Article
Microbiology
Renu Sudhakar, Navin Adhikari, Saniya Pamnani, Abhipsa Panda, Manish Bhattacharjee, Zeba Rizvi, Sadaf Shehzad, Dinesh Gupta, Puran Singh Sijwali
Summary: Despite the challenges posed by drug-resistant parasite strains, repurposing existing drugs for malaria treatment is an attractive option. Bazedoxifene, a selective estrogen receptor modulator, has shown potent inhibitory activity against Plasmodium falciparum and Plasmodium berghei. It inhibits the formation of hemozoin, a byproduct of hemoglobin degradation by the malaria parasite, and could potentially be repurposed as an antimalarial drug.
MICROBIOLOGY SPECTRUM
(2022)
Article
Endocrinology & Metabolism
Christine A. Cabelka, Cory W. Baumann, Angus Lindsay, Andrew Norton, Nick C. Blixt, Gengyun Le, Gordon L. Warren, Kim C. Mansky, Susan A. Novotny, Dawn A. Lowe
Summary: The tissue-selective effects of Bazedoxifene (BZA) on musculoskeletal system in Ovariectomized (OVX) female mice indicate that BZA may act as an estrogen receptor agonist in skeletal muscle, as it has been seen in bone, providing minor benefits to the musculoskeletal system.
JOURNAL OF ENDOCRINOLOGY
(2021)
Article
Pharmacology & Pharmacy
Adam Olaitan Abdulkareem, Priya Tiwari, Zahid Rasool Lone, Hina Iqbal, Satish Gupta, Rajesh Kumar Jha, Debabrata Chanda, Kumaravelu Jagavelu, Kashif Hanif
Summary: This study investigated the ameliorative effects of ormeloxifene, a selective estrogen receptor modulator, in pulmonary hypertension. The results showed that ormeloxifene promoted the synthesis of 17β-estradiol, alleviated inflammation, and improved the NOX4/HO1/Nrf/PPAR gamma/PGC-1 alpha axis, thereby attenuating pulmonary hypertension.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Endocrinology & Metabolism
Bo Mi Kim, Sung Eun Kim, Dong-Yun Lee, DooSeok Choi
Summary: In this study, 40 postmenopausal Korean women underwent 12 months of TSEC treatment, showing a significant increase in total hip bone mineral density and specific changes in the parameters of HSA. The findings suggest that TSEC treatment could potentially improve bone geometry in postmenopausal women, providing a promising option for fracture prevention and osteoporosis.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Obstetrics & Gynecology
Joann V. Pinkerton
Summary: Selective estrogen receptor (ER) modulators have variable tissue-specific estrogen agonist and antagonist activities. Ospemifene is approved to treat dyspareunia, while lasofoxifene is in development for resistant ER positive breast cancer.
CLINICAL OBSTETRICS AND GYNECOLOGY
(2021)
Review
Endocrinology & Metabolism
Beilei Bi, Yi Jiang, Yin Shi, Fan Ruan
Summary: The aim of this study was to evaluate the efficacy of bazedoxifene plus conjugated estrogens in treating menopausal symptoms in postmenopausal women. The results showed that treatment with BZA/CE significantly reduced the number of hot flushes, the percentage of parabasal cells, and the time to fall asleep compared to placebo. Sleep disturbance and total MENQOL also showed significant improvement. Additionally, BZA 20 mg/CE 0.625 mg was more effective than BZA 20 mg/CE 0.45 mg in improving menopausal symptoms.
GYNECOLOGICAL ENDOCRINOLOGY
(2022)
Review
Chemistry, Medicinal
Neha Bhatia, Shreejita Hazra, Suresh Thareja
Summary: The discovery of SERDs has revolutionized anticancer research, particularly in the treatment of ER+ breast cancer. These drugs are considered essential due to the high prevalence of ER+ breast cancer cases and the development of endocrine resistance. This review provides an overview of the pathophysiology of SERDs, their interaction with FDA-approved drugs, and the current research and design strategy for these therapeutics.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Ravindran Vini, Vishnu Sunil Jaikumar, Viji Remadevi, Swathy Ravindran, Juberiya M. Azeez, Anjana Sasikumar, Shankar Sundaram, Sreeharshan Sreeja
Summary: 27-hydroxycholesterol (27-HC) is an endogenous selective estrogen receptor modulator (SERM) that has adverse effects on breast cancer. Pomegranate extract, which contains ellagitannins and ellagic acid, can compete with 27-HC. Urolithins, especially urolithin A (UA) and urolithin B (UB), derived from pomegranate, have antiproliferative and estrogenic activities, and UA can act as an antagonist to 27-HC in breast cancer cells, making it a potential SERM.
PHYTOTHERAPY RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Jin Bai, Yao Li, Guofeng Yan, Jing Zhou, Alejandra Garcia Salmeron, Olamide Tolulope Fategbe, Sathish Kumar, Xuejin Chen, Dong-Bao Chen
Summary: This study found that endogenous estrogens selectively stimulate uterine artery CBS expression through specific estrogen receptors in pregnant rats, leading to increased production of hydrogen sulfide and enhanced uterine blood flow during pregnancy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Obstetrics & Gynecology
Andrea R. Genazzani, Patrizia Monteleone, Andrea Giannini, Tommaso Simoncini
Summary: Menopausal symptoms can significantly impact a woman's personal and social life, leading to reduced quality of life and productivity. Hormone therapy (HT) has been controversial due to concerns about cardiovascular risks and cancer, but recent studies have shown benefits in relieving symptoms and reducing certain health risks.
HUMAN REPRODUCTION UPDATE
(2021)
Article
Obstetrics & Gynecology
Sarah R. Hoffman, Samuel Governor, Kimberly Daniels, Ryan M. Seals, Najat J. Ziyadeh, Florence T. Wang, Dingwei Dai, Cheryl N. Mcmahill-Walraven, Patty Shuminski, Vera Frajzyngier, Xiaofeng Zhou, Rongjun Shen, Renu K. Garg, Nicole Fournakis, Stephan Lanes, Daniel C. Beachler
Summary: This study compared the risk of endometrial cancer, endometrial hyperplasia, and breast cancer among women using conjugated estrogens/bazedoxifene (CE/BZA) with those using estrogen/progestin combination hormone therapy (EP). The results showed that women using CE/BZA might have slightly higher risks of endometrial cancer and endometrial hyperplasia, but a lower risk of breast cancer in the first years of use.
MENOPAUSE-THE JOURNAL OF THE NORTH AMERICAN MENOPAUSE SOCIETY
(2023)
Article
Biochemical Research Methods
Masato Okano, Mitsuhiko Sato, Shinji Kageyama
Summary: Bazedoxifene, a selective estrogen receptor modulator, is included in the prohibited list by WADA. A method was developed to detect and quantify bazedoxifene and its metabolites in human urine.
DRUG TESTING AND ANALYSIS
(2022)
Article
Biotechnology & Applied Microbiology
Hanbit Song, Pyung-Gang Lee, Junyeob Kim, Joonwon Kim, Sang-Hyuk Lee, Hyun Kim, Uk-Jae Lee, Jin Young Kim, Eun-Jung Kim, Byung-Gee Kim
Summary: Multiple regiospecific enantiomers of hydroxy-(S)-equol were synthesized from daidzein and genistein through consecutive reduction and oxidation reactions. A one-pot synthesis pathway for 6-hydroxyequol was developed, and the estrogenic and antioxidative activities of each regio-isomer were evaluated.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2022)
Article
Biotechnology & Applied Microbiology
Sisi Qin, James N. Ingle, Wootae Kim, Huanyao Gao, Richard M. Weinshilboum, Liewei Wang
Summary: The study identified potential pathways, including ribosome and AMP-activated protein kinase (AMPK) signaling, regulated by ZNF423 or ZNF423 rs9940645 SNP. The findings suggest that AMPK signaling is modulated by the ZNF423 rs9940645 SNP and may affect metformin response in breast cancer, potentially serving as a biomarker for personalized metformin treatment.
PHARMACOGENETICS AND GENOMICS
(2021)
Article
Virology
Gen Miao, Haoran Peng, Hailin Tang, Yangang Liu, Xu Zheng, Bin Liu, Liangliang Jiang, Wanda Tang, Yanhua He, Yan Liu, Hao Ren, Ping Zhao, Zhongtian Qi, Cuiling Ding
Summary: In this study, the antiviral efficacy of 18 selective estrogen receptor modulators (SERMs) against SARS-CoV-2 infection was evaluated. Six SERMs showed excellent antiviral effects in cell and animal experiments. Bazedoxifene acetate, in particular, was identified as a potential agent against coronaviruses, acting on the penetration stage of viral infection by altering cholesterol distribution and endosome acidification.
JOURNAL OF MEDICAL VIROLOGY
(2022)
Review
Endocrinology & Metabolism
Jemima E. Schadow, David Maxey, Toby O. Smith, Mikko A. J. Finnila, Sarah L. Manske, Neil A. Segal, Andy Kin On Wong, Rachel A. Davey, Tom Turmezei, Kathryn S. Stok
Summary: This study systematically reviewed the published parameters for assessing subchondral bone in human osteoarthritis using computed tomography. The study identified clinically meaningful parameter categories and emphasized the importance of quantification and standardized measurement methods for improving the evaluation of disease progression.
Article
Endocrinology & Metabolism
Lindsay L. Loundagin, Kim D. Harrison, Xuan Wei, David M. L. Cooper
Summary: This study developed new techniques to define zones of BMU activity based on the 3D morphology of remodeling spaces in rabbit cortical bone and integrated morphological data with the BMU longitudinal erosion rate (LER) to elucidate the spatial-temporal coordination of BMUs and estimate mineral apposition rate (MAR). The results showed that the manual and semi-automated methods accurately defined the zones of remodeling spaces, and these techniques have the potential to assess dynamic parameters of bone resorption and formation.
Article
Endocrinology & Metabolism
Soroush Masrouri, Farzad Esmaeili, Maryam Tohidi, Fereidoun Azizi, Farzad Hadaegh
Summary: This study examined the association between estimated glomerular filtration rate (eGFR) decline and fracture incidence. The results showed that rapid kidney function decline (RKFD) can increase the incidence of fractures among the general population.
Article
Endocrinology & Metabolism
Steven J. Meas, Gabriella M. Daire, Michael A. Friedman, Rachel Denapoli, Preetam Ghosh, Joshua N. Farr, Henry J. Donahue
Summary: Age- and disuse-related bone loss both lead to decreases in bone mineral density, cortical thickness, and trabecular thickness and connectivity. It is important to experimentally compare these two mechanisms at a structural and transcriptomic level to better understand their similarities and differences. This study compares the effects of hindlimb unloading and aging on bone microarchitecture and gene expression in mice, finding that while both induce similar changes, aging has a greater impact on the transcriptome and tissue level.
Correction
Endocrinology & Metabolism
Masaru Matsuoka, Sho Tsukamoto, Yuta Orihara, Rieko Kawamura, Mai Kuratani, Nobuhiko Haga, Kenji Ikebuchi, Takenobu Katagiri
Article
Endocrinology & Metabolism
Rachel Kohler, Amy Creecy, David R. Williams, Matthew R. Allen, Joseph M. Wallace
Summary: Osteogenesis imperfecta is a hereditary bone disease that weakens bones and increase fracture risk. Current interventions mainly focus on increasing bone mass, but the compromised tissue-level material properties are not addressed. A study found that a RAL analog could reduce fracture risk, but further development is needed for optimal results in patients with osteogenesis imperfecta.
Article
Endocrinology & Metabolism
So Jeong Park, Eunhye Ji, Hyun Ju Yoo, Kyunggon Kim, Sunghwan Ji, Ji Yeon Baek, Jin Young Lee, Hee-Won Jung, Il-Young Jang, Eunju Lee, Namki Hong, Beom-Jun Kim
Summary: The study analyzed the relationship between serum lumican levels and osteosarcopenia in older adults, showing that older adults with osteosarcopenia had lower serum lumican levels. Lower serum lumican levels were associated with reduced bone mass and grip strength, indicating that lumican levels could be used as a biomarker for assessing the risk of osteosarcopenia, osteoporosis, or sarcopenia in older adults.
Article
Endocrinology & Metabolism
Michael B. Chavez, Michelle H. Tan, Tamara N. Kolli, Natalie L. Andras, Brian L. Foster
Summary: This study revealed the complex mechanisms by which disabling BSP functional domains led to profound and distinct changes in cementoblast cell functions, including dysregulated gene expression and reduced mineralization.
Article
Endocrinology & Metabolism
Julien Seiller, Blandine Merle, Romain Fort, Emilie Virot, Solene Poutrel, Giovanna Cannas, Arnaud Hot, Roland Chapurlat
Summary: The purpose of this study was to assess the prevalence of bone fragility in sickle cell patients and to evaluate the potential risk factors and associated complications.
Article
Endocrinology & Metabolism
Chirantap Oza, Anuradha Khadilkar, Pranay Goel, Madhura Karguppikar, Nikhil Shah, Nikhil Lohiya, Shruti Mondkar, Prashant Patil, Hemchand Prasad, Ankita Maheshwari, Dipali Ladkat, Neha Kajale, Chidvilas More, Devarati Khurjekar, Vaman Khadilkar
Summary: This study revealed that BoneXpert (BX) can be used for accurate assessment of bone age and screening of bone health in Indian children and youth with type-1 diabetes (T1D). 51.5% of T1D subjects showed significantly decreased metacarpal index (MCI). Height, Tanner stage, and vitamin D concentrations were positively correlated with MCI, while HbA1c and disease duration were negatively correlated with MCI.
Article
Endocrinology & Metabolism
Mariam R. Farman, Catherine Rehder, Theodora Malli, Cheryl Rockman-Greenberg, Kathryn Dahir, Gabriel Angel Martos-Moreno, Agnes Linglart, Keiichi Ozono, Lothar Seefried, Guillermo del Angel, Gerald Webersinke, Francesca Barbazza, Lisa K. John, Sewmi M. A. Delana Mudiyanselage, Florian Hoegler, Erica Burner Nading, Erin Huggins, Eric T. Rush, Ahmed El-Gazzar, Priya S. Kishnani, Wolfgang Hoegler
Summary: The ALPL gene variant database serves as an archive for interpreting the clinical significance of ALPL gene variants, facilitating the reclassification of VUS and continuous updates. The project establishes an international expert consortium, providing a multidisciplinary collaboration framework to improve genetic counseling and medical decision-making for HPP patients.
Article
Endocrinology & Metabolism
Giovanni Adami, Davide Gatti, Maurizio Rossini, Alessandro Giollo, Matteo Gatti, Francesco Bertoldo, Eugenia Bertoldo, Amy S. Mudano, Kenneth G. Saag, Ombretta Viapiana, Angelo Fassio
Summary: Certain diseases requiring glucocorticoids are independently associated with an increased risk of fractures. Chronic obstructive pulmonary disease (COPD) and neurological diseases are associated with both vertebral and non-vertebral fracture risk, while rheumatoid arthritis (RA) and inflammatory bowel disease (IBD) are only associated with non-vertebral fractures.
Article
Endocrinology & Metabolism
Frank C. Ko, Rong Xie, Brandon Willis, Zoe G. Herdman, Bryan A. Dulion, Hoomin Lee, Chun-do Oh, Di Chen, D. Rick Sumner
Summary: Intramembranous bone regeneration is important in joint and tooth replacement, but its underlying mechanisms are not well understood. This study found that increased periostin gene expression preceded increases in osteogenic genes during bone regeneration. Using a genetic mouse model, the researchers discovered that cells transiently expressing periostin played a critical role in intramedullary intramembranous bone regeneration.
Article
Endocrinology & Metabolism
T. Savikangas, T. H. Suominen, M. Alen, T. Rantalainen, S. Sipila
Summary: Regular exercise, especially high-intensity physical activity, can help slow down age-related bone loss and prevent a decline in femoral neck bone mineral density.
Article
Endocrinology & Metabolism
Mishaela R. Rubin, Ruban Dhaliwal
Summary: The increased risk of fractures observed in adults with type 1 diabetes (T1D) cannot be solely explained by modest decreases in areal bone mineral density (BMD). Accumulation of advanced glycation endproducts (AGEs) in bone has been suggested as a possible cause for the increased bone fragility in diabetes. Although the evidence linking AGEs and fractures in individuals with T1D is limited, recent data show that AGEs, as measured by skin intrinsic fluorescence, are a risk factor for lower BMD in T1D. Further research is needed to determine if there is a causal relationship between fractures and AGEs in T1D. If confirmed, this could lead to interventions that can reduce AGE accumulation and ultimately reduce fractures in T1D patients.