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Product Name: Azadirachtin
Synonym name: Azadirachtin A
Catalogue No.: BP0224
Cas No.: 11141-17-6
Formula: C35H44O16
Mol Weight: 720.721
Botanical Source: Indian neem tree Azadirachta indica
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:
Azadirachtin has antifungal activity, it used as insecticides.
References:
Annu Rev Entomol. 2019 Oct 8.
Botanical Insecticides in the Twenty-First Century-Fulfilling Their Promise?
METHODS AND RESULTS:
Academic interest in plant natural products with insecticidal properties has continued to grow in the past 20 years, while commercialization of new botanical insecticides and market expansion of existing botanicals has lagged considerably behind. Insecticides based on pyrethrum and neem (Azadirachtin) continue to be standard bearers in this class of pesticides, but globally, their increased presence is largely a consequence of introduction into new jurisdictions. Insecticides based on plant essential oils are just beginning to emerge as useful plant protectants. Some countries (such as Turkey, Uruguay, the United Arab Emirates, and Australia) have relaxed regulatory requirements for specific plant extracts and oils, while in North America and the European Union, stricter requirements have slowed progress toward commercialization of new products.
CONCLUSIONS:
Botanicals are likely to remain niche products in many agricultural regions and may have the greatest impact in developing countries in tropical regions where the source plants are readily available and conventional products are both expensive and dangerous to users.
Toxins (Basel). 2019 Oct 5;11(10). pii: E579.
In Vitro Activity of Neem (Azadirachta indica) Oil on Growth and Ochratoxin A Production by Aspergillus carbonarius Isolates.
Aspergillus carbonarius is a saprobic filamentous fungus, food spoiling fungus and a producer of ochratoxin A (OTA) mycotoxin.
METHODS AND RESULTS:
In this study, the in vitro antifungal activity of neem oil (0.12% p/p of Azadirachtin) was evaluated against the growth of six strains of A. carbonarius and the production of OTA. Four different concentrations of neem oil were tested in addition to three incubation times. Only the concentration of 0.3% of neem oil inhibited more than 95% of the strain's growth (97.6% ± 0.5%), while the use of 0.5% and 1.0% of neem oil showed lower antifungal activity, 40.2% ± 3.1 and 64.7% ± 1.1, respectively. There was a complete inhibition of OTA production with 0.1% and 0.3% neem oil in the four strains isolated in the laboratory from grapes.
CONCLUSIONS:
The present study shows that neem essential oil can be further evaluated as an auxiliary method for the reduction of mycelial growth and OTA production.
HPLC of Azadirachtin
HNMR of Azadirachtin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
260.6000
1.9000
No
No
No
No
No
No
No
Azadirachtin is a natural triterpene compound derived from the fruit of the chinaberry tree (Azadirachta indica), attracting attention for its remarkable biological activity. As one of the most important active components in the neem tree, neem extract has a variety of pharmacological effects, including anti-cancer, antimalarial, anti-inflammatory, and insecticidal activities. In recent years, with advances in natural product pharmacology and molecular biology technologies, the mechanism of action of invintin has gradually been revealed, especially in inducing apoptosis, regulating signaling pathways, and targeting various disease-related molecules, showing unique advantages. This paper aims to systematically review the chemical structure and physicochemical properties of indierin, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation and pharmacokinetic characteristics, and to explore its potential and future development directions in clinical application.
Neem is a tetracyclic triterpene compound, with a molecular formula of C35H44O16 and a molecular weight of 720.7 Da. Its structure is complex, containing multiple oxidized functional groups and a cyclic skeleton, exhibiting highly stereochemical characteristics. The LogP value of neem in neem is about 1.9, indicating moderate lipid solubility, which facilitates cell membrane penetration. Its polar surface area (TPSA) reaches as high as 260.6 Ų, indicating strong molecular polarity that may affect its bioavailability and transmembrane transport capacity. Inernein contains 16 hydrogen bond receptor sites, giving it the potential to form multiple hydrogen bonds with protein targets.
From a physicochemical perspective, inderine does not easily cross the blood-brain barrier (BBB), which limits its use in central nervous system diseases but also reduces the risk of CNS toxicity. Toxicological evaluation showed that the LD50 of indierin reached 5000 mg/kg, with negative hepatotoxicity, cardiotoxicity, and hERG channel inhibition, and Ames-induced mutagenic test results negative, indicating high safety and solid druggability.
Neem is mainly found in the fruit of the neem tree (Azadirachta indica), which is widely distributed in India and Southeast Asia, especially in the seeds and peels of mature fruits, where the content is relatively high. As a traditional medicinal plant, the chinaberry tree is widely used among the people for antibacterial, anti-inflammatory, and insect-repellent purposes.
Neem extraction is usually done using organic solvent extraction methods, with commonly used solvents including ethanol, methanol, and ethyl acetate. The extraction process generally includes fruit drying, crushing, solvent extraction, filtrate concentration, and purification steps. To improve purity, column chromatography (silica gel column, reversed-phase column) and high-performance liquid chromatography (HPLC) techniques are often used for separation and purification. In recent years, the application of supercritical CO2 extraction and microwave-assisted extraction technology has significantly improved the extraction efficiency and purity of neem extraction, while also being more environmentally friendly and energy-saving.
Neemin exhibits significant cytotoxicity and proliferative inhibition in various cancer cell lines. Its anti-cancer mechanism mainly works by inducing tumor cell apoptosis, blocking the cell cycle, and inhibiting tumor-related signaling pathways. Studies have shown that neemin can regulate the expression of Bcl-2 family proteins, inhibit the anti-apoptotic protein Bcl-2, promote the activity of the pro-apoptotic protein Bax, and activate mitochondrial pathways to induce apoptosis. Additionally, neemin activates Apaf-1 and caspase-3, promoting an apoptotic cascade that ultimately leads to tumor cell death.
Inneemin has an inhibitory effect on malaria parasites, especially showing potential efficacy in malaria-resistant strains. Its mechanism of action may involve inhibiting the metabolic enzyme activity of malaria parasites and interfering with the developmental cycle of parasites within host cells, offering potential for the development of novel antimalarial drugs.
Ininerin exerts its anti-inflammatory effect by inhibiting activation of nuclear factor κB (NF-κB) signaling pathway, reducing the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6. This mechanism has been validated in various inflammatory models, demonstrating its promising application in treating inflammatory diseases.
As a natural insecticide, inerin demonstrates strong insect resistance by inducing insect cell apoptosis and interfering with insect development. Its mechanism involves activation of apoptosis signals within insect cells and interference with the nervous system, and has been widely used in agricultural pest control.
The main mechanisms by which neemin induces apoptosis include the synergistic effects of mitochondrial pathways and death receptor pathways. In the mitochondrial pathway, neemin regulates the Bcl-2/Bax ratio, promoting loss of mitochondrial membrane potential, releasing cytochrome c, which in turn activates Apaf-1 and caspase-3, initiating apoptosis. In the death receptor pathway, indierin promotes apoptosis by regulating tumor necrosis factor receptor (TNFR) signaling.
Additionally, neem extract exerts anti-inflammatory effects by inhibiting the NF-κB signaling pathway, blocking the transcription of pro-inflammatory genes. As a key regulatory factor of various inflammation and tumor-related genes, NF-κB inhibition helps alleviate inflammatory responses and suppress tumor progression.
In disease models such as otitis media, inarxin acts on several key targets, including signal transduction and transcription activator factor 3 (STAT3), protein kinase Cδ (PRKCD), nuclear factor E2-related factor 2 (NFE2L2), hypoxia-inducible factor 1α (HIF1A), and topoisomerase IIα (TOP2A). These targets involve cell proliferation, oxidative stress response, inflammation regulation, and apoptosis, indicating the potential of inerin to regulate diseases through multiple targets and pathways.
The relatively large molecular weight (720.7 Da) and high polar surface area (TPSA 260.6 Ų) pose challenges to its oral bioavailability. A high number of hydrogen bond receptors (16) may limit its ability to diffuse across membranes, affecting absorption. Nevertheless, its LogP value is moderate (1.9), which is favorable for cell membrane penetration.
Toxicological evaluation showed that neemin was safe, had no significant hepatic or cardiac toxicity, and did not inhibit hERG channels, reducing the risk of potential arrhythmias. A negative Ames test indicates no mutagenicity and is suitable for further drug development.
Current pharmacokinetic research is relatively limited, and metabolic pathways in vivo are not fully understood. Preliminary data indicate that neemin is metabolized stably in the body, mainly metabolized by hepatic enzymes, and excreted through bile and urine. It is difficult to cross the blood-brain barrier, limiting the development of central nervous system-related indications.
With its multiple pharmacological activities, ininerin shows broad clinical application prospects. In the field of anti-cancer treatment, neem can serve as an adjunct therapy to enhance chemotherapy effects and reduce side effects. Its anti-inflammatory properties give it potential application value in chronic inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease. For infectious diseases such as otitis media, neem may improve inflammation and promote tissue repair by regulating targets like STAT3 and NFE2L2.
Moreover, the natural insecticidal properties of inerin provide a green and environmentally friendly solution for agricultural biopesticide development, reducing the use of chemical pesticides and lowering environmental pollution.
Future research should focus on improving the bioavailability of inerin, optimizing delivery routes and dosage form design, and combining nanocarrier technology to achieve targeted delivery. At the same time, it conducts an in-depth analysis of its pharmacokinetic characteristics and long-term safety evaluation, laying a foundation for clinical translation. Systematic research on multi-target mechanisms of action also helps identify new indications and promotes the translation of neemin into clinical drugs.
As a natural triterpenoid compound with a complex structure and diverse activity, inditerpene has become a hot topic in natural product pharmacology research due to its remarkable anti-cancer, antimalarial, anti-inflammatory, and insecticidal activities. Its unique mechanism involves apoptosis induction, signaling pathway regulation, and multi-target intervention, demonstrating the advantages of natural products in multidimensional disease regulation. Despite druggability challenges such as large molecular weight and strong polarity, inerin still demonstrates good safety and potential clinical value. In the future, the integration of modern drug design and delivery technology is expected to promote the widespread application of neem in medicine and agriculture, becoming an important model for innovative natural product drug development.
Shenshuai
Wenjing
Hedandan
