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1.
Z Naturforsch C J Biosci ; 79(9-10): 275-284, 2024 Sep 25.
Article in English | MEDLINE | ID: mdl-38780470

ABSTRACT

Cymbopogon proximus comprises several phytoconstituent classes that are reported to possess anticancer activity; however, studies on the anticancer potentials of the plant are lacking. C. proximus was extracted using solvents with increasing polarity. In-vitro cytotoxic activity of C. proximus extracts was examined against liver (HepG2), lung (A549), prostate (PC3), and bone (MG63) cell lines using MTT assay in comparison to doxorubicin. Flow cytometry was used to analyze the cell cycle for identification of the phase of inhibition. Chemical composition of the most active fraction was examined using the GC/MS technique. Molecular docking was used to explore the mechanism of cytotoxicity against A549, and the results were confirmed by Western blot analysis. Petroleum ether fraction was the highly effective fraction against A549 with IC50 = 14.02 ± 2.79. GC/MS analysis of Pet.Eth led to the identification of nine compounds in unsaponifiable matter and 27 components in the saponifiable fraction. Di-N-octyl phthalate, 3-ß-hydroxylean-11.13(18)-dien-30-oic acid methyl ester, elemol hydrocarbons, linoelaidic acid and linoleic acid demonstrated the lowest docking binding scores and similar binding modes against CDK2 as compared to that attained by the native ligand R-Roscovitine "CDK2 ATP inhibitor". Western blot analysis demonstrated that CDK2/cyclinA2 protein expression has been suppressed in A549 cell lines by Pet.Eth fraction.


Subject(s)
Cyclin A2 , Cyclin-Dependent Kinase 2 , Gas Chromatography-Mass Spectrometry , Molecular Docking Simulation , Plant Extracts , Humans , Cyclin-Dependent Kinase 2/chemistry , Cyclin-Dependent Kinase 2/metabolism , A549 Cells , Plant Extracts/pharmacology , Plant Extracts/chemistry , Cyclin A2/metabolism , Phytochemicals/pharmacology , Phytochemicals/chemistry , Lung Neoplasms/drug therapy , Lung Neoplasms/pathology , Lung Neoplasms/metabolism , Hep G2 Cells , Cell Line, Tumor , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Cell Cycle Checkpoints/drug effects , Cell Proliferation/drug effects
3.
Cell Biochem Funct ; 41(6): 642-657, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37342005

ABSTRACT

The hepatoprotective effects of methanol extract of Mimusops elengi Linn. (M. elengi L.) leaves and isolated pure myricitrin (3-, 4-, 5-, 5, 7-five hydroxyflavone-3-O-α-l-rhamnoside) (Myr) were evaluated in male rats exposed to γ-irradiation. The extraction of M. elengi L. leaves was performed using ethyl acetate (EtOAC). Seven groups of rats were used: control group, irradiated (IRR) group (6 Gy of γ-rays in a single dose), vehicle group (oral administration of 0.5% carboxymethyl cellulose for 10 days), EtOAC extract group (100 mg/kg body weight of extract, orally for 10 days), EtOAC + IRR group (administration of extract and exposure to γ-rays on Day 7), Myr group (50 mg/kg body weight Myr, orally for 10 days), and Myr + IRR group (administration of Myr and exposure to γ-rays on Day 7). High-performance liquid chromatography and 1H-nuclear magnetic resonance were used to isolate and characterize the compounds from M. elengi L. leaves. Enzyme-linked immunosorbent assay was used for biochemical analyses. Identified compounds were Myr, myricetin 3-O-galactoside, myricetin 3-O-rahmnopyranoside (1 → 6) glucopyranoside, quercetin, quercitol, gallic acid, α-,ß-amyrin, ursolic acid, and lupeol. Serum aspartate transaminase and alanine transaminase activities were significantly increased, while serum protein and albumin levels were significantly decreased after irradiation. Hepatic levels of tumor necrosis factor-α, prostaglandin 2, inducible nitric oxide synthase, interleukin-6 (IL-6), and IL-12 were increased following irradiation. Improvements were observed in most serological parameters after treatment with extract or pure Myr, with histological analyses confirming decreased liver injury in treated rats. Our study demonstrates that pure Myr has a greater hepatoprotective effect than M. elengi leaf extracts against irradiation-induced hepatic inflammation.


Subject(s)
Mimusops , Plant Extracts , Rats , Male , Animals , Plant Extracts/pharmacology , Plant Extracts/chemistry , Mimusops/chemistry , Liver , Body Weight , Plant Leaves
4.
Sci Rep ; 13(1): 7635, 2023 05 11.
Article in English | MEDLINE | ID: mdl-37169909

ABSTRACT

Iron overload causes multiorgan dysfunction and serious damage. Alnus incana from the family Betulaceae, widely distributed in North America, is used for treating diseases. In this study, we investigated the iron chelating, antioxidant, anti-inflammatory, and antiapoptotic activities of the total and butanol extract from Alnus incana in iron-overloaded rats and identified the bioactive components in both extracts using liquid chromatography-mass spectrometry. We induced iron overload in the rats via six intramuscular injections of 12.5 mg iron dextran/100 g body weight for 30 days. The rats were then administered 60 mg ferrous sulfate /kg body weight once daily using a gastric tube. The total and butanol extracts were given orally, and the reference drug (deferoxamine) was administered subcutaneously for another month. After two months, we evaluated the biochemical, histopathological, histochemical, and immunohistochemical parameters. Iron overload significantly increased the serum iron level, liver biomarker activities, hepatic iron content, malondialdehyde, tumor necrosis factor-alpha, and caspase-3 levels. It also substantially (P < 0.05) reduced serum albumin, total protein, and total bilirubin content, and hepatic reduced glutathione levels. It caused severe histopathological alterations compared to the control rats, which were markedly (P < 0.05) ameliorated after treatment. The total extract exhibited significantly higher anti-inflammatory and antiapoptotic activities but lower antioxidant and iron-chelating activities than the butanol extract. Several polyphenolic compounds, including flavonoids and phenolic acids, were detected by ultraperformance liquid chromatography-electrospray ionization-quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOF-MS) analysis. Our findings suggest that both extracts might alleviate iron overload-induced hepatoxicity and other pathological conditions characterized by hepatic iron overload, including thalassemia and sickle-cell anemia.


Subject(s)
Alnus , Chemical and Drug Induced Liver Injury , Iron Overload , Rats , Animals , Antioxidants/metabolism , Plant Extracts/chemistry , Iron Overload/metabolism , Iron/metabolism , Liver/metabolism , Chemical and Drug Induced Liver Injury/pathology , Anti-Inflammatory Agents/pharmacology , Butanols/metabolism
5.
J Ethnopharmacol ; 295: 115439, 2022 Sep 15.
Article in English | MEDLINE | ID: mdl-35667581

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Viscum cruciatum Sieb is a well-known medicinal plant in Jordan containing various secondary metabolites. It has traditionally been used to treat many ailments, most notably cancer. However, there is a significant gap between scientific research and its value in traditional medicine. AIM OF THE WORK: To evaluate the antiproliferative activity of different V. cruciatum extracts against MCF-7 breast cancer cell lines and recognize the affected cell cycle phase. Besides, identifying the bioactive components present in the active extract using LC/MS technique. Also, to determine the possible mechanism of action by in silico and in-vitro study. MATERIALS AND METHODS: V. cruciatum was extracted using solvents with increasing polarity. The antiproliferative effects of the extracts against MCF-7 cell lines were evaluated using SRB assay. Further, flow cytometry was used to identify the inhibited phase of the cell cycle, while LC/MS-MS technique was used to analyze the chemical composition of the most active extract. After that, the putative mechanism of action was investigated through in-silico docking, molecular dynamic simulation for compounds with the highest docking scores, and Western blot analysis of cyclin-dependent kinases (CDK2/4/6). RESULTS: The chloroform/methanol 90/10 (ChMe) extract showed the most potent antiproliferative effect against MCF-7 cells (IC50 = 23.8 µg/mL), and cell cycle arrest at the G0/G1phase. Furthermore, LC-MS/MS analysis revealed the presence of several polyphenolics belonging to the flavonoids and phenolic acids classes. Additionally, quercetin-4'-glucoside, 3, 5, 7-trihydroxy-4'-methoxy flavone, and hesperetin-7-O-neohesperidoside demonstrated the highest docking binding scores and stable complexes against CDK2 and CDK4/6. Moreover, RMSD (root-mean-square deviation), RMSF (root-mean-square fluctuation), Rg (radius of gyration), and energy analysis during molecular dynamic simulation indicated the stable binding of the studied complexes. These results were supported by Western blot analysis, which revealed the downregulation of CDK2, CDK4, and CDK6 protein expression in MCF-7 cell lines. CONCLUSION: These findings emphasized the potential breast anticancer activity of the V. cruciatum ChMe extract by arresting the G0/G1 phase of the cell cycle, which could be related to its flavonoid content. Moreover, the results provided experimental support for the traditional anticancer activity of V. cruciatum, and its ChMe extract might be a source of chemoprotective or chemotherapeutic isolates.


Subject(s)
Antineoplastic Agents, Phytogenic , Viscum , Antineoplastic Agents, Phytogenic/therapeutic use , Apoptosis , Cell Cycle , Cell Line, Tumor , Cell Proliferation , Chromatography, Liquid , Flavonoids/pharmacology , G1 Phase Cell Cycle Checkpoints , Humans , MCF-7 Cells , Plant Extracts/therapeutic use , Tandem Mass Spectrometry
6.
J Trace Elem Med Biol ; 70: 126924, 2022 Mar.
Article in English | MEDLINE | ID: mdl-35007915

ABSTRACT

BACKGROUND: Cadmium is a potential environmental pollutant with worldwide health problems. Many Ficus species are reported to have an extensive diversity of traditional uses, among them the treatment of reproductive toxicity. OBJECTIVES: This study set out to evaluate the effect of Ficus natalensis extract on the testicular impairments induced by cadmium chloride (CdCl2) and investigated the potential mechanisms associated with its treatment. METHODS: Thus, 40 male albino rats were categorized into 4 groups (n = 10); group I (control), group II (cadmium-treated group) orally received 5 mg/kg/day CdCl2 for one month, group III (cadmium + Ficus natalensis extract) orally received 5 mg/kg/day CdCl2 for one month plus 200 mg/kg/day Ficus natalensis extract for another month, and group IV (cadmium + reference drug (mesterolone) orally received 5 mg/kg/day CdCl2 for one month plus 4.16 mg/kg/day mesterolone for another month. RESULTS: At the end of experiment, CdCl2 administration markedly induced histological and histo-morphometric changes with a substantial (p < 0.05) decrease in the sperm count, sperm motility, serum TAC, serum testosterone, downregulation in the mRNA expression levels of testicular 17ß-HSD and StAR, in addition to a significant increase in serum TNF-α and testicular MDA level compared to the control group. Conversely, the treatment with Ficus natalensis methanolic extract as well as the reference drug significantly ameliorated the above-mentioned adverse effects induced by CdCl2. CONCLUSIONS: Our results suggested that Ficus natalensis extract can attenuate the CdCl2-induced testicular impairments via inhibiting the oxidative cell damage and inflammation that contributed to CdCl2 toxicity.


Subject(s)
Cadmium Chloride , Ficus , Animals , Antioxidants/metabolism , Cadmium/toxicity , Cadmium Chloride/toxicity , Male , Oxidative Stress , Plant Extracts/metabolism , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Rats , Sperm Motility , Testis
7.
Arch Physiol Biochem ; 128(2): 382-393, 2022 Apr.
Article in English | MEDLINE | ID: mdl-31711319

ABSTRACT

Liver fibrosis is a grave problem worldwide, and the development of this condition is the first step towards cirrhosis. In fact, when lesions of different aetiologies chronically affect the liver, it triggers fibrogenesis, the resulting damage and the progression of fibrosis cause serious clinical influences including severe complications, expensive treatments, and death in end-stage liver disease. Although impressive progress has been reported in understanding the pathogenesis of liver fibrosis, no effective agent has been developed to prevent or reverse the fibrotic process directly. This article reviews natural products, herbal medicines and nutritional components that exhibited an anti-fibrotic activity through different mechanisms of action, including suppressing of cytokine production, inhibition of hepatic stellate cells "HSCs" propagation, modulation of the molecular mechanisms leading to hepatic fibrosis, free radical scavenging and anti-inflammatory properties.


Subject(s)
Biological Products , Biological Products/pharmacology , Biological Products/therapeutic use , Fibrosis , Hepatic Stellate Cells , Humans , Liver Cirrhosis/drug therapy , Liver Cirrhosis/prevention & control , Plant Extracts/pharmacology , Plant Extracts/therapeutic use
8.
Drug Chem Toxicol ; 45(1): 367-377, 2022 Jan.
Article in English | MEDLINE | ID: mdl-31778078

ABSTRACT

The aim of the current study was to examine and compare the cardioprotective activities of the chloroform and petroleum extracts the leaves of Casuarina suberosa in isoproterenol (ISO)-induced cardiac tissue oxidative stress. Rats were categorized into 6 groups as follows: control group, vehicle or Tween 80-treated group, ISO-treated group, chloroform extract + ISO treated group, petroleum ether extract + ISO treated group and Reference drug (Captopril) + ISO treated group. ISO injection significantly (p < 0.05) increased the activities of cardiac marker enzymes (CK-MB, LDH, ALT, and AST), cardiac troponin-I, levels of lipid peroxides (MDA), nitric oxide (NO), and vascular endothelial growth factor (VEGF), serum angiotensin-converting enzyme (ACE) activity and neutrophil infiltration marker; myeloperoxidase (MPO) in the cardiac tissues. Pretreatment with chloroform or petroleum ether extracts significantly (p < 0.05) prevented the ISO-induced alteration; they upregulated VEGF expression. Histopathological findings corroborated biochemical results. These extracts exerted a cardioprotective effect by alleviating oxidative stress.


Subject(s)
Cardiotonic Agents , Animals , Cardiotonic Agents/metabolism , Cardiotonic Agents/pharmacology , Cardiotonic Agents/therapeutic use , Myocardium/metabolism , Oxidative Stress , Plant Extracts/metabolism , Plant Extracts/pharmacology , Rats , Rats, Wistar , Vascular Endothelial Growth Factor A/metabolism , Vascular Endothelial Growth Factor A/pharmacology
9.
Drug Chem Toxicol ; 45(5): 2341-2351, 2022 Sep.
Article in English | MEDLINE | ID: mdl-34167392

ABSTRACT

Cardiovascular ailments result in a great rate of mortality all over the world. Myocardial infarction is a common presentation of cardiovascular disease. The current work aimed to investigate and compare the cardioprotective potentials of methanolic extracts from the aerial parts from Bauhinia purpurea and Bauhinia madagascariensis in adrenaline-induced cardiotoxicity in rats. The rats were categorized into five groups as follows: control group, adrenaline-treated group, Bauhinia purpurea extract + adrenaline treated group, Bauhinia madagascariensis+ adrenaline treated group, reference drug (captopril) + adrenaline treated group. The extracts as well as the reference drug were orally administered for 21 consecutive days. On day 22, adrenaline was injected as a single dose for 2 consecutive days. The adrenaline injection caused a significant increase (p < 0.05) in serum cardiac markers (ALT, AST, CK-MB, LDH), angiotensin-converting enzyme (ACE) and matrix metalloproteinase (MMP-9), inducible nitric oxide synthase (iNOS) activities, tumor necrosis factor-α (TNF-α) cardiac lipid peroxides (MDA) levels and a significant decline (p < 0.05) in cardiac reduced glutathione (GSH) levels compared to their corresponding controls. The pretreatment extracts significantly ameliorated (p < 0.05) these alterations. Histopathological investigations supported the biochemical data. Bauhinia madagascariensis extract exerted a significant anti-inflammatory activity than that of Bauhinia purpurea. In addition, Bauhinia madagascariensis extract revealed a significant inhibitory activity on ACE compared to that of Bauhinia purpurea, (p < 0.05). These data reveal that both extracts had a strong protective activity against adrenaline-induced cardiotoxicity via improving cardiac function, reducing ECG and histopathological changes that could be mediated in part through its anti-oxidant, anti-inflammatory effects, inhibition of ACE, MMP-9, and iNOS.


Subject(s)
Bauhinia , Animals , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Antioxidants/pharmacology , Cardiotoxicity , Epinephrine , Matrix Metalloproteinase 9 , Methanol , Plant Components, Aerial , Plant Extracts , Rats
10.
Arch Physiol Biochem ; 126(2): 116-128, 2020 May.
Article in English | MEDLINE | ID: mdl-30269604

ABSTRACT

Chronic hepatitis C virus (HCV) infection is a significant public health problem, with a worldwide prevalence of approximately 170 million. Current therapy for HCV infection includes the prolonged administration of a combination of ribavirin and PEGylated interferon-α, for over a decade. This regimen is expensive and often associated with a poor antiviral response and unwanted side effects. A highly effective combination treatment is likely required for the future management of HCV infections and entry inhibitors could play an important role. Currently, no entry inhibitor has been licensed for the prophylactic treatment of hepatitis C. Therefore, additional agents that combat HCV infection are urgently needed and must be developed. Many phytochemical constituents have been identified that display considerable inhibition of HCV at some stage of the life cycle. This review will summarise the current state of knowledge on natural products and their possible activities in the context of HCV infection.


Subject(s)
Antiviral Agents/therapeutic use , Biological Products/therapeutic use , Flavonoids/therapeutic use , Hepacivirus/drug effects , Hepatitis C, Chronic/drug therapy , Antiviral Agents/chemistry , Antiviral Agents/isolation & purification , Aquatic Organisms/chemistry , Biological Products/chemistry , Biological Products/isolation & purification , Clinical Trials as Topic , Drug Therapy, Combination , Flavonoids/isolation & purification , Hepacivirus/genetics , Hepacivirus/growth & development , Hepacivirus/metabolism , Hepatitis C, Chronic/pathology , Hepatitis C, Chronic/virology , Humans , Interferon-alpha/therapeutic use , Plant Extracts/chemistry , Ribavirin/therapeutic use
11.
Nat Prod Res ; 33(12): 1832-1833, 2019 Jun.
Article in English | MEDLINE | ID: mdl-29417837

ABSTRACT

The diuretic activity of ethanolic extract of Panicum repens was investigated in rats. A single oral dose of 500 mg/kg of P. repens extract were given to rats, after 24 h, urine volume, its sodium and potassium concentrations were estimated. Treatment with P. repens extract caused a significant increase in tested parameters as compared to their corresponding controls, p < 0.05.


Subject(s)
Diuretics/pharmacology , Panicum/chemistry , Plant Extracts/pharmacology , Plant Roots/chemistry , Rhizome/chemistry , Administration, Oral , Animals , Diuretics/administration & dosage , Diuretics/chemistry , Drug Evaluation, Preclinical/methods , Ethanol/chemistry , Male , Plant Extracts/analysis , Plant Extracts/chemistry , Potassium/urine , Rats, Wistar , Sodium/urine
12.
Arch Physiol Biochem ; 125(2): 128-135, 2019 May.
Article in English | MEDLINE | ID: mdl-29457523

ABSTRACT

Hyperlipidemia is an abnormality of lipid metabolism, characterized by an elevation of total cholesterol, triglyceride, and low density lipoprotein-cholesterol, and/or a decreasing of high density lipoprotein cholesterol in circulating levels. Hyperlipidemia has been ranked as one of the greatest risk factors contributing to prevalence and severity of coronary heart diseases. Hyperlipidemia-associated lipid disorders are considered the cause of atherosclerotic cardiovascular disease. There has been a growing interest in natural products and their role in the maintenance and improvement of health and wellness. The cholesterol-lowering effect of dietary plants has been well studied and various natural products were shown to be helpful in lowering plasma cholesterol levels and encouraging safety profile. The main focus of this review is to describe what we know to date of natural products, along with their lipid-lowering mechanisms, which are either through inhibition of cholesterol absorption, inhibition of cholesterol synthesis or antioxidant mechanisms.


Subject(s)
Biological Products/pharmacology , Hyperlipidemias/drug therapy , Animals , Biological Products/therapeutic use , Humans
13.
Planta Med ; 84(12-13): 964-970, 2018 Aug.
Article in English | MEDLINE | ID: mdl-29763943

ABSTRACT

A phytochemical study of n-hexane, CHCl3, and CHCl3-MeOH extracts of Aphanamixis polystachya leaves led to the isolation of 10 compounds. Five of them turned out to be new natural compounds, including two mexicanolide-type (1, 2: ) and three polyoxyphragmalin-type (3: -5: ) limonoids, together with two known andirobin-type limonoids (6, 7: ) and three phenolic derivatives. The structures of the new compounds were established on the basis of spectroscopic methods to be 8-hydro-14,15-en-cabralin (1: ), 3-deacetyl-8-hydro-cabralin-14,15-en-3-one (2: ), 20,22-dihydroxy-21,23-dimethoxytetrahydrofuran khayanolide A (3: ), 1-deacetyl-3-dehydroxy-3-oxokhaysenelide E (4: ), and meliaphanamixin A (5: ). All compounds were isolated for the first time from this species. The ability of the isolated limonoids to interact with the molecular chaperone Hsp90 was tested. Compounds 6: and 7: were the most active.


Subject(s)
HSP90 Heat-Shock Proteins/metabolism , Limonins/metabolism , Meliaceae/chemistry , Cell Survival/drug effects , Humans , Jurkat Cells , Limonins/chemistry , Limonins/isolation & purification , Plant Leaves/chemistry , Surface Plasmon Resonance
14.
Arch Physiol Biochem ; 124(5): 383-389, 2018 Dec.
Article in English | MEDLINE | ID: mdl-29268636

ABSTRACT

Diabetes is a group of metabolic diseases characterised by hyperglycemia resulting from defects in insulin secretion, insulin action, or both. The chronic hyperglycemia of diabetes is associated with long-term damage and dysfunction of many organs. Diabetes caused 1.5 million deaths in 2012, with hyperglycemia causing an additional 2.2 million deaths, as it is associated with increased risk of cardiovascular and other diseases. Various types of plants have been used for several centuries worldwide not only as dietary supplements but also as traditional treatment regimens for many diseases. So far, a large number of traditionally claimed plant medicine has been tested for diabetes and some of them showed a promising therapeutic potential. The main focus of this review is to describe what we know to date of herbal extracts, along with their glucose-lowering mechanisms, which are either through insulin-mimicking activity, enhanced ß-cells regeneration, or glucose uptake.


Subject(s)
Diabetes Mellitus, Type 1/therapy , Diabetes Mellitus, Type 2/therapy , Hyperglycemia/prevention & control , Hypoglycemia/prevention & control , Hypoglycemic Agents/therapeutic use , Plant Extracts/therapeutic use , Animals , Antioxidants/adverse effects , Antioxidants/therapeutic use , Combined Modality Therapy/adverse effects , Diabetes Mellitus, Type 1/blood , Diabetes Mellitus, Type 1/drug therapy , Diabetes Mellitus, Type 1/metabolism , Diabetes Mellitus, Type 2/blood , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/metabolism , Dietary Supplements/adverse effects , Drugs, Chinese Herbal/adverse effects , Drugs, Chinese Herbal/therapeutic use , Humans , Hypoglycemia/chemically induced , Hypoglycemia/etiology , Hypoglycemic Agents/administration & dosage , Insulin Resistance , Insulin Secretion/drug effects , Plant Extracts/adverse effects
15.
Pharmacogn Mag ; 13(Suppl 3): S484-S488, 2017 Oct.
Article in English | MEDLINE | ID: mdl-29142403

ABSTRACT

BACKGROUND: Dipterygium glaucum Decne. herb is one of the common traditional plants with multiple medicinal uses. OBJECTIVE: To isolate the major constituents and to investigate the antioxidant, antimicrobial, and cytotoxic activities of this herb. MATERIALS AND METHODS: Methanolic extract of D. glaucum herb was fractionated using n-hexane, dichloromethane, and n-butanol. Butanol fraction was chromatographed using column chromatography and preparative thin layer chromatography to isolate the major constituents. Isolated compounds were elucidated by means of spectroscopic methods, including 1D, 2D NMR (1H, 13C, DEPT, COSY, HSQC, HMBC, NEOSY) and MS analysis. Total phenolic content using Folin-Ciocalteu reagent and antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay of the total methanolic extract were evaluated. Cytotoxic potential of both methanolic extract and butanol fraction was tested using a crystal violet viability assay. Antimicrobial activities of both extracts were investigated using diffusion agar technique. RESULTS: Apigenin 6, 8-di-C-glucopyranoside (vicenin-2), quercetin-3`-O-methyl-3-O-glucopyranoside, quercetin-3`-O-methyl-3-O-galactopyranoside, quercetin-3-O-ß-D-glucopyranoside, and quercetin-3-O-ß-D-galactopyranoside were isolated and elucidated. Total phenolic content was (83.89 mg gallic acid equivalent/g extract). The EC50 value of scavenging DPPH radical was 152.0 ± 2 mg/mL. Butanol fraction showed the highest cytotoxic activity against cervical and breast carcinoma cells (IC50 3.6 and 6.1 mg/mL, respectively). Both methanolic extract and butanol fraction showed wide spectrum antimicrobial activity against Gram-positive and Gram-negative bacteria and some fungi. The highest activity was from methanolic extract against Enterococcus faecalis (83.25%) and against Candida tropicalis (77.03%) as compared to reference antibiotics. CONCLUSION: Data obtained from this study demonstrate that D. glaucum possesses significant antioxidant, cytotoxic, and antimicrobial activities which could be ascribed to its flavonoidal content. SUMMARY: Dipterygium glaucum Decne. herb is one of the common traditional plants with multiple medicinal uses in KSAFive flvonidal glycosides were isolated and elucidatedThis study demonstrated that D. glaucum possesses significant antioxidant, cytotoxic, and antimicrobial activities. Abbreviations used: KSA: Kingdom of Saudi Arabia; TLC: Thin Layer Chromatography; DPPH: 2,2`-diphenyl-1-picrylhydrazyl; EC50: Half maximal effective concentration; IC50: Half maximal inhibitory concentration; DMSO: dimethyl sulfoxide; NMR: Nuclear Magnetic Resonance; ESIMS: Electrospray ionization mass spectrometry; MeOH: Methyl alcohol.

16.
Nat Prod Res ; 30(24): 2791-2797, 2016 Dec.
Article in English | MEDLINE | ID: mdl-27010619

ABSTRACT

Phytochemical investigation of Encephalartos villosus Lehm. leaves afford two new illudalane sesquiterpenes namely Encephaldiene 1 and Encephaldiene 2 together with four known flavone glycosides, Luteolin-7-rutinoside, Luteolin-7-glucoside, Luteolin-7-rhamnoside and Apigenin-7-glucoside. The structures of the isolated compounds were elucidated by means of spectroscopic methods including 1D and 2D NMR experiments along with HRESIMS spectrometry. Antimicrobial activity of CHCl3 and MeOH extracts was investigated. Both extracts showed antibacterial activity against Gram-positive bacteria Streptococcus pneumonia and Bacillus subtilis, and antifungal activity against Aspergillus fumigatus. While CHCl3 extract showed additional activity against Gram-negative bacteria Escherichia coli.

17.
Z Naturforsch C J Biosci ; 70(5-6): 139-44, 2015.
Article in English | MEDLINE | ID: mdl-26098699

ABSTRACT

The hypolipidemic effect of an ethanolic extract from the roots and rhizomes of Panicum repens L. was investigated in rats suffering from high-cholesterol, diet-induced hyperlipidemia, and the phytochemicals in the extract were analyzed. The extract was administered p.o. in doses of 250 mg/kg/day together with cholesterol at a dose of 100 mg/kg/day for 7 weeks. The high-cholesterol diet caused a significant increase in total lipids, total cholesterol (TC), total triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and the atherogenic index, whereas the level of high-density lipoprotein cholesterol (HDL-C) was significantly decreased. Administration of the P. repens extract (p<0.05) significantly reduced the rise of the serum levels of total lipids, TC, TG, and LDL-C, as well as the atherogenic index, whereas it significantly increased (p<0.05) the level of HDL-C. HPLC analysis of the phenolics and flavonoids in the extract revealed the presence of gallic acid, chlorogenic acid, chicoric acid, primulic acid, rutin, apigenin-7-glucoside, and quercetin. In conclusion, the P. repens extract was found to possess hypolipidemic activity in high-fat, diet-induced hyperlipidemic rats.


Subject(s)
Hyperlipidemias/drug therapy , Panicum/chemistry , Plant Extracts/therapeutic use , Plant Roots/chemistry , Rhizome/chemistry , Animals , Cholesterol, Dietary/administration & dosage , Flavonoids/analysis , Hypolipidemic Agents/therapeutic use , Kidney Function Tests , Lipids/analysis , Lipids/blood , Liver/chemistry , Liver Function Tests , Male , Mice , Phenols/analysis , Plant Extracts/pharmacology , Rats , Rats, Wistar
18.
Planta Med ; 79(14): 1341-7, 2013 Sep.
Article in English | MEDLINE | ID: mdl-23929245

ABSTRACT

Four new clerodane diterpenes (1-4) and one new phenylpropanoid (5) have been isolated from Clerodendrum splendens aerial parts, together with nine known compounds. Their structures were determined by spectroscopic and spectrometric analysis and chemical methods. The absolute configuration of the 15,16-diol moiety in 4 was determined by Snatzke's method. Antiproliferative activity of diterpenes in HeLa cells was also evaluated. The IC50 values were 98 ± 11 µM for 3 and 101 ± 8 µM for 1, respectively.


Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Clerodendrum/chemistry , Diterpenes, Clerodane/isolation & purification , Phenols/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/therapeutic use , Diterpenes, Clerodane/chemistry , Diterpenes, Clerodane/pharmacology , Diterpenes, Clerodane/therapeutic use , HeLa Cells , Humans , Molecular Structure , Neoplasms/drug therapy , Phenols/chemistry , Phenols/pharmacology , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/therapeutic use
19.
J Med Chem ; 56(4): 1583-95, 2013 Feb 28.
Article in English | MEDLINE | ID: mdl-23362862

ABSTRACT

The potential of heat shock protein 90 (Hsp90) as a therapeutic target for numerous diseases has made the identification and optimization of novel Hsp90 inhibitors an emerging therapeutic strategy. A surface plasmon resonance (SPR) approach was adopted to screen some iridoids for their Hsp90 α binding capability. Twenty-four iridoid derivatives, including 13 new natural compounds, were isolated from the leaves of Tabebuia argentea and petioles of Catalpa bignonioides. Their structures were elucidated by NMR, electrospray ionization mass spectrometry, and chemical methods. By means of a panel of chemical and biological approaches, four iridoids were demonstrated to bind Hsp90 α. In particular, the dimeric iridoid argenteoside A was shown to efficiently inhibit the chaperone in biochemical and cellular assays. Our results disclose C9-type iridoids as a novel class of Hsp90 inhibitors.


Subject(s)
Antineoplastic Agents/chemistry , HSP90 Heat-Shock Proteins/antagonists & inhibitors , Iridoids/chemistry , Adenosine Triphosphatases/antagonists & inhibitors , Antineoplastic Agents/pharmacology , Bignoniaceae/chemistry , Cell Proliferation/drug effects , Cell Survival/drug effects , Citrate (si)-Synthase/chemistry , Drug Screening Assays, Antitumor , HeLa Cells , Humans , Iridoids/isolation & purification , Iridoids/pharmacology , Kinetics , Molecular Docking Simulation , Stereoisomerism , Structure-Activity Relationship , Surface Plasmon Resonance , Thermodynamics
20.
Phytochemistry ; 76: 172-7, 2012 Apr.
Article in English | MEDLINE | ID: mdl-22189050

ABSTRACT

Eight compounds, nagilactone C 7-O-α-L-arabinopyranosyl-(1→4)-ß-D-xylopyranoside, nagilactone C 7-O-ß-D-glucopyranosyl-(1→4)-ß-D-xylopyranoside, nagilactone C 7-O-ß-D-xylopyranoside, nagilactone A 7-O-α-L-arabinopyranosyl-(1→4)-ß-D-xylopyranoside, 2ß,15S,16,17,19-pentahydroxy-isopimar-8(14)-ene 17-O-ß-D-glucopyranoside, 2ß,15R,16,17,19-pentahydroxy-isopimar-8(14)-ene 17-O-ß-D-glucopyranoside, 1-(2,6,6-trimethyl-4-hydroxycyclohexenyl)-1-hydroxy-buta-1-en-3-one 4-O-ß-D-glucopyranoside, and vitexin 2″-O-ß-D-(6'''-acetyl)-glucopyranoside together with 13 known compounds, were isolated from the leaves of Podocarpus elongatus. Structures were elucidated by 1D and 2D NMR spectroscopy as well as by ESI mass spectrometry and chemical methods. The absolute configurations of the 15,16-diol moieties in two compounds were determined using Snatzke's method.


Subject(s)
Butylated Hydroxytoluene/chemistry , Diterpenes/isolation & purification , Flavones/chemistry , Glycosides/chemistry , Plant Leaves/chemistry , Tracheophyta/chemistry , Acids/chemistry , Chemical Fractionation/methods , Chromatography, High Pressure Liquid/methods , Diterpenes/chemistry , Flavones/isolation & purification , Glycosides/isolation & purification , Hydrolysis , Magnetic Resonance Spectroscopy , Molecular Conformation , Plant Extracts/chemistry , Spectrometry, Mass, Electrospray Ionization
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