Development and evaluation of Hedyotis corymbosa (L.) extract containing phytosomes: a preclinical approach for treatment of neuropathic pain in rodent model.

PURPOSE: The study was aimed to encapsulate Hedyotis corymbosa extract (HCE) into phytosomes to improve its therapeutic efficacy in neuropathic pain by enhancing the bioavailability of chief chemical constituent Hedycoryside -A (HCA). METHODS: For preparing phytosomes complexes (F1, F2, and F3), HCE and phospholipids were reacted in disparate ratio. F2 was chosen to assess its therapeutic efficacy in neuropathic pain induced by partial sciatic nerve ligation. Nociceptive threshold and oral bioavailability were also estimated for F2. RESULTS: Particle size, zeta potential and entrapment efficiency for F2 were analysed as 298.1 ± 1.1 nm, -3.92 ± 0.41 mV and 72.12 ± 0.72% respectively. F2 gave enhanced relative bioavailability (158.92%) of HCA along with a greater neuroprotective potential showing a significant antioxidant effect and augmentation (p < 0.05) in nociceptive threshold with the diminution in damage to nerves. CONCLUSION: F2 is an optimistic formulation for enhancing the HCE delivery for the effective treatment of neuropathic pain.

Discovery of the Potential Biomarkers for Discrimination between Hedyotis diffusa and Hedyotis corymbosa by UPLC-QTOF/MS Metabolome Analysis.

Hedyotis diffuse Willd. (HD) and Hedyotis corymbosa (L.) Lam. (HC), two closely related species of the same genus, are both used for health benefits and disease prevention in China. HC is also indiscriminately sold as HD in the wholesale chain and food markets. This confusion has led to a growing concern about their identification and quality evaluation. In order to further understand the molecular diversification between them, we focus on the screening of chemical components and the analysis of non-targeted metabolites. In this study, UPLC-QTOF-MSE, UNIFI platform and multivariate statistical analyses were used to profile them. Firstly, a total of 113 compounds, including 80 shared chemical constituents of the two plants, were identified from HC and HD by using the UNIFI platform. Secondly, the differences between two herbs were highlighted with the comparative analysis. As a result, a total of 33 robust biomarkers enabling the differentiation were discovered by using multivariate statistical analyses. For HC, there were 18 potential biomarkers (either the contents were much greater than in HD or being detected only in HC) including three iridoids, eight flavonoids, two tannins, two ketones, one alcohol and two monoterpenes. For HD, there were15 potential biomarkers (either the contents were much greater than in HC or being detected only in HD) including two iridoids, eight flavonoids, one tannin, one ketone, and three anthraquinones. With a comprehensive consideration of the contents or the MS responses of the chemical composition, Hedycoryside A and B, detected only in HC, could be used for rapid identification of HC. The compounds 1,3-dihydroxy-2-methylanthraquinone and 2-hydroxy-3-methylanthraquinone, detected only in HD, could be used for rapid identification of that plant. The systematic comparison of similarities and differences between two confusing Chinese herbs will provide reliable characterization profiles to clarify the pharmacological fundamental substances. HC should not be used as the substitute of HD.

Colored LED Lights: Use One Color Alone or with Others for Growth in Hedyotis corymbosa In Vitro?

In recent years, light-emitting diode (LED) technology has been applied to improve crop production and induce targeted biochemical or physiological responses in plants. This study investigated the effect of different ratios of blue 450 nm and red 660 nm LEDs on the overall plant growth, photosynthetic characteristics, and total triterpenoid production in the leaves of Hedyotis corymbosa in vitro plants. The results showed that a high proportion of blue LED lights had a positive effect on enhancing photosynthesis and the overall biomass. In addition, blue LED lights were shown to be more effective in controlling the production of the total triterpenoid content compared with the red LED lights. Moreover, it was also found that plants grown under a high proportion of red LEDs exhibited reduced photosynthetic properties and even induced damage to the photosynthetic apparatus, which indicated that the blue or red LED lights played contrary roles in Hedyotis corymbosa.

Potential Use of Colored LED Lights to Increase the Production of Bioactive Metabolites Hedyotis corymbosa (L.) Lam.

Hedyotis corymbosa (L.) Lam is a wild herb that is used in traditional Indian, Chinese, and African medicine. Light-emitting diode (LED) technology is paving the way to enhance crop production and inducing targeted photomorphogenic, biochemical, or physiological responses in plants. This study examines the efficiency of H. corymbosa (L.) Lam production under blue 450 nm and red 660 nm LED lights for overall plant growth, photosynthetic characteristics, and the contents of metabolite compounds. Our research showed that blue LED lights provided a positive effect on enhancing plant growth and overall biomass. In addition, blue LED lights are more effective in controlling the production of sucrose, starch, total phenolic compounds, and total flavonoid compared to red LED lights. However, blue and red LED lights played essential but different roles in photosynthetic characteristics. Our results showed the potential of colored LED light applications in improving farming methods and increasing metabolite production in herbs.

Evaluation of antinociceptive effect of ethanol extract of Hedyotis corymbosa Linn. whole plant in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Hedyotis corymbosa (Linn.) Lam. is a small herb commonly called as khetpapra, traditionally used to treat a wide range of diseases including abdominal pain, arthritis and inflammation. This study was conducted to evaluate the antinociceptive effect of ethanol extract of Hedyotis corymbosa (EEHC) whole plant. MATERIALS AND METHODS: The antinociceptive activity of EEHC was evaluated in mice using both chemical- and heat-induced pain models such as acetic acid-induced writhing, hot plate, tail immersion, formalin, and glutamate tests at 50, 100, and 200mg/kg doses. In order to verify the possible involvement of opioid receptors in the central antinociceptive effect of EEHC, the effects found in hot plate and tail immersion tests were antagonized with naloxone. RESULTS: EEHC produced a dose-dependent antinociceptive effect against the chemical- and heat-induced pain in mice, significantly at 100 and 200mg/kg doses. These findings suggest that the action of EEHC involves both peripheral and central antinociceptive mechanisms. The antinociceptive activity of EEHC was significantly attenuated by pretreatment with naloxone, indicating the influence of opioid receptors on the exertion of EEHC action centrally. CONCLUSIONS: This study reports the antinociceptive activity of Hedyotis corymbosa and possible underlying mechanism(s) that supports the traditional use of this plant in the treatment of different painful conditions.

Application of novel loop-mediated isothermal amplification (LAMP) for rapid authentication of the herbal tea ingredient Hedyotis diffusa Willd.

Hedyotis diffusa Willd. (Baihuasheshecao) is an ingredient of herbal teas commonly consumed in the Orient and tropical Asia for cancer treatment and health maintenance. In the market, this ingredient is frequently adulterated by the related species Hedyotis corymbosa (L.) Lam. The objective of this study is to develop a novel loop-mediated isothermal amplification (LAMP) technique to differentiate H. diffusa from its adulterant H. corymbosa. A set of four internal control primers (F3, FIP, BIP and B3) were designed based on six loci in the internal transcribed spacer (ITS) for LAMP of both H. diffusa and H. corymbosa. Two specific primers (S_F3 and S_FIP) were designed for specific LAMP detection of H. diffusa only. Our data showed that LAMP was successful for both H. diffusa and H. corymbosa in internal control. In contrast, only H. diffusa was detected in specific LAMP using the specific primers S_F3 and S_FIP. This study showed that LAMP was useful to differentiate H. diffusa from its adulterant H. corymbosa. This study is significant for the verification of the authenticity for better quality control of this common herbal tea ingredient. The strategy of including an internal control assures the quality of the concerned DNA region for LAMP.

Authentication of the anti-tumor herb Baihuasheshecao with bioactive marker compounds and molecular sequences.

Baihuasheshecao (Hedyotis diffusa), a Chinese herb for cancer treatment, is frequently adulterated by a related species Hedyotis corymbosa. DNA sequencing of the complete internal transcribed spacer region was applied to differentiate H. diffusa from H. corymbosa and other closely related species. The molecular data showed that four out of seven herb samples of Baihuasheshecao were adulterants. Chemical analyses by TLC and HPLC were used to authenticate H. diffusa and H. corymbosa. Two marker compounds were identified exclusively in H. diffusa: 6-O-(E)-p-coumaroyl scandoside methyl ester (compound 1) and 10(S)-hydroxypheophytin a (compound 2). Both compounds showed moderate anti-proliferation effect on PC3 human androgen-independent prostate cancer cells, while compound 2 also showed strong anti-proliferation effect on LNCaP human androgen-sensitive prostate cancer cells. Accordingly, these bioactive marker compounds could be applied to verify the authenticity and assess the quality of Baihuasheshecao.

A Study of hepatoprotective activity of Hedyotis corymbosa. Linn, in albino rats.

Hedyotis corymbosa Linn is spreading, suffruticose annual, belongs to family Rubiaceae frequently met with in field through out India, usually during rainy season. This plant is used for their medicinal properties as a folk medicine to treat jaundice, mouth wash in toothache. Hence the present study was aimed to investigate the hepatoprotective activity of ethanolic extract of Hedyotis corymbosa which was separated in to different fractions against carbon tetrachloride intoxification. The results indicate that, Intoxification with CCl(4) increase the levels of SGOT and SGPT. The elevated levels of SGOT and SGPTwere significantly decreased by ether and butanol fractions at P<0.001 and butanone and ethanol at p<0.05, where as petroleum ether and ethyl acetate did not shown any significant reduction in the level of SGOT and SGPT.