In this paper, we report the design and moleculardocking study of analogues of antimycin A 3 as inhibitors of anti-apoptotic Bcl-2 of breast cancer. Twenty designed compounds and the original antimycin A 3 were docked based on their interaction with breast tumor receptor binding target Bcl-2. The docking resulted in the five top-ranked compounds, namely, compounds 11, 14, 15, 16, and 20, which have a lower ∆G binding energy, better affinity and stronger hydrogen bonding interactions to the active site of Bcl-2 than antimycin A 3. Among those five top-ranked compounds, analogue compounds 11 and 14, which have an 18-membered tetralactone core and 18-membered tetraol core, respectively, exhibited the strongest hydrogen bond interaction, formed high stability conformation, and demonstrated the greatest inhibitory activity on the catalytic site of Bcl-2.
Colitis Ulcerative is a major public health problem throught the worldwide. Recently many studies have focused to finding antinflammatory based on the natural product. The study was aimed to investigative the inhibitory activity of Phaleria macrocarpa leaves extract on goblet cell in colitis ulcerative. Methods: In this study, Swiss mice were induced by 2% dextran sodium sulfate during a week. Phaleria macrocarpa leaves extract each dose of 100, 200, and 300 mg daily and aspirin 0.2 mg, administered orally. Histopathological examination of the colon tissue (hematoxylin-eosin staining) was done by counting the number of goblet cells a in five randomly selected fields visual. The results: Phaleria macrocarpa leaves extract significantly inhibit the depletion of the count of goblet cells (P 0.000) in colitis. Phaleria macrocarpa leaves extract significantly reduce the amount of focus of inflammation (P 0.000) in colitis. Conclusion: Our results indicated that may have inhibitory activity in colitis through inhibiting reduction in the number of goblet cell.
Background: Hemorrhoids are rectoanal venous plexus swelling that causes inflammation, pain, and bleeding. Plants with phenolic compounds are known to improve venous tone and anti-inflammation. Soursop leaves (Annona muricata L.) known contain phenolic compounds and have been used to cure inflammation. However, studies on anti-inflammatory soursop leaves for hemorrhoids are still limited. Objective: This study aims to analyze the effect of Soursop Leaves Ethanol Extract (SLEE) on the histopathological features and expression of COX-2 and TNFα in rectoanal tissue. Method: Swiss mice 20 weeks induced 3 times with 6% croton oil through the anus. SLEE doses of 100, 200, and 400 mg/Kg and aspirin as a positive control were given orally for 7 days. Histopathological examination of the rectoanal tissue of mice was assessed by counting cell necrosis, inflammation, vasodilation, and edema using hematoxylin-eosin. Positive cells expressing COX-2 and TNFα were counted on inflammatory epithelial cells using immunohistochemistry. Results: Administration of SLEE at all doses showed different levels of inflammation, necrosis, vasodilatation and edema in histopathology of rectoanal tissue P <0.00. All three doses of SLEE show significant anti-inflammatory effects on hemorrhoidal tissue. SLEE doses of 200, 400 mg/Kg significantly decreased COX-2 P <0.05 compared to negative controls, and SLEE doses of 100, 200, and 400 mg/Kg significantly decreased TNFα P <0.05 compared to negative controls. Conclusions: SLEE can reduce inflammation and has the potential to be developed as a natural remedy for hemorrhoids.
Abstract:The purpose of this research was to evaluate the immunomodulator and antiplasmodial activities of Indonesian propolis extracts. This research utilized not only hypersensitivity reaction which measures the humoral immunity by SRBC-immunized mice but also the activity and capacity of peritoneum macrophage phagocytosis in Plasmodium berghei-infected mice. The parasitaemia number was calculated using blood smear method every day for 4 day after the mice had been infected P. berghei to identify the antiplasmodial activity. The research results reveal that propolis hydroalcoholic solution (PHS) has a strong immunomodulatory activity but weak antiplasmodial activity.
: Colon cancer is a major public health problem throughout the worldwide. Recently, many studies have focused on finding chemoprevention based on the natural compound. The present study was aimed to investigate the inhibitory activity of Indonesian soybean in comparison with soybean meal extract in colitis-associated mouse colon carcinogenesis. Methods: In this study, Swiss Webster mice were induced by azoxymethane 10 mg/kg body weight followed by administration of 2% dextran sodium sulfate during a week. Soybean, soybean meal extract at each dose of 75, 150, and 200 mg daily and aspirin 0,39 mg/kg body weight daily (equivalent to 150 mg for a 70 kg human) administered orally. Histopathological examination of the colon tissue (hematoxylin-eosin staining) was done by counting the number of goblet cells and micro vessel density in ten randomly selected fields visual. The results: Soybean and soybean meal significantly reduced the count of goblet cell (P<0,05) in colitis-associated colon carcinogenesis mice. Soybean extract is also significantly reduced the number of micro vessel density (P<0,001) in colitis-associated colon carcinogenesis mice. Otherwise, there were no significant effects of the soybean meal extract on the number of micro vessel density in colitis-associated colon carcinogenesis mice. Conclusion: Our results indicate that Indonesian soybean and soybean meal extract may have inhibitory activity in colitis-associated colon carcinogenesis through inhibiting reduction in the number of goblet cell and micro vessel density. Indonesian soybean may have Inhibitory activity better than soybean meal.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
customersupport@researchsolutions.com
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.