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Frontiers in Pharmacology 2021Advanced liver fibrosis can lead to cirrhosis, resulting in an accelerated risk of hepatocellular carcinoma and liver failure. Fuzheng Huayu formula (FZHY) is a...
Advanced liver fibrosis can lead to cirrhosis, resulting in an accelerated risk of hepatocellular carcinoma and liver failure. Fuzheng Huayu formula (FZHY) is a traditional Chinese medicine formula treated liver fibrosis in China approved by a Chinese State Food and Drug Administration (NO: Z20050546), composed of bge., (Carr.) Franch., cultured (BerK.) Sacc. Mycelia, (Turcz.) Baill., Lamb., and (Thunb.) Makino. However, the main active substances and mechanism of FZHY are unclear. The aim of this study is to identify a novel anti-fibrotic compound, which consists of the main active ingredients of FZHY, and investigate its mechanism of pharmacological action. The main active ingredients of FZHY were investigated by quantitative analysis of FZHY extracts and FZHY-treated plasma and liver in rats. The anti-fibrotic composition of the main active ingredients was studied through uniform design , and its mechanism was evaluated in carbon tetrachloride (CCl)- and bile duct ligation (BDL)-induced liver fibrosis models in rats and mice, and transforming growth factor beta 1-induced LX-2 cell activation model . A novel Chinese medicine, namely JY5 formula, consisting of salvianolic acid B, schisantherin A, and amygdalin, the main active ingredients of FZHY, significantly alleviated hepatic hydroxyproline content and collagen deposition in CCl-and BDL-induced fibrotic liver in rats and mice. In addition, JY5 inhibited the activation of hepatic stellate cells (HSCs) by inactivating Notch signaling and . In this study, we found a novel JY5 formula, which exerted anti-hepatic fibrotic effects by inhibiting the Notch signaling pathway, consequently suppressing HSCs activation. These results provide an adequate scientific basis for clinical research and application of the JY5 formula, which may be a potential novel therapeutic candidate for liver fibrosis.
PubMed: 34630075
DOI: 10.3389/fphar.2021.671152 -
Heliyon Nov 2023Cancer recurrence following surgery is a serious and worrying problem for the patient. Common treatment strategies, such as chemotherapy, radiotherapy, and surgery, are...
Cancer recurrence following surgery is a serious and worrying problem for the patient. Common treatment strategies, such as chemotherapy, radiotherapy, and surgery, are restricted because of low uptake of the drugs, poor pharmacokinetic properties, and toxicity issues for healthy tissues. The development of engineering platforms for improving the postoperative treatment of cancer can help solve this problem. In this study, the ceria-tannic acid nanoparticles (CeTA-NPs) were successfully synthesized and characterized. Chitosan-polyvinyl/alcohol (S-PVA) hydrogels containing CeTA NPs (S-PVA/CeTA) and amygdalin as an anticancer substance were fabricated using freeze-thaw and immersion-drying techniques. The swelling and degradation behaviors, antibacterial activity, and biocompatibility of as-prepared hydrogel were done. The apoptotic effects of amygdalin/CS-PVA/CeTA hydrogel were evaluated by flow cytometry technique on a human colorectal cancer (SW-480) cell line. The CeTA-NPs were investigated as antibacterial and cross-linker agents for greater stability of the hydrogel network. The S-PVA/CeTA hydrogel demonstrated good safety and antibacterial activity. The results of swelling and biodegradation suggest that S-PVA/CeTA hydrogels can inspire long-time application. The anticancer effects of the amygdalin/CS-PVA/CeTA hydrogel were confirmed by apoptosis results. Hence, amygdalin/CS-PVA/CeTA hydrogel can be a promising candidate for long-time biomedical application.
PubMed: 38027646
DOI: 10.1016/j.heliyon.2023.e21835 -
ACS Omega Mar 2022Amygdalin is an effective component of the traditional Chinese medicine bitter almond, peach kernel, and plum kernel. It has pharmacological effects, such as relieving...
Amygdalin is an effective component of the traditional Chinese medicine bitter almond, peach kernel, and plum kernel. It has pharmacological effects, such as relieving cough and asthma. In a study of the crystallization process, we found a series of solvatomorphs of amygdalin (including hydrate). Interestingly, in the structures of these solvatomorphs, the same characteristic structural fragment is present, that is, amygdalin dihydrate. Multiple analytical techniques were used to characterize the solvatomorphs, such as X-ray diffraction and thermogravimetry-mass spectrometry. Void calculations of water and solvent were used to analyze the occupied volume in the unit cell of the corresponding solvatomorphs to explain the formation mechanism of the solvatomorphs from the perspective of space. To elucidate the formation mechanism of the solvatomorphs with this kind of characteristic structure from the perspective of energy, theoretical calculations based on density functional theory were applied, such as energy decomposition and molecular electrostatic potential surfaces. In addition, the transformation phenomenon between these solvatomorphs and amygdalin was identified, and the transformation pathways are described in detail.
PubMed: 35309495
DOI: 10.1021/acsomega.1c07314 -
Frontiers in Microbiology 2022Amygdalin (Amy) is metabolized into cyanide , which may lead to fatal poisoning after oral administration. The defense mechanisms against toxic cyanide have not yet been...
Amygdalin (Amy) is metabolized into cyanide , which may lead to fatal poisoning after oral administration. The defense mechanisms against toxic cyanide have not yet been adequately studied. In this study, comparative toxicokinetics study of Amy was performed in normal and pseudo germ-free rats. The efficiency of cyanide release was significant higher in normal group when given a single oral dose of 440 mg/kg (50% median lethal dose). Thiocyanate, the detoxification metabolite, was firstly detected in feces, caecum, and intestinal microbiota incubation enzymic system. The results suggest intestinal microbiota is involved in bidirectional regulation of toxicity and detoxification of Amy. We further identified the species related to cyanogenesis of Amy with metagenomic sequencing, such as , , and . Functional analysis of microbiota reveals the detoxification potential of intestinal microbiota for cyanide. Sulfurtransferase superfamily, such as rhodanese, considered as main detoxification enzymes for cyanide, are largely found in , , , etc. Besides, cyanoamino acid metabolism pathway dominated by may contribute to the detoxification metabolism of cyanide. In summary, intestinal microbiota may be the first line of defense against the toxicity induced by Amy.
PubMed: 36504787
DOI: 10.3389/fmicb.2022.1030516 -
Insects Oct 2022(Busck) (Lepidoptera: Tortricidae), Oriental fruit moth (OFM), attacks fruits and shoots of the economically important trees in Rosaceae. Amygdalin is a cyanogenic...
(Busck) (Lepidoptera: Tortricidae), Oriental fruit moth (OFM), attacks fruits and shoots of the economically important trees in Rosaceae. Amygdalin is a cyanogenic glucoside of rosaceous plants that may be related to the seasonal patterns of infestation in many pests. The amygdalin concentration of fruits and shoots of peach, pear, and apple varies over the growing season. However, the relationship between the amygdalin concentration and performance has not been reported. Here, we measured the performance (feeding, growth, development, and fecundity) of larvae (as subsequent adults) reared on artificial diets with six amygdalin concentrations (0, 3, 6, 12, 24, and 48 mg/g), and we then calculated the population parameters. We found that these different concentrations of amygdalin affected the developmental time and fecundity, except for the proportion of larvae feeding on the diet and the survival rates of larvae and pupae. When compared with the control diet without amygdalin, diets with 3 or 6 mg/g (low and moderate concentrations) of amygdalin shortened developmental times and increased the number of eggs laid by females; however, a diet with 12 mg/g (moderate concentration) of amygdalin only increased the number of eggs laid by females and did not affect the larval and pupal developmental rate. A diet with 48 mg/g (high concentration) of amygdalin prolonged developmental times and reduced the number of eggs laid by females when compared with the control diet without amygdalin. Furthermore, the intrinsic rate of increase (r) for insects reared on diets with 3 or 6 mg/g (low and moderate concentrations) of amygdalin versus the control diet without amygdalin showed a slightly improved population growth. However, this increase in the r value did not persist over ten successive generations of rearing on the same diet. We concluded that the diet with 6 mg of amygdalin per g of diet can enhance the performance and population growth of , but the effects of amygdalin are concentration-dependent.
PubMed: 36354798
DOI: 10.3390/insects13110974 -
Saudi Journal of Biological Sciences Sep 2020Amygdalin a naturally occurring compound, predominantly in the bitter kernels of apricot, almond, apple and other members of Rosaceae family. Though, amygdalin is used...
Amygdalin a naturally occurring compound, predominantly in the bitter kernels of apricot, almond, apple and other members of Rosaceae family. Though, amygdalin is used as an alternative therapy to treat various types of cancer but its role in cancer pathways has rarely been explored yet. Therefore, present study was intended with the aim to investigate the alleged anti-cancerous effects of amygdalin specifically on PI3K-AKT-mTOR and Ras pathways of cancer in human body. Computational modelling and simulation techniques were used to assess the effect of amygdalin on PI3K-AKT-mTOR and Ras pathways using different level of dosage. It was observed that amygdalin had direct and substantial contribution to regulate PI3K-mTOR activities on threshold levels while the other caner pathways were effected indirectly. Consequently, amygdalin is a down-regulator of a cancer within a specified amount and contribute considerably to reduce various types of cancer in human. Furthermore, and analyses of amygdalin could be of helpful to authenticate its pharmacological effects.
PubMed: 32884428
DOI: 10.1016/j.sjbs.2020.06.041 -
Molecules (Basel, Switzerland) Nov 2022Breast cancer is the most diagnosed cancer among women, and its incidence and mortality are rapidly growing worldwide. In this regard, plant-derived natural compounds...
BACKGROUND
Breast cancer is the most diagnosed cancer among women, and its incidence and mortality are rapidly growing worldwide. In this regard, plant-derived natural compounds have been shown to be effective as chemotherapeutic and preventative agents. Apricot kernels are a rich source of nutrients including proteins, lipids, fibers, and phenolic compounds and contain the aromatic cyanogenic glycoside amygdalin that has been shown to exert a cytotoxic effect on cancer cells by affecting the cell cycle, inducing apoptosis, and regulating the immune function.
METHODS
Here, we describe a previously unexplored proapoptotic mechanism of action of amygdalin in breast cancer (MCF7) cells that involves the modulation of intracellular proteolysis. For comparative purposes, the same investigations were also conducted upon cell treatment with two apricot kernel aqueous extracts from L.
RESULTS
We observed that both the 20S and 26S proteasome activities were downregulated in the MCF7 cells upon 24 h treatments. Simultaneously, the autophagy cascade resulted in being impaired due to cathepsin B and L inhibition that also contributed to a reduction in cancer cell migration. The inhibition of these proteolytic systems finally promoted the activation of apoptotic events in the MCF7 cells.
CONCLUSION
Collectively, our data unveil a novel mechanism of the anticancer activity of amygdalin, prompting further investigations for potential application in cancer preventative strategies.
Topics: Female; Humans; Amygdalin; Proteolysis; Breast Neoplasms; Prunus armeniaca; Apoptosis
PubMed: 36364419
DOI: 10.3390/molecules27217591 -
Establishment of a Sonotrode Ultrasound-Assisted Extraction of Phenolic Compounds from Apple Pomace.Foods (Basel, Switzerland) Nov 2022Apple pomace is the main by-product from apple processing in the juice industry and is considered a source of polyphenols with several health bioactivities. Thus, this...
Apple pomace is the main by-product from apple processing in the juice industry and is considered a source of polyphenols with several health bioactivities. Thus, this research focuses on the establishment of the ultrasound-assisted extraction of total phenolic compounds, focusing on phloretin and phloridzin, with high antioxidant activity from apple pomace, using a sonotrode. We used a Box-Behnken design of 15 experiments with 3 independent factors (ethanol (%), time (min) and amplitude (%)). The responses evaluated were the sum of phenolic compounds, phloretin and phloridzin measured by HPLC-MS-ESI-TOF, and antioxidant activity measured by DPPH, ABTS and FRAP. The validity of the model was confirmed by ANOVA. Further, it was carried out using a comparison between different apple pomaces with or without seeds extracted by the optimal conditions. Phloretin and phloridzin accounted for 7 to 32% of the total phenolic compounds in the apple pomaces. Among all the apple pomace analyzed, that of the variety Gala had the highest phenolic content and antioxidant activity. The presence of the cyanogenic compound amygdalin was detected in apple pomaces that contained seeds accompanied with a higher content of phloretin and phloridzin but a lower content of flavan-3-ols.
PubMed: 36496617
DOI: 10.3390/foods11233809 -
Saudi Journal of Biological Sciences Jan 2020Phytochemical composition, in vitro antioxidant and antiproliferative activity against HepG2 cells were studied in the kernels of apricot cultivars grown in the northern...
Phytochemical composition, in vitro antioxidant and antiproliferative activity against HepG2 cells were studied in the kernels of apricot cultivars grown in the northern areas of Pakistan. Relatively, the kernel of Habbi cultivar/AP-12 depicted significant potential to scavenge DPPH and ABTS+ free radicals as well as oxygen radical absorbance capacity along with highest contents of total flavonoids, phenolics, chlorogenic and syringic acids on dry weight basis. The average concentration of quercetin ranged 0.072-1.343 mg/100 g, and of EGCG from 0.713 to 6.521 mg/100 g with maximum concentration in Hulappa/AP-3 and Kho Chali-Khatta 3/AP-17, respectively. Amygdalin content was highest (1145 mg/100 g) in the kernel of Balaani/AP-14. Highest inhibition of HepG2 cells was found in the kernel of Waflu Chuli/AP-9 (EC50 = 15.70 ± 3.77 mg/mL). The PCA showed significant contributions of polyphenols and flavonoids towards biochemical assays, while CA revealed similarities and associations among various cultivars. Our study revealed that Habbi, Waflu Chuli, Thukdeena and Balaani kernels are rich sources of bioactive compounds and possess significant antioxidant and anticancer activity and can contribute considerably in the prevention and treatment of chronic health disorders.
PubMed: 31889831
DOI: 10.1016/j.sjbs.2019.06.013 -
Stem Cells International 2020Chondrogenesis and subsequent osteogenesis of mesenchymal stem cells (MSCs) and angiogenesis at injured sites are crucial for bone fracture healing. Amygdalin, a...
Chondrogenesis and subsequent osteogenesis of mesenchymal stem cells (MSCs) and angiogenesis at injured sites are crucial for bone fracture healing. Amygdalin, a cyanogenic glycoside compound derived from bitter apricot kernel, has been reported to inhibit IL-1-induced chondrocyte degeneration and to stimulate blood circulation, suggesting a promising role of amygdalin in fracture healing. In this study, tibial fractures in C57BL/6 mice were treated with amygdalin. Fracture calluses were then harvested and subjected to radiographic, histological, and biomechanical testing, as well as angiography and gene expression analyses to evaluate fracture healing. The results showed that amygdalin treatment promoted bone fracture healing. Further experiments using MSC-specific transforming growth factor- (TGF-) receptor 2 conditional knockout (KO) mice ( ) and C3H10 T1/2 murine mesenchymal progenitor cells showed that this effect was mediated through TGF-/Smad signaling. We conclude that amygdalin could be used as an alternative treatment for bone fractures.
PubMed: 32963548
DOI: 10.1155/2020/8811963