scholarly journals Ethanolic Extract of Papaya (Carica papaya) Leaf Exhibits Estrogenic Effects In Vivo and In Silico

2012 ◽  
Vol 3 (2) ◽  
pp. 384
Author(s):  
Raisatun Nisa Sugiyanto ◽  
Rahmi Khamsita ◽  
Marvin Lambertus ◽  
Rohmad Yudi Utomo ◽  
Ratna Asmah Susidarti
Keyword(s):  
Estrogen Receptor ◽  
In Silico ◽  
Carica Papaya ◽  
Ethanolic Extract ◽  
The Body ◽  
Female Rats ◽  
Sprague Dawley ◽  
Docking Score ◽  
Estrogenic Effect

The menopause women have the low level of estrogen in the body. The lack of estrogen changes physiological function in women’s body that affects in health condition. Carica papaya L. leaf contains flavonoid quercetin which exhibits estrogenic effect. The aim of this study is to determine the estrogenic effect of papaya leaves extract (PLE) in vivo, and in silico. Papaya leaves were extracted by ethanol 70% maceration. The in silico study were done by molecular docking between quersetin and Estrogen Receptor (ERα and ERβ) to obtain the docking score. Based on this study, docking score of quercetin was almost similar to the native ligand of ER. The in vivo study was done as follow: 36 female rats Sprague Dawley divided into six groups.  The groups are shame-ovariectomized (S-OVX), control ovariectomized (OVX), CMC-Na control (OVX+CMC-Na), positive control (OVX+Estradiol), and the PLE treatment groups dose 750 mg/kgBW (OVX+750mg/kgBW) and dose 1000 mg/kgBW (OVX+1000 mg/kgBW). Administrations of PLE were done in three weeks orally, while estradiol was administrated intraperitonially. The mammae and uterine were sliced for analysis. Based on the study, the treatment of PLE increased the number of mammae lobules and uterine weight as well as estrogen does.  In summary, PLE can be developed as a source of phytoestrogens.Keywords: Carica papaya L., phytoestrogen, estrogen receptor, mammae lobule, uterine

scholarly journals Estrogenic Activity of Ethanolic Extract of Papaya Peels (Carica Papaya L.) on Uterine Weight and Mammae Gland Proliferation on Ovariectomy Rats

2018 ◽  
Vol 9 (2) ◽  
pp. 86 ◽  
Author(s):  
Dhania Novitasari ◽  
Devyanto Hadi Triutomo ◽  
Fitriana Hayyu Arifah ◽  
Anselma Ivanawati ◽  
Zahrotul Ulum ◽  
...  
Keyword(s):  
Estrogenic Activity ◽  
Ethanolic Extract ◽  
Female Rats ◽  
Ovariectomized Rats ◽  
Uterine Weight ◽  
Sprague Dawley ◽  
In Vivo Test ◽  
Female Reproductive Health ◽  
Agnor Staining

Papaya bark is one of Indonesia's natural wealth that contains flavonoid compounds such as myricetin and kaempferol that included in the phytoestrogen compounds. The aim of this study is to examine the estrogenic effects of ethanolic extract of papaya peels (EEPP), on the development of mammae gland and the increasing of uterine weight. The in vivo test was performed with ovariectomy in Sprague Dawley female rats that caused the rats to be in an estrogen deficiency state. After 30 days of treatment, animals are sacrificed to take the uterus and mammae glands. Measurement of uterine weight and mammae gland are observed by hematoxylin-eosin staining method to know the lobulus development and AgNOR staining to determine the proliferation level of mammae gland epithelial cells. The test results showed that EEPP concentration of 500 and 1000 mg/kgBW were able to increase uterine weight and proliferation of mammae gland. From the results of this study, papaya bark has the potential to be one of the phytoestrogens compound to maintain female reproductive health and woman beauty.Keyword: ethanolic extract of papaya peels (EEPP), phytoestrogen, ovariectomized rats, uterine weight, mammae proliferation

scholarly journals The Combination of High Calcium Milk with Citrus maxima Peels Ethanolic Extract Increased Bone Density of Ovariectomized Rats

2017 ◽  
Vol 6 (2) ◽  
pp. 42
Author(s):  
Ragil S. Dianingati ◽  
Annisa Novarina ◽  
Amanita K. Hana ◽  
Laeli Muntafi'ah ◽  
Endang Lukitaningsih
Keyword(s):  
Estrogen Receptor ◽  
Bone Density ◽  
Female Rats ◽  
Ovariectomized Rats ◽  
Menopausal Woman ◽  
Good Prospect ◽  
Sprague Dawley ◽  
Docking Score ◽  
High Calcium ◽  
Citrus Maxima

Osteoporosis is a common problem in menopause woman. The main cause is lack of estrogen hormone. Commonly, prevention therapy is by consuming high calcium milk, but it is not effective. Bali orange’s peel (Citrus maxima Merr.) is a waste material but known contains phytoestrogen according to previous study. Considering of this result, fortification of high calcium milk and Bali orange’s peel is expected to be an effective solution for osteoporosis in menopause woman. This research began with extraction of Bali orange’s peel (BPE) using ethanol 70% by maceration method. Ovariectomized Sprague Dawley female rats as the model of post menopausal woman were treated by BPE for 28 days. The doses of BPE was given to rats is 500 and 1000 mg/KgBW combined with high calcium milk. Bone density was determined using digital microradiography, the profile showed the increase of bone density in group that treated with combination of BPE 1000 mg/Kg BW and high calcium milk compare to control and given only milk groups. Docking molecular showed that BPE’s active compound which are hesperidin and naringin have interaction with estrogen receptor α and β. Docking score of naringin with ER α and β are -19,97; -18,99 respectively. Meanwhile the docking score of hesperidin with ER α and β are -19,98; +49,92 respectively. Overall, the result of this research showed that fortification of BPE with high calcium milk has good prospect to develop as effective therapy of osteoporosis.Keywords : Citrus maxima Merr., phytoestrogen, osteoporosis, high calcium milk, estrogen receptor 

scholarly journals Ethanolic Extract of Papaya (Carica papaya) Leaves Improves Blood Cholesterol Profiles and Bone Density in Ovariectomized Rats

2012 ◽  
Vol 3 (3) ◽  
pp. 426
Author(s):  
Raisatun Nisa Sugiyanto ◽  
Rahmi Khamsita ◽  
Ratna Asmah Susidarti
Keyword(s):  
Bone Density ◽  
Total Cholesterol ◽  
Carica Papaya ◽  
Good Condition ◽  
Ethanolic Extract ◽  
Positive Control ◽  
The Body ◽  
Blood Cholesterol ◽  
Ovariectomized Rats ◽  
Sprague Dawley

Bone loss and disturbance in the blood cholesterol profiles modulation are two effects caused by menopauses syndromes. As the estrogen concentration in the body decreased drastically, menopause women need the replacement of estrogen to keep the regulation of several physiological functions in the body, such as bone generation and cholesterol regulation in a good condition. Phytoestrogen in Carica papaya leaves, such as quercetin, could be one of the potential agents for the estrogenic effect. The aim of this study is to know the effects of papaya leaf extract (PLE) on the blood cholesterol profiles and bone density in ovariectomized rats. Thirty six female Sprague Dawley rats divided into six groups.  The groups were sham-treated ovx (S-OVX), ovariectomized rats (OVX), CMC-Na control (OVX+CMC-Na), positive control (OVX+Estradiol), and the PLE treatment groups dose 750 mg/kgBW (OVX+750mg/kgBW) and dose 1000 mg/kgBW (OVX+1000 mg/kgBW). Administrations of PLE were done in three weeks orally and estradiol administrated intraperitonially. In the end of the treatment, the blood sample of tested animals was collected for the blood cholesterol determination (LDL, HDL, triglyceride, and total cholesterol) and the femur bones were examined for the bone density. Based on the results, PLE dose of 750 mg/kgBW a day in ovariectomized rats showed estrogenic effects in modulating blood cholesterol profile by lowering total cholesterol levels. Meanwhile, PLE dose of 1000 mg/kgBW significantly increased the bone density (p<0.05). Thus, PLE is potential to overcome the negative effects of post-menstrual women especially in the cholesterol blood profiles and bone density.Keywords : Carica papaya, phytoestrogen, bone density, blood cholesterol, ovariectomized rats

Ruthenium Complexes for 1- and 2-Photon Photodynamic Therapy: From In Silico Prediction to In Vivo Applications

2020 ◽  
Author(s):  
Johannes Karges ◽  
Shi Kuang ◽  
Federica Maschietto ◽  
Olivier Blacque ◽  
Ilaria Ciofini ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
In Silico ◽  
Aqueous Solubility ◽  
The Body ◽  
Photon Absorption ◽  
Multicellular Tumor Spheroids ◽  
Spectral Window ◽  
Photon Excitation ◽  
Polypyridine Complexes

<div>The use of photodynamic therapy (PDT) against cancer has received increasing attention overthe recent years. However, the application of the currently approved photosensitizers (PSs) is somehow limited by their poor aqueous solubility, aggregation, photobleaching and slow clearance from the body. To overcome these limitations, there is a need for the development of new classes of PSs with ruthenium(II) polypyridine complexes currently gaining momentum. However, these compounds generally lack significant absorption in the biological spectral window, limiting their application to treat deep-seated or large tumors. To overcome this drawback, ruthenium(II) polypyridine complexes designed in silico with (E,E’)-4,4´-bisstyryl 2,2´-bipyridine ligands showed impressive 1- and 2-Photon absorption up to a magnitude higher than the ones published so far. While non-toxic in the dark, these compounds were found phototoxic in various 2D monolayer cells, 3D multicellular tumor spheroids and be able to eradicate a multiresistant tumor inside a mouse model upon clinically relevant 1-Photon and 2 Photon excitation.</div>

scholarly journals A New Symmetrical Thiazolidinedione Derivative: In Silico Design, Synthesis, and In Vivo Evaluation on a Streptozotocin- Induced Rat Model of Diabetes

Processes ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 1294
Author(s):  
Samuel Álvarez-Almazán ◽  
Gabriel Navarrete-Vázquez ◽  
Itzia Irene Padilla-Martínez ◽  
José Correa-Basurto ◽  
Diana Alemán-González-Duhart ◽  
...  
Keyword(s):  
Rat Model ◽  
In Silico ◽  
Female Rats ◽  
Therapeutic Effects ◽  
Acute Oral Toxicity ◽  
Oral Toxicity ◽  
In Vivo Evaluation ◽  
Docking Simulations ◽  
Ppar Γ

By activating PPAR-γ, thiazolidinediones normalize glucose levels in animal models of type 2 diabetes and in patients with this pathology. The aim of the present study was to analyze 219 new derivatives in silico and select the best for synthesis, to be evaluated for acute oral toxicity in female rats and for control of diabetes-related parameters in a rat model of streptozotocin-induced diabetes. The best compound was chosen based on pharmacokinetic, pharmacodynamic, and toxicological parameters obtained in silico and binding orientation observed by docking simulations on PPAR-γ. Compound 1G was synthesized by a quick and easy Knoevenagel condensation. Acute oral toxicity was found at a dose greater than 2000 mg/Kg. Compound 1G apparently produces therapeutic effects similar to those of pioglitazone, decreasing glycaemia and triglyceride levels in diabetic animals, without liver damage. Moreover, it did not cause a significant weight gain and tended to reduce polydipsia and polyphagia, while diminishing systemic inflammation related to TNF-α and IL-6. It lowered the level of endogenous antioxidant molecules such as reduced glutathione and glutathione reductase. In conclusion, 1G may be a candidate for further testing as an euglycemic agent capable of preventing the complications of diabetes.

scholarly journals Activation of Penile Proadipogenic Peroxisome Proliferator-Activated Receptor with an Estrogen: Interaction with Estrogen Receptor Alpha during Postnatal Development

PPAR Research ◽  
2008 ◽  
Vol 2008 ◽  
pp. 1-10 ◽  
Author(s):  
Mahmoud M. Mansour ◽  
Hari O. Goyal ◽  
Tim D. Braden ◽  
John C. Dennis ◽  
Dean D. Schwartz ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Alpha ◽  
Corpus Cavernosum ◽  
Cellular Level ◽  
Transitional Epithelium ◽  
Peroxisome Proliferator ◽  
Sprague Dawley ◽  
Peroxisome Proliferator Activated Receptor ◽  
Receptor Alpha

Exposure to the estrogen receptor alpha (ER) ligand diethylstilbesterol (DES) between neonatal days 2 to 12 induces penile adipogenesis and adult infertility in rats. The objective of this study was to investigate the in vivo interaction between DES-activated ER and the proadipogenic transcription factor peroxisome proliferator-activated receptor gamma (PPAR). Transcripts for PPARs , , and and 1a splice variant were detected in Sprague-Dawley normal rat penis with PPAR predominating. In addition, PPAR1b and PPAR2 were newly induced by DES. The PPAR transcripts were significantly upregulated with DES and reduced by antiestrogen ICI 182, 780. At the cellular level, PPAR protein was detected in urethral transitional epithelium and stromal, endothelial, neuronal, and smooth muscular cells. Treatment with DES activated ER and induced adipocyte differentiation in corpus cavernosum penis. Those adipocytes exhibited strong nuclear PPAR expression. These results suggest a biological overlap between PPAR and ER and highlight a mechanism for endocrine disruption.

scholarly journals Greater natriuretic response to ENaC inhibition in male versus female Sprague-Dawley rats

2020 ◽  
Vol 318 (2) ◽  
pp. R418-R427 ◽  
Author(s):  
Reham H. Soliman ◽  
Jermaine G. Johnston ◽  
Eman Y. Gohar ◽  
Crystal M. Taylor ◽  
David M. Pollock
Keyword(s):  
Protein Expression ◽  
Time Of Day ◽  
Female Rats ◽  
Female Rat ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Endothelin System ◽  
Males And Females ◽  
Epithelial Sodium Channel Enac

Genes for the epithelial sodium channel (ENaC) subunits are expressed in a circadian manner, but whether this results in time-of-day differences in activity is not known. Recent data show that protein expression of ENaC subunits is higher in kidneys from female rats, yet females are more efficient in excreting an acute salt load. Thus, our in vivo study determined whether there is a time-of-day difference as well as a sex difference in the response to ENaC inhibition by benzamil. Our results showed that the natriuretic and diuretic responses to a single dose of benzamil were significantly greater in male compared with female rats whether given at the beginning of the inactive period [Zeitgeber time 0 (ZT0), 7 AM] or active period (ZT12, 7 PM). However, the response to benzamil was not significantly different between ZT0 and ZT12 dosing in either male or female rats. There was no difference in renal cortical α-ENaC protein abundance between ZT0 and ZT12 or males and females. Given previous reports of flow-induced stimulation of endothelin-1 (ET-1) production and sex differences in the renal endothelin system, we measured urinary ET-1 excretion to assess the effects of increased urine flow on intrarenal ET-1. ET-1 excretion was significantly increased following benzamil administration in both sexes, but this increase was significantly greater in females. These results support the hypothesis that ENaC activity is less prominent in maintaining Na+ balance in females independent of renal ET-1. Because ENaC subunit genes and protein expression vary by time of day and are greater in female rat kidneys, this suggests a clear disconnect between ENaC expression and channel activity.

Effects of lead and/or cadmium on the distribution patterns of some essential trace elements in immature female rats

2011 ◽  
Vol 30 (12) ◽  
pp. 1914-1923 ◽  
Author(s):  
Lin Wang ◽  
Xuelei Zhou ◽  
Dubao Yang ◽  
Zhenyong Wang
Keyword(s):  
Trace Elements ◽  
Inductively Coupled Plasma ◽  
Distribution Patterns ◽  
The Body ◽  
Female Rats ◽  
Control Group ◽  
Sprague Dawley ◽  
Inductively Coupled ◽  
Lead And Cadmium ◽  
Essential Trace Elements

Lead acetate (300 mg/L) and/or cadmium chloride (50 mg/L) were administered as drinking water to Sprague-Dawley rats for 9 weeks to investigate the effects of concurrent exposure to lead and cadmium on the distribution patterns of five essential trace elements. Inductively coupled plasma mass spectrometry was used to determine the concentrations of zinc, copper, manganese, selenium and iron in the urine at different exposure times, as well as their levels in the renal cortex and serum at the end of treatment. Compared with the control group, exposure to lead and/or cadmium resulted in a significant increase in the urinary excretion of these five elements during the experiment, whereas significant decreased levels of these elements were found in kidney and serum. In conclusion, increased urinary loss of antioxidant trace elements due to lead and/or cadmium exposure induced the deficiency of antioxidants in the body, which could result in further oxidative damage. Moreover, there was an obvious synergistic effect of lead combined with cadmium on the distribution patterns of these essential trace elements, which may be related to the severity of co-exposure to these two metals.

scholarly journals Investigation of biological activities of Colocasia gigantea Hook.f. leaves and PASS prediction, in silico molecular docking with ADME/T analysis of its isolated bioactive compounds

2020 ◽  
Author(s):  
Safaet Alam ◽  
Nazim Uddin Emon ◽  
Mohammad A. Rashid ◽  
Mohammad Arman ◽  
Mohammad Rashedul Haque
Keyword(s):  
Molecular Docking ◽  
Binding Affinity ◽  
In Silico ◽  
Castor Oil ◽  
Biological Activities ◽  
Kappa Opioid Receptor ◽  
Soluble Extract ◽  
Docking Score

AbstractBackgroundColocasia gigantea is locally named as kochu and also better known due to its various healing power. This research is to investigate the antidiarrheal, antimicrobial, and antioxidant possibilities of the methanol soluble extract of Colocasia gigantea.MethodsAntidiarrheal investigation was performed by using in vivo castor oil induced diarrheal method where as in vitro antimicrobial and antioxidant investigation have been implemented by disc diffusion and DPPH scavenging method respectively. Moreover, in silico studies were followed by molecular docking analysis of several secondary metabolites were appraised with Schrödinger-Maestro v 11.1.ResultsThe induction of plant extract (200 and 400 mg/kg, b.w, p.o), the castor oil mediated diarrhea has been minimized 19.05 % (p < 0.05) and 42.86 % (p < 0.001) respectively. The methanolic extract of C. gigantea showed mild sensitivity against almost all the tested strains but it shows high consistency of phenolic content and furthermore yielded 67.68 μg/mL of IC50 value in the DPPH test. The higher and lower binding affinity was shown in beta-amyrin and monoglyceryl stearic acid against the kappa-opioid receptor (PDB ID: 4DJH) with a docking score of -3.28 kcal/mol and -6.64 kcal/mol respectively. In the antimicrobial investigation, Penduletin and Beta-Amyrin showed the highest and lowest binding affinity against the selected receptors with the docking score of -8.27 kcal/mol and -1.66 kcal/mol respectively.ConclusionThe results of our scientific research reflect that the methanol soluble extract of C. gigantea is safe which may provide possibilities of alleviation of diarrhea and as a potential wellspring of antioxidants which can be considered as an alternate source for exploration of new medicinal products.

scholarly journals Estrogenic Effect of Bambusa arundinacea, Trichosanthes dioica and Punica granatum on Rats

2022 ◽  
Author(s):  
Akanksha Awasthi ◽  
Mamta F. Singh ◽  
Saurabh Sharma
Keyword(s):  
Wistar Rats ◽  
Estrogenic Activity ◽  
Ethanolic Extract ◽  
Punica Granatum ◽  
Mature Female ◽  
Female Rats ◽  
Vaginal Opening ◽  
Estrogenic Effect ◽  
Female Wistar Rats ◽  
Trichosanthes Dioica

Background: Phytoestrogens have recently become a hot topic among scientists. Phytoestrogens’ estrogen-like properties have led to their widespread use in the reproductive system. The aim of this research was to see whether the ethanolic extract of Bambusa arundinaceae, Trichosanthes dioica and Punica granatum had any estrogenic activity in female wistar rats. Methods: In female wistar rats, the estrogenic effect was studied using a uterotropic assay, vaginal cytology and vaginal opening. In ovariectomized immature and mature female wistar rats, a 400 mg/kg body weight (b.w.) dose of ethanolic extract of Bambusa arundinaceae, Trichosanthes dioica and Punica granatum was given. Result: When compared to ovariectomized control rats, the uterine wet weight increased significantly. The estrogen-treated rats had only cornified epithelial cells, indicating the existence of oestrogen, as well as 100% vaginal opening. At 400 mg/kg b.w., the ethanolic extract of Bambusa arundinaceae, Trichosanthes dioica and Punica granatum demonstrated promising estrogenic activity, as evidenced by uterotropic assays, vaginal opening measurements and histopathological changes. As a result of this research, it’s possible to infer that the ethanolic extract of Bambusa arundinaceae, Trichosanthes dioica and Punica granatum play an important role in estrogenic activity in female rats.

Sign in / Sign up

Export Citation Format

Share Document