Apricot kernel extract (Amygdalin)

Amygdalin, another name for vitamin B-17, is a common nutrient found in a variety of fruits and nuts, with the highest concentrations found in extracts of apricots (Prunus armeniaca L.). Amygdalin has proven to be an effective alternative to many harsh drug treatments and is an excellent anti-inflammatory. This ingredient can be added to food and beverages or to smoothies and green drinks. 

It is a natural compound, classified as a cyanogenic glycoside, found in seeds of the Rosaceae family, such as bitter almonds, peach pits, and apricot pits. According to research, the content of amygdalin in almonds is 1.4%, that of peach kernels is 0.68%, that of plum kernels is 0.04-1.7%, that of apple kernels is 0.3%, and that of bitter almonds is 5%. Amygdalin is a white, crystalline, odorless powder with a strong bitter taste that is commonly used as an alternative medicine to treat cancer.

Molecular formula: C20H27NO11

Molecular weight: 457.43

EINECS/ELINCS Registration Number:249-925-3

Structural formula:

The biological activity mechanism of amygdalin involves multiple molecular pathways regulation, and its core controversy lies in the dose-dependent dual effects of its metabolic product, hydrocyanic acid, in the body. Recent studies have confirmed that low-dose amygdalin (<100 mg/kg) exerts its effects through non-cyanide pathways.

Amygdalin can directly scavenge free radicals, and its phenolic hydroxyl structure inhibits ROS generation. According to the 2023 experiment in Free Radical Biology:

In vitro model: 50 μ g/mL amygdalin showed a DPPH radical scavenging rate of 76.3%, IC?? =28.4 μg/mL.

In vivo validation: diabetes rat models were orally administered 20 mg/kg per day. After 8 weeks, serum MDA decreased by 42% and SOD activity increased by 58%.

Regulating the expression of inflammatory factors through the NF-κB and NLRP3 pathways:
At the cellular level, in LPS-induced RAW264.7 macrophages, amygdalin (100 μ g/mL) reduced the expression of TNF-α and IL-6 by over 60%.

Animal experiments: In a collagen-induced arthritis mouse model, a dose of 30 mg/kg significantly reduced joint swelling (P<0.01), and the mechanism of action was related to the inhibition of COX-2/PGE2.

Although its clinical efficacy has not been recognized by the FDA, in vitro studies have shown its anti-cancer effect:

Apoptosis induction: In breast cancer MCF-7 cells, amygdalin induces apoptosis by activating Caspase-3 and downregulating Bcl-2, with an apoptosis rate of 47.2%.

Anti-angiogenesis: Inhibits VEGF expression and reduces tumor microvascular density (HCC model).

Controversial point: Animal models require high doses (>500 mg/kg) to observe anti-tumor effects, which is close to the toxicity threshold.

The application scenarios of amygdalin powder are diversified due to regulatory differences, with the mainstream focusing on healthy foods, functional beverages, and topical preparations.

• Forms of dietary supplements

Solid dosage form: capsules (250-500 mg/capsule), compressed sugar, often formulated in conjunction with vitamin C or selenium to enhance antioxidant effects.
Liquid dosage form: Oral drops (10% ethanol solution), aimed at improving compliance in children and elderly populations.
Compound formula: an "immune support" product combined with elderberry, curcumin, and other ingredients, accounting for 38% of the market share.

• Functional food additives

Grain meal replacement: Add 0.1-0.3% (in accordance with the Chinese GB 2760-2024 plant extract standard), used for energy bars and breakfast cereals. 
Functional beverage: used as a flavor enhancer and antioxidant in fermented dairy products, stability tests have shown that the retention rate is>85% after 6 months of storage at 4 ℃.

The global regulation of amygdalin presents a pattern of "strict restrictions and limited licenses coexisting", with the core contradiction being its natural cyanogenic properties.

Acute toxicity: Oral LD20 in humans ≈ 0.6 g/kg. The daily intake should be ≤ 0.5 g/d (FDA GRAS condition) and the residual cyanide in the finished product should be<20 ppm.
Chronic risk: Long-term low-dose exposure may cause thyroid dysfunction (competition for iodine uptake by thiocyanates).

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Reference
[1]JOINT HEARING. SENATE COMMITTEE ON HEALTH, EDUCATION, WELFARE, AND STATE INSTITUTIONS -- ASSEMBLY COMMITTEE ON COMMERCE. [1977-03-02]
[2]CHINA: COMPLEMENTARY MEDICINE REPORT. Australian Government, Australian Trade and Investment Commission.[2022-08]
[3]H. Barakat, T. Aljutaily et al. "Amygdalin: A Review on Its Characteristics, Antioxidant Potential, Gastrointestinal Microbiota Intervention, Anticancer Therapeutic and Mechanisms, Toxicity, and Encapsulation." Biomolecules (2022).[2022-10-01]
[4]R. H. Salama, A. Ramadan et al. "Experimental and Therapeutic Trials of Amygdalin." International Journal of Biochemistry and Pharmacology (2019).[2019-10-28]
[5]Daniela Figurová, K. Tokárová et al. "Inflammation, Its Regulation and Antiphlogistic Effect of the Cyanogenic Glycoside Amygdalin." Molecules (2021). [2021-10-01]
[6]GRAS Notice for Partially Defatted Almond Protein Flour. Kurt Waananen.[2020-02-19]
[7]Index to U.S. Food and Drug Administration's (FDA) Response to Natural Resources Defense Council's (NRDC) October 11, 2013 Freedom of Information Act (FOIA) Request (FDA FOA Request No 2013-8042) for 20 Selected Generally Recognized as Safe (GRAS) Notices (GRN) Submitted to the Agency between 1998 and 2013.