Metabolism / Metabolites
Incubation of alpha-cedrol and caryophyllene oxide with Neurospora crassa /identified/ 12beta-hydroxy cedrol, 10alpha-hydroxycedrol, and 3beta-hydroxy cedrol, and 12beta-hydroxy caryophyllene oxide as major metabolites, respectively. The antibacterial and radical scavenging activities of the metabolites were evaluated in vitro using broth microdilution and bioauthographic techniques. However, no significant antibacterial and antioxidant activities were observed ...
Microbial transformation of (+)-cedrol was investigated by using Staphylococcus epidermidis and found that stereospecific hydroxylation of (+)-cedrol occurred at the C-3 position to form (+)-(3S)-3-hydroxycedrol.

Toxicity Summary
IDENTIFICATION AND USE: Cedrol forms colorless crystals. It is found in the wood of cypresses and cedars such as Cedrus atlantica, Cupressus sempervirens, and Juniperus virginiana. It is used in fragnances and as a flavor ingredient in foods and traditional medicine. HUMAN EXPOSURE AND TOXICITY: In an exposure study, odorized and blank air was presented to 26 healthy adult volunteers. A constant concentration of cedrol was presented for 10 minutes with 8 minute blank air intervals. Cedrol caused a relaxant effect with decreased heart rate, respiratory rate, systolic and diastolic blood pressure and increased baroreflex activity. Parasympathetic activity was increased and sympathetic activity was decreased. In another exposure study, a maximization test was carried out with 8% cedrol in petrolatum on 25 male volunteers. Sensitization reactions were observed in 2/25 volunteers. In a pre-test for a human maximization study, no irritation was observed to 8% cedrol, when applied for 48 hr under occlusion on five volunteers. In another study, Pyrolae herba (PHVO) was evaluated for antiproliferative activity against human chondrosarcoma cells. A total of 12 components in PHVO were identified. The major compounds included cedrol (17.08%). PHVO demonstrated potent antitumor activity against SW1353 cells, suggesting its potential use as a therapeutic agent in the treatment of chondrosarcoma. In another study, the aim was to investigate the inhibitory effects of cedrol on the activities of eight major human cytochrome P-450 (CYP) enzymes to assess potential cedrol drug interactions. Cedrol, was found to be a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) values of 0.9 uM, comparable with that of a selective CYP2B6 inhibitor, thioTEPA (Ki, 2.9 uM). Cedrol also markedly inhibited CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 uM, whereas beta-cedrene moderately blocked CYP3A4. Cedrol at 100 microM negligibly inhibited CYP1A2, CYP2A6, and CYP2D6 activities. Cedrol weakly inhibited CYP2C8, CYP2C9, and CYP2C19 activities, but beta-cedrene did not. These in vitro results indicate that cedrol should be examined for potential pharmacokinetic drug interactions in vivo due to their potent inhibition of CYP2B6 and CYP3A4. ANIMAL STUDIES: A 28-day oral toxicity study was conducted to evaluate toxicity of cedrol in rats. Sixty rats were randomly divided into five groups (10 males or 10 females per group) and a control group of 10 animals. Approximately 0.169% w/v of cedrol was administered at dose of 8.4 mg/kg/day in 20 rats (10/sex) seven days per week via gavage to all the animals for 30 days. Crooked incisors and a swollen mouth were observed in one male rat on day 28. Decrease in absolute brain weight and brain-and ovary-to body weight was observed in female rats. However, these findings were not consistent between the sexes and absence of correlative clinical changes made the consideration of these non-adverse findings of limited toxicological significance. Open epicutaneous tests were carried out in outbred male and female guinea pigs with 8% cedrol, no sensitization reactions were observed. In another study on the sedative effects of cedrol, rats and mice were exposed at 1.0 liter/ minute for 30 minutes. Cumulative spontaneous motor activity was found to be significantly decreased in the cedrol exposed group.

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Non-Human Toxicity Values
LD50 Rabbit Dermal > 5g/kg

[1]. Inhibitory effects of cedrol, β-cedrene, and thujopsene on cytochrome P450 enzyme activities in human liver microsomes. J Toxicol Environ Health A. 2014;77(22-24):1522-32.

[2]. Cedrol Enhances Extracellular Matrix Production in Dermal Fibroblasts in a MAPK-Dependent Manner. Ann Dermatol. 2012 Feb;24(1):16-21.

Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol.
Cedrol has been reported in Mappianthus iodoides, Basella alba, and other organisms with data available.

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Therapeutic Uses
Cedrol, beta-cedrene, and thujopsene are bioactive sesquiterpenes found in cedar essential oil and exert antiseptic, anti-inflammatory, antispasmodic, tonic, astringent, diuretic, sedative, insecticidal, and antifungal activities. These compounds are used globally in traditional medicine and cosmetics. /Traditional use/

C15H26O

222.372

222.198

77-53-2

65575

White to off-white solid powder

1.0±0.1 g/cm3

277.2±8.0 °C at 760 mmHg

55-59 °C(lit.)

115.5±10.9 °C

0.0±1.3 mmHg at 25°C

1.519

4.77

1

1

0

16

321

5

C[C@@H]1CC[C@@H]2[C@]13CC[C@@]([C@H](C3)C2(C)C)(C)O

SVURIXNDRWRAFU-OGMFBOKVSA-N

InChI=1S/C15H26O/c1-10-5-6-11-13(2,3)12-9-15(10,11)8-7-14(12,4)16/h10-12,16H,5-9H2,1-4H3/t10-,11+,12-,14-,15+/m1/s1

(3R-(3alpha,3Abeta,6alpha,7beta,8aalpha))-octahydro-3,6,8,8-tetramethyl-1H-3a,7-methanoazulen-6-ol

Eudesmol Cedrol AI3-02178

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

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

DMSO : ~110 mg/mL (~494.67 mM)
H2O : < 0.1 mg/mL

Solubility in Formulation 1: 2.75 mg/mL (12.37 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 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: ≥ 2.75 mg/mL (12.37 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 27.5 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: ≥ 2.75 mg/mL (12.37 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 27.5 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.)