木立芦荟不同叶龄叶的解剖学和组织化学及其植物化学研究

应用植物解剖学、组织化学、荧光显微观察与植物化学技术相结合,研究了木立芦荟不同叶龄叶的解剖结构、叶绿素和类胡萝卜的含量、芦荟素的含量及其合成和贮藏结构的特点。结果表明:芦荟素由同化薄壁组织产生,叶绿体的基质为其合成场所。芦荟素细胞可能是芦荟素早期贮存的场所,随着芦荟素细胞的逐渐萎缩老化,维管束鞘细胞成为贮藏芦荟素的代替场所。同一植株的叶随着叶龄的增长,维管束的密度降低,芦荟素细胞占维管束横切面的百分比减小,同化薄壁组织细胞中的叶绿体逐步衰老、解体,芦荟素含量逐渐降低,但不同叶龄叶中叶绿体色素的含量与芦荟素含量间没有明显的相关性。     

中华芦荟叶的解剖学、组织化学和植物化学研究

用解剖学,组织化学和植物化学方法研究了中华芦荟（Aloe vera L.var.chinensis(Haw.)Berg.)叶的结构,芦荟素的含量及其可能的储藏和合成场所,解剖学研究结果表明,中华芦荟叶的结构由表皮,同化薄壁组织,维管束和储水组织组成,其旱生结构特征比较明显,表皮具厚的角质层,外切向壁次生加厚,气孔下陷,中央储水组织发达,绿色组织没有明显的分化,其中,5个细胞环绕的气孔器和叶基出现的第二轮维管束在芦荟属中首次报道,具有种的特征,中华芦荟叶中所含的蒽醌类次生代谢物主要是芦荟素（barbaloin or aloin),其含量和叶位及同一叶的不同部位有关,植株上剖嫩叶及每一叶的上部含量高于下部老叶和叶的中部,叶基部含量最低,比较被测的解剖学指标和植物化学分析的结果发现,叶中维管束的密度和芦荟素的含量呈明显的正相关,用5％Pb(CH3COOH)2沉淀处理及5％NaOHR颜色反应检测芦荟素的储藏物合成部位,初步结果表明,位于韧皮部端的数个发达大型薄壁细胞是芦荟素的储藏场所,而绿色组织和维管束鞘是可能的合成场所。     

Phytochemistry and antimycobacterial activity of Chlorophytum inornatum

In a project to investigate plant derived natural products from the Liliaceae with activity against fast-growing strains of mycobacteria, we have identified two new metabolites from Chlorophytum inornatum. The active principle, a new homoisoflavanone (1) was identified as 3-(4'-methoxybenzyl)-7,8-methylenedioxy-chroman-4-one. The metabolite assigned as 7-(1'-hydroxyethyl)-2-(2'-hydroxyethyl)-3,4-dihydrobenzopyran (2) was characterised by extensive 1- and 2D NMR spectroscopy. The antimycobacterial activity of this plant was mainly due to the homoisoflavonoid which exhibited minimum inhibitory values ranging from 16-256 microg/ml against four strains of fast-growing mycobacteria.     

Synthesis of bis-Schiff bases of isatins and their antiglycation activity

Bis-Schiff bases 1–27 have been synthesized and their in vitro antiglycation potential has been evaluated. Compounds 21 (IC₅₀ = 243.95 ± 4.59 μM), 20 (IC₅₀ = 257.61 ± 5.63 μM), and 7 (IC₅₀ = 291.14 ± 2.53 μM) showed an excellent antiglycation activity better than the standard (rutin, IC₅₀ = 294.46 ± 1.50 μM). This study has identified a series of potential molecules as antiglycation agents. A structure–activity relationship has been studied, and all the compounds were characterized by spectroscopic techniques.     

Synthesis and antiglycation potentials of bergenin derivatives

Bergenin (1), major bioactive compound isolated from methanolic extract of Mallotus philippinensis, displayed moderate AGE inhibition activity (IC₅₀ = 186.73 μM). A series of derivatives of bergenin (3a-k) containing variety of aromatic acids were synthesized under mild conditions by modification of sugar part. Selective esterification of hydroxyl groups on the sugar part enhanced antiglycation potential of bergenin. Compounds 3j and 3k exhibited potent antiglycation activity with the IC₅₀ values of 60.75 and 12.28 μM, respectively.     

Phytochemistry and pharmacognosy

During the past 50 years there have been tremendous advances in chemical and biological techniques of analysis that have transformed research in pharmacognosy. The PSE has regularly held symposia of relevance to pharmacognosy and some of these are briefly reviewed in the area of natural products from higher plants. These symposia have charted the developments that link pharmacognosy with phytochemistry and illustrate the application of increasingly more sophisticated analytical techniques to the discovery of biologically active compounds. Plants have yielded clinical drugs, either as natural product molecules, or as synthetic modifications, particularly for chemotherapeutic treatment of cancer and malaria. Aspects of biotechnology, traditional medicines and herbal medicinal products are briefly discussed.     

The relationship between antiglycation activity and procyanidin and phenolic content in commercial grape seed products

Eight commercial grape seed products (GSPs) were assessed for their inhibition of the formation of advanced glycation end-products in vitro. All 8 commercial GSPs included in this study were potent inhibitors of advanced glycation end-product formation with IC(50) values ranging from 2.93 to 20.0?μg/mL. Total procyanidin content ranged from 60% to 73%. HPLC-DAD-ELSD results indicate that (+)-catechin, (-)-epicatechin, procyanidin B1, and procyanidin B2 were predominant and ubiquitously present in all the products under study, while gallic acid and procyanidin B4 were present in relatively minor amounts. The IC(50) values correlated with total phenolic content, and multiple regression analysis indicated that IC(50) is a linear function of the concentration of gallic acid and procyanidins B1, B2, and B4. Based on this study, GSPs have the potential to complement conventional diabetes medication toward disease management and prevention.     

Phytochemistry of proanthocyanidins

Procyanidin A from Aesculus hippocastanum differs from the B type procyanidin in that it is difficultly soluble in water, gives a higher yield of cyanidin when heated in butanolic HCl and the production of cyanidin continues beyond the 2 hr period sufficient for maximum production in the case of B type procyanidin. Anthocyanidin production and tannic acid equivalent (TAE) of extracts of species in which A and D type procyanidins have been reported to occur have been studied. Evidence of their presence was also found in Ribes laurifolium. Preparations of prodelphinidin from leaves of red currant and sainfoin had approximately twice the anthocyanidin production and the astringency of procyanidin B. Sources especially rich in prodelphinidin were a number of Ribes spp., Salix cinerea and Platanus acerifolia, from all of which the tannin was easily extracted. Some other species such as Pilea cadieri, although rich in prodelphinidin, are not suitable as sources because of the inextractability of the tannin.     

Antioxidant and antiglycation properties of Hydnora johannis roots

Natural extracts or compounds that possess both antioxidant and antiglycation activities might have great therapeutic potential for treating diabetic complications. The main purpose of this study was to evaluate the antioxidant and antiglycation properties of aqueous and EtOH (70%) extracts as well as three isolated compounds (protocatechuic acid, catechin and vanillin) from Hydnora johannis (Hydnoraceae) roots. The antioxidant activity of both extracts and isolated compounds was tested by measuring their capacity to scavenge DPPH and ABTS radicals. The glucose-induced advanced glycation end-product (AGE) formation of the extracts and isolated compounds was also carried out using in vitro glucose-bovine serum albumin (BSA-glucose) assay. Results showed that the ethanolic (70%) extract as well as isolated protocatechuic acid and catechin exhibited strong antioxidant and inhibitory effect of AGE formation. Thus, H. johannis roots with its high amount of protocatechuic acid (≈ 3.75 mg/100 g) and catechin (≈ 26.9 mg/100 g) could be a natural candidate for studies of herbal complement to diabetes treatment since it combines antioxidant and anti-AGE formation activities.     

Tyrosinase inhibitory components from Aloe vera and their antiviral activity

A new compound, 9-dihydroxyl-2'-O-(Z)-cinnamoyl-7-methoxy-aloesin (1), and eight known compounds (2–9) were isolated from Aloe vera. Their structures were elucidated using 1D/2D nuclear magnetic resonance and mass spectra. Compound 9 exhibited reversible competitive inhibitory activity against the enzyme tyrosinase, with an IC₅₀ value of 9.8?±?0.9?µM. A molecular simulation revealed that compound 9 interacts via hydrogen bonding with residues His244, Thr261, and Val283 of tyrosinase. Additionally, compounds 3 and 7 were shown by half-leaf assays to exhibit inhibitory activity towards Pepper mild mottle virus.     

Bis-coumarins; non-cytotoxic selective urease inhibitors and antiglycation agents

The current study is concerned with the identification of lead molecules based on the bis-coumarin scaffold having selective urease inhibitory and antiglycation activities. For that purpose, bis-coumarins (1-44) were synthesized and structurally characterized by different spectroscopic techniques. Eight derivatives 4, 8-10, 14, 17, 34, and 40 demonstrated urease inhibition in the range of IC₅₀ = 4.4 ± 0.21–115.6 ± 2.13 μM, as compared to standard thiourea (IC₅₀ = 21.3 ± 1.3 μM). Especially, compound 17 (IC₅₀ = 4.4 ± 0.21 μM) was found to be five-fold more potent than the standard. Kinetic studies were also performed on compound 17 in order to identify the mechanism of inhibition. Kinetic studies revealed that compound 17 is a competitive inhibitor. Antiglycation activity was evaluated using glycation of bovine serum albumin by methylglyoxal in vitro. Compounds 2, 11-13, 16, 17, 19–22, 35, 37, and 42 showed good to moderate antiglycation activities with IC₅₀ values of 333.63–919.72 μM, as compared to the standard rutin (IC₅₀ = 294.46 ± 1.5 μM). Results of both assays showed that the compounds with urease inhibitory activity did not show any antiglycation potential, and vice versa. Only compound 17 showed dual inhibition potential. All compounds were also evaluated for cytotoxicity. Compounds 17, 19, and 37 showed a weak toxicity towards 3 T3 mouse fibroblast cell line. All other compounds were found to be non-cytotoxic. Urease inhibition is an approach to treat infections caused by ureolytic bacteria whereas inhibition of glycation of proteins is a strategy to avoid late diabetic complications. Therefore, these compounds may serve as leads for further research.     

Chromones and anthrones from Aloe marlothii and Aloe rupestris

A phytochemical investigation of the leaf exudate of Aloe marlothii has resulted in the isolation of a new chromone (7-O-methylaloeresin A) and a new anthrone (5-hydroxyaloin A 6'-O-acetate). Furthermore 7-O-methylaloesin was isolated as a natural product for the first time from the leaf exudate of Aloe rupestris. The structure elucidation of these compounds was based on spectral data including 2D NMR. The chemotaxonomic value of 7-O-methylaloesin in Aloe series Asperifoliae and section Pachydendron is discussed.     

Phytochemistry and pharmacognosy of the genus Psorospermum

The genus Psorospermum Baker (tribe Vismieae, family Guttiferae, subfamily Hypericoideae) comprises 55 species, mainly of which are represented by shrubs or small trees typically growing in tropical regions of South America, Africa, and Madasgascar. Most of the species of the title genus have been used for centuries in the ethnomedical traditions of indigenous African populations as febrifugal, antidote against poisons, purgative, stomachic, and as a remedy for the treatment of leprosy, skin diseases (like dermatitis, scabies and eczemas), and subcutaneous wounds. Phytochemicals isolated from Psorospermum spp. comprise alkaloids, simple and prenylated anthraquinones, flavonoids, long chain alcohols and hydrocarbons, steroids, tannins, terpenes, and simple and prenylated xanthones. The reported biological activities of the above mentioned natural compounds refer to anti-bacterial, anti-protozoal, anti-fungal, anti-viral, anti-cancer, anti-oxidant, and neuroprotective effects. The aim of this review is to examine in detail from a phytochemical and pharmacologically points of view what is reported in the current literature about the properties of phytopreparations or individual active principles obtained from plants belonging to Psorospermum genus.