Ratzenhofer M, Richter K, Schauenstein E
Exp Pathol (Jena). 1975;11(1-2):83-106.
4-hydroxy-2,3-transpentenal (HPE) represents the 5-C-homologue of a series of hitherto unknown alpha,beta-unsaturated aldehydes. The marked inhibition of DNA-biosynthesis by these chemical compounds, particularly by HPE, suggests blocking of mitosis by HPE due to direct action on the S-phase. It is known that DNA-biosynthesis as well as energy metabolism are generally more disturbed by HPE in animal tumor cells (Ehrlich ascites and solid tumors, NK/Ly sarcoma 37, sarcoma 180, plasmocytoma G, murine Harding-Passey melanoma) than in normal cells (liver, kidney, jejunum, spleen, thymus); for details see BICKIS et al. 1969; RINDLER et al. 1970; KAPFER et al. 1972). After systemic administration of HPE the concentration of the cytotoxic agent in the blood caysed a bituceabke but merely selective inhibition of the metabolism in experimental animal tumors; however, it was not sufficient to produce therapeutic results. The low stability of HPE in the blood and in the peritoneal cavity is to be attributed to its affinity to SH-groups. Therefore the biological tests had to be confined to the local administration of HPE. In this histological study of the action of HPE the substance was administered directly to the human portio vaginalis uteri (ecto- and endocervix) in cases of carcinomatous alterations, in cases of non-carcinomatous affections as well as in normal portions.
In this test 42 women were treated with HPE. 3 patients were observed clinically only, the other 39 cases were investigated also histologically. The histological studies were performed on the extirpated uterus (36 cases), the resected portio (1 case) and only on a conus (2 cases). In 17 of these patients examined histologically the portio was clinically free of pathological symptoms. They suffered from such more or less commonplace gynecological disorders as displacement of the uterus, incontinentia urinae relativa, uterus myomatosus, endometriosis and cystical adnexal tumors. 7 patients suffered from ectopies, 8 from Ca coli uteri, 7 were affected by invasive cancer of the cervix. 8 of the patients were older than 50 years, the others were aged between 25 and 50 years. Mode of HPE administration: 1. Application of a small HPE-soaked linen patch fixed on a Sta Seal impression of the vagina (Sta Seal=dental silicon impression paste). 2. Application by means of a small linen patch in a portio cap. The inner surface of a portio cap corresponding to the vaginal uterus in shape and size was coated with a circular linen patch. The unneeded segment was cut off. After moistening with the aldehyde (HPE) it was fit tightly to the inner surface of the cap and, in situ, to the portio surface as well. In several cases the portio did not fill the cap completely and did not contact the tissue in the region of the os uteri. Consequently, there the aldehyde effect was lower than in the lateral regions of the portio. Therefor 3...
4-羟基-2,3-反式戊烯醛（HPE）代表了一系列迄今未知的α,β-不饱和醛的5碳同系物。这些化合物，特别是HPE对DNA生物合成的显著抑制，表明HPE由于对S期的直接作用而阻断有丝分裂。已知DNA生物合成以及能量代谢在动物肿瘤细胞（艾氏腹水瘤和实体瘤、NK/Ly肉瘤37、肉瘤180、浆细胞瘤G、小鼠哈丁-帕西黑色素瘤）中通常比在正常细胞（肝脏、肾脏、空肠、脾脏、胸腺）中更容易受到HPE的干扰；详情见比基斯等人1969年的研究；林德勒等人1970年的研究；卡普费尔等人1972年的研究。全身给药HPE后，血液中细胞毒性剂的浓度导致实验动物肿瘤代谢受到一定程度但只是选择性的抑制；然而，这不足以产生治疗效果。HPE在血液和腹腔中的低稳定性归因于其对SH基团的亲和力。因此，生物学试验不得不局限于HPE的局部给药。在这项关于HPE作用的组织学研究中，该物质直接施用于患有癌性病变、非癌性病变以及正常部位的人子宫阴道部（宫颈外口和宫颈内口）。
在该试验中，42名女性接受了HPE治疗。3名患者仅进行临床观察，其他39例也进行了组织学研究。组织学研究在切除的子宫（36例）、切除的宫颈部（1例）以及仅在宫颈锥切组织（2例）上进行。在这些接受组织学检查的患者中，有17例宫颈部临床无病理症状。她们患有或多或少常见的妇科疾病，如子宫移位、相对性尿失禁、子宫肌瘤、子宫内膜异位症和囊性附件肿瘤。7例患者患有子宫颈异位，8例患有子宫颈癌，7例患有浸润性宫颈癌。8名患者年龄超过50岁，其他患者年龄在25至50岁之间。HPE给药方式：1. 将一块浸泡过HPE的小亚麻布贴片固定在阴道的斯塔密封印模上（斯塔密封=牙科硅印模膏）。2. 通过在宫颈帽中的一块小亚麻布贴片给药。宫颈帽的内表面形状和大小与阴道子宫相对应，涂有一块圆形亚麻布贴片。将不需要的部分剪掉。用醛（HPE）湿润后，它紧密贴合在帽的内表面，并且在原位也贴合在宫颈部表面。在一些情况下，宫颈部没有完全填满帽，并且在子宫颈区域没有接触到组织。因此，在那里醛的作用比在宫颈部的外侧区域要低。因此3...
