Synonym name:
Catalogue No.: BP0690
Cas No.: 61371-55-9
Formula: C8H8O4
Mol Weight: 168.148
Botanical Source: roots of Griffonia simplificola
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.
Description:
Griffonilide is islolated from the tubers of Tylosema esculentum (morama).
References:
Phytother Res. 2015 Jul 21.
Therapeutic and Prophylactic Potential of Morama (Tylosema esculentum): A Review.
Tylosema esculentum (morama) is a highly valued traditional food and source of medicine for the San and other indigenous populations that inhabit the arid to semi-arid parts of Southern Africa.
METHODS AND RESULTS:
Morama beans are a rich source of phenolic acids, flavonoids, certain fatty acids, non-essential amino acids, certain phytosterols, tannins and minerals. The plant's tuber contains Griffonilide, behenic acid and starch. Concoctions of extracts from morama bean, tuber and other local plants are frequently used to treat diarrhoea and digestive disorders by the San and other indigenous populations. Information on composition and bioactivity of phytochemical components of T. esculentum suggests that the polyphenol-rich extracts of the bean testae and cotyledons have great potential as sources of chemicals that inhibit infectious microorganisms (viral, bacterial and fungal, including drug-resistant strains), offer protection against certain non-communicable diseases and promote wound healing and gut health. The potential antinutritional properties of a few morama components are also highlighted.
CONCLUSIONS:
More research is necessary to reveal the full prophylactic and therapeutic potential of the plant against diseases of the current century. Research on domestication and conservation of the plant offers new hope for sustainable utilisation of the plant.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Natural products, as an important source of drug discovery, have attracted much attention due to their structural diversity and biological activity. Griffonilide is a natural butenolide with a unique structure, which was first isolated from the roots of the plant Semiaquilegia adoxoides. This compound often coexists with shikonin glycosides and exhibits significant biological activity, especially in the field of anti-inflammatory drugs, demonstrating potential medicinal value. In recent years, with the in-depth study of the mechanisms of inflammation related diseases, gliflozin has become a hot topic in natural product pharmacology research due to its ability to regulate various inflammation related molecular targets. This article will provide a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action of gliflozin, and explore its clinical application prospects and future research directions based on drug evaluation and pharmacokinetic characteristics.
Griffonilide has a molecular formula of C9H12O3 and a molecular weight of 168.1480, and belongs to the butenolide class of compounds. Its structural core contains a five membered lactone ring, accompanied by unsaturated double bonds, giving it certain chemical reactivity. The LogP value of this compound is -0.4284, indicating strong hydrophilicity and a water solubility of 65.7040, indicating good solubility in polar solvents. The polar surface area (TPSA) is 66.7600, indicating that it has moderate polarity and is conducive to interacting with biomolecules. It is worth noting that gliflozin has a high blood-brain barrier penetration ability, which has potential advantages for the treatment of central nervous system related diseases. In addition, the hERG channel inhibition experiment showed a negative result, indicating a low risk of cardiac toxicity; The Ames test result is 0.9, indicating a low risk of genotoxicity and meeting the basic requirements for safe drug use.
Glivelin mainly comes from the roots of Semiaquilegia adoxoides, a plant in the Ranunculaceae family. This plant is widely distributed in some parts of China and has traditionally been used to treat inflammation and related diseases. Glivelin often coexists with shikonin compounds, indicating its synergistic effect in plant metabolic pathways.
The common methods for extracting gliflozin include solvent extraction and chromatographic separation. Generally, ethanol or methanol is used as the extraction solvent, and crude extracts are obtained through ultrasound assisted extraction or reflux extraction. Subsequently, separation and purification were carried out using techniques such as silica gel column chromatography and reverse phase high performance liquid chromatography (RP-HPLC), ultimately obtaining high-purity gliflozin. In recent years, with the promotion of green chemistry concepts, new technologies such as supercritical CO2 extraction and microwave-assisted extraction have also been attempted to be applied to the extraction of this compound to improve efficiency and reduce environmental pollution.
The pharmacological activity of gliflozin is mainly anti-inflammatory, and related studies have shown that it has regulatory effects on various inflammatory mediators and signaling pathways. In vitro cell models, gliflozin can significantly inhibit the expression of pro-inflammatory cytokines such as IL-6 and TNF - α, reducing inflammatory response. In addition, it also has an inhibitory effect on the activity of inflammation related enzymes such as cyclooxygenase (PTGS1, PTGS2) and nitric oxide synthase (NOS2), reducing the production of inflammatory mediators.
In animal experiments, gliflozin has shown good anti-inflammatory effects and can alleviate tissue swelling and cell infiltration in chemically induced inflammation models. Its anti-inflammatory effect is closely related to the regulation of various inflammatory signaling pathways, especially in the regulation of STAT3 and NF - κ B signaling pathways. In addition, the regulatory effect of gliflozin on inflammation related ion channels such as TRPV1 and TRPA1 suggests that it may play a role in the relief of pain and neuroinflammation.
The anti-inflammatory mechanism of gliflozin involves synergistic regulation of multiple targets and pathways. Its main molecular targets include:
In summary, gliflozin exerts significant anti-inflammatory and analgesic effects through multi-target synergistic effects, regulating inflammatory signaling pathways.
The pharmacological evaluation of glibenclamide shows that it has good potential for drug development. Its molecular weight is 168.1480, which meets the Lipinski rule for drug molecular weight requirements. The LogP value is -0.4284, indicating its strong hydrophilicity, which is beneficial for in vivo distribution and absorption. The TPSA is 66.7600, and moderate polarity helps to pass through the cell membrane. High water solubility (65.7040) is beneficial for formulation development and in vivo absorption.
The high penetration ability of the blood-brain barrier suggests its potential advantages in the treatment of central nervous system diseases. The hERG channel inhibition experiment results were negative, reducing the risk of cardiac toxicity. The Ames test result is 0.9, indicating a low risk of genotoxicity and good safety.
At present, there is limited research on the pharmacokinetics of gliflozin, but preliminary data indicate that it is well absorbed orally, metabolically stable in vivo, mainly cleared through the liver metabolic enzyme system, and has a moderate half-life. Further systematic pharmacokinetic and toxicological studies are needed in the future to provide support for clinical applications.
As a multi-target anti-inflammatory natural product, gliflozin has broad clinical application prospects. Inflammation, as a common pathological basis for various diseases including rheumatoid arthritis, inflammatory bowel disease, neuroinflammation, and certain metabolic disorders, has the potential to become a candidate molecule for novel anti-inflammatory drugs by regulating key inflammatory factors and signaling pathways.
Its excellent blood-brain barrier penetration gives it unique advantages in central nervous system inflammation and pain management, which may be applied as an adjuvant therapy for neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. In addition, the low toxicity and good pharmacological properties of gliflozin provide favorable conditions for its clinical translation.
Future research should focus on in-depth analysis of its mechanism of action, optimizing its structure to enhance activity and pharmacokinetic properties, and conducting systematic pharmacological and safety evaluations. At the same time, combining modern drug delivery technology, developing new formulations to improve their bioavailability and targeting. The implementation of multicenter clinical trials will be a key step in verifying their clinical efficacy and safety.
As a natural product of butenolide derived from Semiaquilegia adoxoides, gliflozin exhibits significant medicinal value due to its unique chemical structure and multi-target anti-inflammatory activity. Its regulation of key inflammatory molecules such as IL-6, STAT3, and NF - κ B reveals its complex and effective anti-inflammatory mechanism. The drug efficacy evaluation shows that it has good potential for drug development, especially in the application of central nervous system inflammatory diseases with broad prospects.
Although research on gliflozin is still in its infancy, its various advantages make it a candidate drug worth exploring in the field of natural product pharmacology. In the future, through systematic pharmacology, pharmacokinetics, and clinical research, it is expected to promote the translation of gliflozin into clinical applications, providing new strategies and choices for anti-inflammatory treatment.
