Alfredo J. Gallegos

The zoapatle I — A traditional remedy from Mexico emerges to modern times

A review of publications from 1529 to 1982 related to the zoapatle was made. Historical, biological, ethnobotanical, agricultural, clinical and chemical studies were noted; most of the early publications were written by Mexican scientists, in Spanish. More recent ones appear in the form of patents dealing with the isolation, characterization and total synthesis of some of its constituents. From this review, ideas emerged that might contribute to the understanding and rational use of this plant, or its chemical constituents, as a new, safe, reliable, inexpensive and - hopefully soon - a widely used interceptive agent.

The zoapatle III — Biological and uterotonic properties of aqueous plant extract

Differences in uterotonic activity were observed between zoapatle Montanoa (Cerv.), plants growing in their natural habitat and plants growing in an experimental agricultural plot. Details of an in vitro analogic model for assaying uterotonic potency in guinea pig strips is described. Important species differences on the uterine response to zoapatle aqueous crude extract were noticed in rats, hamsters, guinea pigs, cats and Rhesus monkeys. The need for proper biological evaluation of chemical substances already isolated from zoapatle specimens, is mentioned, and the advantages of working with zoapatle specimens grown under controlled ecological conditions are pointed out.

Intrauterine devices and menstrual blood loss a comparative study of eight devices during the first six months of use

An experiment was conducted to determine changes in menstrual blood loss caused by IUDs. 78 volunteer women of similar age and parity were randomly selected from among those requesting IUDs from the outpatient department of the National Medical Center of the Mexican Institute of Social Security. Menstrual blood loss and hemoglobin were measured for 1-2 control cycles and for 6 postinsertion cycles. Of the 8 different types of IUDs used, the Lippes Loop and the copper-releasing devices caused a statistically significant increase in blood loss and a related decrease in hemoglobin. The steroid-releasing devices caused no significant increase in blood loss and no significant changes in hemoglobin concentration. The rigid copper devices caused the greatest increase in blood loss. The noted changes were clearly established by the 3rd postinsertion cycle.

The zoapatle V — The effect of kauradienoic acid upon uterine contractility

Kauradienoic acid was obtained from the hexanic extract of M. tomentosa (Cerv) leaves by chromatographic separation. This substance influenced the in vitro contractility of the rat, dog and guinea pig uterine strips. It also induced strong contractions of the guinea pig uterus in vivo when administered intravenously, without changes on arterial blood pressure. The effects produced by the plant infusion, the hexanic extract and pure species were compared. The hexanic of other utero-active compounds in M. tomentosa in addition to those already described is discussed.

Tissue localization of radioactive chlormadinone acetate and progesterone in the human

Abstract Chlormadinone acetate 1-2-H 3 (C.A.) ∗∗ ∗∗Chlormadinone acetate. This compound was prepared by Dr. Walter Hafferl from Syntex Research. or progesterone -7-H 3 was administered intravenously to patients 8 hours before hysterectomy, and at this time tissue samples were taken for counting. The highest tissue concentration (dpm/g. wet tissue) of chlormadinone acetate (7 cases) in the tissues examined was found to be in the subcutaneous abdominal fat. All the patients were in different phases of the menstrual cycle. In the genital tract, the greatest amount of radioactivity was found in the fallopian tube, endocervix, or cervical mucus per se (6 out of 7 cases). The average urinary excretion of C.A. over 3 days was 17.5% of the total dose. In contrast, only 3 out of 6 patients treated with progesterone showed the highest concentration in the subcutaneous abdominal fat. These patients were in the proliferative phase of the cycle. The remaining patients, in the follicular phase, showed maximum concentration of radioactivity in skin, uterus, and uterine fibroids. In addition, progesterone was not concentrated by the mucous producing tissues of the genital tract in any of the patients. The average urinary excretion of progesterone over 3 days was 32.58% of the total dose.

The Zoapatle VI. Revisited

A review of new Zoapatle publications was made, including five chemical compounds characterized recently. Relative potency of Kaurenoic acid, Kauradienoic acid (its mixture), Zoapatanol and Montanol was estimated in an in vitro guinea pig uterine assay. Kaurene compounds were several times more potent than Montanol and Zoapatanol as uteroactive substances. Zoapatle aqueous crude extract made from Montanoa frutescens had a strong in vitro uterine potency and unique in vivo characteristics in several biological systems, described in detail in the following five publications.

Subcellular distribution of lysosomal enzymes in the human endometrium. I. Normal menstrual cycle

Abstract The changes in the activity and in the subcellular distribution of three lysosomal enzymes have been studied in the normal human endometrium during the menstrual cycle by the use of highly sensitive fluorimetric technics. Total activity of lysosomal enzymes increased during the maturation of the endometrial tissue from the proliferative to the secretory phase. This increase is greater (105%) for N-acetyl-β-D-glucosaminidase, than for acid phosphatase (77%) or β-glucuronidase (65%). During the proliferative phase the relative activity of the three enzymes found free in the cell cytoplasm was similar and ranged from 21% for N-acetyl-glucosaminidase to 32% for β-glucuronidase. The main difference found between the proliferative and the secretory phase of the menstrual cycle was a drastic increase -- both absolute and relative -- of the cytoplasmic free activity of the lysosomal enzymes. The increase in total free activity represented approximately two, three and four times the amount found free during the proliferative phase for β-glucuronidase, acid phosphatase and N-acetyl-glucosaminidase, respectively. In all cases the relative activity found free represented almost 50% of the total enzymatic activity. The membrane bound activity of the three enzymes also showed a significant increase during the secretory phase, although less dramatic than the free activity.

EEG abnormalities found in healthy women under contraceptive medication. II. Long term studies.

In a previous study EEG abnormalities were detected in 2 of 24 healthy women during the 1st 3 months of treatment with various ovulatory and anovulatory contraceptive regimens. The present study is a follow up of the same group of women to detect possible EEG abnormalities occurring at the 6th and 12th months of treatment and those occurring within the 1st month after discontinuation of contraception. Only 17 women were studied (the 7 others were excluded due to voluntary treatment termination and pregnancy); they were divided into groups: 1) coil (5 cases) 2) microdoses (5 cases) and 3) sequential (4 cases) and combined (3 cases). In each case 3 consecutive pairs of routine EEG recordings (during the 6th and 12th months of contraceptive treatment and within 1st month of contraceptive discontinuation) and an equal number of plasma samples for progesterone/17 beta estradiol determination were taken. EEG routine recordings were also practiced during menstruation and during sleep. Procedures for routine EEG recordings and interpretation hormone determination standardization of dates and statistical significance of changes along the menstrual cycle were done as in the previous study. 4 of 7 patients in group 3 (the anovulatory sequential and combined contraceptive regimen) exhibited subclinical pseudoparoxysmal EEG discharges at the 6th and 12th months of treatment. These abnormalities may be due to the effect of specific hormone content of these particular compounds as they were not seen in control records taken before and after treatment and were seen on dates corresponding to the secretory phase of ovulatory cycles and concomitant to hormonal changes reflecting ovarian inhibition. In the coil group no abnormal EEG signs were observed in patients before during and after the regimen. 1 patient in the microdose group was found to have EEG abnormalities but the abnormalities were not attributed to the hormone content of the compound as abnormal EEG signs were found before and after treatment and were not concomitant to ovarian inhibition. No EEG abnormalities were observed in records taken during menstruation and during sleep of all the subjects.

The zoapatle II--botanical and ecological determinants.

A collection of Montanoa (Cerv) specimens was conducted throughout Mexico. Twenty-one specimens were classified, some of them grown in the greenhouse and transplanted in an agricultural experimental field station in the Valley of Mexico. In vitro uterotonic potency was assayed and the results expressed as equivalents of oxytocine, by using estrogenized guinea pig uterine strips. A great variation of uterotonic potency was observed among the wild plants. A clear decrease and uniformity of uterotonic potency was found in plants grown in the experimental field. The study points out the importance of ecological variations in expression of the plants biological activity.

The zoapatle. XI: Effects elicited by Montanoa tomentosa and Montanoa frutescens on rat uterine strips

Zoapatle aqueous crude extract (ZACE) obtained from Montanoa tomentosa (M.t.) inhibits the in vitro spontaneous contractility pattern of rat uterine tissue. The opposite effect was observed with ZACE from Montanoa frutescens (M.f.) in the same preparation. Both plant extracts, M.t. and M.f., increased the in vitro spontaneous contractility pattern in the uterine guinea pig assay. In depolarized uterine tissue, propranolol (beta-blocker) inhibited the relaxing effect induced by M.t.. Atropine (cholinergic antagonist) abolished the increase in uterus contractility produced by the presence of M.f.