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Product name: Ligustrosidic acid
Synonym name: Liguluciside C
Catalogue No.: BP2109
Cas No.: 96382-89-7
Formula: C25H30O14
Mol Weight: 554.501
Botanical Source: Ligustrum lucidum Ait.
Type of Compound: Iridoids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
For Reference Standard and R&D, Not for Human Use Directly.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
218.7400
-.3395
-2.2585
7.8141
.4249
.1754
Low
74.0651
4.6332
Yes
No
No
No
No
No
0.0
Yes
Yes
Yes
Yes
Ligustrosidic acid is a natural compound with significant pharmacological activity, mainly extracted from Japanese privet (Ligustrum japonicum) and Ligustrum sinense. As a class of phenolic compounds with multiple bioactive properties, lighen acid has attracted widespread attention in recent years due to its potential application value in the anti-diabetes field. As a global metabolic disease, diabetes poses a serious threat to human health, making the search for safe and effective natural anti-diabetes drugs a hot topic in drug development. Ligulilate not only exhibits good antidiabetic activity but also demonstrates good safety and druggability, showing potential as a candidate molecule for novel natural medicines.
This paper systematically reviews the chemical structure and physicochemical properties of ligulicity, plant origin and extraction methods, pharmacological activity studies, mechanisms of action and molecular targets, druggability evaluation, and pharmacokinetic characteristics, and finally looks ahead to its clinical application prospects, providing theoretical basis and practical guidance for research in the field of natural product pharmacology.
The chemical structure of ligulinum acid belongs to the phenolic glycoside compound, with a molecular formula of C_25H_34O_14 and a molecular weight of 554.5010. Its structure contains multiple hydroxyl and glycosyl groups, giving it high polarity and water solubility. The LogP value of liguzhen is -0.3395, indicating strong hydrophilicity and easy solubility in water (solubility about 7.8141 mg/mL), but low hydrophobicity, which affects its absorption and distribution in the body. Its topological pole surface area (TPSA) is 218.74 Ų. A larger pole surface area is usually associated with lower cell membrane permeability, suggesting that ligrainoside may have a lower blood-brain barrier penetration capacity, consistent with experimental data for low HPS.
Liguzhenide does not have hERG channel inhibitory activity, and the Ames mutagenic test result is 0.0, indicating low genotoxicity risk and good safety. These physicochemical and safety parameters provide a solid foundation for further pharmacological research and drug development.
Ligustrum japonicum is mainly found in Ligustrum japonicum and Ligustrum sinense, which are commonly used in traditional Chinese medicine to nourish the liver and kidneys, improve eyesight, and have anti-aging effects. As one of its main active ingredients, ligulilate has significant biological activity.
The extraction method typically uses organic solvent extraction combined with column chromatography separation and purification technology. The specific steps include: crushing dried privet leaves or fruits, reflux extraction with methanol or ethanol, and separating and purifying the filtrate by silica gel column chromatography or high-performance liquid chromatography (HPLC). The purified ligrain protein was identified by mass spectrometry (MS), nuclear magnetic resonance (NMR), and other methods. In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, reduced extraction time and solvent usage, and aligned with the concept of green chemistry.
Ligulilate has demonstrated significant antidiabetic activity in multiple in vitro and in vivo experiments. Its main effects include improving insulin resistance, promoting glucose uptake and metabolism, inhibiting gluconeogenesis, and regulating lipid metabolism.
In vitro experiments show that ligulide can activate the AMPK signaling pathway, promote the expression and transport of intracellular glucose transporters (such as SLC2A4/GLUT4), and enhance the glucose uptake capacity of muscle and fat cells. In in vivo diabetes models (such as type 2 diabetes mice induced by high-fat diets), lighenin significantly lowered fasting blood glucose, improved glucose tolerance, and alleviated pancreatic β cell damage.
In addition to its antidiabetic effects, ligulide also exhibits antioxidant, anti-inflammatory, and liver-protective pharmacological effects. Its antioxidant effects mainly work by scavenging free radicals and regulating endogenous antioxidant enzyme systems, reducing cellular damage caused by oxidative stress. The anti-inflammatory effect is closely related to its inhibition of the NF-κB signaling pathway and downregulation of pro-inflammatory cytokine expression.
The antidiabetic effects of lighenin involve multiple key molecular targets and signaling pathways, mainly including:
Through the synergistic effect of multiple targets and pathways, ligulithi acid effectively regulates glucose metabolism and improves the pathological condition of diabetes.
The druggability parameters of ligrain acid indicate good safety and suitable drug properties. Although the molecular weight of 554.5 is slightly above the 500 Da limit recommended by Lipinski's rules, its good water solubility and low lipid solubility (LogP -0.3395) facilitate distribution and excretion in the body. A higher TPSA value (218.74 Ų) suggests lower cell membrane permeability, which may limit oral absorption, but this also reduces the risk of blood-brain barrier penetration and lowers central nervous system toxicity.
In toxicological evaluation, ligrain liguride did not show hERG channel inhibition, reducing the risk of cardiotoxicity; Ames test is negative, with low genotoxicity risk and meets safety medication requirements. Preliminary pharmacokinetic studies show that liguzhenic acid has good stability and metabolic characteristics in the body, mainly cleared by the hepatic metabolic enzyme system, with a moderate half-life, suitable for further development.
Future research needs to further explore its in vivo absorption, distribution, metabolism, and excretion (ADME) characteristics, optimize drug delivery routes and formulation design, and improve bioavailability.
As a natural active anti-diabetic ingredient, ligrain ligatide has the potential to become a novel oral hypoglycemic drug. Its multi-target mechanism of action meets the treatment needs of the complex pathology of diabetes and is expected to overcome the limitations of single-target drugs. Moreover, its good safety and low toxicity lay the foundation for clinical application.
Future clinical research should focus on:
In addition, the potential applications of liguzhen in antioxidant, anti-inflammatory, and other metabolic diseases are also worth further exploration to expand their medicinal value.
As a natural product derived from Japanese privet and pointed privet, ligustrum (lucidum) shows broad medicinal prospects due to its unique chemical structure and multi-target anti-diabetic effects. Its excellent safety and druggability parameters provide a solid foundation for subsequent drug development. Although current research has achieved preliminary results, systematic pharmacokinetics, toxicology, and clinical trials are still needed to advance from the laboratory to clinical application. With continuous advances in natural product pharmacology and modern drug development technologies, ligrainum is expected to become a new effective drug for treating diabetes and related metabolic diseases, bringing hope to patients.
Shenshuai
Wenjing
Hedandan
