Artemisinin and its derivatives help fight various cancers | 青蒿素及其衍生物具有良好的抗癌效果

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The discovery of artemisinin is one of the most important contributions made by Chinese researchers in medicine. Artesunate (English name: Artesunate), also known as artesunate, is synthesized on the basis of dihydroartemisinin, a derivative of artemisinin. Because artemisinin is insoluble in water, this affects its application; researchers have developed many derivatives of artemisinin for more convenient and effective application of such drugs, and artesunate is one of the most important. Artesunate is soluble in water, so it can be given intramuscularly, intravenously or orally. The World Health Organization recommends intramuscular or intravenous artesunate as first-line therapy for falciparum malaria.

In recent years, studies have found that artesunate, in addition to treating malaria, can also be used to treat cancer, and it has attracted more and more attention.

Why artesunate can treat cancer?

The anti-malarial principle of artemisinin and its derivatives is to produce free radicals through the reaction between the semi-endoperoxy group of the drug and heme (heme contains iron), and the Plasmodium that causes malaria contains a large amount of heme , the free radicals formed in the body of the malaria parasite will cause the death of the malaria parasite.

Since 1993, researchers have been working on the anticancer effects of artemisinin and its derivatives. Why can artemisinin kill cancer cells? Like Plasmodium, cancer cells contain high concentrations of free iron, and artemisinin can react with free iron to generate free radicals, and a large number of free radicals can kill cancer cells. Compared with normal cells, cancer cells can accumulate a higher concentration of free iron. Therefore, the advantage of artemisinin drugs as anticancer drugs lies not only in their ability to kill cancer cells, but also in their ability to kill normal cells. Very little toxicity. This is very important. The biggest disadvantage of traditional chemotherapy drugs is that they have serious toxic effects on normal cells, so too many chemotherapy drugs cannot be used. Studies have found that the ability of dihydroartemisinin, a derivative of artemisinin, to kill leukemia cells is 100 times that of normal blood cells; when dihydroartemisinin kills breast cancer cells and normal breast cells, it is also observed that dihydroartemisinin The ability of hormones to kill cancer cells is much greater than the ability to kill normal cells. The advantage of artemisinin’s low toxicity to normal cells has also been confirmed in other types of normal cells.

Which cancers can artemisinin treat in experiments?

In the past 20 years, researchers have studied the killing effect of artemisinin and its derivatives (dihydroartemisinin and artesunate) on a variety of cancer cells, including brain tumors, breast cancer, cervical cancer, Intestinal cancer, endometrial cancer, gastric cancer, liver cancer, leukemia, lung cancer, lymphoma, melanoma, nasopharyngeal cancer, oral cancer, osteosarcoma, ovarian cancer, pancreatic cancer, prostate cancer, skin cancer and thyroid cancer, etc. Artemisinin and its derivatives have varying degrees of killing effects on almost all tested cancer cells.

Artesunate can kill neuroblastoma cells that are insensitive to chemotherapeutic drugs, and only one of the 16 cell lines and 2 primary cultured cell lines is less sensitive to artesunate, so Artesunate has great potential for the treatment of neuroblastoma.

Researchers in the US analyzed the anticancer activity of artesunate against 55 cancer cell lines from the National Cancer Institute’s Developmental Therapy Program. Artesunate showed the best killing effect on leukemia and colon cancer cell lines; it was the least sensitive to non-small cell lung cancer cell lines; in addition to melanoma, breast cancer, ovarian cancer, prostate cancer, brain tumors, and kidney cancer Cancer cell lines have a better killing effect. Compared with other standard cytotoxic drugs, artesunate and standard cytotoxic drugs have similar killing effect on cancer cells within the same drug concentration range. In addition, the researchers tested the killing effect of artesunate on leukemia cell lines resistant to doxorubicin, vincristine, methotrexate, and hydroxyurea. Artesunate and these drugs have no cross-resistance and can be effectively Kill cancer cells.

In animal experiments, the anticancer effect of artemisinin and its derivatives has been further confirmed. The tumor models that have been tested include breast cancer, pancreatic cancer, ovarian cancer, oral cancer, esophageal cancer, liver cancer, intestinal cancer, lung cancer, brain tumor, leukemia, osteosarcoma, etc.

What types of cancer can artesunate treat clinically?

A preliminary study by a clinical center in the United States shows that intravenous injection of high-dose vitamin C combined with artesunate can effectively improve the treatment effect of advanced breast cancer, and the combined application of the two can play a synergistic effect (the effect is greater than the sum of the two drugs) Effect). Patients with stage 4 breast cancer who did not receive combined intravenous vitamin C and artesunate had a survival rate of 74% after 1 year and 68% after 2 years; The survival rate of cancer patients after 1 year and 2 years is 90%. Of note, treatment with intravenous vitamin C and artesunate did not cause side effects. These preliminary results suggest that a combination of intravenous high-dose vitamin C and artesunate may improve survival in patients with stage 4 breast cancer.

A Chinese study has shown that artesunate combined with standard chemotherapy can effectively improve survival and delay cancer progression in advanced non-small cell lung cancer. Patients who received artesunate plus standard chemotherapy had a 1-year survival rate of 45.1%, compared with 32.7% for patients who received standard chemotherapy without artesunate.

Bowel cancer (also known as colorectal cancer) is a common cancer, accounting for approximately 10% of new cancers worldwide each year. The 5-year survival rate of colorectal cancer is about 60%, and patients urgently need cheap and effective drugs to prolong their survival time. Doctors in the UK studied whether artesunate could prevent bowel cancer from recurring after treatment. They randomly divided 20 patients with early bowel cancer who could receive surgery into two groups, one group received 200 mg of artesunate orally every day for 14 days before surgery, and the other group was a control group that took a placebo. At a follow-up of 42 months after surgery, only 1 of 9 patients who received artesunate had recurrence of bowel cancer, compared with 6 of 11 patients who did not receive artesunate. Artesunate treatment did not cause side effects. In order to obtain more reliable data, this research group is currently conducting a larger clinical trial.

In addition, in clinical trials, artesunate has also treated a small number of melanoma, cervical cancer and other cancers. Artesunate has shown its safety characteristics.

Why hasn’t artesunate been widely used to treat cancer patients?

If any drug is to be used clinically, it must be proven safe and effective through clinical trials. The price of artesunate is very cheap, and the cost in clinical trials is only about 7 yuan per day. The cost of organizing a clinical trial with a considerable scale (generally more than 100 people, sometimes tens of thousands) is quite high. The vast majority of clinical trials are funded and organized by pharmaceutical companies. Even if artesunate has broad application prospects in the treatment of cancer in the future, the pharmaceutical companies producing artesunate will not spend high expenses to fund clinical trials in this area, because it will be difficult for them to obtain such cheap drugs in the future return. In addition, sometimes the funding for drug clinical trials comes from government agencies or charitable organizations that fund research, and these organizations are more willing to fund new drugs than to fund old drugs to make wedding dresses for others. This is what makes it difficult to develop new uses for old drugs. Government agencies or charities funding research should be more supportive in this area in the future.

Because it is difficult to obtain funding from pharmaceutical companies, government agencies and charities, the British research team was able to conduct a larger clinical trial of artesunate in the treatment of bowel cancer by soliciting funds from the public.

Promise of artesunate in cancer treatment

In cancer cell tests, animal experiments, and limited clinical trials, artesunate was effective in killing cancer cells. In addition, artesunate is safe in both malaria and cancer clinical trials; it does not cause serious side effects like conventional chemotherapy drugs in cancer treatment. Artesunate is often used in combination with standard cancer treatments (surgery, chemotherapy, radiation, etc.) to treat cancer. Artesunate is expected to become one of the routine drugs for cancer.

Since artesunate is an old drug with a new use, the health supervision department should relax the supervision so that cancer patients can benefit from the treatment of artesunate as soon as possible.

 

青蒿素的发现是中国的科研人员在医学上做出的最重要的贡献之一。青蒿琥酯(英文名称:Artesunate),也称为青蒿脂,它是在青蒿素的衍生物双氢青蒿素的基础上合成的。由于青蒿素不溶于水,这影响了它的应用;科研人员们开发出了很多青蒿素的衍生物以便更方便有效地应用这类药物,青蒿琥酯是其中最重要的一种。青蒿琥酯可以溶于水,因此可以用于肌肉注射,静脉注射或者口服。世界卫生组织推荐肌肉或静脉注射青蒿琥酯为治疗恶性疟疾的一线疗法。

近年来的研究发现,青蒿琥酯除了可以治疗疟疾之外,还可以用来治疗癌症,并且越来越受到关注。

为什么青蒿琥酯可以治疗癌症?

青蒿素及其衍生物发挥抗疟疾的原理是通过药物的半内过氧基团和血红素(血红素含有铁元素)发生反应生产自由基,而引起疟疾的疟原虫体内含有大量的血红素,疟原虫体内形成的自由基会引起疟原虫的死亡。

自1993年以来,科研人员一直致力于研究青蒿素及其衍生物的抗癌作用。为什么青蒿素可以杀死癌症细胞呢?与疟原虫一样,癌症细胞内含有高浓度的自由铁元素,青蒿素可以与自由铁元素反应而生成自由基,大量的自由基可以杀死癌症细胞。与正常的细胞相比,癌症细胞内可以积聚更高浓度的自由铁元素,因此青蒿素类药物做为抗癌药物的优点不仅在于它对癌症细胞有杀伤能力,还在于它对正常细胞的毒性很小。这一点是很重要的,传统的化疗药物的最大缺点是对正常的细胞也有很严重的毒性作用,因此不能用太多的化疗药物。研究发现,青蒿素的衍生物双氢青蒿素杀伤白血病细胞的能力是杀伤正常血液细胞能力的100倍;比较双氢青蒿素杀伤乳腺癌细胞核正常乳腺细胞时也观察到双氢青蒿素杀伤癌症细胞的能力远大于杀伤正常细胞的能力。青蒿素对正常细胞毒性小的优点也在其它类型的正常细胞中得到证实。

青蒿素在实验中可以治疗哪些癌症?

在过去的20多年中,科研人员研究了青蒿素及其衍生物(双氢青蒿素和青蒿琥酯)对多种癌症细胞的杀伤作用作用,包括脑肿瘤,乳腺癌,宫颈癌,肠癌,子宫内膜癌,胃癌,肝癌,白血病,肺癌,淋巴瘤,黑色素瘤,鼻咽癌,口腔癌,骨肉瘤,卵巢癌,胰腺癌,前列腺癌,皮肤癌和甲状腺癌等。青蒿素及其衍生物几乎对所有测试过的癌症细胞有不同程度的杀伤作用。

青蒿琥酯可以杀死对化疗药物不敏感的神经母细胞瘤细胞,16个细胞细胞系和2个原代培养的细胞株中只有一个细胞系对青蒿琥酯的敏感性较低,因此青蒿琥酯对于治疗神经母细胞瘤有非常大的潜力。

美国的研究人员分析了青蒿琥酯对美国国家癌症研究所的发展治疗计划的55个癌症细胞系的抗癌活性。青蒿琥酯对白血病和结肠癌细胞系表现出最好的杀伤效果;而对非小细胞肺癌细胞系敏感性最低;另外对黑色素瘤,乳腺癌,卵巢癌,前列腺癌,脑肿瘤,和肾癌细胞系有较好的杀伤作用。与其它标准的细胞毒性药物相比,在同样的药物浓度范围内,青蒿琥酯和标准的细胞毒性药物具有相似的杀伤癌症细胞的作用。此外,研究人员测试了青蒿琥酯对抵抗阿霉素,长春新碱,甲氨蝶呤,羟基脲的白血病细胞系的杀伤作用,青蒿琥酯和这些药物没有交叉耐药,可以有效地杀死癌症细胞。

在动物实验中,青蒿素及其衍生物的抗癌作用得到了进一步的证实。已经测试过的肿瘤模型包括,乳腺癌,胰腺癌,卵巢癌,口腔癌,食管癌,肝癌,肠癌,肺癌,脑肿瘤,白血病,骨肉瘤等。

在临床上,青蒿琥酯可以治疗哪些类型的癌症?

美国一个临床中心的初步研究显示,静脉注射大剂量维生素C联合应用青蒿琥酯可以有效地改善晚期乳腺癌的治疗效果,这两者的联合应用可以发挥协同作用(作用大于两种药物相加的效果)。没有接受联合静脉维生素C和青蒿琥酯治疗的4期乳腺癌患者1年后的生存率为74%,2年后为68%;而接受静脉维生素C和青蒿琥酯治疗的4期乳腺癌患者1年后和2年后的生存率均为90%。值得注意的是,静脉维生素C和青蒿琥酯治疗并不会引起副作用。这项初步结果表明联合应用静脉注射大剂量维生素C和青蒿琥酯可以提高4期乳腺癌患者的生存率。

一项中国的研究表明,青蒿琥酯联合标准的化疗可以有效地提高晚期非小细胞肺癌的生存率和推迟癌症的进展。接受青蒿琥酯联合标准的化疗的患者1年的生存率为45.1%,而不用青蒿琥酯只接受标准的化疗的患者1年的生存率为32.7%。

肠癌(又称为结直肠癌)是一种常见的癌症,全世界每年大约10%的新发癌症为肠癌。肠癌的5年生存率为60%左右,患者急需价格便宜且有效的治疗药物来延长生存时间。英国的医生研究了青蒿琥酯是否可以阻止肠癌的治疗后复发。他们把20位可以接受手术治疗的早期肠癌患者随机分为两组,一组在手术之前14天每天口服200毫克青蒿琥酯,另外一组为口服安慰剂的对照组。在手术后随访42个月,接受青蒿琥酯治疗的9位患者中只有1位患者的肠癌复发,而没有接受青蒿琥酯治疗的11位患者中的6位患者发生了癌症复发。青蒿琥酯治疗并没有引起副作用。为了获得更可靠的数据,这个研究组目前正在开展更大规模的临床试验。

另外,在临床试验中,青蒿琥酯还治疗了例数不多的黑色素瘤,宫颈癌等癌症。青蒿琥酯均表现了其安全的特性。

为什么青蒿琥酯还没有广泛地用于治疗癌症患者?

任何药物如果要进入临床应用,必需经过临床试验证明它是安全有效的。青蒿琥酯的价格很便宜,在临床试验中的花费每天只有7元人民币左右。而组织一项具备相当规模的临床试验(一般在100人以上,有时上万人)的花费相当高。绝大多数的临床试验是由药厂资助并组织实施的。即使青蒿琥酯将来在治疗癌症方面有广泛的应用前景,青蒿琥酯的生产药厂不会花费高昂的费用来资助这方面的临床试验,因为他们以后很难从这么便宜的药物上面获得回报。另外,有时候资助药物临床的经费来源于政府机构或者资助研究的慈善机构,而这些机构更愿意资助新药,不愿意资助老药新用来为别人做嫁衣。这就是开发老药的新用途的困难之处。政府机构或者资助研究的慈善机构以后应该在这方面给予更大的支持。

由于很难获得药厂,政府机构以及慈善机构的资助,英国研究小组通过向公众募集资金才得以开展更大规模的青蒿琥酯治疗肠癌的临床试验。

青蒿琥酯治疗癌症的前景

在癌症细胞测试,动物实验以及有限的临床试验中,青蒿琥酯都可以有效地杀死癌症细胞。另外,无论是在治疗疟疾还是在治疗癌症的临床试验中,青蒿琥酯都是很安全的;在治疗癌症时,它并不像常规的化疗药物一样引起严重的副作用。青蒿琥酯通常联合标准的癌症治疗措施(手术,化疗和放疗等)来治疗癌症。青蒿琥酯有望成为癌症的常规药物之一。

由于青蒿琥酯属于老药新用,卫生监管部门应该放宽监管,使癌症患者尽早受益于青蒿琥酯的治疗。

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