Pharmacological properties of Crocus Sativus Linn (Saffron)

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Pharmacological properties of Crocus Sativus Linn (Saffron)

A. AntiAlzheimer activity:

The main carotenoid constituent, trans crocin, the digentibiosyl ester of Crocetin inhibited A beta fibrillogenesis formed by oxidation of the amyloid beta peptide fibrils in Alzheimers disease. The water methanol extract of Crocus sativus stigmas inhibited beta fibrillogenesis in a concentration and timedependent manner at lower concentrations than it’s another constituent dimethylcrocetin.

B. Antitussive activity:

The ethanolic extract of Crocus sativus and its constituent Safranal, was found to reduce the number of cough in guinea pigs when injected intra peritoneally where a nebulized solution of citric acid (20%) was used to induce cough.

C. Hypolipidemic activity:

Crocin one of the constituents of Saffron was shown to produce hypolipidemic effect in the dose range of 25 mg/kg to 100 mg/kg body weight in diet induced hyperlipidemic rats by inhibiting pancreatic lipase thereby leading to malabsorbtion of fat and cholesterol producing hypolipidemic effect.

D. Anticonvulsant activity:

Crocin, the coloring agent of Saffron, on peripheral administration to rats was found to induce a dose dependent decrease in the incidence of both minimal clonic seizures and generalized tonicclonic seizures following pentylene tetrazole administration. This effect of safranal was thought to be mediated at?least in part, through GABA benzodiazepine receptor complex. Another component of Saffron, crocin did not showed any effect in pentylenetetrazole induced convulsions in mice.

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E. Antipruritic and Emmolient effects:

Crocus sativus in a topical formulation at a concentration of 0.025%v/w was found to have beneficial effects, with atopic dermatitis, ichthyosis vulgaris, and other xerotic diseases of mild severity.

F. Antinociceptive and Antiinflammatory activity:

The aqueous and ethanolic extracts of saffron stigmas and petals were reported to posses anti nociceptive and anti inflammatory activity both of, acute and chronic as evidenced by effects in writhing test, xylene induced ear oedema in mice and formalininduced edema in the rat paw. This supports its traditional use as, an anti?edematogenic remedy.

G. Antioxidant activity:

The methanolic extract of Crocus sativus and its components such as safranal, crocin etc. were reported to possess radical scavenging activity, suggesting its use as a cosmetic to treat age related disorders, as a food supplement etc.
Crocin was found to possess greater antioxidant capacity than alphatocopherol in neuronally differentiated pheochromocytoma cells deprived of glucose, whose absence caused peroxidation of their cell membrane lipids and decreased intercellular superoxide dismutase activity. These effects were reversed by crocin, promising it as a unique and potent antioxidant that combats oxidative stress in neurons. Further it was also said to increase the levels of various enzymes such as the glutathione reductase, glutathione Stransferase and also maintains the functional levels of other antioxidants suggesting it as a potential antioxidant.


H. protection form genotoxicity:

The aqueous extract of saffron prevented the genotoxicity produced by certain drugs such as cisplatin, urethane, cyclophosphamide and mitomycin C in mice bone marrow micronucleus test. Further there was an increase of hepatic enzymes such as the glutathione stransferase in those animals pretreated with saffron. It was also reported to prevent the oxidative stress induced by these drugs through attenuation of the lipid peroxidation with a simultaneous increase of liver enzymes such as the superoxidedismutase, catalase and non enzymatic antioxidants suggesting that the chemopreventive effects of saffron are mediated through modulation of lipid peroxidation, antioxidants and detoxification systems.

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I. Prevention of acetaldehydeinduced inhibition of LongTerm potentiation in rat:

The alcoholic extract of Crocus sativus prevented ethanol and acetaldehyde induced inhibition of hippocampal long term potentiation in the dentate gyrus of anesthetized rats suggesting its use to prevent aversive effects induced by ethanol and acetaldehyde, its primary metabolite.

J. Cardioprotection:

Crocetin, the main active constituent of saffron was found to decrease the level of cardiac marker lactate dehydrogenase activity and also increase mitochondrion potential in a cardiac myocyte treated with noradrenaline, suggesting its cardioprotective action. Saffron was also showed to possess calcium antagonistic activity.
This antagonistic activity was through the blockade of extracellular Ca (2+) influx through receptor?operated Ca (2+) channels and potential dependent Ca (2+) channels. In another study, crocetin by virtue of its strong antioxidant activity prevented the cardiac hypertrophy induced by norepinephrine by increasing the levels of the antioxidant enzymes such as myocardial superoxide dismutase, catalase, glutathione peroxidase and also significantly improved the myocardial pathological histological changes induced by norepinephrine.


K. Antidiabetic activity:

Crocetin, the active constituent of saffron was found to possess anti diabetic activity in fructose fed rats as it alleviated free fatty acid induced insulin insensitivity and dysregulated mRNA expression of adiponectin, TNF alpha and leptin in primary cultured rat adipocytes suggesting the possibility of crocetin treatment as a preventive strategy of insulin resistance and related diseases.
Advanced glycation end products are known to cause the oxidative reaction that usually results in endothelial cell apoptosis and thus result in diabetic vascular complications. Crocetin by virtue of its good antioxidant capacity and calcium antagonistic activity or stabilization may be a good remedy for diabetic vascular complications.


L. In Respiratory disorders:

The relaxant effect of Crocus sativus on smooth muscle was evident as shown in guinea pig tracheal chain experiment. The relaxation produced with the aqueous ethanolic extract and safranal in comparison with saline as negative control, and theophylline, was comparable to or even higher than that relaxation produced with theophylline suggesting its use in the treatment of various respiratory disorders like asthma etc.

M. Effects on ocular blood flow and retinal function:

Crocin analogs isolated from Crocus sativus were found to increase blood flow by vasodilation to the retina and choroid, also facilitate retinal function recovery thereby preventing ischeamic retinopathy and age related macular degeneration that results in blindness.

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N. Anti Parkinson’s activity:

In a model of middle cerebral artery occlusion (model of acute cerebral ischemia) in rats, the decrease in the activity of enzymes such as superoxide dismutase, Na+K+ATPase, catalase etc: was countered by pre treating the animals with crocetin, which suggests the usage of Crocus sativus in focal ischeamia.
Parkinson’s disease, a neurodegenerative disorder is mainly characterized by the degeneration of neurons in the substantia nigra by reactive oxygen species or by injection of certain chemicals like 6 hydroxy dopamine leading to the death of neurons. In experimental rats, pre treated with crocetin, there was an increase in the antioxidant capacities of enzymes followed by protection from the deleterious effects of hydroxy dopamine thus presenting itself as a good treatment to combat this devastating disorder.


O. Effect on learning and memory behaviour:

Behavioural and electrophysiological studies have demonstrated that saffron extract affects learning and memory in experimental animals. Aqueous extract of saffron was reported to improve ethanol induced impairments of learning behavior in mice and ethanol induced inhibition of hippocampal long term potentiation, a form of activity dependent synaptic plasticity that may underlay learning and memory. These effects of saffron extract were attributed to crocin (crocetin digentiobiose ester), but not crocetin. Saffron extract or its active constituents, crocetin and crocin, may be useful for the treatment for neurodegenerative disorders accompanying memory impairment. Crocin was also showed to prevent the death of neurons provoked by internal and external apoptotic stimuli by suppressing the TNF α induced cell death.

P. Effects on blood pressure:

The aqueous and ethanolic extracts of Crocus sativus petals showed a decrease in blood pressure in a dose dependent manner in anaesthetised rats, in isolated rat vas deferens, guinea pig ileum etc. where responses were initiated by electrical stimulation. This decrease in blood pressure was proposed to be mediated postsynaptically.

Q. Antidepressant activity:

Crocus sativus petals and hydro alcoholic extracts of the stigmas have shown to possess anti depressant activity in a week double blind, randomized and placebo controlled trial and in animal based pre clinical studies. This antidepressant activity was similar to the activity of standard drugs imipramine and fluoxetine.

R. Effects on uterus:

In traditional medicine, the herb is used for promoting and regulating menstrual periods. It also soothes lumber pains, which accompany menstruation. Saffron is also beneficial in the treatment of other ailments concerning women such as leucorrhoea and hysteria. Pessaries of Saffron were used in painful conditions of the uterus. A polyherbal formulation containing Saffron when used at the doses of 1000 and 2000 mg/kg was reported to produce contractions of uterus in rats.

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S. Anticancer and antitumour activity:

Ethanolic extracts of Crocus sativus increased the life span of Swiss albino mice, which were intraperitoneally transplanted with sarcoma 180 cells, Ehrlich ascites carcinoma or Dalton’s lymphoma ascites tumours. Saffron in the presence of the T cell mitogen phytohemagglutinin stimulated a non specific proliferation of T lymphocytes invitro. This suggests that saffron’s antitumour activity might be immunologically mediated.
The use of Crocetin in lung cancer was found to decrease the lipid peroxidation, glutathione metabolizing enzymes and also revert the histopathological changes relevant to tumour incidence proving it as a potential antitumour agent.
Crocetin was found to exert a small inhibitory effect on the development of skin tumours induced in nude mice by the application of dimethyl benzanthracene, dimethyl benz [α] anthracin and croton oil. In rats, crocins revealed a great protective effect against hepatocarcinogenic compounds such as aflatoxin B1 and dimethylnitrosamine, partially suppressing chronic hepatic damage. Crocetin has been found to be a potent inhibitor of skin tumour promotion induced by O tetradecanoylphorbol acetate in mice.
Topical administration of saffron extracts inhibited the initiation/promotion of dimethylbenz[α] anthracene induced skin tumours in mice, delaying the onset of papiloma formation and reducing the mean number of papillomas per mouse.
This antitumour effect of saffron was attributed to the increase in the levels of ß carotene and vitamin A in the serum of the experimental animals receiving saffron. The study demonstrated.
that crocetin had no cytotoxic effect on colony formation of different tumor cells, but had a dose?dependent inhibitory effect on DNA, RNA, and protein synthesis in these human malignant cells. Further a novel glucoconjugate isolated from corms and callus of Saffron was showed to possess cytotoxic activity against different tumor cells derived from fibrosarcoma, cervical epithelioid carcinoma, and breast carcinoma.
Crocin and diglucosylcrocetin inhibited early tumor antigen expression of adenovirus infected cells crocetin esters were less potent than crocin itself in this concern.


T. Cellular and molecular effects:

It has been demonstrated that crocin posseses antiapoptotic effects on non cancerous cells. Crocin suppresses cell death induced by tumour necrosis factor alpha (TNF α), cysteine protease mRNAs and simultaneously restores the cytokine induced reduction of TNF α and mRNA expression.

U. Crocetin and haemorrahagic shock:

Crocetin, a Saffron derived carotenoid, was shown to improve post shock recovery of cellular adenosine triphosphate and to increase overall survival in an experimental model of hemorrhagic shock. In this model, crocetin caused the suppression and subsequent expression of messenger ribonucleic acid for tumor necrosis factor,interleukin and inducible nitric oxide synthase.

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