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Crocus sativus
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Evidence of Activity
Pharmacokinetics (ADME)
A novel, ultra-fast liquid chromatography—tandem mass spectrometry (UFLC-MS/MS) method quantified the active metabolites in rat plasma following oral administration of 40 mg/kg of saffron (Crocus sativus) extract. Girme 2021
Intestinal absorption of orally administered crocin was found to be marginal compared to that of its aglycone, crocetin, in rats, with intestinal microbiota playing a major role in the conversion and hence pharmacology of the parent glycosidic compound. Shakya 2020
A review identified five attributes of safranal that it shares with common drugs, such as optimum lipophilicity, high permeability, low blood-to-plasma ratio, and high plasma protein binding, which are, however, compromised by its low oral bioavailability. Dogra 2020
Plasma crocetin levels reached their maximum 60-90 min after oral administration of saffron (Crocus sativus) extract tablets to human subjects (N = 13); in in-vitro digestion experiments, crocin isomers showed 40% bioaccessibility, whereas safranal levels increased 2-fold following digestion. Almodóvar 2020
A systematic review of evidence relating to potential biomarkers of herb and spice intake, including that of saffron, found peer-reviewed published data on most. Vázquez-Fresno 2019
A novel metabolomics strategy used to determine the metabolic fingerprint following intraperitoneal administration of trans-crocin 4 in mice identified annotated metabolites which may be associated with neuroprotection and which are closely related to Alzheimer's disease. Karkoula 2019
A study determined the binding affinities of safranal and crocin to human serum albumin, revealing that it may solubilize and transport both compounds to target tissues. Salem 2019
Crocetin monoglucuronide, a crocin metabolite found in the blood and brain of rats following oral administration of crocin-1, showed neuroprotective activity against amyloid ß toxicity in vitro. Zhu 2019
A novel sustained release Crocus sativus extract improved in vitro dissolution profile, significantly enhanced plasma exposure, and doubled crocetin/crocin ratio in plasma compared, as well as reversed memory deficits and amyloid ß accumulation in mice with no oral toxicity up to 2000 mg/kg. Bharate 2018
After intravenous and oral administration of a lyophilized aqueous extract of saffron (27.8 ± 0.1% crocin), crocetin was found to be distributed largely to the liver and kidneys in mice. Oral bioavailability and stability of the extract were also determined. Christodoulou 2018
Binding of safranal to human serum albumin was elucidated using fluorescence spectra and molecular docking analyses. Ali 2018
The review addresses the pharmacokinetics of saffron constituents, emphasizing low oral bioavailability of crocin due to intestinal conversion to crocetin, and distribution of the latter to various tissues, including the central nervous system. Hosseini 2017
Crocin and crocetin were shown to bind to the sub-domain IIA of human serum albumin (HSA), accompanied by hydrogen bonding at Tyr138, while differently affecting HSA folding, as shown by spectroscopic methods. Jafarisani 2017
Picrocrocin (Pc) and crocetin sugar esters were found to be highly bioaccessible (60-75%), but transported across intestinal Caco-2 cells, following in vitro digestion procedure, only at 0.2-0.5% (10-fold lower than crocetin). Pc also suppressed human adenocarcinoma and hepatocarcinoma cells. Kyriakoudi 2015
Conversion of glycosylated crocins from saffron extract to trans-crocetin is reported to occur mainly in intestinal cells, with trans-crocetin, but not crocin-1, penetrating the intestinal barrier, and permeating the blood-brain barrier. Lautenschläger 2015
Chemical changes of crocin (crocetin esters) during gastrointestinal digestion were investigated in vitro. Kyriakoudi 2013
An HPLC method for the determination of crocetin in human serum was developed. Mohammadpour 2013
Crocetin was determined in the plasma of healthy human volunteers, after consumption of saffron tea (200mg of saffron in 80°C water). Concentration was high after 2h (1.24-3.67μM) and still in the quantitation range after 24h (0.10-0.24), with both cis- and trans-isomers detected. Chryssanthi 2011
The pharmacokinetics of crocetin (7.5-22.5 mg) were investigated in healthy adult human volunteers (5 men and 5 women). Crocetin was found to be rapidly absorbed and detected within an hour of administration, reaching maximum concentrations (up to 279.7 ng/ml) in 4.0-4.8 h. Umigai 2011
Investigation of the pharmacokinetic properties of crocin following oral administration in rats indicate that orally administered crocin is not absorbed either after a single dose or repeated doses and crocin is excreted largely through the intestinal tract following oral administration. Xi 2007
A rapid, precise, reliable, sensitive and specific HPLC method was developed for the determination of crocin-1 with lowest detectable concentration of 0.42 mg x L(-1) in rabbit plasma, and the pharmacokinetics in rabbit was studied. [Article in Chinese] Tang 2004
An HPLC method was developed, for the determination of crocetin in rat plasma and the pharmacokinetics in rats was studied which revealed that Crocetin was shown to be quickly absorbed in rats. [Article in Chinese] Liu 2002
History of Record
April 2019
November 2021