Advances On The Chemical Composition And Medicinal Value Of Coffee Beans Ⅱ
Nov 01, 2022
3.1 Protect the nerves of coffee
3.1.1 Prevention of Parkinson's disease (PD)
Epidemiological studies have found that coffee beans can inhibit the production of PD. Studies have found that caffeine in coffee beans competitively inhibits adenosine A1 receptors (A1R) and enhances the release and transmission of dopamine [47]; coffee bean extract can also reduce inflammation by increasing the number of bifidobacteria At the same time, it reduces the oncogenic process of α-synuclein in the enteric nervous system, and reduces the probability of pathogenic factors being transmitted from the gut to the brain, thereby reducing the occurrence of PD [48]. In a study of neonatal male PD patients [49], coffee drinkers had lower shaking scores than non-coffee drinkers, and coffee intake was negatively correlated with tremor severity in these patients. Lee et al. [50] found that eicosanol-serotonin in coffee beans can reduce the neuroinflammatory response of MPTP-induced PD, and reduce the incidence of PD in mice by inhibiting oxidative stress index and activating c-Jun amino-terminal kinase.
3.1.2 Prevention of Alzheimer's disease (AD)
Coffee beans can protect against Alzheimer's disease through a variety of mechanisms:
①Caffeine in coffee beans protects neurons by reducing the levels of up-regulated CD45, TLR2, CCL4 and other pro-inflammatory factors and oxidative stress markers in AD animals [51];
② Chlorogenic acid and caffeic acid in coffee beans can restore cholinergic defects caused by AD by inhibiting the activities of acetylcholinesterase and butyrylcholinesterase [52];
(3) The acids in coffee beans can effectively inhibit the glutamate excitotoxicity leading to AD [53]; Mohamed et al. [54] found that green coffee bean extract can regulate the brain insulin signaling cascade, and can reduce AD induced by insulin resistance. Has neuroprotective effect. Some scholars [55] studied the relationship between coffee intake and AD pathological state in vivo. The results suggest that high coffee intake can suppress AD risk by reducing pathological brain amyloid deposition. Trigonelline in coffee beans can protect neurons in AD rat model from damage by inhibiting oxidative stress, inflammatory response and astrocyte activity [56].
3.1.3 Prevention of neurocognitive decline
Cognitive decline has become an increasingly serious problem in the middle-aged and elderly population. Cognitive impairment will progress to dementia, which is a persistent and irreversible state. Therefore, the best solution to this problem is to reduce the probability of cognitive impairment. 5-CQA in coffee beans prevents cognitive dysfunction in mice by reducing the mouse hippocampal plaque, reducing neuronal damage, and reducing Abeta deposition [57]. Dutch scholars [58] investigated the cognitive decline of elderly men within 10 years and found that the cognitive ability of men who drink coffee decreased by 1.2%, and the cognitive ability of men who did not drink coffee decreased by 1.4%.
3.1.4 Prevention of epilepsy
Caffeic acid in coffee beans can reduce the apoptosis of hippocampal and prefrontal cortex cells in epileptic rats[59]
, reduce the oxidative stress products produced by the rat state epilepticus [60], and has neuroprotective effect on persistent epilepsy rats. In addition to the neuroprotective effects listed above, Kahweol in coffee beans can regulate the neuroprotective activity of antioxidant enzymes in human neuroblastoma cells through the p38/Nrf2 signaling pathway [61], and can also regulate the dorsal root ganglia of rats. Analgesic effect [62].
3.2 Prevention of type 2 diabetes
Diabetes is a disease affected by both genetic factors and environmental factors. With the development of society, the incidence rate is increasing year by year. Diabetes and its complications have gradually become the fourth largest disease in the world. Reducing blood sugar and suppressing the risk of diabetes is the best way to prevent such diseases. The way. Type 2 diabetes is the predominant form of diabetes and is caused by a combination of insulin resistance and insufficient insulin secretion. Epidemiological studies have found that moderate coffee consumption can reduce the risk of type 2 diabetes [63].
A study found that decaffeinated coffee was more able to reduce the risk of type 2 diabetes [64]
. Polyphenols in coffee beans have anti-diabetic effects on patients with type 2 diabetes by accelerating glucose metabolism, reducing insulin resistance and glycated hemoglobin levels [65]. Chlorogenic acid in coffee beans can inhibit type 2 diabetes by regulating the glucose and lipid metabolism in high-fat, high-sugar and streptozotocin-induced type 2 diabetic rats [66]. Trigonelline in coffee beans can prevent type 2 diabetes by reducing blood sugar and blood lipid levels, improving insulin sensitivity index, and up-regulating antioxidant enzyme activity [67]. Kahweol in coffee beans accelerates glucose-stimulated insulin secretion and increases glucose uptake in human skeletal cells, thereby reducing the risk of type 2 diabetes in people [68].
3.3 Anti-cancer
3.3.1 Colorectal cancer
Although the most effective methods for colorectal cancer are surgery and adjuvant therapy, the mortality rate of colorectal cancer is still high, so chemoprevention as an effective means of preventing colorectal cancer should be paid attention to. coffee
Kahweol in bean has been shown to have significant cancer-preventive effects, inhibiting colorectal cancer by promoting the expression of apoptotic factor Caspase-3, reducing the expression of anti-apoptotic factors (Bcl-2, phosphorylated Akt), and inhibiting the expression of HSP70 protein tumor growth [69]. Caffeic acid in coffee beans can inhibit the activity of two protein kinases (MEK1 and TOPK) activated during mitosis in colorectal cancer cells, thereby inhibiting the phosphorylation of proline-directed serine/threonine kinases (ERKs), transcription factors ( AP-1, NF-IIB) activation, thereby inhibiting the tumor transformation of jb6p+ cells induced by oncogenes (TPA, EGF and HRAS) [70]. Bessler et al. [71] studied the mechanism by which caffeine balances peripheral blood mononuclear cells (PBMC) with human colon cancer cells (HT-29) and human colon adenocarcinoma cells (RKO). The secretion of inflammatory cytokines improves the inflammatory state, thereby inhibiting the progression of colorectal cancer.
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3.3.2 Liver cancer
Zhao [72]
et al conducted a meta-analysis between coffee intake and the incidence of liver cancer, and found that coffee intake was inversely related to the risk of liver cancer, and high doses of coffee were more effective. Kahweol, Cafestol, and diterpenoids in coffee beans can act as blockers to block a variety of enzymes involved in hepatocarcinogenesis; they can also alter xenotoxicity by inducing glutathione-S-transferase and inhibiting N-acetyltransferase Metabolism to fight liver cancer [73]. Wiltberger et al. [74] drinking coffee before and after liver transplantation in patients with liver cancer and found that patients with postoperative coffee intake (>3 cups per day) had longer overall survival time than other patients. body-mediated liver cancer cells. Caffeine and chlorogenic acid in coffee beans can induce cell division phase II
Detoxification enzymes and antioxidant enzymes can inhibit the expression or reduce the activity of phase I activating enzymes, thereby preventing liver cancer [75].
3.3.3 Prostate cancer
Coffee beans can inhibit the development of prostate cancer. The mechanism of six active substances in coffee beans inhibiting prostate cancer was studied. By evaluating apoptosis-related proteins, androgen receptors and chemokines, it was found that Kahweol and Cafestol could inhibit the proliferation and migration of prostate cancer cells [76]. Kolberg et al. [77] studied the effect of coffee extract on the regulation of select genes in human PC3 (prostate cancer cells) and nude mouse PC3 xenografts, and found that coffee extract inhibited the activity of NF-κB in PC3 cells in vitro and in xenografts. thereby inhibiting prostate cancer. Montenegro et al[78] conducted microwave-assisted extraction of four kinds of coffee beans after roasting to different degrees, and found that the inhibitory effect of coffee extract on human prostate cancer (DU145) cell line was stronger than that of PC3 cell prostate cancer cell line, and it had a stronger inhibitory effect on mitotic S and S and P. G2/M cell cycle arrest is greater and can effectively prevent prostate cancer.
3.3.4 Lung cancer
Studies have found [79] that the active substance chlorogenic acid in coffee beans has a significant inhibitory effect on human lung cancer (A549) cell line, and the mechanism is that recombinant human annexin (Annexin A2) is the chlorogenic acid in A549 cell line. Covalently bound to the target, chlorogenic acid inhibits the binding of Annexin A2 to the p50 subunit of NFκB protein, thereby inhibiting the expression of anti-apoptotic genes (cIAP1, cIAP2) downstream of the NF-IIB signaling pathway in and out of A549 cells, thereby inhibiting A549 Cell proliferation and migration. In addition, coffee can also act as an inhibitor of oxidative stress transcription factor Nrf2, blocking Nrf2-dependent proteasome activity, thereby promoting apoptosis of pancreatic cancer cells [80]; extracts of Robusta coffee can induce The S phase of breast cancer cells increases, the number of G2/M decreases, which affects mitochondrial morphology and triggers apoptosis [81];
3.4 Anti-inflammatory
Inflammatory response is a biological defense process mediated by endogenous substances in the organism, and its main role is to remove harmful stimuli. Studies have shown that caffeine in coffee beans may play a role in neurodegenerative diseases
Overregulation of A2A-type adenosine receptors controls microglial responses and inhibits neuroinflammation [82], and can also inhibit lipopolysaccharide-induced mouse monocytes by activating the phosphorylation of NF-κB protein and mitogen-activated protein kinase. Inflammatory responses in macrophage leukemia cells (RAW264.7) [83]. Chlorogenic acid in coffee beans and its metabolites caffeic acid and ferulic acid have inhibitory effects on the inflammatory response of human microvascular endothelial cells, by reducing the secretion of interleukin 6 (IL-6), interleukin 8 ( IL-8), tissue plasminogen activator (T-PA),
Endothelial cell-type plasminogen activator inhibitor (PAI-1) and intercellular adhesion molecule (ICAM-1) [84]. Zhao Haiping et al[85] used homocysteine (Hcy) to induce the peripheral blood leukocytes of 8-week-old male mice, treated with caffeic acid, and detected the expression of myeloperoxidase MPO and p-ERK1/2 in leukocytes. , concluded that caffeic acid can induce the release of inflammatory mediators MCP-1 and MPO in peripheral blood leukocytes of mice by inhibiting the expression of p-ERK1/2, thereby interfering with the inflammatory response. Tan Yinfeng et al. [86] found that coffee grounds extract can reduce the ear swelling rate caused by xylene in mice, and at the same time inhibit the increase of capillary permeability caused by acetic acid in mice, and has anti-inflammatory effect on mice.
3.5 Antioxidant
In recent years, the use of natural antioxidants to combat oxidative stress-related diseases in the body has received extensive attention. Coffee, a commonly used beverage, contains a variety of dietary antioxidants. Studies have found that green coffee extract can effectively scavenge DPPH free radicals and ABTS free radicals [87]. The content of volatile substances such as pyrrole, pyrazine, and furan in coffee beans was significantly positively correlated with the antioxidant capacity of Ferric ion reducing antioxidant power (FRAP) [88]. Kalthoff et al. [89] found that coffee bean extract can inhibit the oxidative stress response induced by the tobacco carcinogen benzpyridine by activating the important gene UGT1A involved in the human metabolic cycle. Chen et al. [90] detected the effect of 5-CQA in coffee beans on the reactive oxygen species (ROS) and glutathione (r-glutamyl custeinal+glycine, r-glutamyl custeinal + glycine) in hepatocytes induced by tert-butyl hydroperoxide. GSH), and found that 5-CQA could act as an Nrf2 activator to inhibit ROS and GSH, and could inhibit oxidative stress-mediated liver damage. Studies have shown that the antioxidant capacity of Arabica coffee beans increases with the degree of roasting [91].
3.6 Liver protection
There is growing evidence that coffee beans may protect against liver disease from a variety of causes. Epidemiological studies have found [92] that coffee intake is negatively correlated with liver disease-related mortality. Drinking more than 2 cups of coffee per day can effectively reduce liver disease mortality. Caffeine in coffee beans can protect rat liver fibrosis induced by diethylnitrosamine (DEN) and carbon tetrachloride (CCl4) through antioxidant effects and inhibition of fibrotic cytokines TGF-beta and PDGF-beta [93]. Coffee bean extract can inhibit non-alcoholic fatty liver disease, and its mechanism is similar to that of coffee
It is related to enhancing the expression of mitochondrial stress proteins and inducing redox state regulators[94]
. Lee et al. [95] found that the diterpenoids Kahweol and Cafestol in coffee beans inhibited CCl4-induced hepatotoxicity by blocking cytochrome isoenzyme p450 (CYP2E1)-mediated biological activation and scavenging free radicals.
3.7 Cardiovascular protection
Meta-analysis shows that moderate coffee consumption (2-4 cups per day) can reduce cardiovascular mortality [96]. Chlorogenic acid in coffee beans inhibits the production of vascular reactive oxygen species, reduces oxidative stress, and increases nitric oxide bioavailability and other mechanisms to reduce blood pressure and vascular hypertrophy in spontaneously hypertensive rats [97]. Some scholars have pointed out that moderate coffee intake can improve coronary artery disease, arrhythmia and heart failure [98]. In a survey of 1227 patients with chronic heart failure, higher coffee intake was found to be inversely associated with atrial fibrillation events [99].
3.6 Liver protection
There is growing evidence that coffee beans may protect against liver disease from a variety of causes. Epidemiological studies have found [92] that coffee intake is negatively correlated with liver disease-related mortality. Drinking more than 2 cups of coffee per day can effectively reduce liver disease mortality.
Caffeine in coffee beans can protect rat liver fibrosis induced by diethylnitrosamine (DEN) and carbon tetrachloride (CCl4) through antioxidant effects and inhibition of fibrotic cytokines TGF-beta and PDGF-beta [93]. Coffee bean extract can inhibit non-alcoholic fatty liver disease, and its mechanism is related to coffee enhancing mitochondrial stress proteins and inducing the expression of redox state regulators [94]. Lee et al. [95] found that the diterpenoids Kahweol and Cafestol in coffee beans inhibited CCl4-induced hepatotoxicity by blocking cytochrome isoenzyme p450 (CYP2E1)-mediated biological activation and scavenging free radicals.
3.7 Cardiovascular protection
Meta-analysis shows that moderate coffee consumption (2-4 cups per day) can reduce cardiovascular mortality [96]. Chlorogenic acid in coffee beans inhibits the production of vascular reactive oxygen species, reduces oxidative stress, and increases nitric oxide bioavailability and other mechanisms to reduce blood pressure and vascular hypertrophy in spontaneously hypertensive rats [97]. Some scholars have pointed out that moderate coffee intake can improve coronary artery disease, arrhythmia and heart failure [98]. In a survey of 1227 patients with chronic heart failure, higher coffee intake was found to be inversely associated with atrial fibrillation events [99].
3.8 Antibacterial
Traditional antibacterial drugs have high resistance, large side effects, and short duration. In this context, natural drugs with antibacterial activity have received great attention. Studies have found that green coffee beans have inhibitory activity against Porphyromonas gingivalis, Prevotella intermedia, Fusobacterium nucleatum and Actinomyces [100]. Caffeine and chlorogenic acid in coffee beans have antibacterial effects on Serratia marcescens, Enterobacter cloacae and Salmonella [101]. Caffeic acid and protocatechuic acid in coffee beans inhibit Legionella pneumophila
Effect [102].
3.9 Protect bones
Trigonelline in coffee beans can reduce bone mineralization in streptozotocin-induced diabetic rats and increase bone density in nicotinamide/streptozotocin-treated rats [103]. Kahweol in coffee beans can prevent the formation of mouse osteoclasts by inhibiting the phosphorylation of extracellular signal-regulated kinase and Akt activated by receptor activator of nuclear factor kappa-B ligand (RANKL) [104] ]. Fukuma et al. [105] found that Cafestol and Kahweol not only inhibited the formation of osteoclasts, but also promoted the differentiation of osteoblasts.
3.10 Lowering blood lipids
Studies have shown a dose-response relationship between higher coffee consumption and lower body fat percentage, suggesting that coffee is associated with lipid lowering [106]. Green coffee bean extract can reduce body weight, serum total cholesterol and triglycerides in high-fat diet-induced rats [107]. Polyphenols in coffee beans by downregulating (SREBP)-1c antibody, acetyl-CoA carboxylase-1 and -2, stearoyl-CoA desaturase-1 and pyruvate dehydrogenase kinase-4 mRNA levels , promote the body's energy metabolism, reduce fat production, thereby inhibiting fat accumulation [108].
3. 11 Others
Coffee beans also protect the reproductive system, promote metabolism and estrogen activity. Al-Megrin et al [109] found that Arabica coffee bean extract could help treat testicular dysfunction induced by type 2 diabetes. Ho et al [110] showed that decaffeinated coffee can
It regulates the genes related to energy metabolism in the brain, thereby promoting energy metabolism in the brain.
4 Conclusion
Coffee is one of the most widely consumed beverages in the world. Before the 20th century, coffee was mainly popular in a small number of countries such as South America and Europe. With the development of society and the spread of coffee culture, coffee was gradually popularized and popularized. The research on the chemical composition and pharmacological effects of coffee has made significant progress, but still There are areas that need to be explored urgently, such as the complex chemical reaction system in the roasting process of coffee beans is not yet fully understood, the quality evaluation indicators and quality control methods of coffee beans are not perfect, the accumulation of adverse reactions of coffee to the long-term drinking of the elderly and children, coffee dependence The formation mechanism and stage method of sexuality are still unclear. Therefore, it is possible to standardize and guide the use of coffee beans by further studying the chemical composition, pharmacological effects and dose-effect relationship of coffee beans, and provide a basis for the high-quality development of the coffee industry.
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