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Product name: (±)-Borneol
Synonym name: Bingpian
Catalogue No.: BP0049
Cas No.: 507-70-0
Formula: C10H18O
Mol Weight: 154.253
Botanical Source: Defensive secretion of the sawflies Pristiphora erichsonii and Pristiphora wesmaeli
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
HPLC of (±)-Borneol
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
20.2300
2.9500
2.9500
High
No
No
No
No
No
No
Borneol ((±)-Borneol), CAS number 507-70-0, is a typical bicyclic monoterpene natural product with a chemical structure consisting of 1,7,7-trimethylbicyclo[2.2.1]heptane with two hydroxyl-substituted positions. As a medicinal ingredient widely used in traditional Chinese medicine and Japanese Kampo medicine, borneol has attracted attention for its remarkable analgesic, anesthetic, and neuroprotective effects. In recent years, with advances in molecular pharmacology and medicinal chemistry technologies, the bioactive mechanisms and molecular targets of borneol have become increasingly elucidated, especially in its potential roles in central nervous system regulation, suppression of inflammatory responses, and metabolic diseases, providing a solid scientific foundation for its clinical application and new drug development.
This paper will systematically review the chemical structure and physicochemical properties of borneol, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics, with a focus on exploring its molecular targeting roles in neuroprotection, anti-inflammation, and metabolic diseases, and looking ahead to its future clinical application potential.
Borneol has the chemical name (±)-Borneol, molecular formula C10H18O, molecular weight 154.25, and belongs to the borneol alkane monoterpene compound. Its structural feature is a double-ring [2.2.1]heptane framework, with two rings connected by bridged carbons, two carbon positions connected to hydroxyl groups, and carbons 1, 7, and 7 each substituted with methyl substitution, forming a stable trimethyl structure. Borneol has two enantiomers, namely (+) and (-) borneol. Its natural source is mostly the (+) type, while synthetic borneol is usually racemic form.
In terms of physicochemical properties, borneol has a LogP value of about 2.95, indicating moderate lipid solubility and easy penetration of lipid membranes, especially the blood-brain barrier (BBB). Its TPSA (topological pole surface area) is 20.23 Ų, and it has 1 hydrogen bond acceptor, all meeting good central nervous system active molecular characteristics. Borneol is a colorless or pale yellow crystalline solid, volatile and has a distinctive cool aroma, with a melting point of about 208-210°C. Its solubility in water is relatively low, but it is easily soluble in organic solvents such as ethanol and ether. Its high blood-brain barrier permeability gives it unique advantages in treating neurological diseases.
Borneol is mainly found in the essential oils of various plants, especially abundant in camphor trees (Cinnamomum camphora) and other Lauraceae plants. In traditional Chinese medicine, borneol is mostly derived from distilled extracts of natural camphor trees, and can also be obtained through chemical synthesis. The content of borneol in plant volatile oils is greatly affected by growth environment, harvest time, and extraction process.
Common extraction methods include steam distillation and organic solvent extraction. Steam distillation is widely used due to its ease of operation and minimal damage to heat-sensitive components. In modern technology, supercritical CO2 extraction has gradually become the preferred method for extracting borneol due to its high efficiency, environmental friendliness, and strong selectivity. After extraction, purification and quantitative analysis are performed using chromatographic separation techniques (such as gas chromatography GC and liquid chromatography LC) to ensure the purity of borneol and the stability of active components.
As a versatile natural product, borneol exhibits rich pharmacological activity, covering nervous system regulation, anti-inflammation, anti-ischemia, antibacterial, and metabolic regulation.
Borneol and its enantiomer (-)—borneol exhibits highly effective positive modulatory effects on GABA_A receptors, especially regulating the human recombinant α1-β2-γ2L GABA_A receptor subtype, showing significant sedative, anxiolytic, and anticonvulsant activities. Its mechanism involves enhancing GABA-mediated chloride ion influx, promoting neuronal inhibitory signaling, thereby exerting central analgesic and anesthetic effects.
Additionally, borneol specifically inhibits nicotinin-type acetylcholine receptor (nAChR)-mediated signal transduction in a non-competitive manner, regulating neural excitability and synaptic transmission, and demonstrates potential neuroprotective effects. Studies on related in vitro blood-brain barrier models show that borneol can inhibit P-glycoprotein function through the NF-κB signaling pathway, improving drug crossing of the blood-brain barrier and suggesting its value in nervous system drug delivery.
Borneol inhibits the IκBα-NF-κB signaling pathway, blocking the translocation of NF-κB from the cytoplasm to the nucleus, significantly reducing the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and exerting good anti-inflammatory effects. In its LPS-induced acute lung injury model, it alleviates lung tissue inflammatory responses and oxidative stress by inhibiting the NF-κB and MAPKs signaling pathways, thereby protecting lung function.
Borneol exhibits significant neuroprotective effects in cerebral ischemia-reperfusion injury models, with mechanisms closely related to its inhibition of the IκBα-NF-κB signaling pathway and inflammatory response. By reducing nerve cell apoptosis and oxidative damage, borneol holds promise as an adjunct therapy for stroke and other neurodegenerative diseases.
Although borneol has relatively limited research in the field of metabolic diseases, it has potential regulatory effects on various hyperglycemia-related targets (such as AMPK, SGLT2, GCK, etc.). Preliminary in vitro and computational simulation studies suggest that borneol may help improve hyperglycemia symptoms by regulating energy and glucose metabolism pathways, warranting further in-depth exploration.
Borneol's multi-target mechanism is the basis for its pharmacological diversity. It mainly involves the following key molecular targets and signaling pathways:
The positive regulatory effects of borneol and its enantiomes on GABA_A receptors are the core mechanisms of its analgesic and anesthetic effects. By enhancing GABA-mediated neuroinhibition, borneol reduces neuronal excitability, relieving pain and anxiety.
Borneol inhibits nAChR non-competitively, regulating neurotransmitter release and nerve conduction, and may participate in its neuroprotective and cognitive regulatory effects.
Borneol inhibits IκBα degradation, blocks NF-κB nuclear translocation, reduces the expression of pro-inflammatory genes, and exerts anti-inflammatory and neuroprotective effects. This mechanism has been validated in models of acute lung injury and cerebral ischemia.
Borneol inhibits activation of MAPKs such as p38, JNK, and ERK, synergistically suppressing inflammatory responses and apoptosis, thereby enhancing tissue repair capacity.
Borneol inhibits P-glycoprotein function through NF-κB-mediated mechanisms, affecting drug transport across the blood-brain barrier and potentially improving the bioavailability of drugs in the central nervous system.
Borneol has potential regulatory effects on hyperglycemia-related targets such as AMPK (energy sensing kinase), SGLT2 (sodium-glucose co-transporter 2), and GCK (glucokinase), suggesting its potential application in metabolic diseases.
The druggability parameters of borneol indicate its promising potential for drug development. Molecular weight 154.25, LogP 2.95, TPSA 20.23 Ų, compliant with Lipinski rules, with good oral absorption and blood-brain barrier permeability. Its hydrogen bond acceptor count is only 1, which facilitates molecular binding to targets and membrane permeation.
Toxicological evaluation showed that borneol had an LD50 of about 4300 mg/kg, low toxicity, no significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition, negative Ames-induced mutagenic test, and good safety.
Pharmacokinetic studies show that borneol is rapidly absorbed orally and widely distributed, especially at high concentrations in the central nervous system. Its metabolism mainly occurs through hepatic enzyme systems, and the activity and clearance mechanisms of these metabolites require further research. Borneo's high blood-brain barrier permeability makes it an ideal candidate for drug development for neurological diseases.
As a traditional Chinese medicine ingredient, borneol, with its multi-target and multi-mechanism pharmacological activity, shows broad clinical application prospects in central nervous system diseases, inflammatory diseases, and metabolic diseases.
Based on its positive regulation of GABA_A receptors and neuroprotective effects, borneol is expected to be used to treat epilepsy, anxiety disorders, cerebral ischemia, and neurodegenerative diseases. In the future, modern pharmaceutical technologies can be combined to develop sustained-release formulations or brain-targeted drug delivery systems to improve treatment outcomes.
Borneol's inhibitory effect on NF-κB and MAPKs signaling pathways makes it a promising molecule for anti-inflammatory drug development, especially suitable for adjunctive therapy of acute lung injury, chronic inflammatory diseases, and autoimmune diseases.
Although borneol's research on hyperglycemia and metabolic syndrome is still in its early stages, its regulatory effects on key targets such as AMPK and SGLT2 suggest its potential as a therapeutic agent for metabolic diseases, warranting systematic pharmacological and clinical studies.
Borneol improves the permeability of the blood-brain barrier by inhibiting P-glycoprotein function, providing a new strategy for central nervous system drug delivery. Combined with other medications, it may enhance efficacy and reduce dosage and toxic side effects.
Future research should focus on clinical efficacy evaluation, pharmacokinetic optimization, and safety monitoring of borneol, integrating modern medicinal chemistry and molecular biology techniques to promote its clinical translation.
Borneol, a classic bicyclic monoterpene natural product, combines excellent pharmacological activity with druggability, especially showing broad application prospects in nervous system regulation, anti-inflammation, and metabolic diseases. Its multi-target and multi-mechanism mode of action provides new ideas and strategies for disease treatment. In the future, in-depth analysis and clinical research on borneol's mechanism of action should be strengthened to promote its development as a safe and effective natural drug or new drug candidate, contributing to human health.
Shenshuai
Wenjing
Hedandan
