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Klinicka Onkologie : Casopis Ceske a... 2019Amygdalin is a natural compound primarily found in seeds of fruit trees. In the human body, it is hydrolyzed to benzaldehyde, glucose, and cyanide, which is considered... (Review)
Review
BACKGROUND
Amygdalin is a natural compound primarily found in seeds of fruit trees. In the human body, it is hydrolyzed to benzaldehyde, glucose, and cyanide, which is considered the active component of amygdalin. The semi-synthetic form of amygdalin is known under the commercial name Laetrile® or as vitamin B17.
PURPOSE
This review aims to provide a comprehensive overview of studies that evaluated the potential therapeutic effects of amygdalin in oncology. Preclinical studies provided information about the mechanisms of action of amygdalin in vitro and in vivo and its toxicity. Recent in vitro studies demonstrated the effects of amygdalin on the cell cycle, apoptosis, and synthesis of cyclooxygenase-2, inducible nitric oxide synthase, E-cadherin, and integrins β1 and β4. However, amygdalin exhibited no or low treatment efficiency in preclinical in vivo studies. Conversely, many case studies describe the anti-tumor effects of amygdalin, but these have not been confirmed in clinical trials. Only two clinical studies published almost 40 years ago focused on the safety of amygdalin administered orally and intravenously. Although these studies reported that amygdalin had no benefit in 178 cancer patients, this compound has recently come to the attention of both scientists and patients. The results of recent in vitro studies are promising and indicate that amygdalin has a oncopreventive effect, although this must be confirmed by in vivo studies and clinical trials. Considering its proven toxicity and unconvincing clinical effects, amygdalin cannot currently be recommended to oncology patients as a supportive treatment.
Topics: Amygdalin; Animals; Antineoplastic Agents, Phytogenic; Humans; Neoplasms
PubMed: 31610669
DOI: 10.14735/amko2019360 -
Journal of Ethnopharmacology Sep 2024Evidence has demonstrated that Chinese medicine formula Xuefu Zhuyu decoction can markedly promote the formation of new hair in patients and mice with alopecia areata...
BACKGROUND
Evidence has demonstrated that Chinese medicine formula Xuefu Zhuyu decoction can markedly promote the formation of new hair in patients and mice with alopecia areata (AA). Amygdalin is one of the active components of Xuefu Zhuyu decoction, but its therapeutic effects and the underlying mechanisms on AA remains largely unrevealed.
PURPOSE
Therefore, this study aims to investigate the therapeutic effects and to probe its molecular mechanisms of inflammation and immune regulation on AA model of C3H/HeJ mice.
STUDY DESIGN
The C3H/HeJ female mice were divided into control, AA, rusolitinib (60 mg/kg), and amygdalin groups (60, 90, and 120 mg/kg, 0.2 ml/10 g, i.g.).
METHODS
The optical microscope was used to observe the feature of the local skin, and the number of lanugo and terminal hair. H&E staining was performed to determine the degree of pathological damage to the skin. ELISA was performed to detect levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) and interferon-γ (IFN-γ) in mice serum. Flow cytometry was carried out to analyze the CD4CD25FOXP3, CD4 and CD8 of skin tissue. And the levels of CD4 and CD8, p-JAK/JAK2, p-STAT3/STAT, and SOCS3 were detected by immunohistochemistry. Western blot and qRT-PCR were employed to examine the expression levels of IL-6, TNF-α, IFN-γ, JAK2, p-JAK, STAT, p-STAT3 and SOCS3 proteins and genes in skin tissues.
RESULTS
Compared with AA group, amygdalin immensely increased the number of vellus hairs and decreased the number of terminal hairs determined by skin microscopy and H&E staining. ELISA, Western blot and qRT-PCR data showed that the levels of IL-6, TNF-α and IFN-γ in serum and skin tissues of AA mice were significantly increased, while amygdalin administration dramatically restrained the contents of the three pro-inflammatory factors. Flow cytometry and immunohistochemistry hinted that amygdalin observably enhanced the number of CD4CD25FOXP3 and CD4 cells, while inhibited the number of CD8 positive cells in mice with AA. Moreover, amygdalin signally reduced JAK2/STAT3 pathway-related protein and gene levels in AA mice.
CONCLUSION
Amygdalin could inhibit inflammatory response and improve immune function in the treatment of AA. The underlying molecular mechanism may be related to inhibition of JAK2/STAT3 pathway.
Topics: Animals; Alopecia Areata; Janus Kinase 2; STAT3 Transcription Factor; Female; Amygdalin; Signal Transduction; Mice, Inbred C3H; Mice; Inflammation; Anti-Inflammatory Agents; Cytokines; Disease Models, Animal
PubMed: 38723918
DOI: 10.1016/j.jep.2024.118317 -
Urologie (Heidelberg, Germany) Jan 2023Alternative medicine is used instead of conventional therapy. Some patients use it in parallel with conventional medicine. (Review)
Review
BACKGROUND
Alternative medicine is used instead of conventional therapy. Some patients use it in parallel with conventional medicine.
OBJECTIVE
Narrative compilation of the evidence on alternative medicine in the (uro)oncological context.
MATERIALS AND METHODS
A selective literature search in MEDLINE via PubMed was performed.
RESULTS
The data on 3‑bromopyruvate, Miracle Mineral Supplement (MMS), insulin-potentiated therapy, base therapy, hyperthermia, Artemisia annua, amygdalin (vitamin B17), Amanita therapy, homeopathy, apitherapy, dendritic cells, galavit, Germanic new medicine, and spiritual healing show either no or little clinical evidence of efficacy or clearly exhibit a negative benefit-risk profile.
CONCLUSIONS
Alternative medicine is pseudo-medicine that may have a positive effect on mental well-being in the short term, but is mostly associated with disadvantages for the patient in the long term.
Topics: Humans; Artemisia annua; Complementary Therapies; Homeopathy; Mental Health; Urogenital Neoplasms
PubMed: 36454273
DOI: 10.1007/s00120-022-01990-6 -
Molecules (Basel, Switzerland) Jun 2023In this study, isomerization conditions, cytotoxic activity, and stabilization of amygdalin from peach kernels were analyzed. Temperatures greater than 40 °C and pHs...
In this study, isomerization conditions, cytotoxic activity, and stabilization of amygdalin from peach kernels were analyzed. Temperatures greater than 40 °C and pHs above 9.0 resulted in a quickly increasing isomer ratio (L-amygdalin/D-amygdalin). At acidic pHs, isomerization was significantly inhibited, even at high temperature. Ethanol inhibited isomerization; the isomer rate decreased with the ethanol concentration increasing. The growth-inhibitory effect on HepG2 cells of D-amygdalin was diminished as the isomer ratio increased, indicating that isomerization reduces the pharmacological activity of D-amygdalin. Extracting amygdalin from peach kernels by ultrasonic power at 432 W and 40 °C in 80% ethanol resulted in a 1.76% yield of amygdalin with a 0.04 isomer ratio. Hydrogel beads prepared by 2% sodium alginate successfully encapsulated the amygdalin, and its encapsulation efficiency and drug loading rate reached 85.93% and 19.21%, respectively. The thermal stability of amygdalin encapsulated in hydrogel beads was significantly improved and reached a slow-release effect in in vitro digestion. This study provides guidance for the processing and storage of amygdalin.
Topics: Amygdalin; Prunus persica; Isomerism; Plant Extracts; Hydrogels
PubMed: 37299025
DOI: 10.3390/molecules28114550 -
Pharmacological Research Oct 2023Community-acquired pneumonia (CAP) is one of the most common infectious diseases, and its morbidity and mortality increase with age. Resistance and mutations development...
Community-acquired pneumonia (CAP) is one of the most common infectious diseases, and its morbidity and mortality increase with age. Resistance and mutations development make the use of anti-infective therapy challenging. Chinese patent medicines (CPMs) are often used to treat CAP in China and well tolerable. However, currently there are no evidence-based guideline for the treatment of CAP with CPMs, and the misuse of CPMs is common. Therefore, we established a guideline panel to develop this guideline. We identified six clinical questions through two rounds of survey, and we then systematically searched relevant evidence and performed meta-analyses, evidence summaries and GRADE decision tables to draft recommendations, which were then voted on by a consensus panel using the Delphi method. Finally, we developed ten recommendations based on evidence synthesis and expert consensus. For the treatment of severe CAP in adults, we recommend Tanreqing injection, Reduning injection, Xuebijing injection, Shenfu injection, and Shenmai injection respectively. For the treatment of non-severe CAP in adults, we recommend Tanreqing injection, Reduning injection, Lianhua Qingwen capsule/granule, Qingfei Xiaoyan Pill and Shufeng Jiedu capsule respectively. CPMs have great potential to help in the fight against CAP worldwide, but more high-quality studies are still needed to strengthen the evidence.
PubMed: 37722517
DOI: 10.1016/j.phrs.2023.106919 -
Journal of Ethnopharmacology May 2020Amygdalin is commonly distributed in plants of the Rosaceae, such as peach, plum, loquat, apple and bayberry, but most notably in the seeds (kernels) of apricot almonds....
ETHNOPHARMACOLOGICAL RELEVANCE
Amygdalin is commonly distributed in plants of the Rosaceae, such as peach, plum, loquat, apple and bayberry, but most notably in the seeds (kernels) of apricot almonds. As a naturally aromatic cyanogenic compound, it has long been used in Asia, Europe and other regions for the treatment of various diseases including cough, asthma, nausea, leprosy and leukoderma. Importantly, in recent years, an increasing attention has been paid to its antitumor effect.
AIM OF THE STUDY
The paper aims to review the pharmacological activities and toxicological effects of amygdalin and provide a reference and perspective for its further investigation.
METHODS
Electronic databases including the Web of Science, Cochrane Library, PubMed, EMBASE, the Chinese Biological Medicine Database, China National Knowledge Infrastructure, Wanfang database and VIP information database were searched up to November 2019 to identify eligible studies. A meticulous review was performed, an in-depth analysis on the pharmacological activity and toxicology of amygdalin was conducted, and perspectives for future research were also discussed.
RESULTS
A total of 110 papers about in vitro/in vivo studies on amygdalin have been reviewed. Analysis on the data suggested that this compound presented pharmacological activities of anti-tumor, anti-fibrotic, anti-inflammatory, analgesic, immunomodulatory, anti-atherosclerosis, ameliorating digestive system and reproductive system, improving neurodegeneration and myocardial hypertrophy, as well as reducing blood glucose. In addition, studies revealed that amygdalin's toxicity was caused by its poisonous decomposite product of benzaldehyde and hydrogen cyanide after oral ingestion, toxicity of intravenous administration route was far less than the oral route, and it can be avoidable with an oral dose ranging from 0.6 to 1 g per day.
CONCLUSION
This paper has systematically reviewed the pharmacology and toxicology of amygdalin and provided comprehensive information on this compound. We hope this review highlights some perspectives for the future research and development of amygdalin.
Topics: Amygdalin; Animals; Humans; Medicine, Traditional
PubMed: 32114166
DOI: 10.1016/j.jep.2020.112717 -
Current Molecular Pharmacology Oct 2021Cell adhesion, as dynamic interactions between cell-cell and cell-matrix, has an essential role in cancer cell migration. Integrins as cell membrane receptors are...
BACKGROUND
Cell adhesion, as dynamic interactions between cell-cell and cell-matrix, has an essential role in cancer cell migration. Integrins as cell membrane receptors are involved in cell adhesion and signal transduction. Aberrant expression of integrins is associated with the cancer cell adhesion.
OBJECTIVE
Targeting the process of cell adhesion and migration could be helpful to prevent cancer cell metastasis. Amygdalin is a cyanoglycoside compound with anti-cancer properties, while its effect on cancer cell adhesion is not completely clear.
METHODS
The cytotoxic effect of amygdalin on breast cancer cell lines (MCF-7 and MDA-MB- 231) and human skin fibroblast cell line as a normal cell, was evaluated through MTT assay. The cell adhesion assay and wound healing assay were performed to determine amygdalin effects on adhesion and migration of cancer cells. Further analysis was carried out to evaluate integrin α and β levels through real-time PCR.
RESULTS
We demonstrated that amygdalin diminished the cell viability of both cell lines in a time and dose-dependent manner, while amygdalin did not have any toxicity on the human skin fibroblast cell line in the same dosages. Following amygdalin treatment, the adhesion of both studied cell lines to fibronectin and collagen I decrease, and this reduction is significantly greater in the case of binding to fibronectin compared to binding to collagen. The MDA-MB-231 cell migration was decreased greater than MCF-7 cells. The levels of α and β integrin were differentially regulated by amygdalin in both cancer cell lines.
CONCLUSION
These results suggest that depending on cancer cell lines, amygdalin affects cancer cell adhesion and migration.
Topics: Amygdalin; Breast Neoplasms; Cell Adhesion; Cell Line, Tumor; Cell Movement; Female; Humans; Integrins; MCF-7 Cells
PubMed: 32778045
DOI: 10.2174/1874467213666200810141251 -
International Journal of Molecular... Sep 2023Cancer 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... (Review)
Review
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.
PubMed: 37762572
DOI: 10.3390/ijms241814270 -
Frontiers in Pharmacology 2022Amygdalin is a naturally occurring glycoside used in traditional Chinese medicine and is known to have anti-cancer properties. Even though the anti-cancer properties of...
Amygdalin is a naturally occurring glycoside used in traditional Chinese medicine and is known to have anti-cancer properties. Even though the anti-cancer properties of amygdalin are well known, its effect on normal cells has not been thoroughly investigated. The aim of the present study was to investigate a possible chemo-protective role of amygdalin against the cytotoxic effects of chemotherapy for normal human cells. Specifically, it was tested in combination with a strong chemotherapeutic drug cisplatin. Human non-tumorigenic MCF12F epithelial cell line, human fibroblasts cells, human breast cancer MCF7 and MDA-MB-231 cells were treated with cisplatin in a dose- and time-depended manner in the absence or presence of amygdalin. When MCF12F cells and fibroblasts underwent pre-treatment with amygdalin followed by cisplatin treatment (24 h amygdalin + 24 h cisplatin), the cell viability was increased (22%, < 0.001) as indicated using MTT assay. As attested by flow cytometry, combination treatment was associated with decreased the percentage of late apoptotic cells compared with monotherapy (fold-change of decrease = 1.6 and 4.5 for 15 and 20 μΜ, respectively). Also, the proteins expression of PUMA, p53, phospho-p53 and Bax decreased, when a combination treatment was used vs. cisplatin alone, while the proapoptotic proteins Bcl-2 and Bcl-xL exhibited an increased tendency in the presence of amygdalin. Moreover, the levels of pro-apoptotic genes , , and mRNA were significantly downregulated (∼83%, ∼66%, and ∼44%, respectively) vs. cisplatin alone, while the mRNA levels of anti-apoptotic genes and were upregulated (∼44.5% and ∼51%, respectively), vs. cisplatin alone after 24 h of combination treatment. The study on the Combination index (CI) assay indicated that amygdalin could be possibly considered as an antagonist to cisplatin (2.2 and 2.3) for MCF12F and fibroblast cells, respectively. In contrast, for the breast cancer MCF7 and MDA-MB-231 cells, amygdalin and cisplatin indicated a synergistic effect (0.8 and 0.65), respectively. Our present findings suggest that amygdalin has chemo-modulatory effect when used in co-treatment with cisplatin and is able to protect normal breast cells as well as the fibroblasts during chemotherapy treatment, indicating a strong selective chemoprotective ability and may contribute to a better quality of life for cancer patients.
PubMed: 36204233
DOI: 10.3389/fphar.2022.1013692 -
Journal of AOAC International Mar 2023Cyanogenic glycosides are secondary metabolites in plants. In almonds and apricot kernels, amygdalin is an abundant cyanogenic glycoside. Upon consumption, amygdalin is...
BACKGROUND
Cyanogenic glycosides are secondary metabolites in plants. In almonds and apricot kernels, amygdalin is an abundant cyanogenic glycoside. Upon consumption, amygdalin is enzymatically metabolized into hydrogen cyanide. Depending on the number of kernels consumed and the amygdalin concentration, ingestion of amygdalin-containing kernels may result in adverse effects. To better understand the US marketplace, the development and validation of analytical methods to reliably measure amygdalin in apricot kernels and almonds is needed to support the collection of occurrence and consumption data in retail products.
OBJECTIVE
The aim of this study was to develop and validate a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the quantitation of amygdalin in apricot kernels and almonds following the U.S. Food and Drug Administration (FDA). Foods Program Guidelines for the Validation of Chemical Methods, 3rd Edition.
METHODS
Apricot kernels and almonds were cryogenically homogenized and extracted using methanol containing an internal standard (IS), geniposide, followed by filtration, dilution, and LC-MS/MS analysis. Matrix effects were minimized using dilution. Quantitation was achieved using an external, solvent-based calibration.
RESULTS
The amygdalin response was linear (r2 > 0.99) over a range of 0.05-50 µg/mL. The recovery of amygdalin spiked at 10-10 000 µg/g in sweet apricot kernels, raw almond, and dry-roasted almond ranged from 90 to 107% with RSDs ≤6%. The method limit of detection and limit of quantitation was 0.8 and 2.5 ng/g, respectively. Amygdalin concentrations in 18 market samples ranged from 2 to 24 000 µg/g. Corresponding estimates of cyanide concentration ranged from 0.2 to 1420 µg/g.
CONCLUSIONS
Method performance meets the acceptance criteria defined by FDA guidelines and is fit for purpose for the analysis of amygdalin in apricot kernels and almonds.
HIGHLIGHTS
An LC-MS/MS method is developed for the quantification of amygdalin in apricot kernels and almonds.
Topics: Amygdalin; Prunus armeniaca; Chromatography, Liquid; Prunus dulcis; Tandem Mass Spectrometry
PubMed: 36453858
DOI: 10.1093/jaoacint/qsac154