The anti-inflammatory properties of saponin (60 and 120 mg/kg, sc) can be used to treat paw edema caused by carrageenan [2].

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Anti-inflammatory activity (carrageenan-induced paw edema in rats): Oral administration of Santonin at 30, 60, and 120 mg/kg significantly and dose-dependently reduced paw edema. Maximal inhibition (73%) was observed at 2 hours at 120 mg/kg (paw volume increase: 0.19±0.02 mL vs control 0.70±0.04 mL). At 3 hours, inhibition was 61% (0.38±0.03 mL vs 0.99±0.05 mL). At 4 hours, inhibition was 57% (0.46±0.03 mL vs 1.07±0.04 mL). Lower dose (15 mg/kg) showed no significant effect. Diclofenac sodium (75 mg/kg) produced 85% inhibition at 2 hours. [2]
- Anti-granuloma activity (cotton pellet granuloma in rats): Santonin at 60 mg/kg/day for 5 days caused 42% inhibition of granuloma formation (increased pellet weight: 28.46±3.27 mg vs control 49.72±4.75 mg). At 120 mg/kg/day, inhibition was 55% (22.37±4.45 mg). Doses of 15 and 30 mg/kg showed no significant effect. Diclofenac sodium (30 mg/kg) caused 59% inhibition (20.35±1.83 mg). [2]
- Antipyretic activity in normal mice: Oral Santonin (15-120 mg/kg) caused dose-dependent reduction in rectal temperature. At 30 mg/kg: from 36.51±0.38°C pre-dose to 33.21±0.20°C at 60 min post-dose. At 60 mg/kg: from 36.58±0.29°C to 33.18±0.17°C at 60 min. At 120 mg/kg: from 36.45±0.34°C to 32.45±0.21°C at 60 min. Effect lasted up to 90 min. [2]
- Antipyretic activity in yeast-induced hyperthermic mice: Subcutaneous injection of 20% brewer’s yeast (2 mL/100 g) elevated rectal temperature to ~38°C. Oral Santonin (15-120 mg/kg) significantly reduced temperature. At 120 mg/kg: from 38.04±0.09°C pre-dose to 32.88±0.40°C at 60 min. Sodium salicylate (300 mg/kg) produced smaller reduction (to 36.30±0.17°C). The antipyretic effect was independent of route of administration. [2]
- Analgesic activity (hot plate test in mice): Santonin at 60 mg/kg increased reaction time from 11.69±0.64 sec pre-dose to 15.32±1.34 sec at 60 min (P<0.05). At 120 mg/kg: from 12.06±0.95 sec to 23.92±2.83 sec at 30 min (P<0.01) and 16.65±1.13 sec at 60 min (P<0.05). Effect declined after 90 min. Morphine (10 mg/kg i.p.) produced similar increase (to 18.81±1.20 sec at 60 min). [2]

Animal/Disease Models: Carrageenan-induced paw edema in rats [2]
Doses: 15, 30, 60 and 120 mg/kg
Route of Administration: subcutaneous injection, single dose
Experimental Results: Inhibition of cotton ball granuloma formation, 120 mg /kg, the inhibition rate was 55%.

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Carrageenan-induced paw edema (rats): Male Wistar rats (180-200 g) were treated orally with Santonin (15, 30, 60, 120 mg/kg) dissolved in distilled water, 1 hour before subplantar injection of carrageenan. Paw volume was measured at 1, 2, 3, and 4 hours after carrageenan. Diclofenac sodium (75 mg/kg) was used as reference. [2]
- Cotton pellet granuloma (rats): Sterilized cotton pellets (30 mg) were implanted in the groin of rats. Santonin (15, 30, 60, 120 mg/kg/day) or distilled water (control) was given orally for 5 consecutive days. Diclofenac sodium (30 mg/kg) was reference. On day 6, pellets were removed, dried overnight at 60°C, and weighed. [2]
- Antipyretic test (mice): Swiss albino mice (25-30 g) received subcutaneous injection of 20% brewer’s yeast suspension (2 mL/100 g) to induce hyperpyrexia. After 24 hours, rectal temperature was measured. Santonin (15-120 mg/kg in water) was given orally, and temperatures recorded at 30, 60, and 90 min post-dose. Sodium salicylate (300 mg/kg) was reference. For normal mice, the same procedure was followed without yeast. [2]
- Analgesic test (hot plate): Mice were placed on a hot plate at 55±0.5°C. Reaction time (licking feet or jumping) was measured before and at 30, 60, 90, 120 min after oral Santonin (15-120 mg/kg) or morphine (10 mg/kg i.p.). [2]

Known toxic dose: 60 mg for children and 200 mg for adults. [1]
- Side effect of excessive intake: xanthopsia (yellow vision), violet appearance of dark surfaces; in serious cases, blindness can result. [1]
- Not only from overdosing but also from prolonged administration due to slow elimination (cumulative poison). [1]
- LD50 for mammals is in the range of 900 mg/kg. [1]

[1]. Quantification of santonin in eight species of Artemisia from Kazakhstan by means of HPLC-UV: Method development and validation. PLoS One. 2017 Mar 16;12(3):e0173714.

[2]. Studies on the antiinflammatory, antipyretic and analgesic activities of santonin. Jpn J Pharmacol. 1994, 64, 3.

α-Santonin is a santonin with the structure 3a,5,5a,9b-tetrahydronaphtho[1,2-b]furan-2,8(3H,4H)-dione, substituted with methyl groups at positions 3, 5a, and 9. It is a plant metabolite with antifungal activity and is also a santonin. Santonins have been reported to exist in Artemisia diffusa, Artemisia herba-alba, and other organisms with relevant data. An insecticide was isolated from the dried, unopened inflorescences of Artemisia maritima and other Artemisia species mainly distributed in Russia, Turkestan, and the Southern Ural region of China. (From Merck, 11th edition) See also: ... See more...

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Santonin is a sesquiterpene lactone, the major constituent of Artemisia cina, formerly used as a powerful anthelmintic drug. It is no longer used in humans due to its toxicity. Kazakhstan is considering its use for veterinary purposes. [1]
- The α-santonin structure was confirmed by NMR spectroscopy (¹H, ¹³C, DEPT, COSY, HMBC, HSQC) and X-ray crystallography (orthorhombic, space group P2₁2₁2, unit cell dimensions a=6.9072(2) Å, b=10.5202(3) Å, c=34.5294(10) Å). [1]
- HPLC-UV method for quantification: retention time ~5.7 minutes on C18 column with water/acetonitrile gradient, detection at 236 nm. Santonin content in A. cina leaves was 1.96 g/100 g dry leaf. Other species: A. frigida 0.22, A. sublesingiana 0.16, A. scoparia 0.04 g/100 g; A. gmelinii, A. schrenkiana, A. terrae-albae, A. absinthium had no detectable santonin. [1]
- The anti-inflammatory, antipyretic and analgesic activities of santonin were demonstrated in this study (details above). The mechanism may involve inhibition of kinin and prostaglandin synthesis, as well as central depressive action. [2]

C15H18O3

246.3

246.126

481-06-1

221071

White to off-white solid powder

1.18g/cm3

423.4ºC at 760mmHg

172-173 °C(lit.)

189.7ºC

2.24E-07mmHg at 25°C

-172.5 ° (C=2, CHCl3)

2.419

0

3

0

18

500

4

C[C@H]1[C@@H]2CC[C@]3(C=CC(=O)C(=C3[C@H]2OC1=O)C)C

XJHDMGJURBVLLE-BOCCBSBMSA-N

InChI=1S/C15H18O3/c1-8-10-4-6-15(3)7-5-11(16)9(2)12(15)13(10)18-14(8)17/h5,7-8,10,13H,4,6H2,1-3H3/t8-,10-,13-,15-/m0/s1

(3S,3aS,5aS,9bS)-3,5a,9-trimethyl-3a,5,5a,9b-tetrahydronaphtho[1,2-b]furan-2,8(3H,4H)-dione

Santonin NSC-4900 NSC4900NSC 4900alpha-Santonin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~62.5 mg/mL (~253.76 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (8.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (8.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (8.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)