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PubMed2005

Protein tyrosine phosphatase 1B inhibitors from Morus root bark.

An organic layer prepared from the Chinese crude drug 'Sang-Bai-Pi' (Morus root bark) was studied in order to identify the inhibitory compounds for protein tyrosine phosphatase 1B (PTP1B). Bioassay-guided fractionation resulted in the isolation of sanggenon C (1), sanggenon G (2), mulberrofuran C (3) and kuwanon L (4) as PTP1B inhibitors, along with moracin O (5) and moracin P (6). Compounds 1-4 inhibited PTP1B with IC(50) values ranging from 1.6+/-0.3 microM to 16.9+/-1.1 microM.

Drugs, Chinese Herbal↗
PubMed2006

Study on capillary electrophoresis-amperometric detection profiles of different parts of Morus alba L.

A high-performance capillary electrophoresis with amperometric detection (CE-AD) method has been developed for the determination of the pharmacologically active ingredients in different parts of Morus alba L. after a relatively simple extraction procedure. This method was also used in the comparison of bioactive constituent difference in the five parts, based on their electropherograms or characteristic "CE-AD profiles". The effects of several factors such as the acidity and concentration of running buffer, separation voltage, applied potential and injection time were investigated to find the optimum conditions. Method detection limits (S/N = 3) ranged from 1.5 x 10(-7) to 1.4 x 10(-8)g/mL for all 10 analytes, and the assay results were satisfactory.

Electrochemistry↗
PubMed2005

Effects of Morus alba leaf extract on the production of nitric oxide, prostaglandin E2 and cytokines in RAW264.7 macrophages.

Morus alba leaf methanolic extract and its fractions (chloroform, butanol, and aqueous fractions) were found to inhibit NO production in LPS-activated RAW264.7 macrophages without an appreciable cytotoxic effect at concentration from 4 to 100 microg/ml. LPS-induced PGE2 production was significantly reduced only by butanol fraction. In addition, M. alba leaf extract and its fractions significantly decreased the production of TNF-alpha. These findings suggest that M. alba leaf extract seems to be able in suppressing inflammatory mediators. Moreover, the inhibitory activities on COX-2 and iNOS of its butanol fraction are warranted for further elucidation of active principles for development of new antiinflammatory agents.

Animals↗
PubMed2005

Antimicrobial activity of 2-arylbenzofurans from Morus species against methicillin-resistant Staphylococcus aureus.

Nine 2-arylbenzofurans isolated from Morus species were tested for their antimicrobial activities against methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant S. aureus (MRSA), Micrococcus luteus, Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa. Among these compounds, chalcomoracin (a leaf phytoalexine of mulberry tree) exhibited considerable antibacterial activity against MRSAs (MICs 0.78 mug/ml).

Anti-Bacterial Agents↗
PubMed2006

Alpha-glucosidase inhibitory effect of mulberry (Morus alba) leaves on Caco-2.

The effects of brewing time on dry weight content and alpha-glucosidase inhibitory active component released from mulberry (Morus alba) tea were studied. Different tea products showed significant differences in inhibitory activity against both sucrase and maltase. The most effective enzyme inhibition was observed when 3 to 5 min brewing time was applied in tea preparation. In a Caco-2 cell culture experiment the tea reduced the liberated glucose contents in both apical and basal sides of the cell monolayers. It can be concluded that hot water extract of mulberry leaves does have inhibitory effect against alpha-glucosidases, sucrase and maltase enzymes, and has a potential to be consumed as antidiabetic herb tea.

Beverages↗
PubMed2026

Precision UV-B irradiation for flavonoid biofortification in indoor-cultivated Morus nigra: Integrated multi-omics and molecular docking insights.

Precision application of UV irradiation represents an effective strategy for improving the quality of functional food crops under controlled environmental conditions. Morus nigra serves as a significant functional food resource in Xinjiang, with its leaves being rich in diverse bioactive compounds with nutritional and health-promoting properties. In this study, a low-dose UV-B treatment regimen was developed to enhance flavonoids in indoor-cultivated M. nigra without growth penalty. Multi-omics revealed a hormone shift (suppressed auxin vs. activated JA signaling). This triggered transcriptional reprogramming of PAL/4CL and CHS/CYP75B1, redirecting carbon flux towards flavonoid biosynthesis. Transient overexpression of MYB, NAC, and TIFY variants validated this regulatory network. The UV-B-induced NAC upregulated key genes and flavonoids, while different TIFY members showed diverse regulatory effects. Molecular docking predicted that the induced flavonoids had hypoglycemic, antioxidant, and anti-browning potential. This study indicates targeted UV-B as a green biofortification strategy for high-value crops in controlled environments.

Flavonoid biosynthesis↗
PubMed2005

Hypolipidemic and antioxidant effects of Morus alba L. (Egyptian mulberry) root bark fractions supplementation in cholesterol-fed rats.

The 70% alcohol extract of the Egyptian Morus alba L. root bark was fractionated over cellulose CC eluted with water, 50% methanol and finally with 100% methanol to yield 3 fractions (MRBF-1, MRBF-2 and MRBF-3), respectively. In continuation of chromatographic purification of 70% alcohol extract fractions of the Egyptian M. alba L. root bark, 4 compounds namely: mulberroside A, 5,7,2'-trihydroxyflavanone-4'-O-beta-D-glucoside and albanols A and B were isolated from MRBF-2 for the first time from the Egyptian plant. Experimentally induced atherosclerosis was produced by feeding rats a diet enriched in coconut oil (25% by weight) and cholesterol (2% by weight) for 21 days. Then, hypercholesterolemic rats were orally administered (MRBF-1, MRBF-2 and MRBF-3 fractions) in a dose of 500 mg kg(-1) day(-1) for 15 successive days, in order to evaluate their expected hypocholesterolemic activity. Lipid profile parameters such as plasma total cholesterol, LDL-C, VLDL-C, LDL:HDL ratio and triglycerides, as well as plasma and liver lipid peroxides and glutathione-S-transferase enzyme levels, serum paraoxonase enzyme level, LDL oxidation, LDL aggregation and LDL retention, were measured. Plasma and liver glutathione-S-transferase enzyme levels were unaffected in all studied groups. The results revealed that the administration of (MRBF-2 and/or MRBF-3) fractions resulted in alleviation of atherosclerotic state. Administration of MRBF-3 significantly retained plasma and liver peroxides towards their normal levels, and also, produced significant increase in resistance towards major atherogenic modifications; namely LDL oxidation, LDL aggregation and LDL retention by 44%, 30%, and 33%, respectively. Thus, it can be concluded that the consumption of MRBF-2 and (MRBF-3, in some extent) fractions of M. alba L. root bark 70% alcohol extract may act as a potent hypocholesterolemic nutrient and powerful antioxidant via the inhibition of LDL atherogenic modifications and lipid peroxides formation in hypercholesterolemic rats.

Animals↗
PubMed2006

Recognition profile of Morus nigra agglutinin (Morniga G) expressed by monomeric ligands, simple clusters and mammalian polyvalent glycotopes.

The carbohydrate binding properties of a novel member of the subfamily of galactose-specific jacalin-related lectin isolated from the bark of black mulberry (Morus nigra) (Morniga G) was studied in detail by enzyme-linked lectinosorbent and inhibition assays using panels of monomeric saccharides, mammalian polyvalent glycotopes and polysaccharides. Among the natural glycans tested for lectin binding, Morniga G reacted best with glycoproteins (gps) presenting a high density of tumor-associated carbohydrate antigens Tn (GalNAcalpha1-Ser/Thr) and Talpha (Galbeta1-3GalNAcalpha1-). Their reactivities, on a nanogram basis, were up to 72.5, 3.9x10(3), 6.0x10(3), 8.8x10(3) and 2.9x10(4) times higher than that of Tn-containing glycopeptides (M.W.<3000 Da), monomeric T, Tn, GalNAc and Gal, respectively. It also reacted well with many multi-antennary N-glycans with II (Galbeta1-4GlcNAc) termini, ABH histo-blood group antigens and their precursors containing high densities of I/II and T/Tn glycotopes, and sialylated T/Tn. Among the mono-, di- and oligosaccharides tested, Thomsen-Friedenreich (T) disaccharide with aromatic aglycon [Galbeta1-3GalNAcalpha1-benzyl (Talpha1-benzyl)] and Tn glycopeptides were the best inhibitors. Molecular modeling and docking studies indicated the occurrence of a primary GalNAcalpha1- and Galbeta1-3GalNAc glycotope-binding site in Morniga G. Using a recently proposed system [Wu, A.M., 2003. Carbohydrate structural units in glycoproteins and polysaccharides as important ligands for Gal and GalNAc reactive lectins. J. Biomed. Sci. 10, 676-688], the binding properties of the combining sites of Morniga G can be defined as follows: (i) the monosaccharide specificity is GalNAc/Gal>>Man/Glc, GlcNAc and lFuc; (ii) the mammalian glycotope specificity is Talpha1-benzyl>T>Tn>GalNAcbeta1-3Gal (P), while B/E (Galalpha1-3/4Gal), I/II (Galbeta1-3/4GlcNAc), S (GalNAcbeta1-4Gal), F/A (GalNAcalpha1-3GalNAc/Gal) and L (Galbeta1-4Glc) are inactive; (iii) the most active ligand is T/Tn; (iv) simple clustered Tn or triantennary N-glycans with II termini (Tri-II) have limited impact; (v) high-density polyvalent glycotopes play a prominent role for enhancing Morniga G reactivity. These results provide evidence for the binding of this lectin to dense cell surface T/Tn glycoconjugates and facilitate future usage of this lectin in biotechnological and medical applications.

Animals↗
PubMed2004

Guangsangons F-J, anti-oxidant and anti-inflammatory Diels-Alder type adducts, from Morus macroura Miq.

Five Diels-Alder type adducts, named guangsangons F, G, H, I, and J, along with two known compounds, mulberrofuran J and kuwanon J, were isolated from Morus macroura Miq. Their structures were determined by means of spectroscopic analyses and chemical methods. These compounds were regarded biogenetically as Diels-Alder type adducts of dehydroprenylphenols and chalcone derivatives, and (1)H NMR variable temperature experiments suggested that they all existed as an equilibrium mixture of conformational isomers in solution. Among the isolated new compounds, guangsangons H, I, and J displayed potent antioxidant activities and moderate anti-inflammatory activities.

Animals↗
PubMed2003

A structural basis for the difference in specificity between the two jacalin-related lectins from mulberry (Morus nigra) bark.

The activity and specificity of a galactose-specific and a mannose-specific jacalin-related lectin from the bark of the black mulberry (Morus nigra) tree has been re-investigated using different experimental approaches. Both lectins definitely behave as polyspecific lectins recognizing galactose, mannose, and glucose even though MornigaG and MornigaM interact preferentially with galactose and mannose, respectively. The exceptionally extended size of the carbohydrate-binding site of both lectins apparently accounts for their polyspecific character. Parallel studies with other mannose-specific jacalin-related lectins confirmed that their exclusive specificity towards mannose/glucose relies on a reduced size of their carbohydrate-binding site.

Binding Sites↗
PubMed2001

Effect of mulberry (Morus indica L.) therapy on plasma and erythrocyte membrane lipids in patients with type 2 diabetes.

BACKGROUND: Mulberry (Morus indica L.) is non-toxic natural therapeutic agent shown to possess hypoglycemic, hypotensive, and diuretic properties. METHODS: The hypoglycemic effect of the mulberry leaves was evaluated by comparing the anti-diabetic activity of the standard drug, glibenclamide. A total of 24 type 2 diabetic patents were divided randomly into two treatment groups: the mulberry agent and glibenclamide, for 30 days. Serum and erythrocyte membrane lipid profiles of the patients were analyzed before and after the treatments. RESULTS: Patients with mulberry therapy significantly improved their glycemic control vs. glibenclamide treatment. The results from pre- and post-treatment analysis of blood plasma and urine samples showed that the mulberry therapy significantly decreased the concentration of serum total cholesterol (12%, p<0.01), triglycerides (16%, p<0.01), plasma free fatty acids (12%, p<0.01), LDL-cholesterol (23%, p<0.01), VLDL-cholesterol (17%, p<0.01), plasma peroxides (25%, p<0.01), urinary peroxides (55%, p<0.01), while increasing HDL-cholesterol (18%, p<0.01). Although the patients with glibenclamide treatment showed marginal improvement in glycemic control, the changes in the lipid profile were not statistically significant except for triglycerides (10%, p<0.05), plasma peroxides (15%, p<0.05), and urinary peroxides (19%, p<0.05). Both treatments displayed no apparent effect on the concentrations of the glycosylated hemoglobin (Hb A(1)c) in diabetic patients. However, the fasting blood glucose concentrations of diabetic patients were significantly reduced by the mulberry therapy. CONCLUSIONS: Mulberry therapy exhibits potential hypoglycemic and hypolipidemic effects in diabetic patients.

Adult↗
PubMed2003

Antioxidant role of mulberry (Morus indica L. cv. Anantha) leaves in streptozotocin-diabetic rats.

BACKGROUND: The antihyperglycemic and antioxidant role of mulberry (Morus indica L.) leaves were investigated. METHODS: Streptozotocin (STZ)-induced diabetic male Wistar rats were used as experimental models; one group was given 25% dry mulberry leaf powder mixed with the standard diet and another group was given standard diet for a period of 8 weeks. The antihyperglycemic and antioxidant role of mulberry was assessed by determining its effect on blood glucose, lipid peroxidation, reduced glutathione (GSH) concentrations and on the activity of glucose-6-phosphate dehydrogenase (G6PDH) and various antioxidant enzymes in erythrocytes and compared with that of controls. RESULTS: Mulberry-treated diabetic rats showed a significant decrease in fasting blood glucose concentrations indicating a good glycemic control. Increased lipid peroxidation and the activity of catalase (CAT) in erythrocytes observed in diabetic controls were significantly decreased by mulberry leaves (48% and 33%, respectively). Decreased GSH concentrations and the activity of glucose-6-phosphate dehydrogenase and antioxidant enzymes viz., glutathione peroxidase (GPx), glutathione reductase (GR), glutathione-S-transferase (GST) and superoxide dismutase (SOD) observed in uncontrolled diabetes were improved (52%, 69%, 151%, 95%, 24% and 106%) by mulberry treatment very efficiently. CONCLUSION: Mulberry leaves possess antihyperglycemic and antioxidant properties.

Animal Feed↗
PubMed2004

Chalcone dimethylallyltransferase from Morus nigra cell cultures. Substrate specificity studies.

A new prenyltransferase (PT) enzyme derived from the microsomal fractions of cell cultures of Morus nigra was shown to be able to prenylate exclusively chalcones with a 2',4'-dihydroxy substitution and the isoflavone genistein. Computational studies were performed to shed some light on the relationship between the structure of the substrate and the enzymatic activity. PT requires divalent cations, particularly Mg(2+), to be effective. The apparent K(m) values for gamma,gamma-dimethylallyldiphosphate and 2',4'-dihydroxychalcone were 63 and 142 microM, respectively. The maximum activity of the enzyme was expressed during the first 10 days of cell growth.

Cells, Cultured↗
PubMed2003

Determination of 1-deoxynojirimycin in Morus alba L. leaves by derivatization with 9-fluorenylmethyl chloroformate followed by reversed-phase high-performance liquid chromatography.

A rapid and reliable method suitable for assays of a large number of Morus alba leaves for 1-deoxynojirimycin (DNJ) has been developed. DNJ in 0.1 g of freeze-dried leaves was double-extracted in 10 mL of aqueous 0.05 M HCl by vortexing for 15 s at room temperature, derivatized with 9-fluorenylmethyl chloroformate (FMOC-Cl), and analyzed by reversed-phase high-performance liquid chromatography (RP-HPLC) equipped with a fluorescence detector. The double extraction recovered > 99% of extractable DNJ from the leaves. Stabilization of FMOC-derivatized DNJ (DNJ-FMOC) was achieved by diluting the reactant with aqueous acetic acid after derivatization. DNJ-FMOC was stable for at least 16 days under acidic conditions at room temperature (24 degrees C). Linearity ranged between 0.3 and 30 microg mL(-1). The intra- and inter-day precision for DNJ-spiked biological samples was between 0.6 and 1.8% and between 3.7 and 4.5%, respectively.

1-Deoxynojirimycin↗
PubMed2003

Antiviral flavonoids from the root bark of Morus alba L.

A prenylated flavonoid, moralbanone, along with seven known compounds kuwanon S, mulberroside C, cyclomorusin, eudraflavone B hydroperoxide, oxydihydromorusin, leachianone G and alpha-acetyl-amyrin were isolated from the root bark of Morus alba L. Leachianone G showed potent antiviral activity (IC(50) = 1.6 microg/ml), whereas mulberroside C showed weak activity (IC(50) = 75.4 microg/ml) against herpes simplex type 1 virus (HSV-1). Their structures were elucidated by spectroscopic methods.

Acyclovir↗
PubMed2003

Kuwanon G: an antibacterial agent from the root bark of Morus alba against oral pathogens.

Kuwanon G was isolated from the ethyl acetate fraction of methanol extract of Morus alba and its structure was elucidated by 13C-NMR, 1H-NMR and FAB-MS. Antibacterial activity of kuwanon G was investigated by the minimum inhibitory concentration (MIC) test and the viable cell count method. MIC of kuwanon G against Streptococcus mutans causing dental caries was determined to be 8.0 microg/ml. The bactericidal test showed that kuwanon G completely inactivated S. mutans at the concentration 20 microg/ml in 1 min. Kuwanon G also significantly inhibited the growth of other cariogenic bacteria such as Streptococcus sobrinus and Streptococcus sanguis, and Porpyromonas gingivalis causing periodontitis. Transmission electron microscopy (TEM) of kuwanon G treated cells demonstrated remarkable morphological damage of the cell wall and condensation of the cytoplasm.

Anti-Bacterial Agents↗
PubMed2006

Venturia inaequalis-inhibiting Diels-Alder adducts from Morus root bark.

In organic apple orcharding there is a continuous need for natural fungicides effective against Venturia inaequalis (Cooke) Winter, the causal agent of apple scab. In this study an in vitro assay is presented for determining the germination inhibitory potential of extracts and pure compounds. From a screening of plant extracts, the methanol extract of Morus root bark revealed distinct V. inaequalis inhibiting qualities, which were subjected to a bioguided fractionation. Among the isolated metabolites [moracins M (1), O/P (2), kuwanon L (3), and sanggenons D (4), B (5), G (6), O (7), E (8), and C (9)] all the Diels-Alder adducts (3-9) showed an antifungal activity with IC50 values between 10 and 123 microM. The in vitro activity of the most active fraction (A5, IC50 39.0 +/- 4.2 microg/mL) was evaluated in vivo, confirming a distinct antifungal activity against V. inaequalis for the tested natural material.

Antifungal Agents↗
PubMed2002

Hepatoprotective and free radical scavenging activities of prenylflavonoids, coumarin, and stilbene from Morus alba.

Chemical investigation of the EtOH extract of Morus alba L. (Moraceae), as guided by free radical scavenging activity, furnished 5,7-dihydroxycoumarin 7-methyl ether (1), two prenylflavones, cudraflavone B (2) and cudraflavone C (3), and oxyresveratrol (4). Compounds 1 and 4 showed superoxide scavenging effects with the IC(50) values of 19.1 +/- 3.6 and 3.81 +/- 0.5 microM, respectively. Compound 4 exhibited a DPPH free radical scavenging effect (IC(50) = 23.4 +/- 1.5 microM). Compounds 2 and 4 showed hepatoprotective effects with EC(50) values of 10.3 +/- 0.42 and 32.3 +/- 2.62 micro, respectively, on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells.

Biphenyl Compounds↗