scholarly journals Potential Mechanisms Responsible for the Antinephrolithic Effects of an Aqueous Extract of Fructus Aurantii

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
Xiaoran Li ◽  
Qiang Liang ◽  
Yunji Sun ◽  
Long Diao ◽  
Ze Qin ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Significant Inhibition ◽  
Control Group ◽  
High Dose ◽  
Crystal Formation ◽  
Crystal Dissolution ◽  
Therapeutic Groups ◽  
Immunohistochemical Analyses

The potential effects of Fa extract on the prevention and treatment of CaOx nephrolithiasis were analyzed in an ethylene glycol- (EG-) induced CaOx crystallization model in rats and anin vitroassay. Multiple biochemical variables were measured in the urine and kidney. Kidney sections were subjected to histopathological and immunohistochemical analyses. Urolithiasis-related osteopontin (OPN) was evaluated by Western blotting. Thein vitroassay revealed the significant inhibition of crystal formation (3.50±1.43) and dilution of formed crystals (12.20±3.35) in the group treated with 1 mg/mL Fa extract compared with the control group (52.30±4.71and53.00±4.54, resp.) (p<0.05). Thein vivoexperiments showed that prophylactic treatment with Fa aqueous extract significantly prevented EG-induced renal crystallization and pathological alterations compared with nephrolithic rats (p<0.05). Significantly lower levels of oxidative stress, oxalate, and OPN expression as well as increased citrate and urine output levels were observed in both the low- and high-dose prophylactic groups (p<0.05). However, in the low- and high-dose therapeutic groups, none of these indexes were significantly improved (p>0.05) except for urinary oxalate in the high-dose therapeutic groups (p<0.05). Fa extract prevented CaOx crystallization and promoted crystal dissolutionin vitro. Additionally, it was efficacious in preventing the formation of CaOx nephrolithiasis in rats.

scholarly journals Neferine induces mitochondrial dysfunction to exert anti-proliferative and anti-invasive activities on retinoblastoma

2020 ◽  
Vol 245 (15) ◽  
pp. 1385-1394
Author(s):  
Jing Wang ◽  
Yanmin Dong ◽  
Qiuming Li
Keyword(s):  
Tumor Volume ◽  
Significant Inhibition ◽  
Control Group ◽  
High Dose ◽  
Tumor Weight ◽  
New Treatment ◽  
Xenotransplantation Model

Retinoblastoma is common primary intraocular malignancy of infants and childhood. Neferine is a major bisbenzylisoquinoline alkaloid derived from the lotus plumule in Nelumbo nucifera. This study evaluated the mitigation role of Neferine on retinoblastoma in vitro and in vivo. Xenotransplantation model was established by injecting WERI-Rb-1 cells subcutaneously. Upon induction of retinoblastoma , mice were intraperitoneally injected with Neferine (0, 0.5, 1, 2 mg/kg) or ethanol every 3 days for 30 days. Tumor weight and tumor volume were measured every three days and compared between four groups. Then, mice were sacrificed and immunohistochemical examination was performed to compare Ki67, VEGF content between groups. WERI-Rb-1 cells were used for in vitro experiments and the anti-angiogenic role of Neferine was assessed by analyzing nodes/HPF number. In WERI-Rb-1 xenotransplantation model, compared with control group, 1 mg/kg Neferine treatment significantly inhibited tumor weight (0.39 ± 0.04 g vs. 0.25 ± 0.03 g, P< 0.05) and tumor volume (2163 ± 165 mm3 vs. 1276 ± 108 mm3, P< 0.05) after 30 days. Compared with ethanol-injected mice, 2 μM Neferine treatment significantly enhanced apoptosis rate (2.1 ± 0.6% vs. 14.6 ± 2.6%, P< 0.05), accompany downregulation of Ki67 (0.09 ± 0.02% vs. 0.01 ± 0.004%, P< 0.05) and VEGF (0.28 ± 0.04% vs. 0.05 ± 0.03%, P< 0.05) expression. Additionally, 2 μM Neferine treatment significantly decreased JC-1 red/green percentage. High-dose Neferine could decrease retinoblastoma angiogenesis in association with a significant inhibition on tumor growth and invasion. These findings suggested that Neferine could be a new treatment or adjuvant against retinoblastoma.

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

Pharmaceutics ◽  
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).

scholarly journals The Chemopreventive Effect of Tanacetum Polycephalum Against LA7-Induced Breast Cancer in Rats and the Apoptotic Effect of a Cytotoxic Sesquiterpene Lactone in MCF7 Cells: A Bioassay-Guided Approach

2015 ◽  
Vol 36 (3) ◽  
pp. 988-1003 ◽  
Author(s):  
Hamed Karimian ◽  
Mehran Fadaeinasab ◽  
Soheil Zorofchian Moghadamtousi ◽  
Maryam Hajrezaei ◽  
Maryam Zahedifard ◽  
...  
Keyword(s):  
Sesquiterpene Lactone ◽  
Histopathological Examination ◽  
Cancer Control ◽  
Control Group ◽  
High Dose ◽  
Mcf7 Cells ◽  
Carcinogenic Effect ◽  
Chemopreventive Effect

Background: Tanacetum polycephalum L. Schultz-Bip is a member of the Asteraceae family. This study evaluated the chemopreventive effect of a T. polycephalum hexane extract (TPHE) using in in vivo and in vitro models. Methods and Results: Five groups of rats: normal control, cancer control, TPHE low dose, TPHE high dose and positive control (tamoxifen) were used for the in vivo study. Histopathological examination showed that TPHE significantly suppressed the carcinogenic effect of LA7 tumour cells. The tumour sections from TPHE-treated rats demonstrated significantly reduced expression of Ki67 and PCNA compared to the cancer control group. Using a bioassay-guided approach, the cytotoxic compound of TPHE was identified as a tricyclic sesquiterpene lactone, namely, 8β- hydroxyl- 4β, 15- dihydrozaluzanin C (HDZC). Signs of early and late apoptosis were observed in MCF7 cells treated with HDZC and were attributed to the mitochondrial intrinsic pathway based on the up-regulation of Bax and the down-regulation of Bcl-2. HDZC induced cell cycle arrest in MCF7 cells and increased the expression of p21 and p27 at the mRNA and protein levels. Conclusion: This results of this study substantiate the anticancer effect of TPHE and highlight the involvement of HDZC as one of the contributing compounds that act by initiating mitochondrial-mediated apoptosis.

scholarly journals In Vitro and In Vivo Tumor Growth Inhibition by Glutathione Disulfide Liposomes

2017 ◽  
Vol 10 ◽  
pp. 117906441769607 ◽  
Author(s):  
Satya S Sadhu ◽  
Shenggang Wang ◽  
Rakesh Dachineni ◽  
Ranjith Kumar Averineni ◽  
Yang Yang ◽  
...  
Keyword(s):  
Cancer Metastasis ◽  
Cell Function ◽  
Survival Rates ◽  
Significant Inhibition ◽  
Control Group ◽  
Tumor Growth Inhibition ◽  
Tumor Proliferation ◽  
Glutathione Disulfide

Glutathione disulfide (GSSG) is an endogenous peptide and the oxidized form of glutathione. The impacts of GSSG on cell function/dysfunction remain largely unexplored due to a lack of method to specifically increase intracellular GSSG. We recently developed GSSG liposomes that can specifically increase intracellular GSSG. The increase affected 3 of the 4 essential steps (cell detachment, migration, invasion, and adhesion) of cancer metastasis in vitro and, accordingly, produced a significant inhibition of cancer metastasis in vivo. In this investigation, the effect of GSSG liposomes on cancer growth was investigated with B16-F10 and NCI-H226 cells in vitro and with B16-F10 cells in C57BL/6 mice in vivo. Experiments were conducted to elucidate the effect on cell death through promotion of apoptosis and the effect on the cell cycle. The in vivo results with C57BL/6 mice implanted subcutaneously with B16-F10 cells showed that GSSG liposomes retarded tumor proliferation more effectively than that of dacarbazine, a chemotherapeutic drug for the treatment of melanoma. The GSSG liposomes by intravenous injection (GLS IV) and GSSG liposomes by intratumoral injection (GLS IT) showed a tumor proliferation retardation of 85% ± 5.7% and 90% ± 3.9%, respectively, compared with the phosphate-buffered saline (PBS) control group. The median survival rates for mice treated with PBS, blank liposomes, aqueous GSSG, dacarbazine, GLS IV, and GLS IT were 7, 7, 7.5, 7.75, 11.5, and 16.5 days, respectively. The effective antimetastatic and antigrowth activities warrant further investigation of the GSSG liposomes as a potentially effective therapeutic treatment for cancer.

scholarly journals Doxorubicin-induced myocardial failure in rats with malignant neoplasm: Protective role of fullerenol C60(OH)24

2008 ◽  
Vol 62 (3) ◽  
pp. 197-204 ◽  
Author(s):  
Rade Injac ◽  
Aleksandar Djordjevic ◽  
Borut Strukelj
Keyword(s):  
Untreated Control ◽  
Malignant Neoplasm ◽  
In Vivo Studies ◽  
Control Group ◽  
High Dose ◽  
Sprague Dawley ◽  
Untreated Control Group ◽  
Cardiac Damage

The therapeutic utility of the anthracycline antibiotic doxorubicin is limited due to its cardiotoxicity. Our aim was to investigate the efficacy of fullerenol C60(OH)24 in preventing single, high-dose doxorubicin-induced cardiotoxicity in rats with malignant neoplasm. In vitro and in vivo studies have shown that fullerenol C60(OH)24, has strong antioxidative potential. Experiment was performed on adult female Sprague Dawley rats with chemically induced mammary carcinomas. All 32 rats (2-5 groups) received i.p. applications of 1-methyl-l-nitrosourea (MNU; 50 mg/kg body weight) on the 50th and 113th day of age. Animals were randomly divided into five groups as follows: (1) Untreated control group - rats received saline only; (2) Cancer control group - rats received MNU and saline; (3) Dox group - rats received MNU and Dox 8 mg/kg; (4) Full/Dox group -rats received MNU and Full 100 mg/kg 30 min before Dox 8 mg/kg; (5) Full group - rats received MNU and Full 100 mg/kg. Tumor incidence was 4.94 +- 0.576 per rat. The animals were sacrificed 2 days after the application of doxorubicin and/or fullerenol, and the serum activities of CK, LDH and ?-HBDH, as well as the levels of MDA, GSH, GSSG, GSH-Px, SOD, CAT, GR and TAS in the heart, were determined. The results obtained from the enzymatic activity in the serum show that the administration of a single dose of 8 mg/kg in all treated groups induces statistically significant damage. There are significant changes in the enzymes of LDH and CK (p < 0.05), after an i.p. administration of doxorubicin/fullerenol and fullerenol. Comparing all groups with untreated control group, point to the conclusion that in the case of a lower oc-HBDH/LDH ratio, results in more serious the liver parenchymal damage. The results revealed that doxorubicin induced oxidative damage and that the fullerenol antioxidative influence caused significant changes in MDA, GSH, GSSG, GSH-Px, SOD, CAT, GR and TAS level in the heart (p < 0.05). Ultra structural analysis of heart tissues from rats treated with doxorubicin and indicated that the hearts of the rats were protected from doxorubicin-induced subcellular damage. Doxorubicin/fullerenol rats did not appear to show significant cardiac damage although occasional focal loss of cristae in the mitochondria was observed. Therefore, it is suggested that fullerenol might be a potential cardioprotector in doxorubicin-treated individuals.

scholarly journals Aqueous Extract of Perilla frutescens var. acuta Relaxes the Ciliary Smooth Muscle by Increasing NO/cGMP Content In Vitro and In Vivo

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1777 ◽  
Author(s):  
Jaeyong Kim ◽  
Huwon Kang ◽  
Hakjoon Choi ◽  
Ara Jo ◽  
Dooi-Ri Oh ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Perilla Frutescens ◽  
Ciliary Muscle ◽  
Control Group ◽  
Dependent Manner ◽  
Sprague Dawley ◽  
Eye Fatigue ◽  
Freeze Dried

The leaves of Perilla frutescens var. acuta (PFA) are commonly used as a traditional medicine in Korea, Japan, and China. We previously showed that PFA attenuates eye fatigue by improving visual accommodation through a clinical study. However, detailed mechanisms and chemical compounds have not been studied. In this study, we analyzed the active compounds in an aqueous extract of PFA involved in ciliary muscle relaxation in vitro and in vivo. NMR and MS analyses showed that the PFA extract contained mainly luteolin-7-O-diglucuronide and apigenin-7-O-diglucuronide. The composition after freeze-drying and spray-drying was similar. Freeze-dried PFA (50 µg/mL, 100 µg/mL, and 200 µg/mL) increased nitric oxide and cGMP levels in ciliary muscle cells isolated from the eyes of rats. [Ca2+]i decreased in a dose-dependent manner. Furthermore, Sprague-Dawley rats treated with freeze-dried PFA (200 mg/kg, orally) showed significantly increased cGMP levels compared with the control group and irradiated with white light. Our results suggest that PFA extract has the potential to reduce eye fatigue by relaxing ciliary muscles.

scholarly journals Inhibitory effect of naphthoquine phosphate against Babesia gibsoni in vitro and Babesia rodhaini in vivo

2021 ◽  
Author(s):  
Shengwei Ji ◽  
Mingming Liu ◽  
Eloiza May Galon ◽  
Mohamed Abdo Rizk ◽  
Bumduuren Tuvshintulga ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Treatment Strategies ◽  
Drug Repurposing ◽  
Significant Inhibition ◽  
Parasite Growth ◽  
New Drugs ◽  
Control Group ◽  
Babesia Gibsoni

Abstract Background: Drug resistance and severe side effects are major challenges in the treatment of babesiosis as they lead to less choices for treatment. Development of new drugs to enrich the treatment strategies and delay the emergence of drug resistance in parasites is still needed. Naphthoquine (NQ) combined with artemisinin treats Plasmodium infection by rapid parasite clearance. The current study repurposed NQ as a babesiosis drug treatment by evaluating the effects of naphthoquine phosphate (NQP) as a single dose treatment for babesiosis. Methods: In vitro anti-Babesia activity of NQP was tested on Babesia gibsoni cultures. The inhibition of parasite growth was verified using a SYBR green I-based fluorescence assay. In vivo efficacy of NQP was evaluated using BALB/c mice infected with Babesia rodhaini. The parasitemia level and hematocrit values were monitored. Results: The half maximal inhibitory concentration of NQP against B. gibsoni in vitro was 3.3 ± 0.5 μM. Oral administration of NQP for 5 successive days at a dose of 40 mg/kg of body weight resulted in significant inhibition on parasite growth compared with the control group. All mice in NQP-treated group survived, whereas the mice in control group died between days 6 and 9 post infection. Conclusion: This is the first study to evaluate the anti-Babesia activity of NQP in vitro and in vivo. The results showed that NQP is a promising drug for babesiosis treatment and drug repurposing may provide new treatment strategies for babesiosis.

scholarly journals Gastroprotective Effects of Lion’s Mane MushroomHericium erinaceus(Bull.:Fr.) Pers. (Aphyllophoromycetideae) Extract against Ethanol-Induced Ulcer in Rats

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Jing-Yang Wong ◽  
Mahmood Ameen Abdulla ◽  
Jegadeesh Raman ◽  
Chia-Wei Phan ◽  
Umah Rani Kuppusamy ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Aqueous Extract ◽  
Gastric Wall ◽  
Toxicity Study ◽  
Control Group ◽  
High Dose ◽  
Sprague Dawley ◽  
Bax Protein ◽  
Acute Toxicity Study

Hericium erinaceusis a famous tonic in oriental medicine. The gastroprotective effects of aqueous extract ofH. erinaceusagainst ethanol-induced ulcers inSprague Dawleyrats were investigated. The possible involvements of lipid peroxidation, superoxide dismutase, and catalase were also investigated. Acute toxicity study was performed. The effects of aqueous extract ofH. erinaceuson the ulcer areas, ulcer inhibition, gastric wall mucus, gross and histological gastric lesions, antioxidant levels, and malondialdehyde (MDA) contents were evaluated in ethanol-induced ulcerin vivo. In acute toxicity study, a high dose of 5 g/kg did not manifest any toxicological signs in rats. The extract promoted ulcer protection as ascertained by a significant reduction of the ulcer area. Furthermore, it exhibited a significant protection activity against gastric mucosal injury by preventing the depletion of antioxidant enzymes. The level of MDA was also limited in rat stomach tissues when compared with the ulcer control group. Immunohistochemistry showed upregulation of HSP70 protein and downregulation of BAX protein in rats pretreated with the extract. The aqueous extract ofH. erinaceusprotected gastric mucosa in ourin vivomodel. It is speculated that the bioactive compounds present in the extract may play a major role in gastroprotective activity.

scholarly journals Evaluation of anti-obesity potential of aqueous extract of Achyranthes aspera Linn. in high fat diet induced obese rats

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Kumaraswamy Athesh ◽  
Rangaraju Sivasubramanian ◽  
Gnanasekaran Jothi ◽  
Pemiah Brindha
Keyword(s):  
Aqueous Extract ◽  
Pancreatic Lipase ◽  
High Fat Diet ◽  
In Vivo Studies ◽  
Control Group ◽  
High Fat ◽  
Achyranthes Aspera ◽  
Obese Rats

Abstract Background Obesity, reached epidemic proportions globally is often associated with life threatening comorbidities. The unavailability of safe and effective long term medications for obesity in modern pharmacotherapy forces the scientific community to explore the potential of Ayurvedic traditional healers as they are considered safe and effective. Objective To explore the anti-obesity potential of aqueous extract of aerial parts of Achyranthes aspera L. (AEAA), a traditional healer in high fat diet (HFD) induced obese rats. Methods AEAA was prepared and subjected to in-vitro pancreatic lipase inhibition assay and in-vivo anti-obesity studies. For in-vivo studies, HFD fed obese prone Wistar albino rats were divided into five experimental groups (Group II to VI): animals fed with standard pellet chow served as normal control (Group I) while, animals continued with HFD alone served as obese control (Group II); Group III, IV and V were administered AEAA at a dose of 100, 200 and 300 mg/kg b.w. respectively along with HFD; and animals administered orlistat (30 mg/kg bw) along with HFD served as standard control (Group VI). All the drugs were administered orally once a day for a period of 60 days. At the end of the experimental period various physical, biochemical and histopathological observations were made. Results In-vitro studies showed AEAA partially but not significantly inhibited the activity of pancreatic lipase. Data of in-vivo studies revealed, significant reduction in body weights, fat pad weights and organ weights upon AEAA treatment. Elevated levels of glucose, insulin, leptin, lipid profiles and antioxidant status were also brought back to normal. Conclusion The obtained results clearly suggested that AEAA possess pronounced anti-obesity potential.

scholarly journals Lacaune ewes with subclinical mastitis: effects of intramammary application of própolis

2021 ◽  
Vol 10 (2) ◽  
pp. e18210211709
Author(s):  
Guilherme Luiz Deolindo ◽  
Vitor Luiz Molosse ◽  
Amanda Dilda ◽  
Lilian Kolling Girardini ◽  
Marcelo Vedovatto ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Staphylococcus Epidermidis ◽  
Subclinical Mastitis ◽  
Treated Group ◽  
Control Group ◽  
In Vitro Test ◽  
In Vivo Test ◽  
Propolis Extract

The aim of this study was to evaluate the antimicrobial potential of the aqueous extract of green propolis in vitro against mastitis-causing and in vivo bacteria, evaluating the efficacy of treatment in Lacaune sheep. In the in vitro test, the minimum inhibitory concentration (MIC) was used; first, the MIC was obtained from the aqueous extract of green propolis for the strain of Staphylococcus. aureus ATCC 25523, defined as 1 mg/ml. For bacterial agents isolated from sheep with mastitis (Staphylococcus epidermidis, Staphylococcus intermedius, Staphylococcus hyicus, Corynebacterium spp. and Acinetobacter spp.), The concentration of 10 mg/ml was determined, while for Streptococcus equinus, Escherichia coli, and hemolytic E. coli, also isolated from sheep with mastitis, the concentration capable of reducing bacterial growth was 100 mg/ml. In the in vivo test, ten sheep were used, distributed in two treatments, five in the control group (CG) that received 2.5 ml of saline (vehicle), and five in the treated group (GT) that received 2.5 ml of aqueous (saline) propolis extract by the mammary route. The propolis dose tested (0.1 g/ml) was not effective for the treatment of mastitis, because the sheep remained positive in the racket test (CMT). The main microorganism isolated in the cases of mastitis in this study was Staphylococcus epidermidis. These results are preliminary; however, at the tested dose, the aqueous extract of green propolis delivered by the mammary route had no curative effect of mastitis.

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