RESUMO
Pongamia pinnata (L.) Pierre (Pongamia) is a tree native to Southeast Asia. Recently, interest in Pongamia focused on its potential as a biofuel source as its seeds contain around 40% oil. However, Pongamia has multiple applications beyond biofuel production. It is a legume, can form symbiotic associations with mycorrhizal fungi, has been shown to be tolerant to drought, salinity, and heavy metals in soil, and has potential to mitigate climate change. Additionally, Pongamia oil has medicinal properties, can be used as biopesticide, insect repellent, to produce soap, and as a source of edible grade vegetable oil. The seed cake can be used as a source of bioenergy, food and feed protein, and organic fertiliser, and the flowers are a good source of pollen and nectar. Pongamia can also bring socio-economic benefits as its ability to restore degraded and contaminated land provides opportunities for local communities through novel valorisation pathways. These multiple applications have potential to form part of a circular bioeconomy in line with sustainable development goals. Although research on the multiple applications of Pongamia has grown considerably, knowledge gaps remain and these need to be addressed so that the full potential of Pongamia can be achieved. Further understanding of the mechanisms underlying its resilience to abiotic stresses, phytoremediation potential and biotic interactions should be a priority, and co-ordinated breeding efforts will be key. Here, we critically review the available literature on Pongamia and highlight gaps in knowledge in which future research should focus on to ensure that the full potential of this versatile tree can be achieved. We conclude that Pongamia can potentially form part of a circular bioeconomy and that harnessing the multiple applications of Pongamia in a holistic manner, with collaboration among key stakeholders, is crucial for the successful application of its benefits far beyond biofuel production.
Assuntos
Millettia , Pongamia , Millettia/metabolismo , Sequestro de Carbono , Biocombustíveis , Melhoramento Vegetal , Árvores/metabolismo , Fatores SocioeconômicosRESUMO
Propolis is a resinous product collected by bees from plant exudates to protect and maintain hive homeostasis. Propolis has been used therapeutically for centuries as folk medicine. Modern research investigating the diversity of the chemical composition and plant sources, biological activity, extraction processes, analytical methods, and therapeutic properties in clinical settings have been carried out extensively since the 1980s. Due to its antimicrobial, anti-inflammatory, and immuno-modulator properties, propolis appears to be a suitable bioactive component to be incorporated into biomaterials. This review article attempts to analyze the potential application of propolis as a biomaterial component from the available experimental evidence. The efficacy and compabitility of propolis depend upon factors, such as types of extracts and types of biomaterials. Generally, propolis appears to be compatible with hydroxyapatite/calcium phosphate-based biomaterials. Propolis enhances the antimicrobial properties of the resulting composite materials while improving the physicochemical properties. Furthermore, propolis is also compatible with wound/skin dressing biomaterials. Propolis improves the wound healing properties of the biomaterials with no negative effects on the physicochemical properties of the composite biomaterials. However, the effect of propolis on the glass-based biomaterials cannot be generalized. Depending on the concentration, types of extract, and geographical sources of the propolis, the effect on the glass biomaterials can either be an improvement or detrimental in terms of mechanical properties such as compressive strength and shear bond strength. In conclusion, two of the more consistent impacts of propolis across these different types of biomaterials are the enhancement of the antimicrobial and the immune-modulator/anti-inflammatory properties resulting from the combination of propolis and the biomaterials.
RESUMO
Propolis is a resinous natural product collected by honeybees (Apis mellifera and others) from tree exudates that has been widely used in folk medicine. The present study was carried out to investigate the fatty acid composition, chemical constituents, antioxidant, and xanthine oxidase (XO) inhibitory activity of Jordanian propolis, collected from Al-Ghour, Jordan. The hexane extract of Jordanian propolis contained different fatty acids, which are reported for the first time by using GC-FID. The HPLC was carried out to identify important chemical constituents such as fatty acids, polyphenols and α-tocopherol. The antioxidant and xanthine oxidase inhibitory activities were also monitored. The major fatty acid identified were palmitic acid (44.6%), oleic acid (18:1∆9cis, 24.6%), arachidic acid (7.4%), stearic acid (5.4%), linoleic acid (18:2∆9-12cis, 3.1%), caprylic acid (2.9%), lignoceric acid (2.6%), cis-11,14-eicosaldienoic acid (20:2∆11-14cis, 2.4%), palmitoleic acid (1.5%), cis-11-eicosenoic acid (1.2%), α-linolenic acid (18:3∆9-12-15cis, 1.1%), cis-13,16-docosadienoic acid (22:2∆13-16cis, 1.0%), along with other fatty acids. The major chemical constituents identified using gradient HPLC-PDA analysis were pinocembrin (2.82%), chrysin (1.83%), luteolin-7-O-glucoside (1.23%), caffeic acid (1.12%), caffeic acid phenethyl ester (CAPE, 0.79%), apigenin (0.54%), galangin (0.46%), and luteolin (0.30%); while the minor constituents were hesperidin, quercetin, rutin, and vanillic acid. The percentage of α-tocopherol was 2.01 µg/g of the lipid fraction of propolis. Antioxidant properties of the extracts were determined via DPPH radical scavenging. The DPPH radical scavenging activities (IC50) of different extracts ranged from 6.13 to 60.5 µg/mL compared to ascorbic acid (1.21 µg/mL). The xanthine oxidase inhibition (IC50) ranged from 75.11 to 250.74 µg/mL compared to allopurinol (0.38 µg/mL). The results indicate that the various flavonoids, phenolic compounds, α-tocopherol, and other constituents which are present in propolis are responsible for the antioxidant and xanthine oxidation inhibition activity. To evaluate the safety studies of propolis, the pesticide residues were also monitored by LC-MS-MS 4500 Q-Trap. Trace amounts of pesticide residue (ng/mL) were detected in the samples, which are far below the permissible limit as per international guidelines.
Assuntos
Antioxidantes/química , Ácidos Graxos/química , Resíduos de Praguicidas/química , Própole/química , Antioxidantes/farmacologia , Ácidos Cafeicos/química , Ácidos Cafeicos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Ácidos Graxos/isolamento & purificação , Flavonoides/química , Flavonoides/isolamento & purificação , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/isolamento & purificação , Resíduos de Praguicidas/isolamento & purificação , Fenóis/química , Fenóis/isolamento & purificação , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/química , Álcool Feniletílico/isolamento & purificação , Rutina/químicaRESUMO
OBJECTIVE: This study was designed to investigate the nutraceutical potential of monofloral Indian mustard bee pollen (MIMBP). METHODS: The nutritional value of MIMBP was examined in terms of proteins, fats, carbohydrates, and energy value. Its chemical composition in terms of total polyphenol and flavonoid content was determined. MIMBP was screened for free flavonoid aglycones by developing and validating a high-performance liquid chromatography-photo diode array (HPLC-PDA) method. MIMBP was analyzed for in vitro antioxidant effect in terms of 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging activity. RESULTS: MIMBP was found to be comprised of proteins ((182.2±5.9) g/kg), fats ((137.7±6.8) g/kg) and carbohydrates ((560.6±17.4) g/kg), which result in its high energy value ((17 616.7±78.6) kJ/kg). MIMBP was found to contain polyphenols ((18 286.1±374.0) mg gallic acid equivalent/kg) and flavonoids ((1 223.5±53.1) mg quercetin equivalent/kg). The HPLC-PDA analysis revealed the presence of kaempferol ((65.4±0.5) mg/kg) and quercetin ((51.4±0.4) mg/kg) in MIMBP, which can be used as markers for determining the quality of bee pollen. The MIMBP extract showed DPPH free radical-scavenging activity with a half maximal inhibitory concentration of 54.79 µg/mL. CONCLUSION: The MIMBP was found to be a rich source of nutrients providing high caloric value, which makes it a candidate for a potential nutraceutical agent. The study also illustrated the high antioxidant content of MIMBP, especially in the principle polyphenols and flavonoids, which suggests its potential role in the prevention of free radical-implicated diseases. The DPPH-scavenging effect of MIMBP further confirmed its antioxidant potential. Additionally, we developed a simple, specific and accurate HPLC-PDA method for the identification and quantification of free flavonoid aglycones. This can be applied in future screenings of the quality of pollen collected by honeybees.
Assuntos
Abelhas/química , Suplementos Nutricionais/análise , Mostardeira/química , Extratos Vegetais/análise , Pólen/química , Animais , Sequestradores de Radicais Livres/análise , Polifenóis/análiseRESUMO
BACKGROUND: Ashwagandharishtha is a liquid polyherbal formulation traditionally prepared by fermentation process using the flowers of Woodfordia fruticosa. It contains roots of Withania somnifera as a major crude drug. Alcohol generated during the fermentation causes the extraction of water insoluble phytoconstituents. Yeasts present on the flowers are responsible for this fermentation. METHODS: Total nine formulations of ashwagandharishtha were prepared by fermentation process using traditional Woodfordia fruticosa flowers (ASG-WFS) and using yeasts isolated from the same flowers. During fermentation, kinetic of alcohol generation, sugar consumption, changes in pH and withanolides extraction were studied. All the formulations were tested for in vitro antioxidant potential by 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging, hydrogen peroxide scavenging and total reducing power assay. The results were compared with standard ascorbic acid. RESULTS: Traditional formulation (ASG-WFS) showed the highest activity (p < 0.001) relative to other formulations and standard ascorbic acid. ASG-WFS showed significant (DPPH) free radical scavenging (78.75%) and hydrogen peroxide scavenging (69.62%) at the concentration of 1000 µg/mL and 100 µg/mL, respectively. CONCLUSION: Traditional process is the best process for preparing ashwagandharishtha to obtain significant antioxidant activity.
RESUMO
BACKGROUND: Inflammatory Bowel Disease (IBD) is marked with chronic inflammation of intestinal epithelium driven by oxidative stress. Traditional treatments with plant extracts gained renewed interest due to their ability to ameliorate the multi factorial conditions like inflammation. We investigated the beneficial effects of Withania somnifera in Trinitro Benzyl Sulfonic Acid (TNBS) induced experimental IBD through a rectally applicable formulation. METHODS: The study included (i) preparation of gel formulation from aqueous Withania somnifera root extract (WSRE), (ii) biochemical assays to determine its performance potential, (iii) testing of formulation efficacy in TNBS-induced IBD rat model, and (iv) histo-patholgical studies to assess its healing and muco-regenerative effect in IBD-induced rats. For this purpose, concentration dependant antioxidant activity of the extracts were evaluated using biochemical assays like (a) inhibition of lipid peroxidation, (b) NO scavenging, (c) H2O2 scavenging, and (d) ferric reducing power assay. RESULTS: The extract, at 500 µg/ml, the highest concentration tested, showed 95.6% inhibition of lipid peroxidation, 14.8% NO scavenging, 81.79% H2O2 scavenging and a reducing capacity of 0.80. The results were comparable with standard antioxidants, ascorbic acid and curcumin. WSRE treatment positively scored on histopathological parameters like necrosis, edema, neutrophil infiltration. The post treatment intestinal features showed restoration at par with the healthy intestine. In view of these results, gel formulation containing an aqueous extract of W. somnifera, prepared for rectal application was tested for its anti-inflammatory activity in TNBS-induced rat models for IBD. Commercially available anti-inflammatory drug Mesalamine was used as the standard in this assay. CONCLUSIONS: Dose of the rectal gel applied at 1000 mg of WSRE per kg rat weight showed significant muco-restorative efficacy in the IBD-induced rats, validated by histo-pathological studies.
Assuntos
Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Doenças Inflamatórias Intestinais/tratamento farmacológico , Mucosa Intestinal/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/uso terapêutico , Withania , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/administração & dosagem , Antioxidantes/farmacologia , Feminino , Géis , Peróxido de Hidrogênio/metabolismo , Doenças Inflamatórias Intestinais/metabolismo , Doenças Inflamatórias Intestinais/patologia , Mucosa Intestinal/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Óxido Nitroso/metabolismo , Extratos Vegetais/farmacologia , Raízes de Plantas , Ratos , Ratos Wistar , Valores de Referência , Ácido TrinitrobenzenossulfônicoRESUMO
A large number of pharmaceuticals exhibit polymorphism; 23% steroids, 60% sulfonamides, and 70% of barbiturates have shown this property. In this study, we have investigated and compared a new technique termed as melt sonocrystallization (MSC) with melt and sonocrystallization (SC) for induction of polymorphism in progesterone (PRG). Polymorphs were characterized by DSC, XRD, FT-IR, and FT Raman spectroscopy. Melt sonocrystallized progesterone (MSC-PRG) contained both the polymorphs, more soluble form II along with less soluble form I, whereas melt progesterone (M-PRG) and sonocrystallized progesterone (SC-PRG) contained only form I. Improvement in dissolution characteristics of both the polymorphs were compared and form II was found to be more readily soluble than form I in deionized water. Reduction in mean particle size of PRG during SC was also determined using laser diffractometer. During stability testing (40°C/75% RH) for 1 month, metastable form II of MSC-PRG was found to be transformed into its more stable state. MSC technique was thus found as a useful tool for induction of polymorphism.
Assuntos
Cristalização/métodos , Avaliação Pré-Clínica de Medicamentos/métodos , Progesterona/química , Progesterona/efeitos da radiação , Sonicação , Temperatura Alta , Solubilidade , Temperatura de TransiçãoRESUMO
Beta amyloid plays a main role in the pathophysiology of Alzheimer's disease by inducing oxidative stress in the brain. Curcumin, a natural antioxidant, is known to inhibit beta amyloid and beta amyloid induced oxidative stress. However, low bioavailability and photodegradation are the major concerns for the use of curcumin. In the present study, we have formulated apolipoprotein E3 mediated poly(butyl) cyanoacrylate nanoparticles containing curcumin (ApoE3-C-PBCA) to provide photostability and enhanced cell uptake of curcumin by targeting. Prepared nanoparticles were characterized for particle size, zeta potential, entrapment efficiency and in vitro drug release. The entrapment of curcumin inside the nanoparticles was confirmed by X-ray diffraction analysis. Physicochemical characterization confirmed the suitability of the method of preparation. The photostability of curcumin was increased significantly in nanoparticles compared to plain curcumin. In vitro cell culture study showed enhanced therapeutic efficacy of ApoE3-C-PBCA against beta amyloid induced cytotoxicity in SH-SY5Y neuroblastoma cells compared to plain curcumin solution. Beta amyloid is known to induce apoptosis in neuronal cells, therefore antiapoptotic activity of curcumin was studied using flow cytometry assays. From all the experiments, it was found that the activity of curcumin was enhanced with ApoE3-C-PBCA compared to plain curcumin solution suggesting enhanced cell uptake and a sustained drug release effect. The synergistic effect of ApoE3 and curcumin was also studied, since ApoE3 also possesses both antioxidant and antiamyloidogenic activity. It was found that ApoE3 did indeed have activity against beta amyloid induced cytotoxicity along with curcumin. Hence, ApoE3-C-PBCA offers great advantage in the treatment of beta amyloid induced cytotoxicity in Alzheimer's disease.
Assuntos
Peptídeos beta-Amiloides/metabolismo , Apolipoproteína E3/química , Curcumina/química , Curcumina/uso terapêutico , Embucrilato/química , Polímeros/química , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/fisiologia , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Citometria de Fluxo , Humanos , Modelos Teóricos , Nanopartículas/química , Espécies Reativas de Oxigênio/metabolismo , Difração de Raios XRESUMO
OBJECTIVES: The aim was to design an alternative solvent-free extraction method using the hydrophilic lipid Gelucire (polyethylene glycol glycerides) for herbal extraction and to confirm the efficacy of extraction using biological screening. METHODS: Bacopa monniera Linn. (BM) was selected for the study. Conventional methanolic extract (MEBM), Ayurvedic ghrita (AGBM) and lipid extracts (LEBM) were prepared and standardised by high-performance thin-layer chromatography (HPTLC). Nootropic activity in rats was evaluated using the two-trial Y-maze test and the anterograde amnesia induced by scopolamine (1 mg/kg i.p.) determined by the conditioned avoidance response. The extracts were administered daily at doses of 100, 200 and 400 mg/kg orally. At the end of the conditioned avoidance response test, brain monoamine levels were estimated by HPLC. KEY FINDINGS: The LEBM, MEBM and AGBM contained 3.56%, 4.10% and 0.005% bacoside A, respectively. Significantly greater spatial recognition was observed with LEBM (P < 0.001 at 400 and 200 mg/kg) and MEBM (P < 0.001 at 400 mg/kg, P < 0.01 at 200 mg/kg) than AGBM. The conditioned avoidance response was significantly higher in the groups treated with high doses of LEBM and MEBM than AGBM. There were significant decreases in brain noradrenaline (P < 0.001) and 5-hydroxytryptamine (P < 0.01) levels and an increase in dopamine levels (P < 0.05) in the LEBM-treated groups compared with the stress control group. CONCLUSIONS: The proposed LEBM is solvent free, does not have the shortcomings associated with conventional extraction, and had comparable nootropic activity to the MEBM.
Assuntos
Amnésia Anterógrada/tratamento farmacológico , Bacopa/química , Encéfalo/efeitos dos fármacos , Nootrópicos/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Amnésia Anterógrada/induzido quimicamente , Amnésia Anterógrada/metabolismo , Animais , Aprendizagem da Esquiva , Encéfalo/metabolismo , Antagonistas Colinérgicos , Cromatografia em Camada Fina , Dopamina/metabolismo , Formas de Dosagem , Lipídeos , Masculino , Aprendizagem em Labirinto , Nootrópicos/isolamento & purificação , Nootrópicos/uso terapêutico , Norepinefrina/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Saponinas/isolamento & purificação , Saponinas/farmacologia , Saponinas/uso terapêutico , Escopolamina , Serotonina/metabolismo , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Triterpenos/uso terapêuticoRESUMO
OBJECTIVES: Piperine is one of the most promising bioenhancers to date. Methods used for its extraction suffer from drawbacks such as use of organic solvents, poor extraction efficiency, tedious and expensive methodology. These methods are not encouraged with a view to reducing global warming. The objective was therefore to develop an alternative solvent-free extraction method. METHODS: An aqueous extract of long pepper fruits was prepared using hydrophilic lipid Gelucire 44/14 as the extracting aid and this was compared with an alcoholic extract. Extracts were characterized using high-performance thin layer chromatography and differential scanning calorimetry. P-glycoprotein (P-gp) inhibitory activity of the aqueous and alcoholic extracts and pure piperine was compared using an in-vitro everted rat intestinal model using ornidazole as the model drug. The study was performed using two oral pretreatment dose levels (10 and 20 mg/kg) and durations (1 and 3 days). Exsorption of ornidazole from serosal to mucosal surface was monitored. KEY FINDINGS: P-gp inhibitory activity of the aqueous extract was comparable with that of pure piperine (P > 0.05) and was significantly higher than the alcoholic extract (P < 0.05). Pure piperine and the aqueous extract exhibited significant P-gp inhibitory activity compared with control, which was irrespective of oral pretreatment dose and duration levels. No significant effect of oral pretreatment duration of the aqueous extract was observed. The observed enhancement in P-gp inhibitory activity of the aqueous extract may have been attributed to the P-gp inhibitory potential of Gelucire 44/14 and its efficient extraction and solubility enhancement ability. CONCLUSIONS: In the field of phytopharmaceuticals efficient and eco-friendly extraction processes are still a goal to be achieved. Extraction with Gelucire 44/14 could be a potential method of extraction for phytopharmaceuticals. Compared with conventional methods of extraction it is more efficient, easier to prepare, eco-friendly and scalable.
Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Benzodioxóis/isolamento & purificação , Benzodioxóis/farmacologia , Piperidinas/isolamento & purificação , Piperidinas/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Polietilenoglicóis , Alcamidas Poli-Insaturadas/isolamento & purificação , Alcamidas Poli-Insaturadas/farmacologia , Solventes , Animais , Cromatografia Líquida de Alta Pressão , Intestinos/efeitos dos fármacos , Masculino , Ornidazol/farmacocinética , Piper/química , Polietilenoglicóis/química , Ratos , Ratos Wistar , Solventes/químicaRESUMO
Incorporation of bisphosphonates in the lipid reduces gastric irritation. Only gastric retention with sustained release allows the drug to reach the duodenum and jejunum and improves the availability of bisphosphonates. Risedronate sodium and Gelucire 39/01 floating matrices were prepared using melt solidification. The sustained release floating matrices were evaluated for in vitro and in vivo floating ability and in vitro drug release. Ageing of the matrices was studied by differential scanning calorimetry, hot stage polarizing microscopy, scanning electron microscopy and in vitro drug release. Ageing causes changes in the crystal structure of Gelucire, which is responsible for an increase in drug release.