Page last updated: 2024-12-11

loa

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Description

lithocholic acid acetate: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID7203539
CHEMBL ID272041
SCHEMBL ID678540
MeSH IDM0012659

Synonyms (14)

Synonym
acetyllithocholic acid
LOA ,
lithocholic acid 3-acetate
CHEMBL272041 ,
(4r)-4-[(3r,5r,8r,9s,10s,13r,14s,17r)-3-acetyloxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]pentanoic acid
bdbm50375582
lithocholic acid acetate
(3beta,5beta,9beta)-3-(acetyloxy)cholan-24-oic acid
SCHEMBL678540
3alpha-acetoxy-5beta-cholanic acid
3-(acetyloxy)cholan-24-oic acid #
3alpha-acetoxy-5beta-cholan-24-oic acid
Q27462645
(r)-4-((3r,5r,8r,9s,10s,13r,14s,17r)-3-acetoxy-10,13-dimethylhexadecahydro-1h-cyclopenta[a]phenanthren-17-yl)pentanoic acid

Research Excerpts

Overview

Loa loa is a subcutaneous filarial parasite of man and is transmitted to humans by chrysops flies. It is endemic in the tropical rain forests of Western Africa.

ExcerptReferenceRelevance
"Loa-Loa is a parasitic infection endemic in the tropical rain forests of Western, Central, and Eastern Africa. "( [Ocular involvement in systemic Loa-Loa filariasis. Case report and review of the literature].
Jaksche, A; Loeffler, KU; Martin, S; Wessels, L, 2004
)
2.05
"Loa loa is a subcutaneous filarial parasite of man and is transmitted to humans by chrysops flies."( Loa loa in the anterior chamber of the eye: a case report.
Barua, N; Barua, P; Das, S; Hazarika, NK, 2005
)
2.49
"Loa loa is a filarial parasite which is mainly confined to West and Central Africa. "( Loa loa microfilariae aspirated during oocyte retrieval.
Camus, M; Devroey, P; Laureys, M; Van Steirteghem, AC; Verheyen, G; Wisanto, A, 1993
)
3.17
"Loa loa is a filarial parasite that is endemic in West and Central Africa. "( Loa loa infection as a cause of migratory angioedema: report of three cases from the Texas Medical Center.
Kielhofner, MA; Rakita, RM; White, AC, 1993
)
3.17
"Loa Loa is a chronic parasitemic disease which is endemic in the tropical rain forests of Western Africa. "( [Surgical worm extraction in loa loa ophthalmia].
Gabel, VP; Heep, M; Sachs, HG, 1998
)
2.03

Effects

ExcerptReferenceRelevance
"L. loa has been associated with fatal encephalopathic reactions in high Loa-infected individuals receiving ivermectin during mass drug administration programs for the control of onchocerciasis and lymphatic filariasis."( Development of a highly sensitive loop-mediated isothermal amplification (LAMP) method for the detection of Loa loa.
Abán, JL; Akue, JP; Fernández-Soto, P; Muro, A; Mvoulouga, PO; Sánchez, MC; Santiago, BV, 2014
)
1.13

Treatment

Loa L3 and treated with 10 mg/kg FLBZ once daily for 5 consecutive days. The treatment of Loa hyper-microfilaraemic individuals with ivermectin produces a clinical spectrum.

ExcerptReferenceRelevance
"loa L3 and treated with 10 mg/kg FLBZ once daily for 5 consecutive days."( Effect of flubendazole on developing stages of Loa loa in vitro and in vivo: a new approach for screening filaricidal agents.
Chunda, VC; Enyong, P; Fombad, FF; Gandjui, NVT; Hoerauf, A; Mackenzie, CD; Metuge, HM; Ndongmo, PC; Njiokou, F; Njouendou, AJ; Ritter, M; Wanji, S, 2019
)
1.49
"The treatment of Loa hyper-microfilaraemic individuals with ivermectin produces a clinical spectrum that parallels that seen in Loa hyper-microfilaraemic humans treated with ivermectin. "( Ivermectin treatment of Loa loa hyper-microfilaraemic baboons (Papio anubis): Assessment of microfilarial load reduction, haematological and biochemical parameters and histopathological changes following treatment.
Agnew, D; Datchoua-Poutcheu, FR; Enyong, P; Esuka, EN; Eversole, RR; Eyong, EJ; Hopkins, A; Kengne-Ouafo, AJ; Mackenzie, CD; Ngwa, CJ; Tendongfor, N; Wanji, S, 2017
)
1.1

Toxicity

New loiasis diagnostics (LoaScope; Loa antibody rapid test) may enable safe mass treatment decisions in co-endemic areas.

ExcerptReferenceRelevance
"The main risk factor of post-ivermectin serious adverse events (SAEs) is the presence of a high Loa loa microfilaremia."( Loa loa microfilarial periodicity in ivermectin-treated patients: comparison between those developing and those free of serious adverse events.
Boussinesq, M; Kamgno, J; Mackenzie, CD; Pion, SD; Thylefors, B, 2009
)
2.01
"Ivermectin (IVM) is exceptionally safe in humans, and is used for mass treatment of onchocerciasis and lymphatic filariasis."( Analysis of the mdr-1 gene in patients co-infected with Onchocerca volvulus and Loa loa who experienced a post-ivermectin serious adverse event.
Bourguinat, C; Boussinesq, M; Geary, TG; Kamgno, J; Mackenzie, CD; Prichard, RK, 2010
)
0.59
"Although ivermectin treatment can induce serious adverse events (SAEs) in individuals harboring high Loa loa microfilaremia (mf), not all patients with high mf levels develop such reactions, suggesting that cofactors may be involved."( Absence of an association between Plasmodium falciparum infection and post-ivermectin Loa-related non-neurologic serious adverse events.
Akame, J; Boussinesq, M; Fokom-Domgue, J; Gounoue, R; Kamgno, J; Nguipdop-Djomo, P; Pion, SD; Thylefors, B; Twum-Danso, NA, 2014
)
0.84
"The wide distribution of Loa loa infection (loiasis) throughout the Democratic Republic of Congo (DRC) is a major obstacle to the plans to eliminate onchocerciasis and lymphatic filariasis (LF) because the standard drug regime is dependent on ivermectin, which cannot be used in co-endemic areas due to the risk of severe adverse events (SAEs)."( Innovative tools for assessing risks for severe adverse events in areas of overlapping Loa loa and other filarial distributions: the application of micro-stratification mapping.
Bockarie, MJ; Cano, J; Kelly-Hope, LA; Molyneux, DH; Stanton, MC, 2014
)
0.93
" Few adverse events were reported and were mostly mild, with few moderate and no serious events."( Efficacy and safety of tribendimidine against Opisthorchis viverrini: two randomised, parallel-group, single-blind, dose-ranging, phase 2 trials.
Akkhavong, K; Duthaler, U; Hattendorf, J; Keiser, J; Odermatt, P; Sayasone, S; Senggnam, K; Vonghachack, Y; Xayavong, S, 2016
)
0.43
" Its control is currently hampered by the lack of a macrofilaricidal drug and by severe adverse events observed when the lone recommended microfilaricide, ivermectin is administered to individuals co-infected with Loa loa."( Filaricidal activities on Onchocerca ochengi and Loa loa, toxicity and phytochemical screening of extracts of Tragia benthami and Piper umbellatum.
Azantsa, BK; Babiaka, SB; Cho-Ngwa, F; Manfo, FP; Mbah, JA; Monya, E; Samje, M, 2016
)
0.87
" Active extracts were generally more toxic to the worms than to cells and showed no acute toxicity to Balb/c mice."( Filaricidal activities on Onchocerca ochengi and Loa loa, toxicity and phytochemical screening of extracts of Tragia benthami and Piper umbellatum.
Azantsa, BK; Babiaka, SB; Cho-Ngwa, F; Manfo, FP; Mbah, JA; Monya, E; Samje, M, 2016
)
0.69
"Individuals with high microfilarial densities (MFDs) of Loa loa are at risk of developing serious adverse events (SAEs) after ivermectin treatment."( Safety and Efficacy of Levamisole in Loiasis: A Randomized, Placebo-controlled, Double-blind Clinical Trial.
Bikita, P; Boussinesq, M; Campillo, JT; Chesnais, C; Hemilembolo, M; Louya, F; Missamou, F; Pion, SDS, 2022
)
0.97
" Safety outcomes were occurrence of SAE and adverse event frequency during the first week."( Safety and Efficacy of Levamisole in Loiasis: A Randomized, Placebo-controlled, Double-blind Clinical Trial.
Bikita, P; Boussinesq, M; Campillo, JT; Chesnais, C; Hemilembolo, M; Louya, F; Missamou, F; Pion, SDS, 2022
)
0.72
"5mg/kg levamisole caused more mild adverse events (10/85 vs."( Safety and Efficacy of Levamisole in Loiasis: A Randomized, Placebo-controlled, Double-blind Clinical Trial.
Bikita, P; Boussinesq, M; Campillo, JT; Chesnais, C; Hemilembolo, M; Louya, F; Missamou, F; Pion, SDS, 2022
)
0.72
" New loiasis diagnostics (LoaScope; Loa antibody rapid test) and risk prediction tools may enable safe mass treatment decisions in co-endemic areas."( An Integrated District Mapping Strategy for Loiasis to Enable Safe Mass Treatment for Onchocerciasis in Gabon.
Atsame, J; Biamonte, M; Diggle, PJ; Ella, SN; Gass, K; Hundley, L; Johnson, O; Ogoussan, K, 2021
)
0.92
" We develop a joint geostatistical modelling framework for the analysis of Ab and Loascope data to delineate whether an area is safe for MDA."( Geostatistical modelling enables efficient safety assessment for mass drug administration with ivermectin in Loa loa endemic areas through a combined antibody and LoaScope testing strategy for elimination of onchocerciasis.
Amoah, B; Atsame, J; Biamonte, M; Diggle, PJ; Ella, SN; Fronterrè, C; Gass, K; Giorgi, E; Hundley, L; Johnson, O; Ogoussan, K, 2022
)
1.16
" In areas where loiasis is co-endemic, this approach is complicated by the risk of serious adverse events following treatment with ivermectin in individuals with a high Loa loa microfilarial density (MFD)."( Evaluating post-treatment Loa loa microfilarial densities to classify serious adverse events caused by ivermectin: a retrospective analysis.
Boullé, C; Boussinesq, M; Chesnais, CB; Chippaux, JP; Garcia, A; Gardon, J; Kamgno, J; Pion, SD; Ranque, S, 2023
)
1.4
"The MFD threshold of 1000 mf per mL within 1 month of treatment, which is commonly used to attribute the occurrence of a serious adverse event to ivermectin, should be revised."( Evaluating post-treatment Loa loa microfilarial densities to classify serious adverse events caused by ivermectin: a retrospective analysis.
Boullé, C; Boussinesq, M; Chesnais, CB; Chippaux, JP; Garcia, A; Gardon, J; Kamgno, J; Pion, SD; Ranque, S, 2023
)
1.21

Dosage Studied

The passage across the placenta of immunogens constitutive of a crude microfilarial Loa loa extract has been investigated. IgG levels were shown to be identical in about half of the mother-cord paired samples. Results showed no difference in the effect of the dosage level on LoaMicrofilaraemia.

ExcerptRelevanceReference
" The passage across the placenta of immunogens constitutive of a crude microfilarial Loa loa extract has been investigated by dosing specific IgG, IgM and IgE antibodies in 92 maternal and corresponding cord blood samples, IgG levels were shown to be identical in about half of the mother-cord paired samples while in the other half the cord serum had a lower titre."( Lack of evidence for transplacental transfer of microfilarial antigens in filariasis due to Loa loa and Mansonella perstans.
Akué, JP; Van Hoegaerden, M, 1986
)
0.72
" Results showed no difference in the effect of the dosage level on Loa microfilaraemia."( [Analysis of the prevention of post-ivermectin Loa loa encephalopathy by administration of initial low dose].
Boussinesq, M; Gardon, J; Kamgno, J, 2000
)
0.8
" The primary objective was to estimate the dose-response relation in terms of cure rate and egg reduction rate."( Efficacy and safety of tribendimidine against Opisthorchis viverrini: two randomised, parallel-group, single-blind, dose-ranging, phase 2 trials.
Akkhavong, K; Duthaler, U; Hattendorf, J; Keiser, J; Odermatt, P; Sayasone, S; Senggnam, K; Vonghachack, Y; Xayavong, S, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Vitamin D3 receptorHomo sapiens (human)IC50 (µMol)30.50000.00000.43746.4300AID1277414; AID1277417
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Vitamin D3 receptorHomo sapiens (human)EC50 (µMol)75.74500.00000.14232.1400AID1277413; AID1277415
G-protein coupled bile acid receptor 1Homo sapiens (human)EC50 (µMol)102.00000.02372.52598.9000AID324923
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (34)

Processvia Protein(s)Taxonomy
negative regulation of DNA-templated transcriptionVitamin D3 receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
cell morphogenesisVitamin D3 receptorHomo sapiens (human)
skeletal system developmentVitamin D3 receptorHomo sapiens (human)
calcium ion transportVitamin D3 receptorHomo sapiens (human)
intracellular calcium ion homeostasisVitamin D3 receptorHomo sapiens (human)
lactationVitamin D3 receptorHomo sapiens (human)
negative regulation of cell population proliferationVitamin D3 receptorHomo sapiens (human)
positive regulation of gene expressionVitamin D3 receptorHomo sapiens (human)
negative regulation of keratinocyte proliferationVitamin D3 receptorHomo sapiens (human)
positive regulation of vitamin D 24-hydroxylase activityVitamin D3 receptorHomo sapiens (human)
positive regulation of bone mineralizationVitamin D3 receptorHomo sapiens (human)
phosphate ion transmembrane transportVitamin D3 receptorHomo sapiens (human)
bile acid signaling pathwayVitamin D3 receptorHomo sapiens (human)
mRNA transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
positive regulation of keratinocyte differentiationVitamin D3 receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
decidualizationVitamin D3 receptorHomo sapiens (human)
intestinal absorptionVitamin D3 receptorHomo sapiens (human)
apoptotic process involved in mammary gland involutionVitamin D3 receptorHomo sapiens (human)
positive regulation of apoptotic process involved in mammary gland involutionVitamin D3 receptorHomo sapiens (human)
regulation of calcidiol 1-monooxygenase activityVitamin D3 receptorHomo sapiens (human)
mammary gland branching involved in pregnancyVitamin D3 receptorHomo sapiens (human)
vitamin D receptor signaling pathwayVitamin D3 receptorHomo sapiens (human)
positive regulation of vitamin D receptor signaling pathwayVitamin D3 receptorHomo sapiens (human)
response to bile acidVitamin D3 receptorHomo sapiens (human)
multicellular organism developmentVitamin D3 receptorHomo sapiens (human)
cell differentiationVitamin D3 receptorHomo sapiens (human)
cell surface bile acid receptor signaling pathwayG-protein coupled bile acid receptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeG-protein coupled bile acid receptor 1Homo sapiens (human)
cellular response to bile acidG-protein coupled bile acid receptor 1Homo sapiens (human)
positive regulation of cholangiocyte proliferationG-protein coupled bile acid receptor 1Homo sapiens (human)
regulation of bicellular tight junction assemblyG-protein coupled bile acid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayG-protein coupled bile acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
DNA-binding transcription factor activityVitamin D3 receptorHomo sapiens (human)
vitamin D response element bindingVitamin D3 receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificVitamin D3 receptorHomo sapiens (human)
DNA bindingVitamin D3 receptorHomo sapiens (human)
nuclear receptor activityVitamin D3 receptorHomo sapiens (human)
protein bindingVitamin D3 receptorHomo sapiens (human)
zinc ion bindingVitamin D3 receptorHomo sapiens (human)
bile acid nuclear receptor activityVitamin D3 receptorHomo sapiens (human)
nuclear retinoid X receptor bindingVitamin D3 receptorHomo sapiens (human)
calcitriol bindingVitamin D3 receptorHomo sapiens (human)
lithocholic acid bindingVitamin D3 receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingVitamin D3 receptorHomo sapiens (human)
protein bindingG-protein coupled bile acid receptor 1Homo sapiens (human)
bile acid receptor activityG-protein coupled bile acid receptor 1Homo sapiens (human)
G protein-coupled bile acid receptor activityG-protein coupled bile acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusVitamin D3 receptorHomo sapiens (human)
nucleusVitamin D3 receptorHomo sapiens (human)
nucleoplasmVitamin D3 receptorHomo sapiens (human)
cytosolVitamin D3 receptorHomo sapiens (human)
RNA polymerase II transcription regulator complexVitamin D3 receptorHomo sapiens (human)
chromatinVitamin D3 receptorHomo sapiens (human)
receptor complexVitamin D3 receptorHomo sapiens (human)
cytoplasmG-protein coupled bile acid receptor 1Homo sapiens (human)
plasma membraneG-protein coupled bile acid receptor 1Homo sapiens (human)
receptor complexG-protein coupled bile acid receptor 1Homo sapiens (human)
plasma membraneG-protein coupled bile acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID1277417Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1233567Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms assessed as inhibition of parasite growth at 100 ug/ml by microtiter plate based assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID324923Agonist activity at human TGR5 expressed in CHO cells by luciferase assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
AID1233553Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms by microtiter plate based assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID324932Agonist activity at human FXR expressed in COS1 cells at 50 uM by luciferase assay relative to 6-enantiomeric chenodeoxy cholic acid2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
AID1277415Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1277420Cytotoxicity against HEK293T cells assessed as reduction in cell viability after 18 hrs by CellTiter-Glo luminescence assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1233559Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as reduction in parasite viability by parasite lactate dehydrogenase assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID1277416Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay relative to 1,25-dihydroxyvitamin D32016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1552618Transactivation of VDR in human Macrophage-like cell assessed as cell differentiation at 10'-5 M measured after 4 days by NBT dye-based assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Development of novel lithocholic acid derivatives as vitamin D receptor agonists.
AID1233568Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms assessed as inhibition of parasite growth at 20 ug/ml by microtiter plate based assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID1744112Agonist activity at VDR in human HL-60 cells assessed as induction of cell differentiation of promyelocytes to monocytes at 1 uM after 4 days by NBT reduction assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID1233565Cytotoxicity against human WI38 cells assessed as inhibition of cell growth at 100 ug/ml by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID1277421Agonist activity at VDR-LBD in human DU145 cells assessed as CYP24A1 expression at 7.5 uM after 18 hrs by qRT-PCR method relative to 1alpha,25-dihydroxyvitamin D32016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1552623Transactivation of human VDR expressed in COS-7 cells transfected with mouse osteopontin VDR incubated for 24 hrs by luciferase based reporter gene assay2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Development of novel lithocholic acid derivatives as vitamin D receptor agonists.
AID1277413Agonist activity at VDR-LBD (unknown origin) expressed in Escherichia coli assessed as SRC2-3 coactivator peptide recruitment after 30 mins by fluorescence polarization assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1277414Antagonist activity against VDR-LBD (unknown origin) expressed in Escherichia coli assessed as inhibition of VDR agonist LG190178-induced SRC2-3 coactivator peptide recruitment after 30 mins by fluorescence polarization assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1233552Cytotoxicity against human WI38 cells by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID1233569Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as inhibition of parasite viability at 100 ug/ml by parasite lactate dehydrogenase assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID1233570Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as inhibition of parasite viability at 20 ug/ml by parasite lactate dehydrogenase assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
AID1233566Cytotoxicity against human WI38 cells assessed as inhibition of cell growth at 20 ug/ml by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (511)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990206 (40.31)18.7374
1990's68 (13.31)18.2507
2000's61 (11.94)29.6817
2010's114 (22.31)24.3611
2020's62 (12.13)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 106.09

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index106.09 (24.57)
Research Supply Index6.36 (2.92)
Research Growth Index4.71 (4.65)
Search Engine Demand Index195.48 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (106.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (1.95%)5.53%
Reviews25 (4.42%)6.00%
Case Studies113 (20.00%)4.05%
Observational2 (0.35%)0.25%
Other414 (73.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]