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The leaves of Morus alba L. are an important herbal medicine in Asia. The systematic isolation of the metabolites of the leaves of Morus alba L. was achieved using a combination of liquid chromatography techniques. The structures were elucidated by spectroscopic data analysis and the absolute configuration was determined based on electronic circular dichroism (ECD) spectroscopic data and hydrolysis experiments. Their biological activity was evaluated using different biological assays, such as the assessment of their capacity to inhibit the aldose reductase enzyme; the determination of their cytotoxic activity and the evaluation of their neuroprotective effects against the deprivation of serum or against the presence of nicouline. Chemical investigation of the leaves of Morus alba L. resulted in four new structures 1 ⁻ 4 and a known molecule 5 . Compounds 2 and 5 inhibited aldose reductase with IC 50 values of 4.33 μM and 6.0 μM compared with the potent AR inhibitor epalrestat (IC 50 1.88 × 10 −3 μM). Pretreatment with compound 3 decreased PC12 cell apoptosis subsequent serum deprivation condition and pretreatment with compound 5 decreased nicouline-induced PC12 cell apoptosis as compared with control cells ( p < 0.001).

Une new flavonoids named as notabilisin K (1), together with four known compounds, morusin (2), mulberrofuran A (3), neocyclomorusin (4) and mornigrol F (5) are separated from 95% ethanol extracts of the twigs of Morus notabilis. Compounds 2-5 are separated from this plant for the first time. Notabilisin I, notabilisin J exhibits certain effect against cells of HCT-116, HepG2 and A2780 with IC50 values ranging from 1.47 μmol x L(-1) to 5.46 μmol x L(-1). Morusin exhibits strong effect against five kinds of human cancer cells (BGC823, A2780, HCT-116, HepG2 and NCI-H1650) with IC50 values ranging from 0.74 μmol x L(-1) to 1.58 μmol x L(-1).

Phytochemical investigation of the twigs of Morus notabilis led to the isolation and characterization of two new flavonoids, notabilisin F (1) and notabilisin G (2). Their structures were elucidated on the basis of extensive spectroscopic analysis.

Chemical investigation of fruits of Mours alba L. lead to the isolation of fifteen compounds by various chromatographies such as silica gel, Sephadex LH-20, RP-C18 column chromatography. Their structures were determined to be: 1-[5-(2-formlfuryl) methyl] dihydrogen 2-hydroxypropane-1, 2, 3-tricarboxylate 2, 3-diethyl ester (1), 1-[2-(furan-2-yl)-2-oxoethyl] pyrrolidin-2-one (2), divaricataester A (3), methyl 1-[2-(furan-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carboxylate (4), 1-[2-(furan-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carboxylic acid (5), L-pyroglutamic acid (6), L-pyroglutamic acid ethyl ester (7), 3-O-caffeoylquinic acid methyl ester (8), 3-O-caffeoylquinic acid ethyl ester (9), 5-O-caffeoylquinic acid methyl ester (10), 5-O-caffeoylquinic acid ethyl ester (11), 4-O-caffeoylquinic acid methyl ester (12), 4-O-caffeoylquinic acid methyl ester (13), 4-O-caffeoylquinic acid (14), 3-O-caffeoylquinic acid (15), respectively, based on the spectral analysis such as NMR, MS etc. Compounds 1-14 were isolated from this genus for the first time, among which 1 was a new compound.

From the fruits of Morus alba, three new alkaloids, mulbaines A (1), B (2), and C (3) were isolated. The structures of these compounds were elucidated on the basis of spectroscopic methods (UV, IR, HR-ESI-MS, 1D, and 2D NMR).

The mulberry tree (Morus alba) plays a key role in agriculture, and its different parts have been used as popular Traditional Chinese Medicines for thousands of years. There are 16 species belonging to the Morus genus. Among them, 11 species distribute in China, most of which have been used as the substitutes of M. alba in local provinces. This review summarizes the structural characters of polyphenols, the main components in Morus, including Diels-Alder-type adducts, flavonoids, 2-arylbenzofurans, and stilbenes, and also their related bioactivities in the last 10 years.

Two new Diels-Alder adducts, yunanensins B and D (1 and 2), were isolated from the stem bark of Morus yunanensis. Their structures were determined by spectroscopic analysis. Compounds 1 and 2 showed moderate antioxidant effects on liver microsomal lipid peroxidation induced by Fe(2+)-Cys system, with inhibitory ratios of 57.1% and 67.9% at a concentration of 10(-5) mol/l.

Three new 2-arylbenzofurans named wittifuran H, wittifuran I and wittifuran U (1-3) were obtained during our ongoing investigation of an ethanol extract from the stem bark of Morus wittiorum. Their structures were elucidated on the basis of spectroscopic data. Compound 2 displayed potent anti-inflammatory activity and selective cytotoxicity against human gastric cancer cell line BGC-823 with an IC(50) value of 1.45μM., (Copyright © 2012 Elsevier B.V. All rights reserved.)

Four new flavonoids, benzokuwanon E (1), hydroxymorusin (2), dicyclokuwanon EA (3), and dicyclokuwanon EB (4), were isolated from Morus australis. Their structures were elucidated on the basis of UV, IR, MS, NMR, and CD spectral data.

Investigation of an ethanol extract from the stem bark of Morus wittiorum led to the isolation of five new 2-arylbenzofuran derivatives that were named wittifuran S, wittifuran T, wittifuran V, wittifuran W and wittifuran X (1-5). Structures were determined on the basis of spectroscopic analysis. Two new wittifurans and five previously isolated compounds were assayed for antioxidant and anti-inflammatory activity., (Copyright © 2010 Elsevier B.V. All rights reserved.)

A new 2-arylbenzofuran derivative, mornigrol D (1), along with two new flavones, mornigrol G (2) and mornigrol H (3), and six known compounds, norartocarpetin (4), dihydrokaempferol (5), albanin A (6), albanin E (7), moracin M (8), and albafuran C (9), were isolated from the barks of Morus nigra. Their structures were elucidated by spectroscopic analysis. Compounds 1 and 9 showed antioxidative activities in vitro with inhibition ratios of 98 and 99% at the concentration of 10(-4) mol/l, and of 74 and 75% at the concentration of 10(-5) mol/l. In addition, compounds 1 and 4 showed potent anti-inflammatory activities (inhibition of release of beta-glucuronidase from rat polymorphonuclear leucocytes induced by platelet activating factor) with inhibitory ratios of 65.9% (P < 0.01) and 67.7% (P < 0.01) at a concentration of 10(-5) mol/l.

Phytochemical investigation of the stem bark of Morus cathayana led to the isolation and identification of six new compounds, cathayanons F-J (1-5) and cathayanin A (6), and two known compounds, cathayanins B-C (7-8). Their structures were elucidated by spectroscopic methods. Compounds 1, 2, 3, 5, and 7 exhibited weak activities against five human cancer cell lines, with IC(50) values ranging from 4.7 to 9.8 microg/ml.

Five new 2-arylbenzofuran derivatives wittifurans A-C, F and G (1-5) have been isolated from the stem bark of Morus wittiorum. Their structures were determined on the basis of spectroscopic analysis. Compounds 1, 3-5 were evaluated for their antioxidant and anti-inflammatory activities respectively.

Two new flavanes, (2R,4S)-2',4'-dihydroxy-2H-furan-(3'',4'':8,7)-flavan-4-ol (1) and (2S)-2',4'-dihydroxy-7-methoxyl-8-butyricflavane (2), together with four known flavonoids, were isolated from the leaves of Morus alba L. Their structures were determined on the basis of spectroscopic analysis.

Four new 2-arylbenzofuran derivatives, moracins V-Y (1-4), together with two known compounds, moracin N (5) and moracin P (6), were isolated from the leaves of Morus alba L. Their structures were elucidated by spectroscopic analysis. Moracins X (3) and Y (4) represent unusual substituted group compared with 2-arylbenzofuran derivatives, which were isolated from the genus Morus. Compounds 2-5 were evaluated for cytotoxicity against several human cancer cell lines.

The investigation on the leaves of Morus alba L. was carried out to find the relationship of the constituents and the pharmacological activities. The isolation and purification were performed by various chromatographies such as silica gel, Sephadex LH-20, RP-C18 column chromatography and so on. Further detailed investigation on the fraction of the ethanol extract of leaves of Morus alba yielded four Diels-Alder type adducts mulberrofuran F1 (1), mulberrofuran F (2), chalcomoracin (3), kuwanon J (4), together with two chalcones morachalcone A (5), isobavachalcone (6), and three flavones norartocarpetin (7), kuwanon C (8), 6-geranylapigenin (9). Their structures were elucidated by the spectral analysis such as NMR, MS etc. Compounds 1, 6 were isolated from this plant for the first time, compounds 4-5, 7-9 were isolated from the leaves of Morus alba L. for the first time, among which 1 was a new compound. Compounds 1-5 were evaluated for the cytotoxicity against A549, Be17402, BGC823, HCT-8 and A2780 cell lines in vitro by MTT method, but only compounds 1-3 showed cytotoxicity against several human cancer cell lines.

Four new 2-arylbenzofuran derivatives, cathafurans A (1), B (2), C (3), and D (4), were isolated from the stem bark of Morus cathayana. Their structures were determined by spectroscopic methods. Compounds 2 and 3 exhibited moderate activities against five human cancer cell lines, with IC(50) values ranging from 6.17 to 9.60 microg/mL.

Six new Diels-Alder-type adducts, wittiorumins A-F ( 1 - 6) along with the three known compounds chalcomoracin ( 7), mulberrofuran J ( 8), and mongolicin F ( 9), were isolated from the stem bark of Morus wittiorum. Their structures including their absolute configurations were determined on the basis of spectroscopic analysis and chemical methods. Some of the isolated compounds ( 1 - 4) were assayed for their antioxidant activities, among which compounds 1 - 3 were active as antioxidants, with inhibitory ratios of 73.0 %, 82.0 %, and 82.0 %, respectively, at a concentration of 10 ( - 5) M.

Three new Diels-Alder type adducts cathayanons C (1), D (2), and E (3), together with one known compound sanggenon C (4), were isolated from the stem bark of Morus cathayana. Their structures were fully elucidated by spectroscopic and chemical methods. Compound 2 showed good anti-oxidation activity with the inhibitory rate of malondialdehyde being 88% at a concentration of 10(- 6) mol/l.

Two new dimeric stilbenes austrafuran B and austrafuran C were isolated from the bark of Morus australis. Their structures were elucidated on the basis of spectroscopic methods.

The investigation on the stem bark of Morus wittiorum was carried out to find its chemical constituents possessing anti-oxidative activity. The isolation and purification were performed by various chromatographies such as silica gel, Sephadex LH-20, RP-C18 column chromatography and so on. Based on the spectral analysis such as NMR, MS, etc., seven 2-arylbenzofuran derivatives were identified as wittifuran D (1), wittifuran E (2), moracin C (3), moracin M (4), moracin P (5), 2-(3,5-dihydroxyphenyl)-5,6-dihydroxybenzofuran (6) and mulberroside C (7). Compounds 1-7 were isolated from this plant for the first time. Among them, 1 and 2 were new compounds. Compounds 3-7 were used to assay antioxidant activity, the inhibitory ratios of compounds 3, 4, 6, at a concentration of 1 x 10(-5) mol x L(-1), to malondialdehyde (MDA) produced during microsomal lipid peroxidation induced by ferrous-cysteine were 73%, 69% and 89% respectively.

Three new compounds including two flavonoids and a new 2-phenylbenzofuran, named morunigrols A-C (1-3), together with three known compounds albafuran A (4), albafuran B (5), and mulberrofuran L (6), have been isolated from the barks of Morus nigra. Their structures have been elucidated by spectroscopic methods.

Objective: To study anti-oxidant phenolic compounds from stem barks of Morus yunanensis., Method: Isolation and purification were carried out by silica gel, Sephadex LH -20 and RP - 18 column chromatography. The chemical structures of constituents were elucidated on the basis of physicochemical properties and spectral data., Result: Eight phenolic compounds were isolated and identified as: mulberrofuran E (1), mulberrofuran K (2), albanol B (3), kuwanon H (4), resveratrol (5), moracin M (6), morachalcone A (7), 3', 5', 2, 4-tetrahydroxy-4-(3-methyl-1-butenyl) stilbene (8)., Conclusion: All the compounds were isolated from the plant for the first time, and compounds 2, 3, 6, 8 showed potent anti-oxidation activities.

Fractionation of the ethanolic extract of the stem bark of Morus yunanensis resulted in the isolation of a new Diels-Alder type adduct and two new flavones, named yunanensin A (1), yunanensol A (2) and yunanensol B (3), respectively, together with a known flavone (4). Their structures were determined on the basis of spectroscopic analysis and chemical methods. Among them, compound 1 showed moderate antioxidant and significant cytotoxic activities, and compound 2 showed potent anti-inflammatory activity.

Objective: To investigate the chemical constituents in the barks of Morus nigra., Method: The nine compounds were isolated and purified by column chromatography over silica gel, LH -20 and preparative HPLC and their structures were identified by various spectroscopic methods., Result: The nine compounds were isolated and identified as olcancolic acid , apigenin, cyclocommunol, morusin, cyclomorusin, kuwanon C, daucosterol, ursolic acid, 63-sitosterol., Conclusion: Olcancolic acid, apingenin, cyclocommunol, morusin, cyclomorusin, kuwanon C, daucosterol were firstly isolated from the M. nigra.

Three new natural products, australisines A-C (1-3, resp.), were isolated from the stem bark of Morus australis, together with eight related compounds, including mulberrofurans E-G, J, and Q, mongolicin C, chalcomoracin, and kuwanon G. Their structures were fully characterized by spectroscopic methods. Compounds 1-3, mulberrofuran G, mongolicin C, and chalcomoracin showed moderate cytotoxic activities against five human cancer cell lines, with IC50 values ranging from 4.6-9.2 microg/ml, as determined by MTT assay.

Five new Diels-Alder type adducts, mongolicins A - E, and nine known compounds, mongolicin F, chalcomoracin, mulberrofuran T, mulberrofuran G, mulberrofuran F, albanol B, kuwanon O, mulberrofuran H and kuwanon H, were isolated from the stem and root bark of Morus mongolica. Their structures were determined by spectroscopic analysis and chiroptical methods. Among them, compounds and showed potent anti-inflammatory activities (inhibition of release of beta-glucuronidase from rat PMNs induced by PAF) with inhibitory ratios of 80.4% (P<0.05) and 77.0% (P<0.001) at a concentration of 10(-5) mol L-1. Compounds and were active as antioxidatives (inhibition of liver microsomal lipid peroxidation induced by Fe2+-Cys system) with inhibitory ratios of 83.6% (P<0.05), 86.0% (P<0.05), and 63.0% (P<0.05) at a concentration of 10(-5) mol L-1.

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.

Fractionation of the ethanolic extract of the stem bark of Morus macroura resulted in the isolation of four new Diels-Alder type adducts, named guangsangons K--N (1, 2, 5, 6), together with two known compounds, mulberrofuran G (3) and K (4). Their structures were determined on the basis of spectroscopic analyses and chemical methods. Furthermore, by means of (1)H-NMR variable temperature experiments and the Cotton curves in the circular dichroism (CD) spectra, the stereochemistry of four new compounds was elucidated. The isolated new compounds showed good activity on anti-oxidant in vitro, with the inhibitory rates of MDA being from 91.8 to 100.0% at concentrations of 10(-5) mol/l.

Five new compounds, named guangsangons A (1), B (5), C (6), D (7), and E (8), along with four known compounds, albafuran C (2), kuwanon X (3), kuwanon P (4), and kuwanon Y (9) 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-Al-der type adducts, and 1H-NMR variable temperature experience suggested that they all existed as an equilibrium mixture of conformational isomers in solution. Compounds 1-3 and 5-9 showed good anti-oxidation activity, with the inhibitory rate of malondialdehyde being from 90.1% to 102.7% at a concentration of 10(-4) mol/L and from 70.9% to 88.1% at a concentration of 10(-5) mol/L. Compounds 1, 5, and 7 showed anti-inflammation activity, with the inhibitory rates of release of lysosome enzyme from polymorphonuclear leukocytes of rats being 19.0% (P > 0.05), 57.3% (P < 0.001) and 24.3% (P < 0.05) at concentrations of 10(-5) mol/L, respectively.

Objective: To study the chemical constituents from the bark of Morus macroura., Method: The compounds were isolated with silica gel column chromatography and their structures were elucidated on the basis of chemical evidences and spectral analysis (IR, EI-MS, 1H-NMR, 13C-NMR)., Result: Five compounds were identified as alpha-amyrin acetate (1), gult-5-en-3 beta-yl acetate (2), 3 beta-hydroxylup-20 (29)-en-28-oic acid (3), 3 beta-hydroxylup-12-en-28-oic acid (4), butyrospermol acetate (5).