 3298-3304, 2020 11 25.
Artículo en Inglés | MEDLINE | ID: mdl-33176095

RESUMEN

Bioassay-guided investigation of the Saudi medicinal and edible plant Cissus rotundifolia yielded seven metabolites, including the new sucrose diester cissuxinoside (1) and the unprecedented cissoic acid (2), belonging to unusual classes of secondary metabolites. Their chemical structures were elucidated through a combination of HR-MS and NMR data. The absolute configuration of cissoic acid was assigned by comparison of experimental and TDDFT-calculated electronic circular dichroism spectra. In addition, three rare C-glycosyl flavones (3-5) were fully characterized, and for 3 and 4 NMR data are reported here for the first time. This study identified 1-O-(4-coumaroyl)-ß-d-glucopyranose (7) as the main compound responsible for the glucose uptake stimulation effect exerted by the extract.


Asunto(s)
Cissus/química , Fenoles/aislamiento & purificación , Glicosilación , Estructura Molecular , Fenoles/química , Análisis Espectral/métodos
17.
Int J Biol Macromol ; 164: 3611-3620, 2020 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-32877714

RESUMEN

Cissus quadrangularis biodegradable natural cellulosic fibers comprehensively characterized to assess their potential as reinforcing materials in polymer composites. Initially, the Cissus quadrangularis fibers were chemically treated with 5% Sodium hydroxide (NaOH) and 5% magnesium carbonate (MgCO3) to improvise the properties of the fiber. The mechanical test result shows that chemically treated 5% MgCO3 fiber show that 4% and 24% improved tensile strength compared to NaOH and untreated ones. The cellulose crystallinity of the treated fiber got increased as the amorphous constituents removed. Further, 5% MgCO3 treatment removed a larger amount of amorphous hemicellulose, lignin, and other impurities present on the fiber surface. Secondly, the composites were fabricated at different combination of MgCO3 (5%, 10%, 15%), plasticizer (5%, 7.5%, 10%), and fiber volume (20%, 25% and 30%) with L9 Taguchi orthogonal array approach. Based on the results, 5% MgCO3, 5% plasticizer, and 30% fiber volume showed significant improvement in Young's modulus, tensile, and flexural strength of 8%, 27%, and 16% respectively. Moreover, there was no notable improvement observed on impact strength for both treated (15.91 KJ/m2) and untreated (13.98 KJ/m2) fiber. The scanning electron microscopy (SEM) micrographs used to examine the interface bonding between fiber and the matrix.


Asunto(s)
Celulosa/química , Cissus/química , Lignina/química , Magnesio/química , Fibras de la Dieta , Polímeros/química , Termogravimetría
18.
Artif Cells Nanomed Biotechnol ; 48(1): 1153-1158, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32924614

RESUMEN

The green approachable of metal nanoparticles is treated to be an eco-friendly path and cost-effectiveness. In this present study, nano copper was synthesized profitably by Cissus vitiginea. The synthesized nano copper was used to evaluate the antioxidant and antibacterial activity against urinary tract infections pathogens. The resulting constructed nanoparticles were characterized by using ultraviolet spectroscopy absorbance around 370 nm. Scanning electron microscopy results showed the distribution of nanoparticles and particles sizes are found to be in the range of 5-20 nm. X-ray diffraction spectrum characteristic diffraction peaks for copper nanoparticles were observed at 2θ ranges 35.5 and 43.2° correspond to lattice planes (1 1 1) and (2 0 2), respectively. X-ray photoelectron spectroscopy shows that two distinct peaks at binding energy resulted that the chemical states of copper. The results serve the evidence that the green mediated nano copper might indeed be the potential source to treat urinary tract infections caused by E. coli, Enterococcus sp., Proteus sp. and Klebsiella sp. This fact-finding conclusion is that C. vitiginea leaf extract based green synthesis nano copper particles proved to effectively kill it or significantly inhibit activity contra to urinary tract infection pathogens and exhibit excellent antioxidant activity.


Asunto(s)
Antioxidantes/síntesis química , Antioxidantes/farmacología , Cissus/química , Cobre/química , Cobre/farmacología , Nanopartículas del Metal/química , Infecciones Urinarias/microbiología , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antioxidantes/química , Tecnología Química Verde , Extractos Vegetales/química
19.
Int J Biol Macromol ; 161: 1358-1370, 2020 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-32750473

RESUMEN

In this study, a new natural fiber obtained from the stem of Cissus vitiginea has been studied for the first time. Chemical composition results confirmed that the proposed fiber has a rich amount of cellulose (65.43 wt%) and lower quantity of hemicellulose compounds (14.61 wt%),which in turn leads to better mechanical characteristics. Various chemical groups distributed over the fiber surface were predicted and reported with the help of Fourier transform infrared spectroscope and nuclear magnetic response spectroscopy. The crystalline nature of the fiber surface was examined using X-ray diffraction spectroscopy and the crystallinity index value was calculated to be 30.5% with 12.69 nm crystallite size. Morphological study was conducted on the fiber using a scanning electron microscope. The thermal stability of the fiber was found to be 304 °C with 68.72 kJ/mol kinetic activation energy. Hence C. vitiginea fiber can be suggested as reinforcement for the thermoplastic green composite.


Asunto(s)
Productos Biológicos/química , Productos Biológicos/aislamiento & purificación , Celulosa/química , Celulosa/aislamiento & purificación , Cissus/química , Fibras de la Dieta , Extractos Vegetales/química , Fenómenos Químicos , Espectroscopía de Resonancia Magnética , Fenómenos Mecánicos , Fitoquímicos/química , Corteza de la Planta/química , Espectroscopía Infrarroja por Transformada de Fourier , Termodinámica , Termogravimetría , Difracción de Rayos X
20.
Food Funct ; 11(9): 7842-7855, 2020 Sep 23.
Artículo en Inglés | MEDLINE | ID: mdl-32812575

RESUMEN

The Cissus quadrangularis (CQ) stem has interesting nutritional and pharmacological properties to promote the health of the skeletal system. It is a well-recognized plant in the conventional system of medicine in India for treating bone and joint-associated complications. This study focuses on identifying the active constituents from the stem and root extracts of CQ and validating its anti-osteoarthritic activity by the in vivo model. Notable levels of phenolics and flavonoids were found in the ethanol extracts of both CQ stem (CQSE) and root (CQRE), among other solvent fractions. UPLC-MS/MS analysis of these selective extracts resulted in different classes of active compounds from both positive and negative ionization modes. By analyzing their mass spectra and fragmentation pattern, 25 active compounds were identified. The CQSE and CQRE extracts, along with the standard drug (naproxen), were further tested in mono-sodium iodoacetate-induced experimental OA animals. The modulatory effects of the test extracts were assessed by haematology, synovial and cartilage marker profiling, radiology and histopathological analysis. The in vivo findings from the biochemical and physiological studies have led to the conclusion that the CQSE extract is a good choice for the management of OA. The results were substantially better than CQ root extract and naproxen drug-treated groups. Thus, CQS has bioactive constituents, which could facilitate recovery from joint tissue damage, cellular metabolism and associated risk factors attributable to dysfunctions in OA incidence and progression.


Asunto(s)
Cissus/química , Progresión de la Enfermedad , Ácido Yodoacético/efectos adversos , Osteoartritis de la Rodilla/inducido químicamente , Osteoartritis de la Rodilla/tratamiento farmacológico , Extractos Vegetales/farmacología , Animales , Modelos Animales de Enfermedad , Femenino , India , Articulación de la Rodilla/patología , Osteoartritis de la Rodilla/diagnóstico por imagen , Ratas , Ratas Wistar
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