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Anti-cancer Chinese herbal medicine XII: whole scorpion

author:Herbalist li

Although the whole scorpion is not included in the list of medicinal and food dual-use, but its edible in the folk has a long history, many people regard it as delicious, many people are really regarded as "snake scorpion", even if it is used in medicine, many people can not accept. However, as a traditional Chinese herbal medicine in China, the whole scorpion is widely used in clinical practice.

Anti-cancer Chinese herbal medicine XII: whole scorpion

Scorpion

The official source of the whole scorpion is the dry whole of the arthropod phylum spider-shaped steel pincer scorpion, which was first contained in the "Shu Bencao", which is spicy and flat, poisonous, returning to the liver meridian, sexual good walking, can breathe wind and antispasm, tongluo analgesia, attack poison and loose knots, is a medicine for the treatment of spastic convulsions, and can also be used to treat rheumatism stubbornness, sores and poison, stroke hemiplegia, tetanus, rheumatic paralysis, migraine headache, sores, fistula, etc. The whole scorpion is a foot yin through the liver medicine, specializing in the liver to dispel the wind, so it cures the diseases of yin and yin; "Materia Medica Truth Seeking Truth" says: Where the children's fetal wind is shaky, the adults are half-sided, the mouth, eyes, mouth and eyes are crooked, the language is astringent, the hands and feet are shaky, the malaria is cold and hot, the deafness is deaf, and it is brought down, all because of the external wind and internal guests, all of which are useless. Because of its good nature, ventilation and pain relief, rheumatic paralysis is also used more, "Jade Catalpa Medication" said that the whole scorpion through the bones, moisture removal, that is, for this meaning. Zhang Shouyi, a famous doctor in modern times, is good at curing wind paralysis, and his understanding of the whole scorpion is the most thorough: the scorpion is a poisonous insect and has a spicy taste. Those who can cure the wind, cover is also good at walking, then the wind can be removed, and the wet paralysis can be profitable. If the wind moves internally, it should be quiet and not moving, as if it is not something that this poisonous insect can try. However, the ancients always used it to cure adults, children who were frightened, and the storm movement within the good, and the young family wind and eclampsia, all of which carried phlegm and rose, and they would reduce their phlegm and open the phlegm, and then they could temporarily calm their flames. Guan Gu Fang mostly uses the scorpion tail, cover the power of this insect, all lies in the tail, the temperament is downward, and this substance in the medicine store is salted, then the salt is also moistened, and it is in direct opposition to the disease of qi and blood. The decoction is light and the three tails are reused to four or five tails, and there are also those who are used in the pill powder, which can be more.

The whole scorpion is mainly produced in Henan and Shandong provinces, and the one produced in Henan is called Nanquan Worm, and the one produced in Shandong is called Dongquan Worm. The whole scorpion in Yuzhou, Henan Province, has two more legs than the whole scorpion in other places, called "ten-legged scorpion" and "ten whole worm", which has been a tribute since ancient times, and is known as "the first scorpion in the world".

Anti-cancer Chinese herbal medicine XII: whole scorpion

The chemical composition of the whole scorpion

1, scorpion venom: studies have shown that scorpion venom is mainly composed of protein and non-protein two parts, the main active component is the protein part, the active protein is divided into toxic proteins and enzyme proteins according to different effects, toxic proteins are mostly molecular weight 6000 ~ 9000 Da polypeptides, containing 3 ~ 4 pairs of disulfide bonds, of which 3 pairs constitute a cyclic core structure. Enzyme proteins mainly include phospholipase A, acetylcholine lipase, hyaluronidase, etc.; The non-protein components are mainly lipids, organic acids and a small number of free amino acids.

2. Protein and amino acids

The protein mass in the whole scorpion protein efficacy component is 50.37%. The amino acids of the whole scorpion contain 17 kinds of amino acids that are essential to the human body such as aspartic acid, glutamic acid, and serine.

3. Fat-soluble ingredients

It mainly includes fatty acids such as palmitic acid, stearic acid, oleic acid and other fatty acids, and saturated fatty acids.

4. Inorganic and trace elements

The whole scorpion contains 29 kinds of inorganic elements, such as Containing Ca, Mg, Fe, Cu, Zn, Mn, Pb and other trace elements, male scorpions in addition to the toxic trace elements Pb is higher than the female scorpion, the rest of the trace elements are significantly lower than the female scorpion.

In addition, whole scorpions also contain polysaccharides and other components.

Anti-cancer Chinese herbal medicine XII: whole scorpion

Pharmacological effects of whole scorpions

The whole scorpion has the effects of antispasmodic, analgesic, attacking and dispersing the knots, etc., and the results of modern pharmacological research have also confirmed that the whole scorpion has good pain, sedation, anticonvulsant, anti-epileptic effect, and the research on the whole scorpion in anticoagulant, thrombolytic and anti-tumor is also quite in-depth.

Antitumor effect of whole scorpion

Whole scorpion can significantly improve the phagocytic function and secretion capacity of macrophages, activate macrophages, this effect is related to the traditional use of whole scorpion for the treatment of sores and fistulas, and modern clinical applications for tumors. The whole scorpion can inhibit the proliferation of multiple tumor cell lines, such as gastric cancer, liver cancer, lung cancer, prostate cancer, cervical cancer, etc., and has a certain inhibitory effect on the growth performance of transplanted tumors.

The histamine-like components contained in the whole scorpion have a certain killing effect on the gastric cancer-823 cell line; the high, medium and low dose groups of the whole scorpion have inhibitory effects on the lung cancer of mice Lewis, and the inhibition effect of low concentration water extract and small molecule oligopeptide is very obvious; it has a strong inhibitory effect on prostate cancer PC-3 cells in vitro, and the scorpion tail effect is more obvious; the whole scorpion induces apoptosis of cervical cancer cells by upregulating the expression of Bax.

In view of the anti-tumor effect of the whole scorpion, modern pharmacology has carried out many studies on its anti-tumor mechanism, mainly in the following aspects.

1. Induce apoptosis

Normal apoptosis is a normal physiological process of the human body, which is regulated by Bcl-2, p53 and other genes, is a dynamic balance process of pro-apoptosis and hinder apoptosis, when the pro-apoptosis process is blocked or hindered when the apoptosis process is overactive, it will induce a variety of diseases, cancer is one of the most representative diseases. Most cancer cells lose or are dysfunctional in the p53 gene, while some cancer cells produce too much Bcl-2 protein, which can enable cancer cells to evade the apoptosis program to obtain immortality, and the whole scorpion can achieve anti-tumor purposes by inducing the apoptosis process. Treatment of breast cancer MDA-MB-231 and colorectal cancer HCT-8 cell lines with scorpion poison, the results found that cancer cells appear G2/M stage enrichment and apoptosis necrosis enrichment, which may be related to scorpion venom increasing ROS, upregulating P53, downregulating the expression of Bcl-2, and ROS is closely related to cancer cell apoptosis, the latest research also found that high expression of P53 can block the cell cycle, so scorpion venom can induce apoptosis and block the cell cycle; there are also studies that show that scorpion venom promotes cytC release and upregulation of caspase-9/caspase-3 protein expression to induce apoptosis in glioma cells; scorpion poison can block the AKT signaling pathway and enhance the sensitivity of temozolomide to induce malignant glioma U251 cell apoptosis in vitro; whole scorpion water leaching cultures cervical cancer cells, and found that whole scorpion water leaching can induce apoptosis by upregulating Bax expression to kill cervical cancer cells, while scorpion venom polypeptide extract (PESV) induces apoptosis of ovarian cancer cells, Blocking the cell cycle so that it is mainly in the G0/G1 phase, it is by upregulating the expression of P27 and Caspase-12, downregulating the expression of Survivin'"; it has also been found that scorpion poison polypeptide extract and scorpion poison anti-cancer polypeptide can promote leukemia, bile duct carcinoma, liver cancer, bladder cancer, oral squamous cell apoptosis, and its mechanism of action is mainly related to down-regulating PI3K, p-Akt, Bcl-2 signaling protein and upregulating p53, caspase3 gene expression13-18.

2. Inhibit cell proliferation

Uncontrolled proliferation of cells is one of the important physiological characteristics of cancer cells, under normal circumstances, a balanced state with apoptosis, together maintaining the normal number of human cells, inhibiting cell proliferation through direct or indirect pathways is another important means of anti-tumor therapy, which also involves a variety of signaling factors and pathways. Experimental studies have found that scorpion venom can inhibit the HIF-1w/PKM2 signal transduction pathway, thereby reducing the ability of cellular aerobic glycolysis, while activating the p38aMAPK signaling pathway and blocking the cell cycle, and ultimately inhibiting the proliferation of glioma cells. In vivo and in vitro experimental results showed that scorpion venom polypeptides can inhibit the proliferation of bowel cancer HCT116 cells by regulating the expression of negative regulators PiP3 and PTEN in the AKT signaling pathway; the effect of scorpion poison anti-cancer polypeptides on the proliferation of leukemia cell lines has been found to inhibit the cyclin DI and NF-KB signaling pathways of the cell cycle regulatory proteins, resulting in cell cycle blocking in the G1 stage and inhibiting cell proliferation. At the same time, experimental studies have also found that it can also inhibit the proliferation of lung cancer A549 cells, mainly by inhibiting the expression of HIF-1a and PTEN and directly inhibiting cell proliferation and blocking the cell cycle; and the inhibition mechanism of ovarian cancer cells and prostate cancer cells has the same place, mainly related to promoting cell cycle inhibition of related protein expression and blocking cell cycle. Li Xiaohui et al. showed that when PESV > 40 μg mL-1 flavor, the inhibitory effect on the proliferation of hepatocellular carcinoma cells was significantly enhanced, and it was also by blocking the cell cycle to inhibit the proliferation of cancer cells. Zhang Weidong's group proposed that the inhibition of PESV on sarcoma cells is related to the promotion of the expression of autophagy-related factors Beclinl and MAPILC3A and the expression of CD133, a marker of tumor stem cells. Some researchers treated lung adenocarcinoma A549, laryngeal cancer Hep-2, and breast cancer MCF-7 with a whole scorpion complex enzyme lysate, and the proliferation of the three cancer cells was significantly inhibited.

1.3 Inhibition of angiogenesis

Cancer cells and human normal tissue cells, its growth, proliferation, migration is inseparable from blood supply and nutritional support, since Professor Poultman J put forward the famous "tumor growth and metastasis depends on neovascularization" theory, inhibition of tumor angiogenesis that is, "starvation of tumors" has been one of the important ways to treat tumors. Vascular endothelial growth factor (VEGF), epidermal growth factor receptor (EGFR), and basic fibroblast growth factor (b FGF) are highly expressed in a variety of tumors and are considered to be important signal converters for angiogenesis, involving mapK, PI3K/Akt and other signaling pathways. A number of studies suggest that whole scorpion extract can inhibit the expression of various angiogenesis-related factors such as VEGF and HPA in the liver cancer tumor microenvironment, thereby inhibiting angiogenesis.

4 Regulate immunity

Tumor cells can evade recognition and attack by the human immune system through complex mechanisms, allowing them to grow and proliferate indefinitely in the body. Scientists have thus explored a new anti-cancer path, that is, blocking the tumor immune escape pathway and remobilizing the body's own immune system to attack cancer cells. As one of the most commonly used anti-cancer Chinese medicines, the mechanism of action of the whole scorpion has a variety of effects, and it has been found that the interaction of scorpion venom with TLR2 family TLR4 may induce immune response by influencing a series of activating transcription factors (NF-KB, AP-1, ERK1/2 and p38) of the signaling pathway, and can also induce the systemic release of granulocyte colony stimulating factor (G-CSF), macrophage CSF (M-CSF), IL-8, monocyte chemotaxin 1 (MCP-1) And enhances cellular immunity. Scorpion toxins can also regulate immunity by affecting ion channels.

5. Inhibit cell invasion and metastasis

Scorpion peptides can not only selectively block the activation of MMP-2, thereby inhibiting the invasion of glioblastoma cells, and can cross the blood-brain barrier and tissue barrier to increase efficacy, but also can downregulate the expression of PTX3 through the NF-KB and Wnt β-catenin signaling pathways, affecting breast cancer, gastric cancer SGC-7901, leukemia pathogen cell proliferation, and ultimately inhibiting the invasion and metastasis of cancer cells.

6. Anticoagulant effect

Most tumor patients have pathological changes such as coagulation, fibrinolysis and hyperplatelet aggregation, which not only allow tumor cells to survive in circulatory transport, but also make the adhesion of tumor cells more stable, thereby promoting distant tumor metastasis, and the degree of cancer cell metastasis and invasion in tumor patients is closely related to the degree of their hypercoagulable state." Scorpion venom can improve the hyperactivity of coagulation, fibrinolysis and platelet aggregation, thereby inhibiting the metastasis of tumors, Jia Jinqiu et al. "Observed the effect of scorpion venom polypeptide extract (PESV) on the blood rheology of nude mice with lung cancer tumor, and randomly divided transplanted lung cancer tumor nude mice into PESV group (subcutaneous injection pesV) and control group (subcutaneous injection of normal saline), PESV group blood rheology indicators have been reduced to varying degrees, it is believed that PESV can reduce the blood viscosity of tumor-bearing nude mice, It has obvious inhibitory effect on the tumor metastasis ability of lung cancer-bearing nude mice.

Anti-cancer Chinese herbal medicine XII: whole scorpion

Modern clinical applications

At present, there are relatively many basic research on scorpion venom, and many researchers believe that scorpion venom has the hope of becoming a new anti-cancer drug, but scorpion venom has not yet been applied to the clinic in the form of a drug, and the main clinical application is the whole scorpion dry body, in addition to the existing Western medical science research, it is also based on the "long-term disease into the network, insects and ants through the network" and "poison attacking poison" theory of Traditional Chinese medicine, in addition, "internal wind dark rotation, liver wind internal movement" is also considered to be a mechanism of cancer cell metastasis, and insect medicine is attributed to the liver through the wind, This is also one of the theoretical bases of Traditional Chinese medicine that is often used as anti-tumor metastasis in Chinese medicines such as Quan Scorpion. As a traditional Chinese medicine that is full of wind, communication and poisoning, the whole scorpion has a long history of medicinal use, and the traditional Chinese medicine theory for modern anti-cancer treatment is also improving day by day, although its chemical composition is complex, but the most studied anti-cancer ingredients are mainly limited to scorpion venom and the active polypeptides extracted from it. The anti-cancer mechanism of the whole scorpion involves almost all aspects of the cancer pathway, which is generally effective for human cancer, confirms the characteristics of the multi-target and multi-channel role of traditional Chinese medicine, and clinical research also affirms the efficacy of the whole scorpion. In the future, it is necessary to continuously improve the theoretical interpretation of chinese medicine of the whole scorpion anti-cancer, in terms of experiments, more in-depth and meticulous study of the anti-cancer components and mechanisms of the whole scorpion, clinical aspects, the need for more multi-sample, multi-center high-quality clinical research, to clarify the compatibility, dosage, dosage form, indications of the whole scorpion, etc., a hundred years more effective and safe use of the whole scorpion, which has a good curative effect of traditional Chinese medicine.

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