In vitro and in vivo antihypertensive and antioxidant activities of fermented roots of Allium hookeri / 中草药·英文版

Objective: To evaluate antihypertensive and antioxidant activities of Allium hookeri root (AHR) fermented with Lactobacillus plantarum, Leuconostoc mesenteroides, and Weissella cibaria. Methods: The novel fermented AHR products using L. plantarum, L. mesenteroides, and W. cibaria were developed and ACE inhibitory activity, DPPH radical scavenging activity, hydroxyl radical scavenging activity, superoxide anion radical scavenging activity, total phenolic content, and total thiosulfinate content were determined. The antihypertensive and antioxidant effects of fermented AHR were further investigated in spontaneously hypertensive rats (SHRs). Results: Administration of fermented AHR to SHRs had an attenuating effect on both diastolic and systolic blood pressure. The SHRs treated with fermented AHR showed lower plasma ACE activity and higher plasma NO levels. Furthermore, fermented AHR administration led to parallel improvements in plasma oxidative stress biomarkers in SHRs. Conclusion: Our results highlight the potential usefulness of fermented AHR for the prevention of hypertension.

Research progress on chemical ingredients of Aleppo Avens and their pharmacological effects / 中草药

Aleppo Avens, a traditional Chinese medicine, has been commonly used for the treatment of headache and dizziness, infantile convulsion, hypertension, lumbar and leg pain, irregular menstruation, and so on. However, the underlying mechanisms of the functions remain unclear. Up to the present, terpenoids (monoterpene, sesquiterpene and three terpenoids), tannins and phenylpropyl esters were found as the main chemical composition in Aleppo Avens. Accumulating studies showed that Aleppo Avens possess the pharmacological profile of anticoagulant, antihypertensive, anti-inflammatory, anticancer, and anti-ischemia. The present paper reviewed the researches of active ingredients and pharmacological effects of Aleppo Avens in recent 40 years, and provided the pharmacological basis for the clinical application and further rational development of Aleppo Avens.

Flax lignan concentrate attenuate hypertension and abnormal left ventricular contractility via modulation of endogenous biomarkers in two-kidney-one-clip (2K1C) hypertensive rats

ABSTRACT The present investigation was designed to study the effect of flax lignan concentrate obtained from Linum usitatissimum L., Linaceae, in two-kidney, one clip (2K1C) hypertension model in Wistar rats. 2K1C Goldblatt model rats were divided randomly into six groups: sham, 2K1C control, captopril (30 mg/kg), flax lignan concentrate (200, 400 and 800 mg/kg). Flax lignan concentrate and captopril were administered daily for eight consecutive weeks. Sham-operated, and 2K1C control rats received the vehicle. Treatment with flax lignan concentrate (400 and 800 mg/kg) significantly and dose-dependently restored the hemodynamic parameters systolic blood pressure, diastolic blood pressure, mean arterial blood pressure and left ventricular functions. The flax lignan concentrate significantly restored the elevated hepatic, renal and cardiac marker enzymes in the serum. It also restored the organs weights (kidney and heart), serum electrolyte level and histological abnormalities. Furthermore, flax lignan concentrate significantly elevated the level of biochemical markers that is enzymatic antioxidants superoxide dismutase, glutathione and decreased malondialdehyde in the heart and kidney tissues. Meanwhile, we found that plasma nitric oxide and plasma nitric oxide synthase contents were significantly increased in the flax lignan concentrate-treated group, and plasma endothelin-1 and renal angiotensin-II levels were significantly lower than 2K1C hypertensive group. In conclusion, the antihypertensive and antioxidant effect of flax lignan concentrate were dose-dependent and at the highest dose (i.e. 800 mg/kg) similar to those of captopril (30 mg/kg). It is suggested that flax lignan concentrate reduced blood pressure by reduction of renal angiotensin-II level, inhibition of plasma endothelin-1 production, induction of the nitric oxide, nitric oxide synthase and in vivo antioxidant defense system.

Current natural products with antihypertensive activity / 中国天然药物

Natural products have been an important source of new drugs, which also played a dominant role in the discovery and research of new drugs for the treatment of hypertension. This review article reviews the recent progress in the research and development of natural lead compounds with antihypertensive activity, including alkaloids, diterpenes, coumarins, flavonoids, and peptides. We summarized their structures, sources, as well as the antihypertensive mechanisms. These information provides instructive reference for the following structural modifications and optimization.

Synthesis of Some New Phthalimides as Anti-metabolic Agents with Chemotherapeutic Effects.

A series of new phthalimides 1(a-f) were synthesized via reaction phthalic anhydride with different amino acids under fusion conditions. Esterification of N-phthaloyl acid derivatives 1(a-f) with methanol in the presence of SOCl2 to producing the corresponding esters 2(a-f). Which on reaction with hydrazine hydrate in boiling n-butanol afforded the corresponding N-phthaloyl acid hydrazides 4(a-f) Reaction of compound (4a) with different aldehydes and ketones yielded the corresponding hydrazone derivatives 5(a-d). Some new phthalimides linked to hetero cyclic moieties such as benzimidazoles, benzoxazines and quinazolines were synthesized. The structure of the synthesized compounds was confirmed from their analytical and spectral data such as, IR spectra, 1H-NMR and mass spectra. Antimicrobial against two types of bacteria and anticancer activity for some of the synthesized imides were evaluated. The results showed that most of them have a good antimicrobial and anticancer activities.

El efecto antihipertensivo de las leches fermentadas / The antihypertensive effect of fermented milks

Existe una gran variedad de leches fermentadas con bacterias lácticas, con propiedades que promueven la salud. Recientemente se ha comunicado que las proteínas de los alimentos pueden, además, ejercer otras funciones in vivo, por medio de sus péptidos con actividad biológica. Estos péptidos se encuentran encriptados dentro de la estructura primaria de las proteínas y pueden ser liberados por fermentación de la leche, hidrólisis enzimática, o bien durante el tránsito gastrointestinal. Las funciones que presentan son diversas, ya que pueden actuar en diferentes sistemas del cuerpo humano: el cardiovascular, el digestivo, el endocrino, el inmune y el nervioso. Los péptidos bioactivos que presentan un efecto en el sistema cardiovascular (antihipertensivo, antitrombótico, antioxidante o hipocolesterolémico) pueden reducir los factores de riesgo para la manifestación de enfermedades crónicas y ayudar a mejorar la salud humana. Los péptidos bioactivos más estudiados son aquellos que ejercen un efecto antihipertensivo a través de la inhibición de la enzima convertidora de angiotensina (ACE). Este documento se enfoca en la producción de péptidos antihipertensivos inhibidores de la ACE en leches fermentadas, en su historia, y en las pruebas in vivo realizadas en ratas y en humanos, donde se ha demostrado su efecto hipotensor.

There is a great variety of fermented milks containing lactic acid bacteria that present health-promoting properties. Milk proteins are hydrolyzed by the proteolytic system of these microorganisms producing peptides which may also perform other functions in vivo. These peptides are encrypted within the primary structure of proteins and can be released through food processing, either by milk fermentation or enzymatic hydrolysis during gastrointestinal transit. They perform different activities, since they act in the cardiovascular, digestive, endocrine, immune and nervous systems. Bioactive peptides that have an antihypertensive, antithrombotic, antioxidant and hypocholesterolemic effect on the cardiovascular system can reduce the risk factors for chronic disease manifestation and help improve human health. Most studied bioactive peptides are those which exert an antihypertensive effect by inhibiting the angiotensin-converting enzyme (ACE). Recently, the study of these peptides has focused on the implementation of tests to prove that they have an effect on health. This paper focuses on the production of ACEinhibitory antihypertensive peptides from fermented milks, its history, production and in vivo tests on rats and humans, on which its hypotensive effect has been shown.

Synthesis and β-adrenergic blocking activity of oxime ether hybrids derived from a natural isochroman-4-one / 中国天然药物

AIM@#In a search for new cardiovascular drug candidates, a series of novel oxime ethers derived from a natural isochroman-4-one were synthesized.@*METHOD@#Compounds 3 and 6, derived from the natural antihypertensive compound 7, 8-dihydroxy-3-methyl-isochroman-4-one (XJP), were designed and synthesized. Subsequently, a series of novel isochroman-4-one oxime ether hybrids were prepared by hybridizing various N-substituted isopropanolamine functionalities to isochroman-4-one oxime. Furthermore, β1-adrenergic blocking activities of the synthesized compounds were assayed using the isolated rat left atria.@*RESULTS@#Twenty target compounds were obtained, and the preliminary structure-activity relationships were deduced. The most promising compound Ic exhibited β1-adrenoceptor blocking activity (inhibition: 52.2%) at 10(-7) mol·L(-1), which was superior to that of propranolol (inhibition: 49.7%).@*CONCLUSION@#The results suggested that natural product XJP/isopropanolamine moiety hybrids may provide a promising approach for the discovery of novel cardiovascular drug candidates.