Anti-proliferative Activities of Two Flavonols with Unsubstituted B-ring from the Leaves of Platanus acerifolia

The anti-proliferative activities against five cancer cell lines of two flavonols (1, 2) with unsubstituted B ring isolated from the ethanol extract of the leaves of Platanus acerifolia were investigated. The results showed that compound 1 possessed a noteworthy anti-proliferative activity against MGC-803 cells with an IC50 value of 17.26±1.04 μM, and compound 2 was less active than 1 with an IC50 value of 20.29±1.37 μM compared with 41.94±1.58 μM for the positive control group. In addition, the results of Hoechst 33258 staining, AO/EB staining and annexinV-FITC assays indicated that 1 caused a significant MGC-803 cellular apoptosis in a dose-dependent manner. The further mechanisms showed that compound 1 induced the production of ROS, decreased the mitochondrial membrane potential, and altered pro- and anti-apoptotic proteins, leading to activation of caspase-9 and caspase-3 in the process of cellular apoptosis. The present investigation indicated that compound 1 could be used as a potential anti-cancer candidate.

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In VivoAntiplasmodial and Analgesic Effect of Crude Ethanol Extract ofPiper guineenseLeaf Extract inAlbinoMice

Scientifica ◽

10.1155/2016/8687313 ◽

2016 ◽

Vol 2016 ◽

pp. 1-6 ◽

Cited By ~ 2

Author(s):

A. Y. Kabiru ◽

G. F. Ibikunle ◽

D. A. Innalegwu ◽

B. M. Bola ◽

F. M. Madaki

Keyword(s):

Body Weight ◽

Analgesic Efficacy ◽

Ethanol Extract ◽

Positive Control ◽

Positive Control Group ◽

Control Group ◽

Piper Guineense ◽

Standard Drug ◽

Analgesic Effects ◽

Dose Dependent

Antiplasmodial and analgesic effects of crude ethanol extract ofPiper guineensewas investigated in mice. The antiplasmodial and analgesic efficacy of the extract was judged on its ability to reduce parasitemia and writhing, respectively, in mice. The antiplasmodial screening involved treating infected mice with 200, 400, and 600 mg/kg body weight of extract while the positive control group was given standard artesunate drug. The analgesic test was carried out by administering 1000, 1500, and 2000 mg/kg body weight of extract to three groups of healthy mice, respectively, after induction of pain with 0.75% acetic acid. The positive control group was given aspirin drug. Parasitemia was reduced by 28.36%, 43.28%, and 62.69% in a dose-dependent pattern in the curative test which was significantly different (P<0.05) from 96.03% of the standard drug. The reduction of writhing by mice given the extract was also dose-dependent (36.29, 45.43, and 59.07%). Aspirin drug was however more effective (86.36%). The extract was safe at 2000 mg/kg body weight. Phytochemical screening revealed the presence of flavonoids, tannins, phlobatannins, terpenoids, and coumarins. Result obtained in this study demonstrated the efficacy of ethanol extract ofPiper guineenseas an antiplasmodial and analgesic agent.

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Rehmannia glutinosa Activates Intracellular Antioxidant Enzyme Systems in Mouse Auditory Cells

The American Journal of Chinese Medicine ◽

10.1142/s0192415x06004545 ◽

2006 ◽

Vol 34 (06) ◽

pp. 1083-1093 ◽

Cited By ~ 9

Author(s):

Hyeon-Hee Yu ◽

Yeon-Hwa Kim ◽

Su-Young Jung ◽

Mee-Kyung Shin ◽

Rae-Kil Park ◽

...

Keyword(s):

Antioxidant Enzyme ◽

Ethanol Extract ◽

Control Group ◽

Cytotoxicity Test ◽

Dependent Manner ◽

Rehmannia Glutinosa ◽

Traditional Use ◽

Enzyme Systems ◽

Dose Dependent ◽

Gpx Activity

Steamed roots of Rehmannia glutinosa (R. glutinosa) have been traditionally used in Oriental medicine for the treatment of auditory diseases such as tinnitus and hearing loss. To investigate whether the ethanol extract of steamed roots of R. glutinosa (SRG) increases activity of antioxidant enzymes and the level of glutathione (GSH), we measured activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX), and glutathione reductase (GR) and GSH level in HEI-OC1 cells after treatment with 5–50 μg/ml of SRG. The SOD and CAT activities were significantly increased in the presence of SRG compared to the control group. Maximal activities of SOD and CAT were observed in these cells exposed to 10 μg/ml of SRG. The GPX activity also increased dramatically in response to the treatment with SRG in a dose-dependent manner. The GR activity was only increased in the presence of 50 μg/ml of SRG compared to the control group. The level of GSH gradually increased in the presence of 5–50 μg/ml of SRG. In the cytotoxicity test, 5–50 μg/ml of SRG did not show any significant cytotoxicity. These results suggest that the traditional use of R. glutinosa for the treatment of auditory diseases may be explained, in part, by activation of intracellular antioxidant enzyme systems. Further studies are necessary to clarify the active constituents of SRG responsible for such biomolecular activities.

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Effects of Enoxaparin Emulsion on Dimethylbenzanthracene-induced Breast Cancer in Female Rats

Research in Molecular Medicine ◽

10.18502/rmm.v5i4.3062 ◽

2018 ◽

Vol 5 (4) ◽

pp. 23

Author(s):

Bolandpayeh M ◽

Hassanpour-Ezzati M ◽

Mousavi Z

Keyword(s):

Breast Cancer ◽

Tumor Growth ◽

Tumor Volume ◽

Positive Control ◽

Female Rats ◽

Positive Control Group ◽

Control Group ◽

Dependent Manner ◽

Angiogenic Proteins ◽

Dose Dependent

Introduction: Enoxaparin is an anticoagulant medication. Anticoagulation inhibits tumor cell-mediated release of angiogenic proteins and diminishes angiogenic response. Angiogenesis is an important event in various cancers such as breast cancer. Angiogenesis provide oxygen and nutrients to tumor cells and causes tumor progression. The aim of the present study was to evaluate the anti-angiogenesis effect of an enoxaparin cream on breast cancer induced by dimethylbenzanthracene in rats. Methods: In this experimental in vivo study, 50 Wistar female rats were divided into negative control (vehicle), positive control (cream base), and 3 groups with enoxaparin treatment (40, 60, and 80 mg/ml). After one month of treatment along with breast cancer induction by dimethylbenzanthracene, breast tissue samples were isolated and stained with hematoxylin-eosin, and tumor growth suppression rate was calculated. Tumor size (length and width) was measured using a clipper, and the tumor volume was calculated using the following formula: V = (L × W × W)/2, where V is tumor volume, W is tumor width, L is tumor length. The data were analyzed using one-way ANOVA and Tukey’s post hoc test. Results: Tumor suppression was significantly increased in enoxaparin treatment groups compared to the positive control group (40 mg/ml of enoxaparin treated versus positive control group; P = 0.017, 60 mg/ml of enoxaparin treated versus positive control; P = 0.015, 40 mg/ml of enoxaparin treated versus positive control; P = 0.009, 60 mg/ml of enoxaparin treated versus 40 mg/ml of enoxaparin treated; P = 0.019, and 80 mg/ml of enoxaparin treated versus 40 mg/ml of enoxaparin treated; P = 0.011 in a dose-dependent manner. Conclusion: Enoxaparin inhibits breast cancer in a dose-dependent manner. The application of enoxaparin cream in patients with breast cancer may considerably reduce tumor growth.

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Comparative Evaluation of Analgesic, Antipyretic & Anti-Inflammatory Effects of Various Extracts of Dried Fruit of Illicium verum Hook.f (Star anise) in Rodents

Walailak Journal of Science and Technology (WJST) ◽

10.48048/wjst.2021.9456 ◽

2021 ◽

Vol 18 (9) ◽

Author(s):

Hafiza TUSEEF ◽

Muhammad Liaquat RAZA ◽

Tahira ASSAD

Keyword(s):

Ethanol Extract ◽

Maximum Effect ◽

Control Group ◽

Dependent Manner ◽

Dried Fruit ◽

Illicium Verum ◽

Anti Inflammatory ◽

Ethanol Extracts ◽

Dose Dependent ◽

Different Doses

The current investigation was designed to evaluate the analgesic, antipyretic, and anti-inflammatory effects of various extracts (methanol, ethanol, and aqueous) of dried fruit of Illicium verum hook.f, using 3 different doses (150, 250, and 350 mg/kg p.o) to verify the traditional uses of this spice. In the hot plate model of analgesia, ethanol extract showed a significant reduction in pain in a dose-dependent manner compared to the control group. The maximum effect was observed at 350 mg/kg dosage i.e., 16.90±0.17 s compared to the control group i.e., 5.03±0.05 s. The antipyretic activity was assessed in rats by Brewer’s yeast induction. The methanol and ethanol extracts produced a significant reduction in rectal temperature compared to the control group throughout the three doses. The maximum effect was observed at 350 mg/kg dosage of ethanol extract i.e., 37.1±0.8* compared to the control i.e., 39.1±0.3. In the paw edema model, methanol and ethanol extracts disclosed a significant reduction in paw edema at 350 mg/kg of dose. The maximum effect was observed at 350 mg/kg dosage of ethanol extract i.e., 0.25±0.23* compared to the control i.e., 0.97±0.4. In a behavioral study, locomotor activity (rearing) and exploratory activity (grooming) in mice was reduced significantly at higher doses (350 mg/kg p.o) involving the three extracts. However, scratching was increased non-significantly at all doses compared to the control group. This study concluded that various extracts of Illicium verum hook.f showed significant analgesic, antipyretic, and anti-inflammatory effects at different doses in a dose-dependent manner with varying potencies. The ethanol extract was found to be more potent among all, followed by methanol and aqueous extracts, whereas maximum effects were observed at 350 mg/kg of dose.

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Cardioprotective effects of Citrullus lanatus rinds in male wistar rats

Nigerian Journal of Animal Production ◽

10.51791/njap.v44i1.448 ◽

2020 ◽

Vol 44 (1) ◽

pp. 123-129

Author(s):

O. G. Akintunde ◽

E. S. Ajibola ◽

S. A. V. Abakpa ◽

B. O. Oluwo ◽

J. O. Olukunle

Keyword(s):

Risk Ratio ◽

Wistar Rats ◽

Citrullus Lanatus ◽

Ethanol Extract ◽

Cardiac Risk ◽

Control Group ◽

Dependent Manner ◽

Significant Difference ◽

Male Wistar Rats ◽

Dose Dependent

Water melon, citrullus lanatus is a common edible fruit belongs to the family of cucumber (Cucurbitacea). The outer part of citrullus lanatus known as the rind is always discarded. This study investigated the effects of ethanol extract of citrullus lanatus rinds orally administered on some liver function enzymes, kidney function markers, cardiac risk ratio, and the atherogenic coefficient indices in male wistar rats. Twenty-five male Wistar albino rats were randomly distributed into five groups (I, II, III, IV and V) of five rats each received 0mg/kg, 100 mg/kg, 200mg/kg, 400mg/kg and 800mg/kg of ethanol extract of Citrullus lanatus rinds respectively for 35days. The result showed that the effects of ethanol extract of citrullus lanatus rinds was not significant difference (p > 0.05) in serum liver enzymes (Aspartate aminotransferase, Alanine aminotransferase, Alkaline phosphatase) in increasing dose dependent manner when compared with control group. There were no significant differences (p > 0.05) in serum levels of urea and creatinine with increasing dose of ethanol extract of Citrullus lanatus rinds in rats when compared with control group. The extract showed significantly higher (p< 0.05) values in the serum HDL, cholesterol but there were significant reduction (p< 0.05) in the serum total cholesterol, triglycerides, LDL, VLDL and non-HDL values in rats at higher doses of the extract when compared with control group. While it was observed that the cardiac risk ratio, the atherogenic coefficient and indices decreased significantly (p< 0.05) in rats at increasing doses of ethanol extract of Citrullus lanatus rinds when compared with control group. This may suggest a likely cardio-protective effects of ethanol extract of Citrullus lanatus rinds in increasing dose dependent manner in rats when compared with control group. In conclusion, it can be inferred that Citrullus lanatus rinds can be consumed by animals without detrimental effect.

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Potency of Sunkist Orange (Citrus sinensisL. Osbeck) against Kidney Histology of White Wistar Rats Induced by Gentamicin

Majalah Obat Tradisional ◽

10.22146/mot.49107 ◽

2020 ◽

Vol 25 (1) ◽

pp. 42

Author(s):

Masdalena Nasution ◽

Chrismis Novalinda Ginting ◽

Edy Fachrial ◽

I Nyoman Ehrich Lister

Keyword(s):

Citrus Sinensis ◽

Cell Damage ◽

Ethanol Extract ◽

Food Supplement ◽

Positive Control ◽

Positive Control Group ◽

Control Group ◽

Anti Cancer ◽

Nephroprotective Activity ◽

Histopathological Results

About 1.7%-58% of all cases of acute kidney failure are caused by gentamicin nephrotoxicity and consequently increasing urea and creatinine levels in the blood which are indications of damage to function. Oranges contain secondary metabolites such as flavonoids, alkaloids, coumarin, limonoid, keratinoid and essential oil that have pharmacological activities such as antioxidants, anti-inflammatory, anti-cancer, and also nephroprotector. The purpose of this study is to evaluate the nephroprotective activity of Citrus sinensis peel ethanol extract (EEKJS) on rats induced by gentamicin. Rats were induced using gentamicin at a dose of 80 mg/kgBW intraperitoneally on the 7th day after induced at a dose of 50 mg/kgBW, 100 mg/kgBW, and 200 mg/kgBW for 7 days. The results obtained from the ethanol extract of Citrus sinensis peel gave nephroprotective with the lowest serum creatinine and urea levels at a dose of 200 mg/kgBW which was 0.4±0.02 mg/dl and 43.33 ± 2.51 mg/dl and difference significantly (p<0.05) with a positive control group which was only induced by gentamicin and histopathological results showed significant cell damage in the positive control group that was only induced by gentamicin, and in the 50 mg/kgBW dose group, 100 mg/kgBW, 200 mg/kgBW had cell repair after gentamicin induction. Citrus sinensis are highly recommended to be a food supplement for kidney protection.

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Ecological and physiological as well as biochemical properties of representatives of the Genus sedum L.

Ecology and Noospherology ◽

10.15421/031417 ◽

2014 ◽

Vol 25 (3-4) ◽

pp. 24-33

Author(s):

O. I. Dzjuba ◽

M. V. Yatsenko

Keyword(s):

Nitric Oxide ◽

Cell Line ◽

Methanol Extract ◽

Hepatoma Cell ◽

Ethanol Extract ◽

Biochemical Properties ◽

Biologically Active ◽

Hepatoma Cell Line ◽

Dependent Manner ◽

Dose Dependent

The article deals with the history of the study and the current state of research of physiological and biochemical properties of the plant genus Sedum that are useful for human and has been used in folk medicine for many years. It was noticed that antioxidant properties of extracts from plants S. sarmentosum, S. sempervivoides, S. takesimense were caused by the presence of phenolic compounds. Methanol extract of plants S. takesimense exhibited strong scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals as well as significant inhibitory effects on lipid peroxidation and low density lipoprotein (LDL) oxidation induced by a metal ion Cu2+. Various immunomodulatory activities of various fractions of plants extracts (S. dendroideum, S. kamtschaticum, S. sarmentosum, S. telephium) are observed. It was shown that the ethanol extract of S. sarmentosum and it’s fractions suppressed specific antibody and cellular responses to ovalbumin in mice. The methanol extract of plants S. sarmentosum reduced the levels of anti-inflammatory markers, such as volume of exudates, number of polymorphonuclear leukocytes, suppressed nitric oxide synthesis in activated macrophages via suppressed induction of inducible nitric oxide synthase (iNOS). Polysaccharides fractions from plants S. telephium inducing productions of tumor necrosis factor alpha (TNF-α), increasing the intensity of phagocytosis in vitro and in vivo. Methanol extract from the whole part of S. kamtschaticum strongly inhibit PGE2 production from lipopolysaccharide-induced RAW 264.7 cells, a mouse macrophage cell line via modulating activity in gene expression of the enzyme cyclooxygenase-2 (COX-2). The methanol extract of plants S. sarmentosum and the major kaempferol glycosides from S. dendroideum have antinociceptive activity. It was noticed that anti-adipogenic activity of extracts from plants S. kamtschaticum were caused by inhibition of peroxisome-proliferator-activated receptor γ (PPARγ) expression and it’s dependent target genes, such as genes encoding adipocyte protein 2 (аР2), lipoprotein lipase (LPL), adiponectin and CD36. Polysaccharides fractions from S. telephium cause inhibition of cell adhesion of human fibroblast (MRC5) to laminin and fibronectin via interfere with integrin-mediated cell behaviour and they contributed to the role of polysaccharides in cell-matrix interaction. The methanol extract of plants S. sarmentosum exhibited a significant inhibitory activity in the chick embryo chorioallantoic membrane angiogenesis in a dose-dependent manner. The crude alkaloid fraction of S. sarmentosum caused a dose-dependent inhibition of cell proliferation on murine hepatoma cell line BNL CL.2 and human hepatoma cell line HepG2 without necrosis or apoptosis. Alkaloids from plants S. sarmentosum may improve survival of hepatoma patients via the inhibition of excessive growth of tumor cells. Plant’s juices have antiviral activity (S. sarmentosum, S. spurium, S. stahlii). Crude ethanol extract S. praealtum have spermicidal activity of the in mice and a relevant inhibitory effect of aqueous extract on human spermatozoa motility as well as an anti-fertilizing activity in rats. Hepatoprotective triterpenes, e.g., δ-amyrone, 3-epi-δ-amyrin, δ-amyrin and sarmentolin were isolated from S. sarmentosum. 2- and 2,6-substituted piperidine alkaloids (e.g., norsedamine, allosedridine, sedamine, allosedamine) are observed in plants S. acre, which in the presence of data on the use of pyridine and piperidine derivatives for treating neurodegenerative diseases (e.g., Alzheimer's disease), points on the promising research in this area. Taking into account that biologically active compounds are accumulated in the aboveground vegetative organs of plants of Sedum, the prospects of further study of the use of Sedum for the purposes of biotechnology and in the pharmaceutical industry becomes apparent. This work extends the existing views regarding the use of plants Sedum.

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Ethanol Extract of Achillea fragrantissima Enhances Angiogenesis through Stimulation of VEGF Production

Endocrine Metabolic & Immune Disorders - Drug Targets ◽

10.2174/1871530321666201230113018 ◽

2020 ◽

Vol 21 ◽

Author(s):

Hana M. Hammad ◽

Amer Imraish ◽

Maysa Al-Hussaini ◽

Malek Zihlif ◽

Amani A. Harb ◽

...

Keyword(s):

Wound Healing ◽

Rural Communities ◽

Ex Vivo ◽

Ethanol Extract ◽

Aortic Ring ◽

Treated Group ◽

Control Group ◽

Dependent Manner ◽

Achillea Fragrantissima

Objective: Achillea fragrantissima L. (Asteraceae) is a traditionally used medicinal herb in the rural communities of Jordan. Methods: The present study evaluated the efficacy of the ethanol extract of this species on angiogenesis in both, ex vivo using rat aortic ring assay and in vivo using rat excision wound model. Results: In concentrations of 50 and 100 µg/ml, the ethanol extract showed angiogenic stimulatory effect and significantly increased length of capillary protrusions around aorta rings of about 60% in comparison to those of untreated aorta rings. In MCF-7 cells, the ethanol extract of A. fragrantissima stimulates the production of VEGF in a dose-dependent manner. 1% and 5% of ethanol extract of A. fragrantissima containing vaseline based ointment was applied on rat excision wounds for six days and was found to be effective in wound healing and maturation of the scar. Both preparations resulted in better wound healing when compared to the untreated control group and vaseline-treated group. This effect was comparable to that induced by MEBO, the positive control. Conclusion: The results indicate that A. fragrantissima has a pro-angiogenic effect, which may act through the VEGF signaling pathway.

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Efek Ekstrak Etanol Kulit Petai (Parkia speciosa Hassk) Terhadap Penurunan Kadar Glukosa Darah Mencit Jantan

Jurnal Katalisator ◽

10.22216/jk.v3i1.2178 ◽

2018 ◽

Vol 3 (1) ◽

pp. 1

Author(s):

Verawaty Verawaty ◽

Dhea Claudia Novel

Keyword(s):

Blood Glucose ◽

Ethanol Extract ◽

Negative Control Group ◽

Positive Control ◽

Negative Control ◽

Control Group ◽

Male Mice ◽

Glucose Levels ◽

The Third ◽

Blood Glucose Levels

Penelitian ini bertujuan untuk melihat pengaruh pemberian ekstrak etanol kulit petai (Parkia speciosa Hassk) terhadap penurunan kadar glukosa darah mencit jantan yang diinduksi aloksan. Hewan percobaan dibagi atas 5 kelompok diantaranya kelompok kontrol negatif, kelompok kontrol positif,dosis I (280 mg/kgBB mencit), dosis II (560 mg/kg BB mencit), dosis III (840 mg/kg BB mencit). Penelitian dilakukan selama 21 hari. Persentase penurunan kadar glukosa darah mencit jantan setelah diberikan ekstrak etanol kulit petai pada hari ke-21 adalah dosis I (77,52 %) lebih besar dibandingkan dengan dosis II (69,5 %) dan dosis III (73,37 %). Data yang diperoleh dianalisis dengan uji Two Way Anova dengan program SPSS 17. Hasil penelitian ini menunjukkan bahwa pemberian ekstrak etanol kulit petai untuk tiga variasi dosis menyatakan perbedaan yang bermakna secara statistik terhadap penurunan kadar glukosa darah mencit jantan.Petai (Parkia speciosa Hassk) has a compound β-sitosterol and stigmasterol that have efficacy to decreased blood glucose levels. This study aimed to determine the effect of ethanol extract of petai peel for decrease blood glucose levels of male mice induced by alloxan. Experimental animals were divided into 5 groups including negative control group, positive control group, the first dose (280 mg/kg in mice), the second dose (560 mg/kg in mice), the third dose (840 mg/kg in mice). The study was conducted for 21 days. After 21 days, the result found that the percentage of blood glucose levels after the male mice given the ethanol extract of petai peel was, the first dose (77.52%) biger than the second dose (69.5%) and the third dose (73.37%). The data obtained were analyzed by Two Way ANOVA using SPSS 17. The results showed that have signicantly difference between three dose variation of ethanol extract of petai peel in blood glucose levels.

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Effect of Synchronous Versus Sequential Regimens on the Pharmacokinetics and Biodistribution of Regorafenib with Irradiation

Pharmaceutics ◽

10.3390/pharmaceutics13030386 ◽

2021 ◽

Vol 13 (3) ◽

pp. 386

Author(s):

Tung-Hu Tsai ◽

Yu-Jen Chen ◽

Li-Ying Wang ◽

Chen-Hsi Hsieh

Keyword(s):

Stereotactic Body Radiation Therapy ◽

In Vivo Studies ◽

Control Group ◽

High Dose ◽

Dependent Manner ◽

Hep G2 ◽

Time Curve ◽

Dose Dependent

This study was performed to evaluate the interaction between conventional or high-dose radiotherapy (RT) and the pharmacokinetics (PK) of regorafenib in concurrent or sequential regimens for the treatment of hepatocellular carcinoma. Concurrent and sequential in vitro and in vivo studies of irradiation and regorafenib were designed. The interactions of RT and regorafenib in vitro were examined in the human hepatoma Huh-7, HA22T and Hep G2 cell lines. The RT–PK phenomenon and biodistribution of regorafenib under RT were confirmed in a free-moving rat model. Regorafenib inhibited the viability of Huh-7 cells in a dose-dependent manner. Apoptosis in Huh-7 cells was enhanced by RT followed by regorafenib treatment. In the concurrent regimen, RT decreased the area under the concentration versus time curve (AUC)regorafenib by 74% (p = 0.001) in the RT2 Gy × 3 fraction (f’x) group and by 69% (p = 0.001) in the RT9 Gy × 3 f’x group. The AUCregorafenib was increased by 182.8% (p = 0.011) in the sequential RT2Gy × 1 f’x group and by 213.2% (p = 0.016) in the sequential RT9Gy × 1 f’x group. Both concurrent regimens, RT2Gy × 3 f’x and RT9Gy × 3 f’x, clearly decreased the biodistribution of regorafenib in the heart, liver, lung, spleen and kidneys, compared to the control (regorafenib × 3 d) group. The concurrent regimens, both RT2Gy × 3 f’x and RT9Gy × 3 f’x, significantly decreased the biodistribution of regorafenib, compared with the control group. The PK of regorafenib can be modulated both by off-target irradiation and stereotactic body radiation therapy (SBRT).

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