Research Progress on Chemical Constituents and Pharmacological Effects of Laportea bulbifera

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  Abstract Laportea bulbifera (Sieb. et Zucc.) Wedd. is a perennial herb of Laportea in Urticaceae. At present, more than 90 compounds have been isolated from L. bulbifera, mainly including flavonoids, coumarins, phenolic acids, esters, ketones, phenylpropanoids and steroids, which have anti-inflammatory and analgesic, immunosuppressive, anti-oxidant, hypoglycemic and lipid-lowering pharmacological effects. This article summarized the research progress of the pharmacological effects and the chemical constituents of L. bulbifera in recent years, hoping to provide references for its further research and development.
  Key words Laportea bulbifera; Chemical composition; Pharmacological effects
  Received: March 5, 2021  Accepted: May 6, 2021
  Supported by Research Fund of Guangxi Colleges and Universities (YB2014192); Guangxi Key R&D Program (GK AB19110027); High-level Innovation Team and Outstanding Scholars Project of Guangxi Colleges and Universities: Zhuang Medical Foundation and Clinical Innovation Team (GJR[2014]07).
  Ao XIE (1999-), female, P. R. China, master, devoted to research about development, identification and quality evaluation of traditional Chinese medicine and ethnic medicine.
  *Corresponding author.
   Laportea bulbifera (Sieb. et Zucc.) Wedd. is a perennial herb of Laportea in Urticaceae, also known as Honghema, Honghuoma, Ruidagun or Wadou, also known as Mafengcao in Fuchuan, Guangxi. The whole herb or roots are used as a medicine. The whole herb tastes pungent and warm in nature. It is a Zhuang medicine for clearing the Gudao, which has the effects of clearing the Gudao and tonifying the spleen and removing food retention. It is often used by Zhuang doctors in the treatment of infantile malnutrition (chancre) and urinary tract stones. The roots of L. bulbifera are pungent in taste and warm in nature, and have the effects of clearing the Longlu and Huolu, dispelling wind and dampness, and promoting blood circulation and relieving pain. Zhuang doctors use the roots to treat rheumatic arthralgia, numbness, bruises and other diseases[1-7]. Since 2003[8], many scholars have carried out chemical and pharmacological research on the L. bulbifera, and extracted and isolated flavonoids from its medicinal parts, such as coumarins, phenolic acids, esters, ketones, phenylpropanoids and sterides. The pharmacological effects of anti-inflammatory and analgesic, immunosuppressive, anti-oxidant, sugar-reducing and lipid-lowering have also been studied[9], but the research content is less and not comprehensive. In this study, the development status of L. bulbifera was summarized, aiming to provide reference for further research and development of its application.   Study on the Chemical Constituents of L. bulbifera
  At present, more than 90 components have been isolated from L. bulbifera, including flavonoids, coumarins, phenolic acids, esters, phenylpropanoids, ketones and steroids, etc., among which coumarins and flavonoids are the main chemical components of L. bulbifera.
  Flavonoids
  Flavonoids are the earliest separated and reported components of L. bulbifera and one of the main chemical components of L. bulbifera. At present, there are 30 kinds of flavonoids isolated from L. bulbifera, mainly including three categories, i.e., flavonoids, flavonols, and isoflavones. Flavonoids in L. bulbifera have strong antioxidant activity[9-15].
  Coumarins
  At this stage, there have been many studies on the coumarins of L. bulbifera, which have good anti-inflammatory and analgesic and immunosuppressive activity. The simple coumarins in L. bulbifera include coumarin, 7-methoxychromen-2-one, scoparone and scopoletin, and other coumarins include 4-hydroxy-6-methoxychromen-2-one, 3,6-dihydroxy-coumarin, 6,6,7,7-tetramethoxyl-8,8-biscoumarin 7,7-dihydroxy-6,6-dimethoxy-8,8-biscoumarin and 7,7-dimethoxy-6,6-biscoumarin[15-17].
  Phenolic acids
  Phenolic acids such as vanillic acid, gallocatechin, epigallocatechin, catechin, epicatechin, chlorogenic acid, 4-O-trans-caffeoylquini acid, neochlorogenic acid, 5-hydroxymethyl-2-furancarboxaldehyde, C-veratroylglycol and 4-hydroxy-5-methoxy-benzoic acid have been isolated from L. bulbifera [10,13-14,17-19].
  Esters
  Wang[19] separated and identified 8 esters from the L. bulbifera, including methyl hexadecanoate, methylhexadec-9-enoate, and ethyl hexadecanoate, 8,11-octadecadienoic acid methyl ester, methyloleate, methyl stearate, ethyl linoleate, and ethyl oleate.
  Phenylpropanoids
  The simple phenylpropanoids in L. bulbifera mainly include (1-p-hydroxy-cis-cinnamoyl) cinnamic acid, 12-hydroxypentanoic acid methyl ester, trans-cinnamic acid, p-coumaric acid, cis-4-coumaric acid, caffeic acid docosanoyl ester, isomerizing and caffeic acid[13-15].
  Ketones
  Lu et al.[20] found 4-(3-α-hydroxy-1-butenyl)-3,5,5-trimethyl-2-cyclohexen-1-one, 4-(3- β-hydroxy-1-butenyl)-3,5,5-trimethyl-2-cyclohexen-1-one, 3-(3-hydroxy-1-butenyl)-2,4,4 -trimethyl-2-cyclohexen-1-one, 2-(2-pentenyl-3-methyl)-4-hydroxy-2-cyclopenten-1-one, 4-(3-hydroxy-1-butyl)-3,5,5-trimethyl-2-cyclohexenone and other ketone compounds.   Sterides
  Xu[21] isolated compounds such as ergosta-4,6,8(14),22-tetraen-3-one, sitostenone, stigmast-4-ene-3,6-dione and stigmast-4,22-diene-3,6-dione from L. bulbifera.
  Other components
  Furthermore, 2,2-oxybis(1-phenylethanol), 1-(2-phenylcarbonyloxy acetyl)benzene, 1H-indole-2-carbaldehyde, betulaprenol 8, betulaprenol 9, linoleic acid, Z-10-eicosenoic acid, hexadec-(4Z)-enoic acid and 9(Z)-octadecenamide were also isolated from L. bulbifera[13,16,21-22].
  Study on the Pharmacological Effects of L. bulbifera
  Immunosuppressive effect
  Immune response is the result of the interaction of various immune cell components under antigen stimulation, which is manifested in the formation of antibodies, or the production of specific immunologically active cells, or the release of various allergic mediators. Therefore, suppression of immune response can be achieved by eliminating antigens or suppressing antibodies, or by suppressing the production of immunocompetent cells[23].
  Yu et al.[25] used a mouse allogeneic skin transplantation model to study the survival time of skin grafts, the recipients spleen lymphocyte proliferation test, the determination of cytokine secretion levels, and the analysis of CD4~+CD25~+T cell subsets. The results showed that the effective part of L. bulbifera could stimulate the distribution of CD4~+CD25~+ on the surface of lymphocytes, regulate the synthesis of cytokines such as IL-2, IL-10 and IFN-γ, inhibit the transformation function of T lymphocytes, and induce host cell immune tolerance, thereby effectively inhibiting skin graft rejection.
  The study by Wang et al.[24] showed that the ethyl acetate part of L. bulbifera could inhibit the expression of bone marrow-derived DC MHc II and the co-stimulatory molecule CD86 and the secretion of IL-12p70 in the supernatant. When drug-treated DC and T cells of the same species were mixed and cultured in different ratios, the ability to stimulate the proliferation of T cells of the same species was significantly reduced, indicating that the ethyl acetate part of L. bulbifera had immunosuppressive activity.
  Su et al.[26-27] used T lymphocyte proliferation experiments and applied enzyme-linked immunoassay (ELISA) to determine the contents of IFN-γ, IL-2 and IL-4 in the supernatant of spleen cells. The results showed that the ethyl acetate part of the ethanol extract of L. bulbifera could inhibit the proliferation of splenic T lymphocytes in a dose-dependent manner in vitro, with an inhibition rate of 35%, and inhibit the secretion of IL-2 and IFN-γ in the supernatant of T cell culture. The ethyl acetate part of the ethanol extract of L. bulbifera had a certain immunosuppressive effect.   References
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