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Structure-tissue exposure/selectivity relationship(STR) correlates with clinical efficacy/safety

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Acta Pharmaceutica Sinica B 2022年第5期12卷 2462-2478页

作者： Wei Gao hongxiang hu Lipeng Dai Miao he hebao Yuan huixia Zhang Jinhui Liao Bo Wen Yan Li Maria Palmisano Mohamed Dit mady Traore Simon Zhou Duxin Sun Department of Pharmaceutical Sciences College of PharmacyUniversity of MichiganAnn ArborMI 48109USA Translational Development and Clinical Pharmacology Bristol Myers SquibbSummitNJ 07920USA

Drug optimization, which improves drug potency/specificity by structure-activity relationship(SAR) and drug-like properties, is rigorously performed to select drug candidates for clinical trials. however,the current drug optimization may overlook the structure-tissue exposure/selectivity-relationship(STR) in disease-targeted tissues vs. normal tissues, which may mislead the drug candidate selection and impact the balance of clinical efficacy/toxicity. In this study, we investigated the STR in correlation with observed clinical efficacy/toxicity using seven selective estrogen receptor modulators(SERMs) that have similar structures, same molecular target, and similar/different pharmacokinetics. The results showed that drug’s plasma exposure was not correlated with drug’s exposures in the target tissues(tumor, fat pad, bone, uterus),while tissue exposure/selectivity of SERMs was correlated with clinical efficacy/safety. Slight structure modifications of four SERMs did not change drug’s plasma exposure but altered drug’s tissue exposure/*** SERMs with high protein binding showed higher accumulation in tumors compared to surrounding normal tissues, which is likely due to tumor EPR effect of protein-bound drugs. These suggest that STR alters drug’s tissue exposure/selectivity in disease-targeted tissues vs. normal tissues impacting clinical efficacy/toxicity. Drug optimization needs to balance the SAR and STR in selecting drug candidate for clinical trial to improve success of clinical drug development.

关键词： Structure-activity-relationship(SAR) Structure-tissue exposure/selectivity relationship(STR) Drug optimization Clinical efficacy/toxicity Drug development

Changes in peripapillary retinal nerve fiber layer thickness in patients with primary open-angle glaucoma after deep sclerectomy

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World Journal of Ophthalmology 2011年第1期1卷 4-10页

作者： Asaad A Ghanem Salah M mady hatem El-Said El-wady Mansoura Oph-thalmic Center Faculty of Medicine Mansoura University 35516 Mansoura Egypt Department of Ophthalmology Benha Univer-sity 2465 Benha Egypt

AIM： To assess changes in peripapillary retinal nerve fiber layer （RNFL） thickness and visual field （VF） in patients with glaucoma after reduction of intraocular pressure （IOP）. METhODS： Thirty-five consecutive patients with bilat-eral high tension glaucoma were included in the study. Thirty-five eyes underwent monocular deep sclerectomy （surgery group） and the medically treated fellow eyes served as controls （control group）. Quantitative analyses of the peripapillary RNFL thickness by optical coherence tomography （OCT） and global VF indices by automated perimetry were performed before surgery and six months after surgery in both eyes. The changes in RNFL thickness overall and by quadrant were evalu-ated and studied with respect to age, best-corrected visual acuity （BCVA）, preoperative global VF indices, postoperative IOP changes, and postoperative changes in global VF indices. Changes observed in RNFL thickness and VF indices were compared between eyes after surgery and fellow eyes. RESULTS： Six months after surgery, the overall IOP decreased from a baseline mean of 24.5 ± 3.2 mmhg to 11.5 ± 2.7 mmhg （P 〈 0.001） at the time of OCT testing. A signifcant increase in the overall mean RNFL thickness was observed after surgery （P 〈 0.001）. The preoperative VF mean deviation was significantly cor-related with a postoperative increase in the RNFL thick-ness （P 〈 0.075）. No correlation was found between RNFL thickness changes and age, BCVA, or changes in the global VF indices. There was no significant difference between eyes with an IOP reduction of more than 50% and those with a reduction in IOP less than 30% （ P = 0.312）.CONCLUSION： A signifcant increase in the peripapil-lary RNFL thickness was associated with IOP reduction by glaucoma filtration surgery as measured by OCT.

关键词： Peripapillary retinal nerve fiber layer thickness Optical coherence tomography Visual field indices Glaucoma medication Deep sclerectomy

Photoswitchable molecular dipole antennas with tailored coherent coupling in glassy composite

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Light(Science & Applications) 2015年第1期4卷 259-266页

作者： mady Elbahri Ahnaf Usman Zillohu Bastian Gothe Mehdi Keshavarz hedayati Ramzy Abdelaziz hala Jarallah El-Khozondar Muhammad Bawa’aneh Moheb Abdelaziz Andrei Lavrinenko Sergei Zhukovsky Shahin homaeigohar Nanochemistry and Nanoengineering Faculty of EngineeringInstitute for Materials ScienceUniversity of KielKaiserstrasse 224143 KielGermany Nanochemistry and Nanoengineering Institute of Polymer ResearchHelmholtz-Zentrum GeesthachtMax-Planck-Strasse 121502 GeesthachtGermany Refractories Ceramics and Building Materials DepartmentNational Research CentreDokkiCairoEgypt Electrical Engineering Department Islamic University of GazaGazaPO Box 108Palestine The hashemite University Department of PhysicsZarqaJordan&Khalifa University of ScienceTechnology&Research(KUSTAR)PO Box 573SharjahUAE DTU Fotonik Technical University of DenmarkOersteds pl.343Kongens LyngbyDK-2800Denmark

here,we introduce the first experimental proof of coherent oscillation and coupling of photoswitchable molecules embedded randomly in a polymeric matrix and acting cooperatively upon illumination with UV *** particular,we demonstrate the specular reflection and Brewster phenomenon alteration of photochromic molecular dipole *** successfully demonstrate the concept of Brewster wavelength,which is based on the dipolar interaction between radiating dipoles and the surrounding matrix possessing a net dipole moment,as a key tool for highly localized sensing of matrix *** also introduce the concept of‘tailored molecular photonic coupling’while highlighting the role of interferences for the design of optically active media by adjusting the photonic response of the medium with the real and imaginary refractive index of photoswitchable molecules in the‘ON’*** results enhance our fundamental understanding of coherent dipole radiation and open a new vein of research based on glassy disordered dipolar composites that act as macroscopic antenna with cooperative action;furthermore,these results have important implications for new design rules of tailored photonics.

关键词： Brewster angle coherent coupling collective oscillation photoswitchable molecular photonics specular reflection

Nutritional Contribution of Some Senegalese Forest Fruits Running across Soudano-Sahelian Zone

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Food and Nutrition Sciences 2011年第6期2卷 606-612页

作者： Nicolas Cyrille Ayessou Cheikh Ndiaye mady Cissé Mathieu Gueye Mama Sakho Université Cheikh Anta Diop - Ecole Supérieure Polytechnique Laboratoire de Formation Continue en Industries Agroalimentaires B.P 5085 Dakar – Fann

As a good food supply for the local people in various Senegalese regions, the forest fruits are becoming very important. They are using between foods or main condiment for dishes in many part of Africa. These fruits represent non negligible sources of vitamins, carbohydrates and minerals. Instead of more commercialized species such as Adansonia digitata L., Detarium senegalensis ***., Saba senegalensis (***.) Pichon, Tamarindus indica L., this article focused on nutritional values of other fruits with little interest or neglected. These species were Ficus gnaphalocarpa, L., Cordyla pinnata (Lepr. ex ***.) Milne-Redh. and Icacina senegalensis, harvested in soudano-sahelian zone;while Sarcocephalus latifolius (Sm.) E.A. Bruce belongs to Sudanese zone. The fruit pulps were isolated and freeze dried before analysis. The results showed that acidity, vitamin C and total minerals were significantly different from one fruit to another. S. latifolius with the highest acidity content (402.43 mg/100 g) and best vitamin C content if 1488 mg/100 g were found. Also as results, S. latifolius provided high protein content nearby the 20%. The caloric contributing (kcal/100 g) were 102.5, 177 and 132 respectively for F. gnaphalocarpa, C. pinnata, and S. latifolius. The ash contents were the same for all species (4.5%), indicating the richness in mineral elements. Furthermore, all species in this study were good sources of iron, copper and zinc. however, small amounts of sodium were noticed in all samples. Analysis of total sugars and their profile showed that I. senegalensis and C. pinnata were more appreciated. These results predicted the useful incomes for forest fruits in human being. Lot of medicinal virtues has been recognized from these fruits. The increase in value and the preservation of the biodiversity are necessary particularly for C. pinnata which presents a serious threat because of the strong income for wood production.

关键词： Cordyla Pinnata Sarcocephalus Latifolius Ficus Gnaphalocarpa Icacina Senegalensis Nutritional Composition Senegal

Systematic Review and Meta-Analysis of the Palatal Surgeries in the Treatment of Obstructive Sleep Apnea

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International Journal of Otolaryngology and head & Neck Surgery 2021年第2期10卷 61-74页

作者： Amr Nabil Rabie Ossama mady Ahmed Negm El-Shazly Alaa Abouzeid Department of Otolaryngology/head and Neck Surgery Faculty of Medicine Ain Shams University Cairo Egypt Department of Otolaryngology/head and Neck Surgery Misr University for Science and Technology Cairo Egypt

Background: This paper aims to examine published articles between January 2008 and January 2019 on the different palatal surgeries performed on OSA patients and the treatment outcomes, which in turn will be used to determine the effectiveness of various palatal surgical techniques in treating OSAS and the most effective of the palatal surgical techniques in treating OSAS. Patients and Methods: The current review followed the guidelines of preferred reporting items for systematic reviews and meta-analysis statement 2009 (PRISMA). The quality of relevant studies was assessed using NIh quality assessment tool for observational cohort and cross-sectional studies as well as NIh tool for quality assessment for case series studies. Results: Meta-analyses of relevant studies showed that the surgical technique that achieved the best reduction on AhI (Apnea/hypopnea Index) was the lateral pharyngoplasty followed by the Anterior Palatoplasty, with a significant mean reduction of [(SMD = −0.848, 95% CI (−1.209 - −0.487), p-value he technique responsible for the best improvement in Epworth Sleepiness Score (ESS) was the Relocation Pharyngoplasty, with a significant mean reduction of [SMD = −0.998, 95% CI (−1.253 - −0.743), p-value h the Expansion Sphincter Pharyngoplasty, with a significant mean reduction of [SMD = 1.011, 95% CI (0.581 - 1.440), p-value he surgical procedure that results in the best post-operative Visual Analogue Scale (VAS) was Z-Palatoplasty, with a significant mean reduction of [SMD = −1.551, 95% CI (−2.049 - −1.052), p-value h changes with a significant mean reduction of [SMD = −2.219, 95% CI (−2.730 - −1.708), p-value howed that expansion sphincter pharyngoplasty achieved the

关键词： Obstructive Sleep Apnea Palatal Surgery ESS AhI VAS Oxygen Saturation Meta-Analysis Systematic Review

Phytochemical Screening, Total Phenolic and Antioxidant Activity of Numerous Extracts from Leaves and Bark of Bauhinia rufescensLam

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Food and Nutrition Sciences 2021年第6期12卷 544-556页

作者： Seid Ali Mahamat Niang Lahat Ayessou Nicolas Cyrille Cisse mady Diop Codou Mar Adam Barka University Abeche Tchad Water Energy Environment and Industrial Processes Laboratory (LE3PI) ESP-UCAD Dakar Sénégal Center for Studies on Food Safety and Functional Molecules (CESAM-RESCIF) ESP-UCAD Dakar Sénégal

Researches for natural antioxidants that play an important role in the prevention of diseases linked to free radicals have increased in recent years. In this study, antioxidant activity of Bauhinia rufescens Lam which is a medicinal plant was investigated. The methanol extract, acetone extract and water extract of leaf and trunk bark had antioxidant activity. Three methods were used: 2,2-diphenyl-1picryl-hydrazyl (DPPH), 2,2’-Azino-bis-(3-ethylbenzoth iazoline-6-sulfonic acid) (ABTS) and ferric ion reducing power (FRAP) by spectrophotometry. Phytochemical screening was carried out followed by the quantification of the total phenolic by the Folin-Ciocalteu method. The analysis of variance (ANOVA) with the STATISTICA 7.1 software revealed significant differences (p 0.05). Percentage inhibition (PI) and IC50 of the extracts were obtained using the OriginPro 8.5 software. These tests show that the bark is as rich in total phenolic as the leaves. The DPPh test shows that at 2.5 mg/ml, the bark and

关键词： Bauhinia rufescens Lam Total Phenolic Antioxidant Activity

Antioxidant Activity of hydro-Acetonic, hydro-Methanolic and Aqueous Leaf and Bark Extracts of Sclerocaria birrea(A. Rich.) hochst

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Food and Nutrition Sciences 2021年第5期12卷 429-438页

作者： Lahat Niang Seid Ali Mahamat Nicolas Cyrille Ayessou mady Cisse Codou Mar Diop Laboratory of Electrochemistry and Membrane Processes (LEPM) ESP-UCAD Dakar Sénégal Center for Studies on Food Safety and Functional Molecules (CESAM-RESCIF) ESP-UCAD Dakar Sénégal Adam Barka University Abeche Tchad

Bioactive compounds in plants are associated with the reduction of chronic diseases. The free radical scavenging activity of different extracts of a medicinal plant, Sclerocarya birrea, has been investigated using the DPPH test, ABTS test and FRAP. Three extracts were prepared from the leaves and bark: hydro-methanolic, hydro-acetonic and aqueous. Phytochemical screening was carried out the standard methods followed by the determination of the polyphenol by Folin-Ciocalteu method. The analysis of variance (ANOVA) with the STATISTICA 7.1 and statistical significance was set at p 0.05. Evolution of percent inhibition (PI) as well as the IC50 of the extracts was obtained using the Origin Pro 8.5 software and Microsoft Excel. The results show that the bark extracts

关键词： Sclerocarya birrea Antioxidant Activity DPPh ABTS Total Phenolic

Schistosomiasis control in Senegal:results from community data analysis for optimizing preventive chemotherapy intervention with praziquantel

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Infectious Diseases of Poverty 2023年第6期12卷 101-102页

作者： Boubacar Diop Khadime Sylla NDèye MBackéKane Oumou Kaltoum Boh Babacar Guèye mady Ba Idrissa Talla Malang Mané Rose Monteil Boniface Kinvi honorat Gustave Marie Zoure Jorge Cano Ortega Pauline Mwinzi Moussa Sacko Babacar Faye Programme National de Lutte Contre les Bilharzioses et les Géo-helminthiases Direction de la Lutte Contre la Maladie (DLM) Ministère de la Santé et de l’Action Sociale (MSAS) Dakar Senegal Department of Parasitology and Mycology Faculty of Medicine Pharmacy and Odontology Université Cheikh Anta Diop de Dakar (UCAD) Dakar Senegal WhO Country Office Dakar Senegal Département de Santé Publique Faculté des Sciences de la Santé Université Amadou Hampathé Ba Dakar Senegal FhI 360 Chargé des Enquêtes et Evaluation des Maladies et des Campagnes de DMM Dakar Senegal Expanded Special Project for Elimination of Neglected Tropical Diseases (ESPEN) WHO Africa Regional Office Brazzaville Congo Service de Parasitologie Institut National de Santé Publique (INSP) Bamako Mali

Background Over the past two decades,preventive chemotherapy(PC)with praziquantel(PZQ)is the major strategy for controlling schistosomiasis in *** objective of this analysis was to update the endemicity of schistosomiasis at community level for better targeting mass treatment with PZQ in *** Demographic and epidemiological data from 1610 community health areas were analyzed using the schistosomiasis community data analysis tool of Expanded Special Project for Elimination of Neglected Tropical Diseases which developed by World health Organization/Africa Ofce(WhO/AFRO).The tool uses a WhO/AFRO decision tree for areas without epidemiological data to determine whether mass treatment should be continued at community *** analysis was *** Overall,the endemicity of 1610 community health areas were updated based on the data from the district endemicity(33.5%)and the form of Join request for selected PC medicine(40.5%).Up to 282(17.5%)and 398(24.7%)of community health areas were classifed as moderate and high endemicity.41.1%of communities were non *** endemicity was more important in Tambacounda,Saint Louis,Matam,Louga and Kedougou.A change in endemicity category was observed when data was disagregted from district level to community *** units classifed non endemic were more important at community level(n=666)compared to district level(n=324).Among 540 areas previously classifed high endemic at district level,392(72.6%)remained high prevalence category,while 92(17.0%)became moderate,43(8.0%)low and 13(2.4%)non-endemics at community *** of implementation units requiring PC was more important at district level(1286)compared to community level(944).Number of school aged children requiring treatment was also more important at district level compared to community *** The analysis to disaggregate data from district level to community level using the WhO/AFRO schistosomiasis sub-distric

关键词： Schistosomiasis Community data analysis Endemicity Praziquantel Senegal

Food habits of Bryconaethiops boulengeri Pellegrin, 1900 (Characiformes: Alestidae) of Djiri River Tributary of the Right Bank of Congo River

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Open Journal of Ecology 2018年第9期8卷 510-521页

作者： M. Mikia I. mady-Goma Dirat A. Tsoumou J. Vouidibio Research Laboratory of Animal Biology and Ecology ENS University Marien Ngouabi Brazzaville Congo Faculty of Sciences and Techniques University Marien Ngouabi Brazzaville Congo

Diet of 300 specimens of Bryconaethiops boulengeri from Djiri River (Congo Brazzaville) caught with cash nets was studied according to the size of fish, sampling stations and hydrological season. Sampling focused on twelve annual withdrawals made during three years. The relative importance index combining numerical and weight percentages of occurrence was calculated and also the sex ratio was evaluated. Bryconaethiops boulengeri consumes terrestrial and aquatic insects and everything that falls into the water (birds feathers, plant debris, fruits, etc.). The percentage of emptiness is 9.66% of the three sampling stations selected;no significant difference in diet was observed whatever the season.

关键词： Djiri River Bryconaethiops boulengeri Food habits Occurrence Eclectic Insectivore