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Chinese Journal of Integrative Medicine Jun 2022To screen the active components from Fuzheng Huayu Recipe (FZHY) and redesign a new recipe composed of the active components, and validate the effect of active...
OBJECTIVE
To screen the active components from Fuzheng Huayu Recipe (FZHY) and redesign a new recipe composed of the active components, and validate the effect of active components formulation from FZHY against liver fibrosis.
METHODS
Thirty-two components from FZHY were evaluated for their activities against liver fibrosis respectively, with 6 kinds of cell models in vitro, including oxidative stressed hepatocyte in L-02, hypoxia injured/proliferative hepatic sinusoidal endothelial cells in SK-HEP-1 and human hepatic sinusoidal endothelial cells (HHSEC), and activated hepatic stellate cell in LX-2. The comprehensive activity of each component against liver fibrosis was scored according to the role of original herbs in FZHY and cell functions in fibrogenesis. Totally 7 active components were selected and combined with equal proportion to form a novel active components formulation (ACF). The efficacy of ACF on liver fibrosis were evaluated on activation of LX-2 and proliferation of HHSEC in vitro and in liver fibrosis model mice induced by dimethylnitrosamine (DMN). Totally 72 mice were divided into 6 groups using a random number table, including normal, high-dose ACF control (20 µ mol/L × 7 components/kg body weight), model, low-, medium-, high-dose ACF groups (5, 10, 20 µ mol/L × 7 components/kg body weight, respectively). Hematoxylin eosin and Sirius red stainings were used to observe inflammation and fibrosis change of liver tissue; scanning electron microscopy (SEM) and transmission electron microscopy (TEM) were utilized to observe the effect of ACF on ultrastructure of hepatic sinusoids.
RESULTS
Fifteen components from FZHY showed higher scores for their activity on against liver fibrosis. Among them, 7 components including tanshinone II A, salvianolic acid B, cordycepin, amygdalin, quercetin, protopanaxatriol, and schizandrin B were recombined with equal proportions to form ACF. ACF at 1,2, 4 µ mol/L showed strong inhibitory effects on activation of LX-2 and proliferation of HHSEC in vitro (all P<0.01). Compared with the model group, ACF attenuated liver collagen deposition, improved sinusoidal capillarization in a dose-dependent manner (all P<0.05).
CONCLUSION
ACF exerts a satisfactory effect against experimental liver fibrosis and attenuates sinusoidal capillarization, which warrant a further research and development for herbal components formulation on liver fibrosis.
Topics: Animals; Body Weight; Drugs, Chinese Herbal; Endothelial Cells; Liver; Liver Cirrhosis; Mice
PubMed: 34581939
DOI: 10.1007/s11655-021-3293-x -
Frontiers in Plant Science 2021Amygdalin, 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...
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 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 and . This study expands the understanding of amygdalin in almond resources and provides the direction for the regulation of amygdalin.
PubMed: 35154172
DOI: 10.3389/fpls.2021.753151 -
Biomolecules Feb 2022Bone diseases such as osteoporosis are the result of osteoclast over-activation. There are many therapeutic agents from natural compounds inhibiting the formation of...
Bone diseases such as osteoporosis are the result of osteoclast over-activation. There are many therapeutic agents from natural compounds inhibiting the formation of osteoclast that have been reported and are continuously being interested. Amygdalin (AD) is isolated from seeds of L. which has many pharmaceutical effects; however, the effect of AD on osteoclast formation and function remains unknown. Therefore, the underlying mechanism of AD on RANKL-induced osteoclast in RAW 264.7 cells was investigated. Molecular docking simulation revealed that AD can bind to the active sites of RANKL with negative binding affinities. Through TRAP activity, bone resorption, and migration, AD effectively inhibited osteoclast differentiation and function. Expression of transcription factors, such as NFATc1, c-fos, and osteospecific genes (including , , , and results) showed an osteoclast differentiated inhibitory effect by AD treatment. In addition, RANKL-induced activation of MAPK, ER stress, and ROS levels in RANKL-induced osteoclast was significantly inhibited while antioxidant enzymes were recovered in the presence of AD. These results suggest that AD may be a potential candidate derived from natural sources for the treatment of osteoclast bone-related diseases.
Topics: Amygdalin; Cell Differentiation; Down-Regulation; Molecular Docking Simulation; NFATC Transcription Factors; Osteoclasts
PubMed: 35204757
DOI: 10.3390/biom12020256 -
Environmental and Molecular Mutagenesis Jun 2023Amygdalin (AMY), a plant secondary metabolite containing nitrile, is a major component of the seeds of Rosaceae family plants. It is known that this compound has many...
Amygdalin (AMY), a plant secondary metabolite containing nitrile, is a major component of the seeds of Rosaceae family plants. It is known that this compound has many pharmacological activities such as cancer prevention, antipyretic, and cough suppressant. In this study, the genotoxic and modulatory effects of amygdalin were assessed by chromosomal aberration (CA), sister chromatid exchange (SCE), and cytokinesis-block micronucleus assay (CBMN) assays using human peripheral lymphocytes (HPLs) in the absence and presence of metabolic activator (S9 mix). Lymphocytes were exposed to various concentrations of amygdalin (0.86, 1.72, 3.43, 6.86, and 13.75 μg/mL) alone and in combination with mitomycin-C (MMC, 0.20 μg/mL) or cyclophosphamide (CP, 12 μg/mL). The mitotic index (MI), replication index (RI), cytokinesis-block proliferation index (CBPI), and cytostasis were also evaluated to determine cytotoxicity. Amygdalin alone did not exhibit genotoxic and cytotoxic effects at all the tested concentrations both in the absence and presence of the S9 mix. In contrast, amygdalin significantly reduced the frequencies of CA (especially at 48 h treatments), SCE, and MN (except 0.86 μg/mL in pre- and simultaneous treatment) induced by MMC in all the tested concentrations and treatment protocols. It has also considerably decreased CP-induced CA and SCE frequencies at all the concentrations (except 0.86 μg/mL) in simultaneous treatment. This study demonstrated that amygdalin alone was not genotoxic, on the contrary, it has revealed modulatory effects against chemotherapy agents that induced genomic damage in human lymphocytes, suggesting its chemopreventive potential.
Topics: Humans; Amygdalin; Mutagens; Lymphocytes; Micronucleus Tests; Chromosome Aberrations; Cells, Cultured
PubMed: 37161892
DOI: 10.1002/em.22543 -
Journal of Medicinal Food Nov 2021Osteosarcoma has a poor prognosis and survival rate due to inadequate chemotherapy, high recurrence ability, high metastasis potential, and almost no radiotherapy being...
Osteosarcoma has a poor prognosis and survival rate due to inadequate chemotherapy, high recurrence ability, high metastasis potential, and almost no radiotherapy being applied. One of the strategies to solve these problems is to develop the pharmacologically active plant metabolite, amygdalin, in combination therapeutic systems. In this project, the antiproliferative effects of amygdalin alone and in binary or ternary combinations with some anticancer drugs (cisplatin, 5-fluorouracil, oxaliplatin, and camptothecin), antiparasitic drugs (metronidazole and miltefosine), and an antigout drug (colchicine) were examined using human bone osteosarcoma cell lines (MG-63 and Saos2), the chondrosarcoma cell line (SW1353), and the normal human cell line (FL). Known half-maximal inhibitory concentration values of the drugs were taken into consideration, and the recommended combination ratios were used in the Chou-Talalay method. The strong synergistic effect commonly seen in the combination of amygdalin with miltefosine, metronidazole, camptothecin, colchicine, oxaliplatin, 5-fluorouracil, and cisplatin dual drug indicates that these combinations can be used in cancer treatment. The synergistic effect caused by amygdalin decreases toxicity by increasing drug yield. However, amygdalin antagonism seen in several combinations may prevent these pairs from being used together. In combination with antagonistic effects, it may be preferable to use amygdalin alone as it generally causes strong antiproliferative effects. Besides, there is a more potent synergism between amygdalin and triple drug combinations. Overall, these results emphasize that amygdalin combinations in treatment of bone cancer are significant.
Topics: Amygdalin; Antiparasitic Agents; Camptothecin; Humans; Oxaliplatin; Pharmaceutical Preparations
PubMed: 33733877
DOI: 10.1089/jmf.2020.0143 -
Molecules (Basel, Switzerland) Jun 2023Given that cancer is a disease that is rampant in the world and especially in Africa, where the population has enormous difficulty treating it, plants are a safer and...
Given that cancer is a disease that is rampant in the world and especially in Africa, where the population has enormous difficulty treating it, plants are a safer and less expensive alternative. Cassava is a plant species valued in Benin because of its numerous medicinal and nutritional virtues. This study evaluated the biological activities of amygdalin from the organs of three cassava varieties most commonly produced in Benin (BEN, RB, and MJ). HPLC analysis was used to quantify amygdalin in cassava organs and derivatives. Phytochemical screening was performed to determine secondary metabolite groups. DPPH and FRAP methods were used to assess antioxidant activity. Cytotoxicity of the extracts was tested on larvae. The anti-inflammatory activity was evaluated in vivo in an albino mouse paw edema model induced by 5% formalin. The anticancer activity was evaluated in vivo on Wistar rats rendered cancerous by 1,2-dimethylhydrazine (DMH) using 5-fluorouracil as a reference molecule. The results showed that the organs of all three-cassava varieties contained glycosides, flavonoids, saponosides, steroids, tannins, coumarins, and cyanogenic derivatives. Young stems and fresh cassava leaves had the highest amygdalin concentrations, with 11,142.99 µg 10 g and 9251.14 µg 10 g, respectively. The derivative was more concentrated in amygdalin, with a content of 401.56 µg 10 g than the other derivatives. The antioxidant activity results showed that the amygdalin extracts were DPPH radical scavengers with IC values ranging from 0.18 mg mL to 2.35 mg mL. The cytotoxicity test showed no toxicity of the extracts toward shrimp larvae. Administration of amygdalin extracts from the leaves of BEN and MJ varieties prevents inflammatory edema. The percentages of edema inhibition varied between 21.77% and 27.89%. These values are similar ( > 0.05) to those of acetylsalicylic acid (25.20%). Amygdalin extract of the BEN variety significantly ( < 0.0001) reduces edema. Both BEN extracts inhibited cancer induction with DMH. In preventive and curative treatments, rats fed with amygdalin extracts showed low anti-cancer activity under the effect of DMH and a significant difference in biochemical results. Thus, the organs of all three cassava varieties studied have secondary metabolites and good antioxidant activity. The leaves contain high levels of amygdalin and can be used as anti-inflammatory and anticancer agents.
Topics: Rats; Animals; Antioxidants; Plant Extracts; Manihot; Amygdalin; Benin; Rats, Wistar; Anti-Inflammatory Agents; Edema
PubMed: 37299029
DOI: 10.3390/molecules28114548 -
Anti-cancer Agents in Medicinal... 2021Despite significant advances in therapeutic interventions, liver cancer is the leading cause of cancer mortality in the world. Potential phytochemicals have shown to be...
BACKGROUND
Despite significant advances in therapeutic interventions, liver cancer is the leading cause of cancer mortality in the world. Potential phytochemicals have shown to be promising agents against many life-threatening diseases because of their low toxicity and potential effectiveness.
OBJECTIVE
The current study aims to conduct an in vitro investigation of the anticancer activity of Apricot Extract (AE) and Amygdalin Containing Fraction (ACF), additionally studying their therapeutic effects on DMBAinduced liver carcinogenesis mice model to highlight their related biochemical and molecular mechanisms.
METHODS AND RESULTS
Amygdalin was isolated from the seeds of P. armeniaca L. Male mice received AE or ACF, DMBA, DMBA+AE, DMBA+ACF, and vehicles. The oxidative stress and antioxidant markers, cell proliferation by flow cytometric analysis of Proliferating Cell Nuclear Antigen (PCNA) expression, angiogenesis marker (VEGF), inflammatory marker (TNF-α), apoptotic, anti-apoptotic and autophagy genes expression (caspase-3, Bcl-2, and Beclin-1) were investigated. AE and ACF were found to stimulate the apoptotic process by up-regulating caspase-3 expression and down-regulating Bcl-2 expression. They also reduced VEGF and PCNA levels and increased the antioxidant defense system. Moreover, AE and ACF treatments also inhibited HepG2 and EAC cell proliferation and up-regulated Beclin-1 expression.
CONCLUSION
This study provides evidence that, in DMBA-induced hepatocarcinogenesis, the key proteins involved in the proliferation, angiogenesis, autophagy, and apoptosis are feasible molecular targets for hepatotherapeutic potential using AE and ACF.
Topics: Amygdalin; Animals; Antineoplastic Agents, Phytogenic; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Hep G2 Cells; Humans; Liver Neoplasms; Liver Neoplasms, Experimental; Male; Mice; Mitochondria; Molecular Structure; Plant Extracts; Prunus armeniaca; Seeds; Structure-Activity Relationship
PubMed: 32510292
DOI: 10.2174/1871520620666200608124003 -
Emergency Medicine Australasia : EMA May 2024Vitamin B17 tablets are sold (online) as an alternative cancer therapy medication. Its use however is not benign, given that it is metabolised into hydrogen cyanide. We...
OBJECTIVE
Vitamin B17 tablets are sold (online) as an alternative cancer therapy medication. Its use however is not benign, given that it is metabolised into hydrogen cyanide. We aimed to measure the number of calls received by the New South Wales Poisons Information Centre (NSW PIC) regarding Amygdalin exposures.
METHODS
A retrospective review of all amygdalin/cyanogenic glycoside product ingestion exposure calls to NSW PIC between 2015 and 2022.
RESULTS
There were 120 unique exposure calls. Eighty-two (68%) were regarding minor exposures, with the remaining 38 (32%) of calls involving patients who had either a signifcant history or symptoms to prompt referral to hospital or were already seeking advice from a treating hospital clinican.
CONCLUSION
There is a significant burden of concern generated from the misuse of cyanogenic glycoside products for cancer prevention and treatment, which can result in hospital admission carrying significant health risk and expenditure.
PubMed: 38807508
DOI: 10.1111/1742-6723.14450 -
Critical Reviews in Food Science and... 2023Food processing, especially the juice industry, is an important sector that generate million tons of residues every. Due to the increasing concern about waste generation... (Review)
Review
Food processing, especially the juice industry, is an important sector that generate million tons of residues every. Due to the increasing concern about waste generation and the interest in its valorization, the reutilization of by-products generated from the processing of popular fruits of the genus (rich in high-added value compounds) has gained the spotlight in the food area. This review aims to provide an overview of the high added-value compounds found in the residues of fruits (peach, nectarine, donut peach, plum, cherry, and apricot) processing and applications in the food science area. Collective (pomace) and individual (kernels, peels, and leaves) residues from fruits processing contains polyphenols (especially flavonoids and anthocyanins), lipophilic compounds (such as unsaturated fatty acids, carotenes, tocopherols, sterols, and squalene), proteins (bioactive peptides and essential amino acids) that are wasted. Applications are increasingly expanding from the flour from the kernels to encapsulated bioactive compounds, active films, and ingredients with technological relevance for the quality of bread, cookies, ice cream, clean label meat products and extruded foods. Advances to increasing safety has also been reported against anti-nutritional (amygdalin) and toxic compounds (aflatoxin and pesticides) due to advances in emerging processing technologies and strategic use of resources.
Topics: Fruit; Prunus; Antioxidants; Anthocyanins; Polyphenols
PubMed: 35285755
DOI: 10.1080/10408398.2022.2050350 -
Experimental Dermatology Nov 2021Psoriasis is a chronic inflammatory skin disease without cure. Systemic and biological therapies are the most effective treatments for patients with severe psoriasis....
Psoriasis is a chronic inflammatory skin disease without cure. Systemic and biological therapies are the most effective treatments for patients with severe psoriasis. However, these drugs can cause serious side effects from extended use. Safe and effective topical drugs are needed to decrease psoriatic plaques and reduce the risk of adverse effects. Amygdalin analogues are stable small molecules that showed benefits in psoriasis xenografts to immune-deficient mice by systemic application. However, whether topical application of these amygdalin analogues could reduce the progression of the psoriatic phenotype in an immune-competent organism is unknown. Here, we analyse the efficiency of topical application of an amygdalin analogue cream on a well-established genetic and immune-competent mouse model of psoriasis. Topical application of an amygdalin analogue cream ameliorates psoriasis-like disease in mice, reduces epidermal hyperplasia and skin inflammation. Amygdalin analogue treatment leads to reduced expression of local pro-inflammatory cytokines, but systemic pro-inflammatory cytokines that are highly expressed in psoriasis patients such as IL-17A, IL6 or G-CSF are also decreased. Furthermore, expression of important mediators of psoriasis initiation and epidermal hyperplasia, such as TNFa, S100A9 and TSLP, is decreased in lesional epidermis after amygdalin analogue treatment. In conclusion, we show that amygdalin analogue reduces the proliferative capacity of psoriasis-like stimulated keratinocytes and their inflammatory response in vivo and in vitro. These results suggest that topical application of amygdalin analogues may represent a safe and effective treatment for psoriasis.
Topics: Administration, Topical; Amygdalin; Animals; Cell Proliferation; Disease Models, Animal; Dosage Forms; Keratinocytes; Mice; Psoriasis
PubMed: 33998705
DOI: 10.1111/exd.14390