Evaluation of the Biological Activity of Glucosinolates and Their Enzymolysis Products Obtained from Lepidium meyenii Walp. (Maca).

Glucosinolates (GLS) were extracted and purified from Lepidium meyenii (Maca) root. Purified GLS were analyzed without desulfation by UPLC-ESI-MS. Glucosinolates were decomposed into benzyl isothiocyanate (BITC) by thioglucosidase. DPPH radical scavenging activity, ABTS radical scavenging activity, and reducing power were used to evaluate antioxidant activity of Maca crude extract (MCE), total GLS, and BITC. Maca crude extract showed the highest antioxidant activity among them, and BITC showed no antioxidant activity at concentrations less than 10 mg/mL. Cytotoxicity on five human cancer cell lines and the inhibition rate of NO production were used to evaluate the activity of anti-cancer and anti-inflammatory of total GLS and BITC. The inhibition rate of NO production of 50 µg/mL BITC can reach 99.26% and the cell viability of 100 µg/mL BITC on five tumor cell lines is less than 3%. The results show that BITC may be used as a promising anti-cancer and anti-inflammatory drug.

First study of in vitro protective effect of Lepidium meyenii (Maca) on frozen-thawed bovine spermatozoa.

Background and Aim: Lepidium meyenii Walp (Maca) is an herbaceous plant that grows in the Peruvian Andes and it has been widely used as a nutritional supplement and fertility enhancer and has been used in the treatment of a variety of diseases, such as rheumatism, respiratory disorders, and anemia. The most notable feature of Maca is its potent antioxidant capacity, which helps in the scavenging of free radicals and protection of cells from oxidative stress. This study aimed to evaluate the in vitro effect of Maca extract on thawed sperm cells from bulls. Materials and Methods: Three dilutions of 1, 10, and 100 mg/mL of Maca extract were incubated with frozen-thawed bovine semen and analyzed at 1, 3, and 24 h of exposure time, evaluating the activity of the extract on the DNA, motility, morphology, viability, integrity of the membrane and acrosome of spermatozoa. Results: The Maca extract improved the studied sperm parameters of motility, acrosome integrity, vitality, and DNA integrity of sperm cells at a concentration of 10 mg/mL, and at 1 mg/mL, an improvement was observed in the morphology and integrity of the membrane. However, the best activity of the Maca extract was observed on the DNA integrity of the sperm, which was effective at the three concentrations evaluated after 24 h of incubation. Conclusion: The results indicate that L. meyenii can help in maintaining spermatozoa cellular integrity after the frozen-thaw process, especially in the protection against DNA fragmentation. Therefore, Maca would be a feasible supplementation to protect sperm to maintain their fertile ability after thawing.

Effects of Oral Administration of Lepidium meyenii on Morphology of Mice Testis and Motility of Epididymal Sperm Cells After Tetrahydrocannabinol Exposure.

Background: Tetrahydrocannabinol (THC) administration is associated with testicular damage and reduced semen quality. Oral administration of Lepidium Meyenii (maca) improves spermatogenesis and sperm motility and count and reduces spermatogenic damage. Objectives: The aim of this study was to evaluate the effect of administration of THC, maca, and their combination on testicular tissue and semen parameters. Materials and Methods: Thirty-six-week-old male mice were classified into control, THC, Maca, and THC + Maca groups. The mice were subjected to Eco Color Doppler ultrasound examination of the testicles before and after treatment. After euthanasia, the epididymis, testes, liver, and kidney were collected for histological examination. For morphometry of the testis, tubular diameters and seminiferous epithelium height were measured. Sperm concentration and sperm motilities were assessed. Differences among the groups were assessed using the Kruskal-Wallis and Dunn's post-hoc test. Results: In all the groups, there were no significant changes in testicular morphology before and after treatment. Histological assessment of the testes showed no alterations in control, no significant alterations in Maca, mild to moderate alterations in THC, and mild alterations in THC + Maca groups. Histological examination of the other organs showed no significant differences among the groups. Tubular diameter showed significantly increased thickening for THC and THC + Maca compared with that for Maca and control. Moreover, seminiferous epithelium height decreased for THC compared with that in the control, Maca, and THC + Maca groups. No statistically significant reduction in the spermatogenic index was observed for THC compared with that for Maca and THC + Maca. Epididymal cross-sections of the groups showed no significant alterations. Sperm concentration and motility were higher for control and THC + Maca groups than in group THC and Maca. Conclusion: In vivo maca administration reduced the deleterious effect of THC on testicular parenchyma and semen production.

A review of the study of active components and their pharmacology value in Lepidium meyenii (Maca).

Lepidium meyenii (Maca) contains several active components, including alkaloids, glucosinolates, isothiocyanates, polysaccharides, polyphenols, and sterols, which make it have the traditional therapeutic uses. In this paper, we summarized the analytical progress of the active components associated with alkaloids, polysaccharides, glucosinolates, sterols, free fatty acids, flavonoids, and natural phenols in Maca by mass spectrometry (MS). Due to the effect of color and type on active components in Maca, we summarized the study of quality evaluation about Maca according to the type and the content of active components such as glucosinolates, essential oils, macamides, and macaenes by MS. Additionally, the research on the change of active components in Maca at different growth stages by MS will be beneficial to full utilization of active components in Maca and other natural resources. We reviewed the study in the visible distribution of amino acids, amide alkaloids, imidazolium alkaloids, and saccharides in Maca by imaging mass spectrometry (IMS). We also reviewed the pharmacology value associated with improvement of reproductive function, anti-stress response, anti-osteoporosis, antitumor activity, clinical research and toxicity of Maca, and so forth. Nevertheless, due to individual differences and limitations of the subjects, further high-quality studies are needed to confirm the clinical efficacy of the plant.

Antioxidant and antitumoral activities of isolated macamide and macaene fractions from Lepidium meyenii (Maca).

In this paper, a UPLC-ESI-MS was established to analyze macamide and macaene fractions from Lepidium meyenii (Maca). The antioxidant activity of Maca crude extract (MCE), total macamides (TMM) and total macaenes (TME) was evaluated by DPPH radical scavenging, ABTS radical scavenging and reducing power. The ability of MCE, TMM and TME against multiple cancer cell lines (leukemia HL-60, lung cancer A549, liver cancer SMMC-7721, breast cancer MCF-7, and colon cancer SW480) was used to evaluate their anticancer activity. The results demonstrate that TMM has the best free radical scavenging ability and reducing power compared to MCE, TME, and TMM, TME has the weakest antioxidant capacity compared to them. The difference in antioxidant properties between TMM and TME may be caused by benzylated alkamide in the chemical structure. TMM also has a good inhibitory effect on the five cancer cells. N-benzyl-(9Z, 12Z, 15Z)-octadecatrienamide (NBot) is the most cytotoxicity inhibitory of the macamides tested. The inhibitory effect of N-benzyl-9Z, 12Z-octadecadienamide (NBod) on colon cancer SW480 is near that of control group, while the inhibitory rates of NBot on leukemia HL-60, lung cancer A549, liver cancer SMMC-7721, and breast cancer MCF-7 are near those of the control group. Hence, NBot can be considered to have great potential as a natural drug with high efficiency and low side effects for cancer therapy.

[Effect of Lepidium meyenii (Maca) on neurotransmitter level and neuro-endocrine-immune network of deficiency-cold and deficiency-heat syndrome rats].

The aim of this paper was to study the effect of Lepidium meyenii(Maca) on cyclic nucleotides, neurotransmitter levels and hypothalamic-pituitary-adrenal axis and immunization of deficiency-cold and deficiency-heat syndrome rats, in order to explore the cold and hot medicinal properties of Maca. SD rats were divided into blank group, deficiency-cold syndrome group, Cinnamomi Cortex of deficiency-cold syndrome(30 g·kg~(-1)) group, high and low-dose Maca groups(2.4, 1.2 g·kg~(-1)), deficiency-heat syndrome group, Phellodendri Chinensis Cortex(PCC) of deficiency-heat syndrome(5 g·kg~(-1)), and high and low-dose Maca groups(2.4, 1.2 g·kg~(-1)). The rats were treated with intramuscular injection of hydrocortisone(20 mg·kg~(-1)) or dexamethasone sodium phosphate(0.35 mg·kg~(-1)) for 21 days to set up the deficiency-cold and deficiency-heat model. The levels of cAMP, cGMP, NE, DA, 5-HT, CRH, ACTH, CORT and IgM, IgG, C3, C4 were detected by radio immunoassay. Both the high-dose Maca group and the low-dose Maca group can significantly improve the overall state and body weight of rats with deficiency-cold syndrome(P<0.01, P<0.05), significantly increasing cAMP, cAMP/cGMP, NE, DA, ACTH(P<0.01, P<0.001), and significantly decreasing 5-HT(P<0.01, P<0.001). However, high-dose and low-dose Maca groups could not improve the deficiency-heat syndrome, and the levels of cAMP, cGMP, cAMP/cGMP, NE, DA, 5-HT and ACTH were not statistically significant. Maca had a significant regulatory effect on CORT, IgM, IgG and C3 content of rats with deficiency-cold and deficiency-heat syndrome(P<0.01, P<0.05, P<0.001). Maca showed the same effect with Cinnamomi Cortex in adjusting the levels of deficiency-cold rats, but in opposition to Phellodendri Chinese Cortex. This paper confirmed that Maca was slightly warm based on its effect on cyclic nucleotide levels and neuro-endocrine-immune networks by the pharmacological experimental method.

Effect of Lepidium meyenii (Maca) on neurotransmitter level and neuro-endocrine-immune network of deficiency-cold and deficiency-heat syndrome rats / 中国中药杂志

The aim of this paper was to study the effect of Lepidium meyenii(Maca) on cyclic nucleotides, neurotransmitter levels and hypothalamic-pituitary-adrenal axis and immunization of deficiency-cold and deficiency-heat syndrome rats, in order to explore the cold and hot medicinal properties of Maca. SD rats were divided into blank group, deficiency-cold syndrome group, Cinnamomi Cortex of deficiency-cold syndrome(30 g·kg~(-1)) group, high and low-dose Maca groups(2.4, 1.2 g·kg~(-1)), deficiency-heat syndrome group, Phellodendri Chinensis Cortex(PCC) of deficiency-heat syndrome(5 g·kg~(-1)), and high and low-dose Maca groups(2.4, 1.2 g·kg~(-1)). The rats were treated with intramuscular injection of hydrocortisone(20 mg·kg~(-1)) or dexamethasone sodium phosphate(0.35 mg·kg~(-1)) for 21 days to set up the deficiency-cold and deficiency-heat model. The levels of cAMP, cGMP, NE, DA, 5-HT, CRH, ACTH, CORT and IgM, IgG, C3, C4 were detected by radio immunoassay. Both the high-dose Maca group and the low-dose Maca group can significantly improve the overall state and body weight of rats with deficiency-cold syndrome(P<0.01, P<0.05), significantly increasing cAMP, cAMP/cGMP, NE, DA, ACTH(P<0.01, P<0.001), and significantly decreasing 5-HT(P<0.01, P<0.001). However, high-dose and low-dose Maca groups could not improve the deficiency-heat syndrome, and the levels of cAMP, cGMP, cAMP/cGMP, NE, DA, 5-HT and ACTH were not statistically significant. Maca had a significant regulatory effect on CORT, IgM, IgG and C3 content of rats with deficiency-cold and deficiency-heat syndrome(P<0.01, P<0.05, P<0.001). Maca showed the same effect with Cinnamomi Cortex in adjusting the levels of deficiency-cold rats, but in opposition to Phellodendri Chinese Cortex. This paper confirmed that Maca was slightly warm based on its effect on cyclic nucleotide levels and neuro-endocrine-immune networks by the pharmacological experimental method.

Chemical Analysis of Lepidium meyenii (Maca) and Its Effects on Redox Status and on Reproductive Biology in Stallions †.

The present study was conducted to assess the chemical composition of Yellow Maca (Lepidium meyenii) and its biological activity on stallions following oral administration of hypocotyl powder. Maca was subjected to methanolic extraction and the chemical analysis was carried out by LC-MS-QTOF (liquid chromatography-mass spectrometry). Our results showed that Maca contains some effective antioxidants, a high percentage of glucosinolates, and other important components with a high antioxidant capacity. To evaluate the plant biological activity in stallions fed with Maca powder for 60 days, the redox status and some reproductive parameters were investigated. Blood and semen samples were collected at 0, 30, 60, and 90 days from the beginning of this study. Blood samples showed a decrease of the reactive oxygen metabolites, evaluated by d-ROMs test, and an increase of the antioxidant barrier in terms of biological antioxidant potential (BAP test), powerful oxidant capacity (OXY-Adsorbent test), and thiols evaluation (-SHp test). Furthermore, semen samples showed a positive trend during Maca administration in the following parameters: ejaculate volumes and sperm concentrations, total and progressive motility, and acrosome integrity.

Inhibition of Fatty Acid Amide Hydrolase (FAAH) by Macamides.

The pentane extract of the Peruvian plant, Lepidium meyenii (Maca), has been demonstrated to possess neuroprotective activity in previous in vitro and in vivo studies (Pino-Figueroa et al. in Ann N Y Acad Sci 1199:77-85, 2010; Pino-Figueroa et al. in Am J Neuroprot Neuroregener 3:87-92, 2011). This extract contains a number of macamides that may act on the endocannabinoid system (Pino-Figueroa et al. in Ann N Y Acad Sci 1199:77-85, 2010; Pino-Figueroa et al., 2011; Dini et al. in Food Chem 49:347-349, 1994). The aim of this study was to characterize the inhibitory activity of four of these maccamides (N-benzylstearamide, N-benzyloleamide, N-benzyloctadeca-9Z,12Z-dienamide, and N-benzyloctadeca-9Z,12Z,15Z-trienamide) on fatty acid amide hydrolase (FAAH), an enzyme that is responsible for endocannabinoid degradation in the nervous system (Kumar et al. in Anaesthesia 56:1059-1068, 2001). The four compounds were tested at concentrations between 1 and 100 µM, utilizing an FAAH inhibitor screening assay. The results demonstrated concentration-dependent FAAH inhibitory activities for the four macamides tested. N-Benzyloctadeca-9Z,12Z-dienamide demonstrated the highest FAAH inhibitory activity whereas N-benzylstearamide had the lowest inhibitory activity. In addition, N-benzylstearamide, N-benzyloleamide, and N-benzyloctadeca-9Z,12Z-dienamide demonstrated time-dependent inhibition when tested after a pre-incubation period, indicating that the mechanism of inhibition for these compounds most likely is irreversible. Of interest, unsaturation in the fatty acid moiety resulted in greater FAAH inhibitory activity. LC/MS/MS analysis demonstrated that FAAH was able to hydrolyze N-benzyloctadeca-9Z,12Z-dienamide, suggesting that N-benzyloctadeca-9Z,12Z-dienamide is also a slow substrate for FAAH. These results provide useful information about the mechanism of action of Lepidium meyenii and may help with the development of new compounds with FAAH inhibitory or modulatory activity.

Composition analysis and antioxidant activity of essential oils, lipids and polysaccharides in different phenotypes of Lepidium meyenii.

The phenotypes of Lepidium meyenii (Maca) relate to their difference of chemical compositions and biological activities. Essential oils, lipids and polysaccharides are the main active components in Maca, all of which showed potential antioxidant effect. The essential oil, lipid and polysaccharide compositions were analyzed by GC-MS after the samples were properly pre-treated from yellow, red and black Maca. The antioxidant properties of the three types of components were examined using the DPPH scavenging assay. The correlation of main compositions and the antioxidant activities was evaluated by a statistical method. In Maca essential oil, lipid and polysaccharide samples, thirty volatile compounds, twenty-nine fatty acids and six monosaccharides had been detected, in which benzeneacetonitrile, unsaturation fatty acids and mannose were predominant ingredients, respectively. In three types of components, the DPPH scavenging effect of essential oil was stronger. All of black Maca essential oil, lipid and polysaccharide showed higher effect than yellow and red phenotype. The total activity of the three types of components showed about 60% of the antioxidant activity of entire Maca. Canonical correlation analysis (CCA) results showed that four essential oils, three fatty acids and four monosaccharaides were positively related to the antioxidant activity. The research is helpful to address the quality attributes and the comprehensive application of different phenotypes of Maca.

Influences of dietary supplementation with Lepidium meyenii (Maca) on stallion sperm production and on preservation of sperm quality during storage at 5 °C.

Stallion semen is damaged by oxidative stress during cooling and transport. Semen processing and extenders have been tested to improve the fertilizing capacity of semen and to preserve semen during transport. Dietary supplementation with natural antioxidants has been proposed to prevent oxidative damages. In this study, for the first time, the effect of dietary supplementation with Lepidium meyenii (Maca) on the characteristics of fresh and chilled stallion semen was evaluated. Maca is a traditional Andean crop used as a nutraceutical for the fertility-enhancing properties that are linked with antioxidant activity. The diet of five stallions was supplemented with 20 g of Maca powder daily for a total of 60 days. A control group of five stallions received the same diet without Maca. Semen was collected once before the administration of Maca (D0), twice during the administration at 30 and 60 days (D30 and D60), and finally twice at 30 and 60 days after the end of the administration (D90 and D120). Ejaculates were processed for cooled shipping at 5 °C and evaluated in the laboratory for total and progressive motility, acrosome integrity, and lipid peroxidation after collection and after 24, 48, and 72 h of storage. Dietary supplementation with Maca improved sperm concentration (from 213 ± 80.4 to 447 ± 73.1 × 106 spz/mL) and total sperm count (from 10,880 ± 4377 to 24,783 ± 4419 × 106 spz). The beneficial effects of Maca supplementation on motility and acrosome integrity in the raw semen were detected from the end of treatment with Maca (D60) until the end of the study (D120). Furthermore, during cooling storage, total motility, progressive motility, and acrosome integrity declined more slowly in the Maca-treated group than in the control group. Lipid peroxidation did not change during cooling storage in either group and did not show a significant difference between the two groups. In this study, the dietary supplementation with Maca increased sperm production and stabilized semen quality during chilled storage.

[Research and application progress of Lepidium meyenii（maca）].

Lepidium meyenii（maca）was a herbaceous plant of the family Cruciferae. It is native to the andes region of South America where the local people had been growing and consuming maca for centuries. The unique chemical composition and physiological function of maca were widely concerned worldwide. It was introduced to China in 2002, and were cultivated successfully in Yunnan, Tibet, Sichuan, Jilin and other places with a certain size. Maca contained not only rich nutrition such as protein, vitamin and mineral matter, but also lots of secondary metabolites as maca alkaloids, glucosinolates, volatile oils, sterols polyphenols and macaenes. Numerous studies suggested that maca may serve effects in resisting oxidation, fatigue resistance, raising fertility, regulating endocrine, enhancing immunity, tumour suppression, treating osteoporosis, regulate blood sugar and protection of nervous system. Maca was approved by the Ministry of Health as a new resource food in 2011, and its related products include food, health foods, cosmetics, etc. Certain exploratory researches were carried to take better advantage of maca's medicinal value. This paper briefly reviewed the research and application progress of maca in recent years from the aspects of botany, chemical composition, function, resources situation and related products development, which was supposed to provide reference for scientific research and utilization of maca.

Research and application progress of Lepidium meyenii（maca） / 中国中药杂志

Lepidium meyenii（maca）was a herbaceous plant of the family Cruciferae. It is native to the andes region of South America where the local people had been growing and consuming maca for centuries. The unique chemical composition and physiological function of maca were widely concerned worldwide. It was introduced to China in 2002, and were cultivated successfully in Yunnan, Tibet, Sichuan, Jilin and other places with a certain size. Maca contained not only rich nutrition such as protein, vitamin and mineral matter, but also lots of secondary metabolites as maca alkaloids, glucosinolates, volatile oils, sterols polyphenols and macaenes. Numerous studies suggested that maca may serve effects in resisting oxidation, fatigue resistance, raising fertility, regulating endocrine, enhancing immunity, tumour suppression, treating osteoporosis, regulate blood sugar and protection of nervous system. Maca was approved by the Ministry of Health as a new resource food in 2011, and its related products include food, health foods, cosmetics, etc. Certain exploratory researches were carried to take better advantage of maca's medicinal value. This paper briefly reviewed the research and application progress of maca in recent years from the aspects of botany, chemical composition, function, resources situation and related products development, which was supposed to provide reference for scientific research and utilization of maca.

(+)-Meyeniins A-C, Novel Hexahydroimidazo[1,5-c]thiazole Derivatives from the Tubers of Lepidium meyenii: Complete Structural Elucidation by Biomimetic Synthesis and Racemic Crystallization.

(+)-Meyeniins A-C (1-3), a novel class of sulfur-containing hexahydroimidazo[1,5-c]thiazole derivatives, were isolated from the tubers of Lepidium meyenii (maca) cultivated in Lijiang, Yunnan province, China. Guided by their biosynthetic hypothesis, a stereocontrolled biomimetic synthesis of meyeniins A-C and their individual enantiomers was efficiently accomplished by a combination of a condensation reaction and Edman degradation. The formation of high-quality crystals for X-ray crystallography occurred much more readily from a racemic mixture of (±)-meyeniin A than with the single enantiomer alone in this case. These extensive strategies, combined with circular dichroism (CD) spectra, allowed the complete structural assignments of (+)-meyeniins A-C. Among them, (+)-meyeniin A showed moderate selective cytotoxicities against the HL-60, A549 and MCF-7 human cell lines with IC50 values of 14.41, 32.22, and 33.14 µM, respectively. To some extent, these findings support traditional applications of maca as healthy nutritional supplements or functional foods for cancer prevention.

Synergistic effect of the hydroalcoholic extract from Lepidium meyenii (Brassicaceae) and Fagara tessmannii (Rutaceae) on male sexual organs and hormone level in rats.

BACKGROUND: Lepidium meyenii is a plant, which has been used in folk medicine to treat infertility and to increase sexual desire. However, few reports have investigated the administration of this plant with other plants having the same properties. OBJECTIVE: The present investigation was designed to evaluate whether the combination of Lepidium meyenii and Fagara tessmannii can improve spermatogenesis and testosterone level in rats. MATERIALS AND METHOD: Twenty male rats were treated daily for 2 weeks with the hydroalcoholic extract of Fagara tessmannii and Lepidium meyenii (Fag + MN) as follow: (vehicle), (0.01 g + 0.5 mg), (0.1 g + 5 mg) and (1 g+ 50 mg)/kg BW. RESULTS: At doses Fag 0.01 g/MN 0.5 mg and Fag 0.1 g/MN 5 mg, the weight of seminal vesicle, prostate, and testis significantly decreased (P < 0.05) while at dose Fag 1 g/MN 50 mg, the weight of epididymis and testis significantly increased (P < 0.05) when compared to the control. We noticed a significant increase of the number of spermatids/test (P < 0.05), epididymis sperm count (P < 0.05), and DSP/test of the rats at dose Fag 1 g/MN 50 mg while at dose Fag 0.01 g/MN 0.5 mg and Fag 0.1 g/MN 5 mg, sperm count was reduced in male organs, particularly in vas deferens (P < 0.05) and epididymis (P < 0.001). The serum testosterone concentration significantly decreased (P < 0.05) at lowest dose Fag 0.01 g/MN 0.5 mg. However, at highest dose Fag 1 g/MN 50 mg, the serum testosterone concentration increased significantly (P < 0.05). The length of stage VII-VIII and IX-I of the seminiferous tubule significantly (P < 0.05) increased while the length of stage II-VI significantly (P < 0.05) decreased. CONCLUSION: The results indicated that the combination of Lepidium meyenii (Black Maca) with Fagara tessmannii can improve male reproductive organs activities.