Peringatan Keamanan

No toxicokinetic data available.

Isoflavone

DB12007

small molecule experimental

Deskripsi

Isoflavone is a soy phytoestrogen and a biologically active component of several agriculturally important legumes such as soy, peanut, green peas, chick peas and alfalfa A33103. Soybean is an exceptionally rich source of dietary isoflavones, where the average isoflavone content is 1-2 mg/gram A33103. The main soy isoflavones are mostly present in glycosylated forms and include DB01645, DB13182, and glycitein, which accounts for approximately 50%, 40%, and 10%, respectively, of the total soybean isoflavone content A33098. The clinical benefits of soy proteins have been studied and demonstrated for many years, with some evidence of soy products associated with a reduced incidences of coronary heart disease, atherosclerosis, type II diabetes mellitus, and breast and prostate cancer A33099. While existing data are consistent or inadequate in supporting most of the suggested health benefits of consuming soy proteins and isoflavones A33099, the trials investigating isoflavone as a potential treatment for atrophy, menopause, and postmenopausal symptoms are ongoing. Isoflavone is found as one of constituents in oral over-the-counter dietary supplements indicated for improved bone mass density and body fat regulation.

Struktur Molekul 2D

Berat 222.243
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of isoflavones is between 4 and 8 h [A33098]. Daidzein has a longer intestinal half-life than genistein due to more rapid degradation of genistein [A33100]. Individual half-life of daidzein and genistein in a human pharmacokinetic study were 7.75 h and 7.77 h, respectively [A33103].
Volume Distribusi Isoflavones are readily distributed to all tissues, and they are known to cross the placental barrier and blood brain barrier [A33103]. They are also distributed to the extra-vascular compartments. In a human study, the volume of distribution of daidzein and genistein were 336.25 L and 258.76 L, respectively [A33103].
Klirens (Clearance) In a human study, the clearance rate for daidzein and genistein were 30.09 L/h and 21.85 L/h, respectively [A33103].

Absorpsi

Following oral ingestion, serum isoflavone concentrations increase in a dose-dependent manner A33098. Isoflavones are metabolized by gut microflora, where they need to undergo deglycosylation in order to be absorbed in the intestine A33103. After oral ingestion, glycosylated isoflavones are rapidly deglycosylated, absorbed and metabolized in intestinal enterocytes and liver, entering the systemic circulation predominantly as conjugates with limited bioavailability A33103. In humans, the mean time to reach peak plasma concentrations (Tmax) for conjugated and unconjugated genistein and daidzein are approximately 5-6 and 6-8 hours, respectively A33103.

Metabolisme

The conversion of glycosylated isoflavones to de glycosylated isoflavones begins in the oral cavity, wherein oral microflora and oral epithelium exhibit ?-glucosidase activity A33103. Further conversion is mediated by intestinal lactase phlorizin hydrolase on the luminal side of the intestinal brush border to form aglycones that diffuses into the enterocytes A33103. The glycosylated isoflavones may also be converted to aglycone in the large intestines by the resident intestinal microflora. Isoflavone aglycones that enter the intestinal cell via passive diffusion are rapidly conjugated into sulfate or glucuronide conjugates A33103. Under the anaerobic, reductive conditions of the colon, genistein undergoes reduction to form dihydrogenistein and further to 5-hydroxyequol, while daidzein is reduced to dihydrodaidzein and equol A33103. Microbial cleavage of the Ring-C of isoflavones produces deoxybenzoin metabolites (DOBs), which retains similar biological activity as unchanged isoflavones and are passively absorbed A33103. There is a large interindividual variation in isoflavone metabolism, leading to circulating concentrations of isoflavone metabolites and parent isoflavones varying up to hundreds-fold A33098. About 25% of the non-Asian and 50% of the Asian population host the intestinal bacteria that convert the daidzein into the isoflavonoid equol, which is a beneficial isoflavonoid A33098.

Rute Eliminasi

Renal excretion is the predominant route of elimination for dietary isoflavones, where approximately 10-60% of total administered dose is excreted in urine A33103. Glucuronide conjugates account for the majority (70-90%) of the isoflavone content in urine, followed by sulphate conjugates (10-25%) and aglycone forms (1-10%) A33103. Fecal excretion is minimal, which accounts for 1-4% of the dietary isoflavone ingested A33103.

Interaksi Obat

727 Data
Cyclosporine Cyclosporine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Isoflavone which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Isoflavone which could result in a higher serum level.

Target Protein

Peroxisome proliferator-activated receptor alpha PPARA
Peroxisome proliferator-activated receptor gamma PPARG

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24898224
    Messina M: Soy foods, isoflavones, and the health of postmenopausal women. Am J Clin Nutr. 2014 Jul;100 Suppl 1:423S-30S. doi: 10.3945/ajcn.113.071464. Epub 2014 Jun 4.
  • PMID: 18492864
    Xiao CW: Health effects of soy protein and isoflavones in humans. J Nutr. 2008 Jun;138(6):1244S-9S. doi: 10.1093/jn/138.6.1244S.
  • PMID: 22228950
    Kalaiselvan V, Kalaivani M, Vijayakumar A, Sureshkumar K, Venkateskumar K: Current knowledge and future direction of research on soy isoflavones as a therapeutic agents. Pharmacogn Rev. 2010 Jul;4(8):111-7. doi: 10.4103/0973-7847.70900.
  • PMID: -
    Chandrasekharan S: Pharmacokinetics of Dietary Isoflavones Journal of Steroids & Hormonal Science.

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