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Cancer rates are increasing, and cancer is one of the main causes of death worldwide. Amygdalin, also known as vitamin B17 (and laetrile, a synthetic compound), is a cyanogenic glycoside compound that is mainly found in the kernels and pulps of fruits. This compound has been proposed for decades as a promising naturally occurring substance which may provide anticancer effects. This is a comprehensive review which critically summarizes and scrutinizes the available studies exploring the anticancer effect of amygdalin, highlighting its potential anticancer molecular mechanisms as well as the need for a nontoxic formulation of this substance. In-depth research was performed using the most accurate scientific databases, e.g., PubMed, Cochrane, Embase, Medline, Scopus, and Web of Science, applying effective, characteristic, and relevant keywords. There are several pieces of evidence to support the idea that amygdalin can exert anticancer effects against lung, breast, prostate, colorectal, cervical, and gastrointestinal cancers. Amygdalin has been reported to induce apoptosis of cancer cells, inhibiting cancer cells’ proliferation and slowing down tumor metastatic spread. However, only a few studies have been performed in in vivo animal models, while clinical studies remain even more scarce. The current evidence cannot support a recommendation of the use of nutritional supplements with amygdalin due to its cyano-moiety which exerts adverse side effects. Preliminary data have shown that the use of nanoparticles may be a promising alternative to enhance the anticancer effects of amygdalin while simultaneously reducing its adverse side effects. Amygdalin seems to be a promising naturally occurring agent against cancer disease development and progression. However, there is a strong demand for in vivo animal studies as well as human clinical studies to explore the potential prevention and/or treatment efficiency of amygdalin against cancer. Moreover, amygdalin could be used as a lead compound by effectively applying recent developments in drug discovery processes.

Ultrasound (US), as a non-invasive and non-ionising technology, has been utilized as an efficient technique for transporting drugs and genes across physiological barriers, such as the blood-brain barrier (BBB), in addition to its use in medical imaging. In Contrast-Enhanced Ultrasound Imaging (CEUS), microbubbles act as an effective delivery vehicle, thereby enhancing cellular uptake of the drug. This characteristic is attributed to the cavitation property of the microbubbles. In this study, we synthesised gH625-tagged pre-Polyglycerolsebacate encapsulating a perfluoropentane core (Pre-PGS-PFP) nanodroplets with improved internalisation properties and the ability to deliver a payload by phase converting to phase convertible nanodroplets upon insonation. Amygdalin, as an anticancerous drug, was loaded in the polymeric shell of Pre-PGS-PFP phase convertible nanodroplets using the solvent displacement method and was conjugated to the membrane-crossing peptide (gH625) using NHS-EDC coupling. The nanodroplets were physicochemically characterized using FTIR, SEM, confocal microscopy and zeta analysis. The nanodroplets were found to load 80.10% of Amygdalin. Cytotoxicity and uptake studies in U87 glioblastoma cells demonstrated that ultrasound-triggered amygdalin release significantly enhanced cell death compared to diffusion-based release or treatment with free Amygdalin. Furthermore, the presence of gH625 further improved cellular uptake due to its membrane-penetrating ability. Overall, the synergistic effect of ultrasound activation and gH625 functionalization facilitated efficient internalization and localized drug release, suggesting a promising strategy for targeted delivery and therapeutic enhancement in the treatment of glioblastoma.

Wild almond species accumulate the bitter and toxic cyanogenic diglucoside amygdalin. Almond domestication was enabled by the selection of genotypes harboring sweet kernels. We report the completion of the almond reference genome. Map-based cloning using an F₁ population segregating for kernel taste led to the identification of a 46-kilobase gene cluster encoding five basic helix-loop-helix transcription factors, bHLH1 to bHLH5. Functional characterization demonstrated that bHLH2 controls transcription of the P450 monooxygenase–encoding genes PdCYP79D16 and PdCYP71AN24, which are involved in the amygdalin biosynthetic pathway. A nonsynonymous point mutation (Leu to Phe) in the dimerization domain of bHLH2 prevents transcription of the two cytochrome P450 genes, resulting in the sweet kernel trait.

Huoxue-Tongluo lyophilized powder for injection (HTLPI), a traditional Chinese medicine preparation, is a compound of Persicae semen and Paeoniae Radix Rubra that is used mainly for treating blood-stasis obstruction syndrome in the acute stage of cerebral ischemic stroke. Amygdalin (AD) and paeoniflorin (PF) are 2 typical bioactive components in HTLPI and were selected as indicators for this pharmacokinetic study of HTLPI. The objective of this study was to investigate the safety profile, tolerability, and pharmacokinetic properties of AD and PF after single and multiple intravenous infusions of HTLPI in healthy Chinese volunteers. Twenty-one healthy Chinese subjects were recruited for this open-label, single ascending-dose (3, 6, and 9 g) and multiple-dose (6 g, once daily) study. Safety profile was assessed by adverse events and physical examination throughout the study. Serial plasma and urine samples were analyzed by HPLC-MS/MS. Pharmacokinetic parameters of AD and PF were calculated using noncompartmental analysis. In the single-dose phase of the study, the mean maximum plasma concentration and the mean area under the plasma concentration−time curve of AD and PF increased proportionally with each dose escalation. In the multiple-dose phase, the steady state was achieved by day 4 after multiple-dose administration of 6 g HTLPI. Mean pharmacokinetic parameters achieved on day 1 were similar to those on day 7. No significant accumulation was observed after repeat doses of 6 g HTLPI. Approximately 79.6% of the administered AD and 48.4% of the administered PF were excreted unchanged in urine within 24 hours. No serious adverse events were observed during the entire study. The pharmacokinetic properties of AD and PF were linear after a single intravenous infusion of HTLPI in the dose range of 3−9 g. No systemic accumulation was observed with repeat doses of HTLPI. Sex had no significant effect on the pharmacokinetic properties of AD and PF. Intravenous infusion of HTLPI was well tolerated in healthy Chinese subjects.

Traditional soaking plum wine production is time-consuming and often results in high levels of bitter amygdalin and toxic cyanide, posing health risks. In this study, response surface methodology (RSM) with a Box–Behnken design was employed to optimize pulsed electric field (PEF) parameters, developing a novel process integrating kernel detoxification and PEF pretreatment to mitigate these hazards, enhance the characteristic aroma (benzaldehyde), and shorten the maceration cycle. The experimental results showed that the contents of bitter amygdalin and cyanide in plum kernels after detoxification and PEF pretreatment were reduced by 62.34% and 59.62%, respectively, compared with the control group, and the contents of both were further reduced with the addition of plum flesh for further soaking in the new process. In addition, the PEF pretreatment also increased the amount of benzaldehyde extracted by 4.63% compared to the control group and resulted in a 10.53% reduction in equilibration time. Moreover, compared to the previous whole-fruit maceration process, the new process resulted in a 37.5% reduction in the final plum wine production cycle. This study provides a practical solution for improving the safety and efficiency of plum wine production and supports the industrial application of PEF technology.

Malignant tumors are the major disease that cause serious damage to human health, and have been listed as the premier diseases which seriously threatened human health by World Health Organization (WHO). In recent years the development of antitumor drugs has been gradually transformed from cytotoxic drugs to improving the selectivity of drugs, overcoming multidrug resistance, development of new targeted drugs and low toxicity with high specificity drugs. Amygdalin is a natural product that owns antitumor activity, less side effects, widely sourced and relatively low priced. All these features make the amygdalin a promising antitumor drugs, if combined with conditional chemotherapy drugs, which can produce synergistic effect. In this paper, we summarized the pharmacological activity, toxicity and antitumor activity of amygdalin, mainly focused on the advanced research of amygdalin on its antitumor effects in recent years, providing new insights for the development of new anticancer drugs, new targets searching and natural antitumor mechanism investigations.

Almond (Prunus dulcis) is the principal Prunus species in which the consumed and thus commercially important part of the fruit is the kernel. As a result of continued selection, the vast majority of almonds have a nonbitter kernel. However, in the field, there are trees carrying bitter kernels, which are toxic to humans and, consequently, need to be removed. The toxicity of bitter almonds is caused by the accumulation of the cyanogenic diglucoside amygdalin, which releases toxic hydrogen cyanide upon hydrolysis. In this study, we identified and characterized the enzymes involved in the amygdalin biosynthetic pathway: PdCYP79D16 and PdCYP71AN24 as the cytochrome P450 (CYP) enzymes catalyzing phenylalanine-to-mandelonitrile conversion, PdUGT94AF3 as an additional monoglucosyl transferase (UGT) catalyzing prunasin formation, and PdUGT94AF1 and PdUGT94AF2 as the two enzymes catalyzing amygdalin formation from prunasin. This was accomplished by constructing a sequence database containing UGTs known, or predicted, to catalyze a 𝛽(1→6)-O-glycosylation reaction and a Basic Local Alignment Search Tool search of the draft version of the almond genome versus these sequences. Functional characterization of candidate genes was achieved by transient expression in Nicotiana benthamiana. Reverse transcription quantitative polymerase chain reaction demonstrated that the expression of PdCYP79D16 and PdCYP71AN24 was not detectable or only reached minute levels in the sweet almond genotype during fruit development, while it was high and consistent in the bitter genotype. Therefore, the basis for the sweet kernel phenotype is a lack of expression of the genes encoding the two CYPs catalyzing the first steps in amygdalin biosynthesis.

The overall incidence of cancer is increasing in recent years. Despite advances in various comprehensive treatments, the mortality of advanced malignant tumors remains at a high level. Numerous pharmacological studies have confirmed that many Chinese herbal medicines possess remarkable antitumor activities. Amygdalin, mainly existing in bitter almond, is reported to have antitumor properties in addition to the antioxidative, antibacterial, anti‐inflammatory and immunoregulatory activities. This article summarizes the structural characteristics of amygdalin, its antitumor mechanisms, and recent progress and achievement in the research of amygdalin, hoping that it could provide theoretical clues for exploring the clinical value of amygdalin against tumors. Amygdalin is known to have an antitumor effect in solid tumors such as lung cancer, bladder cancer and renal cell carcinoma by affecting cell cycle, inducing apoptosis and cytotoxicity, and regulating immune function. Further research is needed to elucidate the pharmacological mechanisms of amygdalin in terms of the optimal dosage, the feasibility of combined use of amygdalin with other antitumor drugs, and even artificial synthesis of the active components in amygdalin, for the sake of enhancing its antitumor activities and reducing its adverse effects for clinical use. Amygdalin is known to have an antitumor effect in solid tumors such as lung cancer, bladder cancer, and renal cell carcinoma by affecting cell cycle, inducing apoptosis and cytotoxicity, and regulating immune function. Further research is needed to elucidate the pharmacological mechanisms of amygdalin in terms of the optimal dosage, the feasibility of combined use of amygdalin with other antitumor drugs, and even artificial synthesis of the active components in amygdalin, for the sake of enhancing its antitumor activities and reducing its adverse effects for clinical use.

Amygdalin, a naturally occurring compound, is one of the main active ingredients of the Chinese raw bitter almond. The variation in amygdalin composition of seed kernels among the six almond species was determined, and relationships with geoenvironmental factors were analyzed. The amygdalin content exhibited great diversity, ranging from 0.0004 to 9.73 g/100 g. The highest level of amygdalin was detected in Tangut almond, with 5.45–9.73 g/100 g. The other kernels showed a range from 3.14 to 6.80 g/100 g in wild almond and from 3.00 to 4.22 g/100 g in longstalk almond. Amygdalin in common almond was almost undetectable. Factor analysis showed that amygdalin content in Prunus spp. kernels increased with altitude and decreased with the degree of aspect. Many environmental factors were closely related to amygdalin content, including annual precipitation (Bio12), UV intensity, and topsoil base saturation (T_BS), which all had a significant effect on amygdalin content. The amygdalin content is closely related to rainfall indicators, especially annual precipitation (Bio12), with the highest factor analysis value (3.63). Water regulates amygdalin in diverse ways. Since amygdalin is water-soluble, water can reduce the inhibitory effect of amygdalin on germination and regulate the synthesis of amygdalin at the late stage of germination by activating the amygdalin synthesis genes CYP79D16 and CYP71AN24 . This study expands the understanding of amygdalin in almond resources and provides the direction for the regulation of amygdalin.