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1.
J Ethnopharmacol ; 333: 118413, 2024 Oct 28.
Article in English | MEDLINE | ID: mdl-38824975

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Novel drugs are needed to address the issue of malarial infection resistance; natural items can be a different source of these medications. Albizia malacophylla (A. Rich.) Walp. (Leguminosae) is listed as one of the antimalarial medicinal plants in Ethiopian folk medicine. However, there are no reports regarding the biological activity or phytochemistry of the plant. AIM OF THE STUDY: Thus, this study aimed to evaluate the A. malacophylla crude extract and solvent fractions' in vivo antimalarial activity utilizing 4-day suppressive, preventative, and curative tests in mice infected with P. berghei. MATERIALS AND METHODS: The parasite Plasmodium berghei, which causes rodent malaria, was used to infect healthy male Swiss Albino mice, weighing 23-28 g and aged 6-8 weeks. Solvent fractions such as methanol, water, and chloroform were given in addition to an 80% methanolic extract at 100, 200, and 400 mg/kg doses. A Conventional test such as parasitemia, survival time, body weight, temperature, and packed cell capacity were employed to ascertain factors such as the suppressive, curative, and preventive tests. RESULTS: Every test substance dramatically reduced the number of parasites in every experiment. Crude extract (with the highest percentage suppression of 67.78%) performs better antimalarial effect than the methanol fraction, which is the most efficient solvent fraction with a percentage suppression of 55.74%. With a suppression value of 64.83% parasitemia level, the therapeutic effects of 80% methanolic crude extract were greater than its curative and preventative effects in a four-day suppressive test. The survival period (17 days) was longer with the hydroalcoholic crude extract dose of 400 mg/kg than with other doses of the materials under investigation. CONCLUSIONS: The results of this investigation validate the antimalarial characteristics of A. malacophylla leaf extract. The crude extract prevented weight loss, a decline in temperature, and a reduction in PCV. The results demonstrate that the plant has a promising antimalarial effect against P. berghei, hence supporting the traditional use of the plant. Therefore, it could serve as a foundation for the development of new antimalarial drugs.


Subject(s)
Albizzia , Malaria , Plant Extracts , Plasmodium berghei , Albizzia/chemistry , Plant Leaves/chemistry , Methanol/chemistry , Solvents/chemistry , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Malaria/drug therapy , Malaria/prevention & control , Disease Models, Animal , Animals , Mice , Male , Body Temperature/drug effects , Weight Loss/drug effects
2.
Bioorg Chem ; 150: 107561, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38936050

ABSTRACT

The antifungal bioactivity potential of the organic extract of silk tree (Albizia kalkora) was investigated in the current study. The crude extracts of A. kalkora and methanol, n-hexane, chloroform, and ethyl acetate fractions were prepared. The antifungal activity of obtained fractions of A. kalkora was studied at different concentrations ranging from 0.39-50 µg/mL. Dimethyl sulfoxide (DMSO) was taken as a toxicity control, whereas thiophanate methyl (TM) as a positive control. All the fractions significantly reduced the FOL growth (methanolic: 9.49-94.93 %, n-hexane: 11.12-100 %, chloroform: 20.96-91.41 %, and ethyl acetate: 18.75-96.70 %). The n-hexane fraction showed 6.25 µg/mL MIC as compared to TM with 64 µg/mL MIC. The non-polar (n-hexane) fraction showed maximum antifungal bioactivity against FOL in comparison with chloroform, methanol, and ethyl acetate fractions. GC/MS analysis exhibited that the n-hexane fraction contained hexadecanoic acid, 9,12,15-octadecatrienoic acid, 9,12-octadecadienoic acid, bis(2-ethylhexyl) phthalate, methyl stearate, and [1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylic acid. The results of in vitro antifungal inhibition were further reinforced by molecular docking analysis. Five virulence proteins of FOL i.e., pH-responsive PacC transcription factor (PACC), MeaB, TOR; target of rapamycin (FMK1), Signal transducing MAP kinase kinase (STE-STE7), and High Osmolarity Glycerol 1(HOG1) were docked with identified phytocompounds in the n-hexane fraction by GC/MS analysis. MEAB showed maximum binding affinities with zinnimide (-12.03 kcal/mol), HOG1 and FMK1with α-Tocospiro-B (-11.51 kcal/mol) and (-10.55 kcal/mol) respectively, STE-STE7 with docosanoic acid (-11.31 kcal/mol), and PACC with heptadecanoic acid (-9.88 kcal/mol) respectively with strong hydrophobic or hydrophilic interactions with active pocket residues. In conclusion, the n-hexane fraction of the A. kalkora can be used to manage FOL.


Subject(s)
Albizzia , Antifungal Agents , Microbial Sensitivity Tests , Molecular Docking Simulation , Plant Extracts , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Albizzia/chemistry , Structure-Activity Relationship , Molecular Structure , Dose-Response Relationship, Drug , Fungicides, Industrial/pharmacology , Fungicides, Industrial/chemistry , Fusarium/drug effects
3.
Chem Pharm Bull (Tokyo) ; 72(5): 454-470, 2024 May 09.
Article in English | MEDLINE | ID: mdl-38644216

ABSTRACT

This study investigates the efficacy of modified Albizia procera gum as a release-retardant polymer in Diltiazem hydrochloride (DIL) matrix tablets. Carboxymethylated Albizia procera gum (CAP) and ionically crosslinked carboxymethylated Albizia procera gum (Ca-CAP) were utilized, with Ca-CAP synthesized via crosslinking CAP with calcium ions (Ca2+) using calcium chloride (CaCl2). Fourier Transform (FT) IR analysis affirmed polymer compatibility, while differential scanning calorimetry (DSC) and X-ray diffraction (XRD) assessed thermal behavior and crystallinity, respectively. Zeta potential analysis explored surface charge and electrostatic interactions, while rheology examined flow and viscoelastic properties. Swelling and erosion kinetics provided insights into water penetration and stability. CAP's carboxymethyl groups (-CH2-COO-) heightened divalent cation reactivity, and crosslinking with CaCl2 produced Ca-CAP through -CH2-COO- and Ca2+ interactions. Structural similarities between the polymers were revealed by FTIR, with slight differences. DSC indicated modified thermal behavior in Ca-CAP, while Zeta potential analysis showcased negative charges, with Ca-CAP exhibiting lower negativity. XRD highlighted increased crystallinity in Ca-CAP due to calcium crosslinking. Minimal impact on RBC properties was observed with both polymers compared to the positive control as water for injection (WFI). Ca-CAP exhibited improved viscosity, strength, controlled swelling, and erosion, allowing prolonged drug release compared to CAP. Stability studies confirmed consistent six-month drug release, emphasizing Ca-CAP's potential as a stable, sustained drug delivery system over CAP. Robustness and accelerated stability tests supported these findings, underscoring the promise of Ca-CAP in controlled drug release applications.


Subject(s)
Diltiazem , Plant Gums , Tablets , Diltiazem/chemistry , Plant Gums/chemistry , Tablets/chemistry , Albizzia/chemistry , Drug Liberation , Cross-Linking Reagents/chemistry , Cross-Linking Reagents/chemical synthesis
4.
Arch Pharm (Weinheim) ; 357(6): e2300543, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38412461

ABSTRACT

The genus Albizia is one of the richest genera in phenolics besides other classes of secondary metabolites including saponins, terpenes, and alkaloids with promising medicinal applications. In the current study, UHPLC-PDA-ESI-MS/MS-based metabolic profiling of leaves of Albizia lebbeck, Albizia julibrissin, Albizia odoratissima, Albizia procera, Albizia anthelmintica, Albizia guachapele, Albizia myriophylla, Albizia richardiana, and Albizia lucidior resulted in the tentative identification of 64 metabolites, mainly flavonoids, phenolic acids, saponins, and alkaloids. Some metabolites were identified in Albizia for the first time and could be used as species-specific chemotaxonomic markers, including: apigenin 7-O-dihydroferuloyl hexoside isomers, apigenin 7-O-pentosyl hexoside, quercetin 3-O-rutinoside 7-O-deoxyhexoside, quercetin 3,7-di-O-hexoside deoxyhexoside, quercetin 7-O-feruloyl hexoside, methyl myricetin 7-O-deoxyhexoside, kaempferol di-3-O-di-deoxyhexoside-7-O-hexoside, and kaempferol 3-O-neohesperidoside 7-O-hexoside. Comparative untargeted metabolomic analysis was undertaken to discriminate between species and provide a chemotaxonomic clue that can be used together with morphological and genetic analyses for more accurate classification within this genus. Moreover, the in vitro antiplasmodial activity was assessed and correlated to the metabolic profile of selected species. This was followed by a molecular docking study and absorption, distribution, metabolism, excretion, and toxicity (ADMET) prediction of the identified budmunchiamine alkaloids, revealing promising interactions with the active site of lactate dehydrogenase of Plasmodium falciparum and good pharmacokinetics and pharmacodynamics, which could help in designing novel antimalarial drugs.


Subject(s)
Albizzia , Antimalarials , Metabolomics , Plant Extracts , Plant Leaves , Plasmodium falciparum , Albizzia/chemistry , Antimalarials/pharmacology , Antimalarials/chemistry , Plasmodium falciparum/drug effects , Plant Leaves/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Tandem Mass Spectrometry , Flavonoids/pharmacology , Flavonoids/chemistry , Chromatography, High Pressure Liquid , Alkaloids/pharmacology , Alkaloids/chemistry , Species Specificity
5.
Biomed Pharmacother ; 165: 115093, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37392651

ABSTRACT

Albizia adianthifolia (Schumach.) (Fabaceae) is a medicinal herb used for the treatment of epilepsy and memory impairment. This study aims to investigate the anticonvulsant effects of Albizia adianthifolia aqueous extract against pentylenetetrazole (PTZ)-induced spontaneous convulsions in mice; and determine whether the extract could mitigate memory impairment, oxidative/nitrergic stress, GABA depletion and neuroinflammation. Ultra-high performance liquid chromatography/mass spectrometry analysis was done to identify active compounds from the extract. Mice were injected with PTZ once every 48 h until kindling was developed. Animals received distilled water for the normal group and negative control groups, doses of extract (40, 80, or 160 mg/kg) for the test groups and sodium valproate (300 mg/kg) for the positive control group. Memory was measured using Y maze, novel object recognition (NOR) and open field paradigms, while the oxidative/nitrosative stresses (MDA, GSH, CAT, SOD and NO), GABAergic transmission (GABA, GABA-T and GAD) and neuro-inflammation (TNF-α, IFN-γ, IL- 1ß, and IL-6) were determined. Brain photomicrograph was also studied. Apigenin, murrayanine and safranal were identified in the extract. The extract (80-160 mg/kg) significantly protected mice against seizures and mortality induced by PTZ. The extract significantly increased the spontaneous alternation and the discrimination index in the Y maze and NOR tests, respectively. PTZ kindling induced oxidative/nitrosative stress, GABA depletion, neuroinflammation and neuronal cells death was strongly reversed by the extract. The results suggest that the anticonvulsant activity of Albizia adianthifolia extract is accompanied by its anti-amnesic property, and may be supported by the amelioration of oxidative stress, GABAergic transmission and neuroinflammation.


Subject(s)
Albizzia , Epilepsy , Kindling, Neurologic , Mice , Animals , Pentylenetetrazole/pharmacology , Antioxidants/therapeutic use , Anticonvulsants/adverse effects , Albizzia/chemistry , Neuroinflammatory Diseases , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Epilepsy/chemically induced , Epilepsy/drug therapy , Seizures/chemically induced , Seizures/drug therapy , Seizures/prevention & control , Memory Disorders/chemically induced , Memory Disorders/drug therapy , Oxidative Stress , Amnesia/drug therapy , Water/pharmacology , gamma-Aminobutyric Acid/pharmacology , Anti-Inflammatory Agents/adverse effects
6.
J Asian Nat Prod Res ; 25(9): 912-917, 2023 Sep.
Article in English | MEDLINE | ID: mdl-36597895

ABSTRACT

One new lignan, julibrissinoside II, along with thirteen known compounds, was isolated from the stem bark of Albizia julibrissin. The structure of julibrissinoside II was determined on the basis of extensive spectroscopic methods, including NMR and CD spectroscopic data. The isolated compounds were tested for their SREBP-1c inhibitory activity at different concentrations using mouse hepatocyte AML12 cell lines. Among them, linoleic acid (2) and 3-O-methylfisetin (4) showed significant SREBP-1c inhibitory activity at the concentration of 100 µM.


Subject(s)
Albizzia , Saponins , Animals , Mice , Albizzia/chemistry , Cell Line, Tumor , Plant Bark/chemistry , Saponins/chemistry , Sterol Regulatory Element Binding Protein 1/antagonists & inhibitors
7.
Nat Prod Res ; 37(13): 2151-2160, 2023 Jul.
Article in English | MEDLINE | ID: mdl-35105225

ABSTRACT

The chemical investigation of the fresh flowers of Albizia lebbeck (L.) Benth. (Fabaceae, Mimosoideae) led to the isolation of two new echinocystic acid saponins. They were isolated by using chromatographic methods and their structures were elucidated by detailed 1H and 13C NMR spectral data including 2 D-NMR (COSY, HSQC, HMBC and APT) spectroscopic techniques, high-resolution electrospray ionization mass spectrometry (HRESIMS) and acid hydrolysis. Their structures were established as 16-hydroxy-3-[[O-ß-D-xylopyranosyl-(1→2)-O-α-L-arabinopyranosyl-(1→6)-2-(acetylamino)-2-deoxy-ß-D-glucopyranosyl]oxy]-(3ß,16α)-olean-12-en-28-oic acid O-6-deoxy-α-L-mannopyranosyl-(1→4)-O-6-deoxy-α-L-mannopyranosyl-(1→2)-ß-D-glucopyranosyl ester (1) and 16-hydroxy-3-[[O-ß-D-xylopyranosyl-(1→2)-O-α-L-arabinopyranosyl-(1→6)-2-(acetylamino)-2-deoxy-ß-D-glucopyranosyl]oxy]-(3ß,16α)-olean-12-en-28-oic acid 6-O-[(2S,3R,4R)-tetrahydro-3-hydroxy-4-(hydroxymethyl)-2-furanyl]-ß-D-glucopyranosyl ester (2). Additionally, the permeability property and the capacity of interaction with biological membranes of compounds 1 and 2 were investigated.


Subject(s)
Albizzia , Fabaceae , Saponins , Triterpenes , Albizzia/chemistry , Molecular Structure , Triterpenes/chemistry , Saponins/chemistry , Flowers
8.
Planta Med ; 89(1): 86-98, 2023 Jan.
Article in English | MEDLINE | ID: mdl-35868332

ABSTRACT

In our ongoing research program on the proapoptotic function of saponins, two previously undescribed saponins, named zygiaosides E (1: ) and F (2: ), were isolated from the leaves of Albizia zygia. Their structures were established based on extensive analysis of 1D and 2D NMR data, HR-ESI-MS analysis, and by chemical degradation. The proapoptotic effect of zygiaoside E (1: ) was evaluated on human malignant melanoma (A375), human epidermoid cancer (A431), and normal Homo sapiens skin tissue (TE 353.SK.) cell lines by cytometric analysis. Zygiaoside E (1: ) induced apoptosis of the two human cancer cell lines (A375 and A431) in a dose-dependent manner at 1 µM but did not induce apoptosis in noncancerous skin cells (TE 353.Sk), even when treated with concentrations up to 15 µM. The underlying mechanism of the apoptosis induction activity of zygiaoside E (1: ) on the mitochondrial membrane potential status in A375 cells was further assessed by monitoring the uptake rate of DiOC6, a mitochondrial specific and voltage-dependent fluorescent dye. The number of malignant melanoma cells emitting high fluorescence levels was decreased when cells were treated with 3 or 5 µM of zygiaoside E (1: ) during either 12 or 24 h, thereby revealing a drop of mitochondrial membrane potential in A375 cells upon treatment, which indicated mitochondrial perturbation.


Subject(s)
Albizzia , Melanoma , Saponins , Triterpenes , Humans , Albizzia/chemistry , Triterpenes/pharmacology , Cell Line, Tumor , Saponins/pharmacology , Saponins/chemistry , Apoptosis , Melanoma/drug therapy , Melanoma/metabolism , Melanoma/pathology , Membrane Potential, Mitochondrial
9.
Molecules ; 27(15)2022 Jul 28.
Article in English | MEDLINE | ID: mdl-35956773

ABSTRACT

Twenty-two compounds were isolated from the fruit of Albizia lebbeck including one unprecedented, rare amino acid-derived zwitterionic and one new flavone derivative. The isolation was performed on repeated column chromatography over silica gel and their structures were determined by 1D-, 2D-NMR and HR-ESI-MS spectra together with reported data in the literature. The chemophenetic significance is also discussed. Some isolated compounds were reported for the first time to be found in the species. Additionally, compound 2 showed antibacterial activity and compounds 1 and 2 revealed moderate cytotoxic activity against the Raw 264.7 cancer cell line with IC50 values of 37.19 µM and 29.36 µM, respectively. Furthermore, a proposed biosynthetic pathway of compound 1 is described.


Subject(s)
Albizzia , Anti-Infective Agents , Antineoplastic Agents , Fabaceae , Albizzia/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Antineoplastic Agents/chemistry , Fruit , Plant Extracts/chemistry , Plant Extracts/pharmacology
10.
J Cosmet Dermatol ; 21(4): 1588-1595, 2022 Apr.
Article in English | MEDLINE | ID: mdl-34021684

ABSTRACT

BACKGROUND: Antioxidants are widely used in cosmetic products as they have beneficial effects on skin and prevent skin from harmful effects of environment. Albizia lebbeck has a significant potential to be used in cosmeceuticals due to its antioxidant activity. OBJECTIVES: The aim of this study was to formulate a stable and effective o/w emulsion-based emulgel containing Albizia lebbeck bark extract, which have considerable antioxidant activity. METHODOLOGY: Antioxidant activity of Albizia lebbeck bark extract was determined by DPPH (2,2-diphenyl-1-picrylhydrazyl) method. Emulgel containing 3% extract was developed by mixing o/w emulsion in Carbopol gel along with a placebo emulgel without extract (base). In vitro evaluation of these emulgels, that is, liquefaction, color, phase separation, centrifugation, and pH change were carried out for a period of 8 weeks at different storage conditions, that is, 8ºC, 25ºC, 40ºC, and 40ºC & 75% relative humidity (RH). In vivo evaluation of emulgels was carried out on 13 healthy female volunteers by measuring various parameters of skin, that is, melanin level, erythema level, moisture content, sebum content, and elasticity at regular time intervals after applying emulgel (both base and test formulation) for 8 weeks. RESULTS: Antioxidant activity of Albizia lebbeck bark extract was 84.7%. Both emulgels (base and test formulation) were stable at all storage conditions. Statistical analysis showed that test formulation produced significant effects (p < 0.05) on melanin, erythema level, moisture content, sebum level, and elasticity of skin. CONCLUSION: It can be concluded that a stable topical emulgel containing 3% Albizia lebbeck bark extract has significant antioxidant effects on human skin.


Subject(s)
Albizzia , Cosmeceuticals , Albizzia/chemistry , Cosmeceuticals/pharmacology , Female , Humans , Plant Bark/chemistry , Plant Extracts , Sebum
11.
Planta Med ; 88(12): 964-974, 2022 Oct.
Article in English | MEDLINE | ID: mdl-34359081

ABSTRACT

Albizia myriophylla has been used in Thai folk medicine for treating inflammation-related diseases. The wood of this medicinal plant is traditionally used as a single herbal drug in the form of an aqueous decoction and as a component in several Thai herbal formulations for the remedy of fever, sore throat, and aphthous ulcers. This study aimed to evaluate in vivo the anti-inflammatory potential and possible mechanism of action of the standardized wood extract of A. myriophylla as well as to investigate the anti-inflammatory activity and physicochemical properties of the developed herbal gel formulation containing standardized wood extract of A. myriophylla. Results of quantitative HPLC analysis demonstrated that the standardized wood extract of A. myriophylla contained 22.95 mg/g of 8-methoxy-7,3',4'-trihydroxyflavone, a bioactive marker compound of A. myriophylla. The standardized wood extract of A. myriophylla (1% w/v) exhibited remarkable inhibition (54.4 - 80.3%) in the croton oil model of topical inflammation at all assessment times, comparable to standard indomethacin (55.3 - 63.6%). Real-time quantitative reverse transcription-polymerase chain reaction was performed to clarify the anti-inflammatory mechanism of standardized wood extract of A. myriophylla, and the result showed that this standardized extract decreased lipopolysaccharide-induced nitric oxide synthase mRNA levels in a dose-dependent manner. The developed herbal gel containing standardized wood extract of A. myriophylla (1% w/w) had good physicochemical characteristics and exhibited potent inhibition (51.4 - 77.8%) of inflammation in a rat ear edema model at all assessment times, comparable to indomethacin gel (33.3 - 40.5%). The notable anti-inflammatory activity of standardized wood extract of A. myriophylla and its developed herbal gel formulation indicates their potential application as natural anti-inflammatory agents.


Subject(s)
Albizzia , Albizzia/chemistry , Animals , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Croton Oil/analysis , Croton Oil/therapeutic use , Croton Oil/toxicity , Edema/chemically induced , Edema/drug therapy , Indomethacin , Inflammation/drug therapy , Lipopolysaccharides/toxicity , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , RNA, Messenger , Rats , Wood/chemistry
12.
Cells ; 10(9)2021 09 10.
Article in English | MEDLINE | ID: mdl-34572034

ABSTRACT

The global population is increasing day by day. To meet the food demand for such a huge number of people, crop production must increase without damaging the environment, and to prevent synthetic chemical herbicides from polluting the environment, controlling weeds using bioherbicides is essential. Accordingly, using phytotoxic substances obtained from plants for biological weed management has attracted attention. The plant Albizia richardiana possesses phytotoxic compounds that have been previously recorded. Hence, we have conducted this research to characterize more phytotoxic compounds in Albizia richardiana. Aqueous methanolic extracts of Albizia richardiana plant significantly restricted the growth of the examined plants lettuce and Italian ryegrass in a species- and concentration-dependent manner. Three active phytotoxic compounds were isolated through various chromatographic methods and identified as compound 1, 2, and 3. Compound 3 exhibited stronger phytotoxic potentials than the other two compounds and significantly suppressed the growth of Lepidium sativum (cress). The concentration of the compounds required for 50% growth reduction (I50 value) of the Lepidium sativum seedlings ranged between 0.0827 to 0.4133 mg/mL. The results suggest that these three phytotoxic compounds might contribute to the allelopathic potential of Albizia richardiana.


Subject(s)
Albizzia/chemistry , Lepidium sativum/growth & development , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plant Weeds/growth & development , Weed Control/methods , Herbicides/pharmacology , Lepidium sativum/drug effects , Plant Weeds/drug effects
13.
Daru ; 29(2): 311-320, 2021 Dec.
Article in English | MEDLINE | ID: mdl-34415547

ABSTRACT

PURPOSE: The enzyme Cyclooxygenases (COX-1 and COX-2) catalyze the formation of prostaglandin, a mediator of the inflammatory pathway. Inflammation related pathological conditions may be alleviated by targeting the Cox enzymes.COX-2 inhibitors that are currently available in the market causes undesirable side effects. Our present study focuses on the in-silico inhibition of COX -2 enzyme by the phytocompounds from Albizia amara and Phyla nodiflora. METHODS: The phytochemicals present in Albizia amara and Phyla nodiflora were analyzed for their COX-2 inhibition potential. Eight compounds from Albizia amara and eleven compounds from Phyla nodiflora obtained from GC-MS analysis was used for the current study. Molecular docking was performed using AutoDock vina. The crystal structure of COX-2 (PDB ID: 5IKR) was obtained from Protein data bank. PyMol was used to remove any solvent, organic and inorganic molecules. Energy minimization of the protein was carried out using SPDBV software. Geometrical optimizations of the ligands were performed using Avogadro software. Celecoxib was used as the positive control. ADMET properties of the compounds were analyzed using SwissADME and ProtoxII online servers. Molecular mechanics/generalized born surface area (MM/GBSA) calculations were performed to evaluate the binding efficiency. Molecular dynamics of the protein and protein-ligand complex was studied for about 100 ns using Desmond package of Schrodinger suite. RESULTS: Among the eighteen compounds, Squalene present in both the plants showed a better binding energy of -7.7 kcal/mol, when compare to other phytocompounds present in the extract. The control celecoxib showed a binding energy of about - 9.4 kcal/mol. The toxicity and ADMET properties of squalene indicated that it is non-toxic and followed Lipinski's rule. Molecular Dynamics (MD) analysis showed that the binding of squalene to the enzyme was stable. CONCLUSION: Squalene could potentially inhibit COX2 and o wing to its properties, squalene can be formulated in gels/creams and could be possibly used for external edema and inflammation.


Subject(s)
Albizzia/chemistry , Cyclooxygenase 2 Inhibitors/pharmacology , Cyclooxygenase 2/metabolism , Lantana/chemistry , Phytochemicals/pharmacology , Squalene/pharmacology , Celecoxib/chemistry , Celecoxib/pharmacology , Crystallography, X-Ray , Cyclooxygenase 2/chemistry , Cyclooxygenase 2 Inhibitors/chemistry , Gas Chromatography-Mass Spectrometry , Hydrogen Bonding , Models, Molecular , Molecular Docking Simulation , Molecular Dynamics Simulation , Phytochemicals/chemistry , Protein Binding , Squalene/chemistry
14.
Int Immunopharmacol ; 99: 107986, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34303280

ABSTRACT

Albiziae Cortex (AC) is a well-known traditional Chinese medicine with sedative-hypnotic effects and neuroprotective ability. However, the bioactive components of AC responsible for the neuro-protective actitivity remain unknown. Here, we investigated the anti-neuroinflammatory effects of (-)-syringaresinol (SYR) extracted from AC in microglia cells and wild-type mice. As a result, (-)-SYR significantly reduced lipopolysaccharide (LPS)-induced production of interleukin - 6 (IL-6), tumor necrosis factor α (TNF-α), interleukin -1 beta (IL-1ß), cycloxygenase-2 (COX-2), and nitric oxide (NO) in BV2 microglia cells. (-)-SYR also significantly reduced M1 marker CD40 expression and increased M2 marker CD206 expression. Moreover, we found that (-)-SYR inhibited LPS-induced NF-κB activation by suppressing the translocation of NF-κB p65 into the nucleus in a concentration-dependent manner. Meanwhile, estrogen receptor ß (ERß) was found to be implied in the anti-inflammatory activity of (-)-SYR in BV2 microglia. In vivo experiments revealed that administration of (-)-SYR in mice significantly reduced microglia/astrocytes activation and mRNA levels of proinflammatory mediators. Taken together, our data indicated that (-)-SYR exerted the anti-neuroinflammatory effects by inhibiting NF-κB activation and modulation of microglia polarization, and via interaction with ERß. The anti-neuroinflammatory activity of (-)-SYR may provide a new therapeutic avenue for the treatment of brain diseases associated with inflammation.


Subject(s)
Estrogen Receptor beta/metabolism , Furans/pharmacology , Lignans/pharmacology , Microglia/metabolism , Albizzia/chemistry , Animals , Anti-Inflammatory Agents/therapeutic use , Cell Survival/drug effects , Cytokines/metabolism , Estrogen Receptor beta/antagonists & inhibitors , Furans/chemistry , Lignans/chemistry , Lipopolysaccharides/pharmacology , MAP Kinase Signaling System/drug effects , Macrophage Activation/drug effects , Male , Mice , Mice, Inbred C57BL , Microglia/drug effects , Neuroinflammatory Diseases/drug therapy , Oncogene Protein v-akt/metabolism , Transcription Factor RelA/metabolism
15.
Molecules ; 26(13)2021 Jun 24.
Article in English | MEDLINE | ID: mdl-34202852

ABSTRACT

Nano-based particles synthesized via green routes have a particular structure that is useful in biomedical applications as they provide cheap, eco-friendly, and non-toxic nanoparticles. In the present study, we reported the effect of various concentrations of Zinc oxide nanoparticles synthesized using A. lebbeck stem bark extract (ZnO NPsAL) as stabilizing agent on rat biochemical profiles and tissue morphology. Adult Wistar rats weighing 170 ± 5 g were randomly classified into eight groups of five rats each; Group A served as a control fed with normal diet and water. Groups B1, B2, C1, C2, D1, D2, and E were treated with 40 mg/kg and 80 mg/kg of the 0.01, 0.05, and 0.1 M biosynthesized ZnO NPsAL and zinc nitrate daily by the gavage method, respectively. The rats were anesthetized 24 h after the last treatment, blood samples, kidney, heart, and liver tissues were collected for biochemical and histopathological analysis. The rats mean body weight, serum alkaline phosphatase, alanine aminotransferase, creatinine, urea, bilirubin, protein, albumin, globulin, total cholesterol, triacylglycerol, and high-density lipoprotein were significantly altered with an increased concentration of biosynthesized ZnO NPsAL when compared with the control group (p < 0.05; n ≥ 5). Furthermore, histopathological analysis of treated rats' kidney, heart, and liver tissue revealed vascular congestion, tubular necrosis, inflammation, and cytoplasmic vacuolation. Biosynthesized ZnO NPsAL showed significant alteration in biochemical parameters and tissue morphology in rats with increasing concentrations of the nanoparticles.


Subject(s)
Albizzia/chemistry , Nanoparticles , Plant Bark/chemistry , Plant Extracts/chemistry , Zinc Oxide , Animals , Male , Nanoparticles/administration & dosage , Nanoparticles/chemistry , Nanoparticles/therapeutic use , Organ Specificity , Rats , Rats, Wistar , Zinc Oxide/adverse effects , Zinc Oxide/chemistry , Zinc Oxide/pharmacology
16.
J Cancer Res Ther ; 17(2): 491-498, 2021.
Article in English | MEDLINE | ID: mdl-34121697

ABSTRACT

AIM OF THE STUDY: The aim of the present study was to explore the antitumor activity of the ethanolic extract of Albizia lebbeck L. pods against Ehrlich ascites carcinoma (EAC) in Swiss albino mice and its cytotoxic effect against HeLa and A549 cell lines in vitro. MATERIALS AND METHODS: Antitumor activity of ethanolic extract of A. lebbeck L. (ALEE) pods was evaluated in Swiss albino mice against EAC cell lines at the doses of 200 and 400 mg/kg body weight which were given by intraperitoneal route of administration and was compared with 5-fluorouracil (5-FU), the reference standard. The extract and 5-FU were administered for 14 consecutive days. After 24 h of the last dose and 18 h of fasting, the mice were sacrificed and the antitumor effect of ALEE was assessed by evaluating tumor volume, viable and nonviable tumor cell count, increase in life span, and hematological parameters of EAC-bearing hosts.In vitro cytotoxicity has been assessed using (2,3-bis[2-Methoxy-4-nitro-5sulfophenyl]-2H-tetrazolium-5-carboxyanilide inner salt assay method and was compared with cisplatin, the reference standard. RESULTS: ALEE showed direct cytotoxicity on EAC cells in a dose-dependent manner. ALEE exhibited a significant (P < 0.001) decrease in the body weight, tumor volume, viable cell count, tumor weight, and elevated the life span of EAC tumor-bearing mice. Hematological profile such as red blood cell, hemoglobin, white blood cell, and platelet count was reverted to the normal level in ALEE-treated mice. CONCLUSION: The results showed that the ethanolic extract of A. lebbeck L. has a powerful antitumor activity because it was effective in significantly inhibiting the tumor growth in both in vivo and in vitro cancer cell lines.


Subject(s)
Albizzia/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Carcinoma, Ehrlich Tumor/drug therapy , Plant Extracts/pharmacology , A549 Cells , Animals , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/therapeutic use , Carcinoma, Ehrlich Tumor/pathology , Drug Screening Assays, Antitumor , Ethanol/chemistry , Female , Fluorouracil/pharmacology , Fluorouracil/therapeutic use , HeLa Cells , Humans , Injections, Intraperitoneal , Lipid Peroxidation/drug effects , Mice , Plant Extracts/isolation & purification , Plant Extracts/therapeutic use
17.
Nat Prod Res ; 35(17): 2831-2839, 2021 Sep.
Article in English | MEDLINE | ID: mdl-31583912

ABSTRACT

An unprecedented saponin is being reported herein together with five known compounds from the methanol extract of the roots of Albizia adianthifolia. The metabolites were obtained over repeated open column chromatography methods and spectroscopic followed by spectrometric techniques. The isolated compounds were tested against eleven Gram-negative bacteria including multidrug resistant strains. The results revealed considerable inhibition of the new saponin against the studied bacteria with MIC values ranging from 16 to 128 µg/mL.


Subject(s)
Albizzia , Anti-Bacterial Agents/pharmacology , Saponins , Albizzia/chemistry , Anti-Bacterial Agents/isolation & purification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Plant Roots/chemistry , Saponins/isolation & purification , Saponins/pharmacology
18.
BMC Vet Res ; 16(1): 427, 2020 Nov 07.
Article in English | MEDLINE | ID: mdl-33160337

ABSTRACT

BACKGROUND: H9N2 Low pathogenic avian influenza virus (LPAIV) raises public health concerns and its eradication in poultry becomes even more important in preventing influenza. AJSAF is a purified active saponin fraction from the stem bark of Albizzia julibrissin. In this study, AJSAF was evaluated for the adjuvant potentials on immune responses to inactivated H9N2 avian influenza virus vaccine (IH9V) in mice and chicken in comparison with commercially oil-adjuvant. RESULTS: AJSAF significantly induced faster and higher H9 subtype avian influenza virus antigen (H9-Ag)-specific IgG, IgG1, IgG2a and IgG2b antibody titers in mice and haemagglutination inhibition (HI) and IgY antibody levels in chicken immunized with IH9V. AJSAF also markedly promoted Con A-, LPS- and H9-Ag-stimulated splenocyte proliferation and natural killer cell activity. Furthermore, AJSAF significantly induced the production of both Th1 (IL-2 and IFN-γ) and Th2 (IL-10) cytokines, and up-regulated the mRNA expression levels of Th1 and Th2 cytokines and transcription factors in splenocytes from the IH9V-immunized mice. Although oil-formulated inactivated H9N2 avian influenza vaccine (CH9V) also elicited higher H9-Ag-specific IgG and IgG1 in mice and HI antibody titer in chicken, this robust humoral response was later produced. Moreover, serum IgG2a and IgG2b antibody titers in CH9V-immunized mice were significantly lower than those of IH9V alone group. CONCLUSIONS: AJSAF could improve antigen-specific humoral and cellular immune responses, and simultaneously trigger a Th1/Th2 response to IH9V. AJSAF might be a safe and efficacious adjuvant candidate for H9N2 avian influenza vaccine.


Subject(s)
Adjuvants, Immunologic/administration & dosage , Albizzia/chemistry , Influenza A Virus, H9N2 Subtype/immunology , Influenza in Birds/prevention & control , Saponins/administration & dosage , Animals , Chickens , Female , Immunity , Immunogenicity, Vaccine , Influenza in Birds/immunology , Mice, Inbred ICR , Orthomyxoviridae Infections/immunology , Orthomyxoviridae Infections/prevention & control , Plant Extracts/administration & dosage , Plant Extracts/immunology , Saponins/immunology , Vaccines, Inactivated/administration & dosage , Vaccines, Inactivated/immunology , Viral Vaccines/administration & dosage , Viral Vaccines/immunology
19.
Artif Cells Nanomed Biotechnol ; 48(1): 1206-1213, 2020 Dec.
Article in English | MEDLINE | ID: mdl-33016139

ABSTRACT

Colon cancer is one of the major prevailing types of cancer worldwide. It has been the most important public health difficulty. Thus, we planned phytoconstituents arbitrated synthesis of gold nanoparticles (AuNPs) and examined their curative efficacy against the colon cancer (HCT-116) cells. In this current study, we formulated the AuNPs by using Albizia lebbeck (AL) aqueous leaf extract by the green method and synthesized AL-AuNPs were distinguished by UV-visible spectroscopy (UV-vis), energy dispersive X-ray diffraction (XRD), selected area (electron) diffraction (SAED) pattern, Fourier transform infrared spectroscopy (FTIR) and high-resolution transmission electron microscopy (HR-TEM). Synthesized AL-AuNPs confirmed by the UV absorption highest at 535 nm and the crystal structure of AL-AuNPs was additionally established by XRD and SAED pattern. HR-TEM images explained the size and morphology allocation of nanoparticles. FTIR analysis confirmed the presence of alkynes, aromatic compounds, and alkenes of biomolecules in AL-AuNPs. Furthermore, AL-AuNPs induced cytotoxicity at the IC50 concentration 48 µg/ml and also induced apoptosis by enhanced ROS production, decreased ΔΨm, apoptotic morphological changes by AO/EtBr and altering pro and anti-apoptotic protein expressions were analyzed in HCT-116 colon cancer cells. The findings of this investigation proved that the AL-AuNPs were revealed the potential anticancer activity against colon cancer (HCT-116) cells.


Subject(s)
Albizzia/chemistry , Anticarcinogenic Agents/chemical synthesis , Anticarcinogenic Agents/pharmacology , Colonic Neoplasms/pathology , Gold/chemistry , Gold/pharmacology , Metal Nanoparticles/chemistry , Anticarcinogenic Agents/chemistry , Apoptosis/drug effects , Cell Proliferation/drug effects , Chemistry Techniques, Synthetic , Green Chemistry Technology , HCT116 Cells , Humans , Plant Extracts/chemistry
20.
Molecules ; 25(9)2020 Apr 28.
Article in English | MEDLINE | ID: mdl-32354185

ABSTRACT

A dibenzylbutane-type lignan (16), along with eight furofuran-type (1-8), five furan-type (9-13), two dibenzylbutane-type (14 and 15), two bibenztetrahydronaphthalene-type lignans (17 and 18), two neolignans (19 and 20), and six phenolic derivatives (21-26) were isolated from an MeOH extract of the stem bark of Albizia julibrissin Durazz. The chemical structures of the obtained compounds were elucidated by nuclear magnetic resonance (NMR) and mass spectrometry (MS) analyses. Of the evaluated compounds, 14 were isolated from A. julibrissin and the Fabaceae family for the first time. Anti-inflammatory effects of the isolated analogs were investigated in terms of the inhibition of the nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophage cells. Ten compounds (10-12, 14, and 17-22) displayed significant dose-dependent inhibitory effects against the NO production, with IC50 values ranging from 5.4 to 19.2 µM. Moreover, eight compounds (1-4, 9, 13, 15, and 16) exhibited moderate inhibitory activities, with IC50 values ranging from 21.0 to 62.5 µM.


Subject(s)
Albizzia/chemistry , Furans/pharmacology , Lignans/pharmacology , Nitric Oxide/antagonists & inhibitors , Phenols/pharmacology , Plant Bark/chemistry , Animals , Dose-Response Relationship, Drug , Drug Design , Furans/chemistry , Inhibitory Concentration 50 , Lignans/chemistry , Magnetic Resonance Spectroscopy , Mass Spectrometry , Mice , Nitric Oxide/metabolism , Phenols/chemistry , Phytochemicals/chemistry , Phytochemicals/pharmacology , RAW 264.7 Cells , Structure-Activity Relationship
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