DL-Borneol is a racemic mixture of D-Borneol and L-Borneol. DL-Borneol is widely used for the treatment of cardiovascular and cerebrovascular diseases in China.

DL-Borneol increases intracellular accumulation of Rho123, and enhances P-gp substrates across the BBB in vitro, and also depresses mdr1a mRNA and P-gp expression. Furthermore, DL-Borneol could activate NF-κB and inhibition of NF-κB with MG132 and SN50 obscures the P-gp decreases induced by DL-Borneol. 10 μg/mL and 20 μg/mL DL-Borneol significantly increase phosphorylation of IκB expression at 30 min after treatment transiently. DL-Borneol treatment decreases P-gp expression in BMECs^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

DL-Borneol significantly suppresses the process of epileptogenesis in PTZ-kindled mice. The biochemical alterations induced by PTZ kindling are ameliorated in DL-Borneol-treated animals which is indicated by decreased LPO and increased SOD, GSH, CAT levels. The distinct neuronal damage observed in the kindled group is counteracted by DL-Borneol. Furthermore, it decreases the levels of GFAP which is manifested by reduced immunostaining^[2]. The pathological damages of ischemia-reperfusion have a significant impact on the pharmacokinetic traits of DL-Borneol and that there are some components in Xingnaojing inhibiting the absorption of DL-Borneol^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

154.25

C₁₀H₁₈O

507-70-0

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL (648.30 mM)

H₂O : < 0.1 mg/mL (insoluble)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (16.21 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (16.21 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (16.21 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (16.21 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (16.21 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (16.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Fan X, et al. Borneol Depresses P-Glycoprotein Function by a NF-κB Signaling Mediated Mechanism in a Blood Brain Barrier in Vitro Model. Int J Mol Sci. 2015 Nov 18;16(11):27576-88.

  [2]. Tambe R, et al. Antiepileptogenic effects of borneol in pentylenetetrazole-induced kindling in mice. Naunyn Schmiedebergs Arch Pharmacol. 2016 May;389(5):467-75.

  [3]. Xu P, et al. Comparative pharmacokinetics of borneol in cerebral ischemia-reperfusion and sham-operated rats. J Zhejiang Univ Sci B. 2014 Jan;15(1):84-91.

Rho123 efflux assay is used to measure the activity of P-gp in BMECs according to previous methods. BMECs grown to confluency in 24-well plates are treated with 5 μg/mL, 10 μg/mL and 20 μg/mL DL-Borneol, DMSO, CsA for 2 h, or with 10 μg/mL and 20 μg/mL DL-Borneol for different times (30 min, 1 h, 2 h, and 4 h). Then BMECs are exposed to 5 μmol/L Rho123 in DMEM for 90 min. After incubation with Rho123, BMECs are washed with ice-cold PBS and solubilized in 1% NaOH. Fluorescence of Rho123 is measured with emission wavelength at 535 nm and excitation wavelength at 485 nm using a fluorescence spectrophotometer^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Rats: The pharmacokinetic study is performed 24 h after reperfusion in the model groups, i.e., 26 h after operation in the SO group. The XNJ subgroup rats are orally administered with XNJ decoction dissolved in 0.7% CMC-Na aqueous solution (10.00 ml/kg body weight (BW)). The pure DL-Borneol subgroup also receives gavages of DL-Borneol suspension (10.00 ml/kg BW). DL-Borneol and XNJ suspensions are administrated respectively at a dosage of 162.0 mg/kg of DL-Borneol. Then 0.5 ml plasma samples are collected into heparinized tubes by the puncture of the retro-orbital sinus at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, and 360 min separately following oral administration. After centrifugation at 6000 r/min for 10 min, plasma samples are stored at −20 °C and analyzed within one week^[3].

Mice: Repeated administration of a subconvulsive dose of PTZ (35 mg/kg, i.p.) on every alternate day for 4 weeks produces kindling in mice. DL-Borneol (5, 10, and 25 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.) are given as a pretreatment prior to each PTZ injection during the progression of kindling. Oxidative stress parameters such as superoxide dismutase (SOD), reduced glutathione (GSH), catalase (CAT), and lipid peroxidation (LPO) are assessed at the end of the study. Neuronal damage is assessed by hematoxylin and eosin staining technique. GFAP is also evaluated in the hippocampus region of the brain by using immunohistochemistry^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Fan X, et al. Borneol Depresses P-Glycoprotein Function by a NF-κB Signaling Mediated Mechanism in a Blood Brain Barrier in Vitro Model. Int J Mol Sci. 2015 Nov 18;16(11):27576-88.

  [2]. Tambe R, et al. Antiepileptogenic effects of borneol in pentylenetetrazole-induced kindling in mice. Naunyn Schmiedebergs Arch Pharmacol. 2016 May;389(5):467-75.

  [3]. Xu P, et al. Comparative pharmacokinetics of borneol in cerebral ischemia-reperfusion and sham-operated rats. J Zhejiang Univ Sci B. 2014 Jan;15(1):84-91.