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The relaxant effect of methanolic extract of yohimbe bark (Pausinystalia yohimbe) on rabbit corpus cavernosum smooth muscles

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Health 2012年第9期4卷 656-659页

作者： Mohamed Hassan Hozeifa Imad Eldin Mohamed Taj Eldin Mohamed Mohamed Ahmed Elhadi Hassan Mohamed Abd Elwahab Sirag Elteyb Nizar Department of Pharmacognosy Faculty of Pharmacy University of Gezira Wad Madani Sudan Department of Pharmacology and Toxicology Medicinal and Aromatic Plant Research Institute National Center for Research Khartoum Sudan Department of Pharmacology Faculty of Pharmacy University of Gezira Wad Madani Sudan

Background: Development and maintenance of penile erection requires the relaxation of corpus cavernosum smooth muscle (CCSM) cells and it is essentially mediated by nitric oxide (NO). Pausinystalia yohimbe bark is traditionally used for the treatment of erectile dysfunction (ED). Objectives and Methods: This study aimed to evaluate the effects of the methanolic extract of P. yohimbe bark (10 mg/ml) on isolated rabbit corpus cavernosum smooth muscle (CCSM). Results: Methanolic extract of P. yohimbe bark blocked contractions in CCSM induced by adrenergic agonists, through facilitating NO release from the endothelial cells. Conclusion: The obtained results revealed that, methanolic extract of P. yohimbe bark caused relaxation of CCSM that validates its traditional aphrodisiac property, thus it could be used to initiate and maintain erection in cases of erectile dysfunction.

关键词： P. yohimbe Bark Corpus Cavernosum Relaxation Nitric Oxide Aphrodisiac Erectile Dysfunction

One-pot Synthesis of lO-Methyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-l,8-dione Derivatives under Microwave Heating without Catalyst

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Chinese Journal of Chemistry 2005年第12期23卷 1646-1650页

作者：华国平章晓镜石枫屠树江徐佳宁王倩朱晓彤张金鹏纪顺俊 Xuzhou Institute of Architectural Technology Xuzhou Jiangsu 221008 China Key Laboratory of Biotechnology for medicinal plants Department of Chemistry Xuzhou Normal University Xuzhou Jiangsu 221116 China Key Laboratory of Organic Synthesis of Jiangsu Province College of Chemistry and Chemical Engineering Suzhou University Suzhou Jiangsu 215006 China

A series of 10-methyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-1,8-dione derivatives were synthesized by one-pot reaction of aldehyde, dimedone or 1,3-cyclohexanedione and methylamine in glycol or water under microwave heating without catalyst. The method has the advantage of short routine and reaction time, high yields as well as friendly environment. And the reaction was not only suitable for aliphatic and aromatic monoaldehyde, but also for aromatic dialdehyde.

关键词： aldehyde dimedone 1,3-cyclohexanedione methylamine 10-methyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-1,8-dione microwave heating

Effects of methanolic extract of Pausinystalia yohimbebark on blood glucose level in normal fasting rats

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Health 2012年第12期4卷 1225-1228页

作者： Hozeifa Mohamed Hassan Taj Eldin Imad Mohamed Elhadi Mohamed Mohamed Ahmed Abd Elwahab Hassan Mohamed Nizar Sirag Department of Pharmacognosy Faculty of Pharmacy University of Gezira Wad Medani Sudan Department of Pharmacology and Toxicology Medicinal and Aromatic Plant Research Institute National Centre of Research Khartoum Sudan Department of Pharmacology Faculty of Pharmacy University of Gezira Wad Medani Sudan

Background: Pausinystalia yohimbe (L.) is a member of the family Rubiaceae. It is a valuable medicinal tree, distributed in evergreen closed-canopy forests in West Africa. It is traditionally used for treatment of erectile dysfunction and diabetes. Objective: This was an attempt to evaluate the effects of methanolic extract of P. yohimbe bark on blood glucose level in normal fasting rats. Methods: Different doses of methanolic extract of P. yohimbe bark (5, 10, 20, 40 and 80 mg/kg/mL) were orally administered to normal fasting rats to assess their effects on blood glucose levels. Results: The methanolic extract of P. yohimbe bark in different concentrations (5, 10, 20, 40 and 80 mg/kg/mL) when administered to normal fasting rats, only a considerable reduction (26.57 mg/dL) was produced by the dose of 20 mg/kg/mL. Conclusion and Recommendation: Although P. yohimbe has long been reported to regulate blood glucose levels;such effect is unclear and remains requiring further studies.

关键词： Pausinystalia yohimbe Bark Yohimbine Fasting Blood Glucose Level Hypoglycemia

Improved Antiproliferative Activities of a New Series of 1,3,4-Thiadiazole Derivatives Against Human Leukemia and Breast Cancer Cell Lines

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Chemical Research in Chinese Universities 2016年第5期32卷 768-774页

作者： LIU Tingting WAN Yichao LIU Renshuai MA Lin LI Minyong FANG Hao Key Laboratory of Chemical Biology Ministry of Education Department of Medicinal Chemistry School of Pharmacy Shandong University Jinan 250012 P. R. China

Twenty-two novel 1,3,4-thiadiazole derivatives were synthesized using different aromatic acids as starting materials, followed by cyclization, coupling and deprotection reaction. The structures of all the target compounds were identified by means of IH nuclear magnetic resonance（NMR）, laC NMR and high resolution mass spectrometer（HRMS）. Further biological evaluations were performed for chronic myelogenous leukemia cell and breast cancer cell. The results suggest that most of the target compounds exhibit potent anti-proliferative activities. Especially, compound 5b shows better antiproliferative activities against MDA-MB-231 and K562 cell lines compared with gossypol.

关键词： Thiadiazole Anti-tumor activity Antiproliferative activity

Effects of methanolic extract of yohimbe bark (Pausinystalia yohimbe) on isolated rabbit aortic strip and rat uterus

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Health 2013年第6期5卷 1016-1020页

作者： Hozeifa Mohamed Hassan Imad Mohamed Taj Eldin Elhadi Mohamed Ahmed Abd Elwahab Hassan Mohamed Nizar Sirag Department of Pharmacognosy Faculty of Pharmacy University of Gezira Wad Medani Sudan Department of Pharmacology and Toxicology Medicinal and Aromatic Plant Research Institute National Centre of Research Khartoum Sudan Department of Pharmacology Faculty of Pharmacy University of Gezira Wad Medani Sudan

Background: medicinal plants contain physiologically active principles that over the years have been exploited in traditional medicine for the treatment of various ailments. Objectives and Methods: This study aimed to investigate the effects of the methanolic extract of Pausinystalia yohimbe bark (5 mg/ml) on isolated rabbit aortic strip and rat uterus. Results: methanolic extract of P. yohimbe bark (5 mg/ml) produced relaxation of the phenylephrine precontracted-rabbit aortic strip. This relaxation may be resulted through nitric oxide (NO), since the pretreatment of the isolated rabbit aortic strip with methylene blue inhibited the NO-mediated relaxation. Moreover, the extract exhibited relaxation of rat uterine muscles, which appeared to be not mediated by activation of β2-adrenoceptors and/or H2 receptors, since the relaxant effect continued even after the pretreatment of the tissue with propranolol and ranitidine respectively. Conclusion: The obtained results revealed that methanolic extract of P. yohimbe bark caused relaxation of both isolated rat uterus and rabbit aortic strip through facilitating the role of endogenous compounds such as NO.

关键词： P. yohimbe Bark Isolated Tissues Aortic Strip Rat Uterus Relaxation Nitric Oxide

Antioxidant,antimicrobial,and α-glucosidase inhibitory activities of saponin extracts from walnut(Juglans regia L.) leaves

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Asian Pacific Journal of Tropical Biomedicine 2023年第2期13卷 60-69页

作者： Youssef Elouafy Adil El Yadini Salma Mortada Mohamed Hnini Hicham Harhar Asaad Khalid Ashraf NAbdalla Abdelhakim Bouyahya Khang Wen Goh Long Chiau Ming My El Abbes Faouzi Mohamed Tabyaoui Laboratory of Materials Nanotechnology and EnvironmentFaculty of SciencesMohammed V University in RabatRabatMorocco Laboratories of Pharmacology and Toxicology Pharmaceutical and Toxicological Analysis Research TeamFaculty of Medicine and PharmacyMohammed V University in RabatRabatMorocco Center of Plant and Microbial Biotechnology Biodiversity and EnvironmentMicrobiology and Molecular Biology TeamFaculty of SciencesMohammed V University in RabatRabatMorocco Substance Abuse and Toxicology Research Center Jazan UniversityJazan 45142Saudi Arabia medicinal and aromatic plants and Traditional Medicine Research Institute National Center for ResearchKhartoumSudan Department of Pharmacology and Toxicology College of PharmacyUmm Al-Qura UniversityMakkahSaudi Arabia Laboratory of Human Pathologies Biology Faculty of SciencesMohammed V University in RabatMorocco Faculty of Data Science and Information Technology INTI International UniversityNilaiMalaysia School of Medical and Life Sciences Sunway UniversitySunway CityMalaysia

Objective:To investigate the relationship between triterpenoid saponin content and antioxidant,antimicrobial,and α-glucosidase inhibitory activities of 70%ethanolic,butanolic,aqueous,supernate and precipitate extracts of Juglans regia ***:Triterpenoid saponins of different Juglans regia leaf extracts were measured by the vanillin *** activity was evaluated against DPPH and ABTS free *** also assessed α-glucosidase inhibitory and antimicrobial activities of the leaf ***’s correlation coefficient was evaluated to determine the correlation between the saponin content and biological ***:The butanolic extract was most effective against DPPH with an IC50of 6.63μg/mL,while the aqueous extract showed the highest scavenging activity against ABTS free radical with an IC50of 42.27μg/***’s correlation analysis indicated a strong negative correlation (r=-0.956) between DPPH radical scavenging activity (IC50) and the saponin content in the samples *** addition,the aqueous extract showed the best α-glucosidase inhibitory activity compared with other *** the extracts had fair antibacterial activity against Bacillus subtilis,Escherichia coli,and Klebsiella pneumoniae except for the aqueous ***:Juglans regia extracts show potent antioxidant,antimicrobial,and α-glucosidase inhibitory *** is a correlation between saponin levels in Juglans regia leaf extracts and the studied ***,additional research is required to establish these relationships by identifying the specific saponin molecules responsible for these activities and elucidating their mechanisms of action.

关键词： Juglans regia leaves Triterpenoid saponin Antioxidant activity DPPH ABTS Antidiabetic activity α-Glucosidase Antimicrobial activity

Indole-tolerant Oxidation of 1,2-Diarylalkynes to 1,2-Diketone Derivatives

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Chemical Research in Chinese Universities 2015年第1期31卷 53-59页

作者： CHENG Xu LI Xiaolong WAN Weili HAO Wenmei HAI Li WU Yong Key Laboratory of Drug-targeting of Ministry of Education Department of Medicinal Chemistry West China School of Pharmacy Sichuan University Chengdu 610041 P. R. China

A new indole-tolerant oxidation condition for the synthesis of 1,2-diketone derivatives from the corresponding 1,2-diarylalkynes was described. By screening a series of oxidation systems on alkynes linked with indole and different substituted aromatic ring, the DMSO/PdCl2/CuCl2 system afforded moderate to good yields despite the existence of electron-rich indole ring.

关键词： Selective oxidation 1,2-Diarylalkyne 1,2-Diketone

Recent Progress in Boosted PDT Induced Immunogenic Cell Death for Tumor Immunotherapy

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Chemical Research in Chinese Universities 2021年第1期37卷 83-89页

作者： LI Jun OU Hanlin DING Dan State Key Laboratory of medicinal Chemical Biology Key Laboratory of Bioactive MaterialsMinistry of EducationCollege of Life SciencesNankai UniversityTianjin300071P.R.China

With the rapid development of materials science,photosensitive materials have been widely used in the field of immunogenic cell death(ICD),which was on account of the reactive oxygen species(ROS)generation by photosensitizer under light irradiation inducing cellular oxidative stress during the dying of *** researches related to photodynamic therapy(PDT)induced ICD were conducted and exhibited brilliant performance in cancer ***,a variety of different strategies for PDT induced ICD have been summarized and discussed to provide researchers more inspiration for cancer immunotherapy.

关键词： Photodynamic therapy Immunogenic cell death Damage-associated molecular pattern

Antioxidant and hepatoprotective effects of Ajuga nipponensis extract by ultrasonic-assisted extraction

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Asian Pacific Journal of Tropical Medicine 2016年第5期9卷 409-414页

作者： Chang-Wei Hsieh Wen-Ching Ko Wai-Jane Ho Chao-Kai Chang Guo-Jhou Chen Jen-Chieh Tsai Department of medicinal Botanicals and Health Applications Da-Yeh University Biotechnology Research Center Da-Yeh University Department of Bioindustry Technology Da-Yeh University

Objective: To investigate suitable condition for extraction of the active components from Ajuga nipponensis(A. nipponensis). Methods: Orthogonal experimental design was used to determine the optimal extraction parameters for ecdysterones and flavonoids. Finally, the hepatoprotective abilities of A. nipponensis extracts were evaluated by CCl_4-induced animal models. Results:Maximum yields of flavonoids(7.87±0.10) mg/g and ecdysterones(0.73±0.02) mg/g could be obtained when the extraction time was 50 min, the extraction temperature was 60 ℃, and the ratio of sample to 70%(v/v) ethanol was 1:20(w/w). The antioxidant property of A. nipponensis was correlated to the concentration of its extracts. At 5 mg/m L, A. nipponensisextract scavenged 84.8% of DPPH radical and had absorbance values of 2.43±0.04 reducing power. Upon CCl_4-induced liver injury, glutamic oxaloacetic transaminase and glutamic pyruvic transaminase decreased significantly after the mice were treated with A. nipponensis. Histological researches also explained that A. nipponensis reduced the extent of liver lesions induced by CCl_4. Conclusions: A. nipponensis exhibited potent antioxidant activity in chemical experimental models and hepatoprotective effect against CCl_4-induced liver damage.

关键词： Ajuga nipponensis Ultrasonic-assisted extraction Orthogonal test Antioxidant hepatoprotection